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Daria Hazuda

Research Profile

Chemicals & Drugs

Living Beings

HIV-1
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HIV Infections

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Publications

TOP 3
David M Margolis; Daria J Hazuda
Combined approaches for HIV cure.
Nichole R Klatt; Michael M Lederman; Jeffrey D Lifson; Michael D Miller; David R Morcock; Molly Perkins; Mariam Quiñones; Julie A Segre; Xiaoyong Sun; Carol L Vinton; Lauren A Canary; Clayton B Deming; Jacob D Estes; Nicholas T Funderburg; Elias K Haddad; Daria J Hazuda; Jason M Brenchley
Probiotic/prebiotic supplementation of antiretrovirals improves gastrointestinal immunity in SIV-infected macaques.
Robert A Ogert; Lisa D Pedicone; David Pound; Ping Qiu; Robert Ralston; Natarajan Ravendhran; Lorenzo Rossaro; Eugene R Schiff; John M Vierling; Janice K Albrecht; Richard Jo Barnard; Clifford A Brass; Eirum Chaudhri; Mitchell N Davis; Stuart C Gordon; Daria J Hazuda; John A Howe; Ira M Jacobson; Paul Y Kwo; Eric J Lawitz; Jonathan McCone; Anita Ym Howe
Resistance-associated amino acid variants associated with boceprevir plus pegylated interferon-α2b and ribavirin in patients with chronic hepatitis C in the SPRINT-1 trial.

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All Publications

2013: David M Margolis; Daria J Hazuda
Combined approaches for HIV cure.
Current opinion in HIV and AIDS 2013;8(3):230-5.
2013: Nichole R Klatt; Michael M Lederman; Jeffrey D Lifson; Michael D Miller; David R Morcock; Molly Perkins; Mariam Quiñones; Julie A Segre; Xiaoyong Sun; Carol L Vinton; Lauren A Canary; Clayton B Deming; Jacob D Estes; Nicholas T Funderburg; Elias K Haddad; Daria J Hazuda; Jason M Brenchley
Probiotic/prebiotic supplementation of antiretrovirals improves gastrointestinal immunity in SIV-infected macaques.
The Journal of clinical investigation 2013;123(2):903-7.
2013: Robert A Ogert; Lisa D Pedicone; David Pound; Ping Qiu; Robert Ralston; Natarajan Ravendhran; Lorenzo Rossaro; Eugene R Schiff; John M Vierling; Janice K Albrecht; Richard Jo Barnard; Clifford A Brass; Eirum Chaudhri; Mitchell N Davis; Stuart C Gordon; Daria J Hazuda; John A Howe; Ira M Jacobson; Paul Y Kwo; Eric J Lawitz; Jonathan McCone; Anita Ym Howe
Resistance-associated amino acid variants associated with boceprevir plus pegylated interferon-α2b and ribavirin in patients with chronic hepatitis C in the SPRINT-1 trial.
Antiviral therapy 2013;18(3):387-97.
2012: Daria J Hazuda
HIV integrase as a target for antiretroviral therapy.
Current opinion in HIV and AIDS 2012;7(5):383-9.
2012: Vincenzo Summa; Joseph P Vacca; Christine Burlein; Giuliano Claudio; Paul J Coleman; Marcello Di Filippo; Jillian DiMuzio; Christine Fandozzi; Marco Ferrara; Adam T Gates; Donald J Graham; Steven Harper; Daria J Hazuda; Nigel J Liverton; Steven W Ludmerer; John A McCauley; Carolyn McHale; Edith Monteagudo; David B Olsen; Vincenzo Pucci; Michael Rowley; Michael T Rudd; Aileen Soriano; Mark Stahlhut; Steven S Carroll
MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants.
Antimicrobial agents and chemotherapy 2012;56(8):4161-7.
2012: Meiqing Lu; Georgia B McGaughey; PM McKenna; Michael D Miller; Sanjeev Munshi; Vandna Munshi; Ying-Jie Wang; Theresa M Williams; Youwei Yan; Neville J Anthony; Peter J Felock; Robert Gomez; Jay A Grobler; Daria J Hazuda; Renee C Hrin; Ming-Tain Lai
Antiviral activity and in vitro mutation development pathways of MK-6186, a novel nonnucleoside reverse transcriptase inhibitor.
Antimicrobial agents and chemotherapy 2012;56(6):3324-35.
2012: Eric J Arts; Daria J Hazuda
HIV-1 antiretroviral drug therapy.
Cold Spring Harbor perspectives in medicine 2012;2(4):a007161.
2012: Ashley N Brown; A Corbin; Jonathan R Adams; Richard J O Barnard; Daria J Hazuda; Robert Kulawy; Arnold Louie; James J McSharry; W Newhard; George L Drusano
Pharmacodynamic analysis of a serine protease inhibitor, MK-4519, against hepatitis C virus using a novel in vitro pharmacodynamic system.
Antimicrobial agents and chemotherapy 2012;56(3):1170-81.
2011: Bach-Yen T Nguyen; Robin D Isaacs; Hedy Teppler; Randi Y Leavitt; Peter Sklar; Marian Iwamoto; Larissa A Wenning; Michael D Miller; Joshua Chen; Ramon Kemp; Wei Xu; Robert A Fromtling; Joseph P Vacca; Steven D Young; Michael Rowley; Michael W Lower; Keith M Gottesdiener; Daria J Hazuda
Raltegravir: the first HIV-1 integrase strand transfer inhibitor in the HIV armamentarium.
Annals of the New York Academy of Sciences 2011;1222():83-9.
2011: Jia Liu; Michael D Miller; Robert M Danovich; Nathan Vandergrift; Fangping Cai; Charles B Hicks; Daria J Hazuda; Feng Gao
Analysis of low-frequency mutations associated with drug resistance to raltegravir before antiretroviral treatment.
Antimicrobial agents and chemotherapy 2011;55(3):1114-9.
2011: David B Olsen; Mary-Ellen Davies; Larry Handt; Kenneth Koeplinger; Nanyan Rena Zhang; Steven W Ludmerer; Donald Graham; Nigel J Liverton; Malcolm MacCoss; Daria J Hazuda; Steven S Carroll
Sustained viral response in a hepatitis C virus-infected chimpanzee via a combination of direct-acting antiviral agents.
Antimicrobial agents and chemotherapy 2011;55(2):937-9.
2011: Marta De Zotti; Wim De Borggraeve; Bernard Kaptein; Quirinus B Broxterman; Sheo B Singh; Peter J Felock; Daria J Hazuda; Fernando Formaggio; Claudio Toniolo
Triple Hyp→Pro replacement in integramide A, a peptaib inhibitor of HIV-1 integrase: Effect on conformation and bioactivity.
Biopolymers 2011;96(1):49-59.
2010: Peter D Williams; Donnette D Staas; Shankar Venkatraman; H Marie Loughran; Rowena D Ruzek; Theresa M Booth; Terry A Lyle; John S Wai; Joseph P Vacca; Bradley P Feuston; Linda T Ecto; Jessica A Flynn; Daniel J DiStefano; Daria J Hazuda; Carolyn M Bahnck; Amy L Himmelberger; Geetha Dornadula; Renee C Hrin; Kara A Stillmock; Marc V Witmer; Michael D Miller; Jay A Grobler
Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold.
Bioorganic & medicinal chemistry letters 2010;20(22):6754-7.
2010: Ming-Tain Lai; Meiqing Lu; Peter J Felock; Renee C Hrin; Ying-Jie Wang; Youwei Yan; Sanjeev Munshi; Georgia B McGaughey; Robert M Tynebor; Thomas J Tucker; Theresa M Williams; Jay A Grobler; Daria J Hazuda; PM McKenna; Michael D Miller
Distinct mutation pathways of non-subtype B HIV-1 during in vitro resistance selection with nonnucleoside reverse transcriptase inhibitors.
Antimicrobial agents and chemotherapy 2010;54(11):4812-24.
2010: Daria J Hazuda
Resistance to inhibitors of the human immunodeficiency virus type 1 integration.
The Brazilian journal of infectious diseases : an official publication of the Brazilian Society of Infectious Diseases 2010;14(5):513-8.
2010: Tamara Bar-Magen; Richard Sloan; Daniel A Donahue; Björn D Kuhl; Alexandra Zabeida; Hongtao Xu; Maureen Oliveira; Daria J Hazuda; Mark A Wainberg
Identification of novel mutations responsible for resistance to MK-2048, a second-generation HIV-1 integrase inhibitor.
Journal of virology 2010;84(18):9210-6.
2010: Hua-Poo Su; Youwei Yan; G Sridhar Prasad; Robert F Smith; Christopher L Daniels; Pravien D Abeywickrema; John C Reid; H Marie Loughran; Maria Kornienko; Sujata Sharma; Jay A Grobler; Bei Xu; Vinod Sardana; Timothy J Allison; Peter D Williams; Paul L Darke; Daria J Hazuda; Sanjeev Munshi
Structural basis for the inhibition of RNase H activity of HIV-1 reverse transcriptase by RNase H active site-directed inhibitors.
Journal of virology 2010;84(15):7625-33.
2010: Meiqing Lu; Winnie Ngo; Ye Mei; Vandna Munshi; Christine Burlein; Marie H Loughran; Peter D Williams; Daria J Hazuda; Michael D Miller; Jay A Grobler; Tracy L Diamond; Ming-Tain Lai
Purification of untagged HIV-1 reverse transcriptase by affinity chromatography.
Protein expression and purification 2010;71(2):231-9.
2010: Ying-Jie Wang; PM McKenna; Renee Hrin; Peter Felock; Meiqing Lu; Kristen G Jones; Craig A Coburn; Jay A Grobler; Daria J Hazuda; Michael D Miller; Ming-Tain Lai
Assessment of the susceptibility of mutant HIV-1 to antiviral agents.
Journal of virological methods 2010;165(2):230-7.
2010: Hemaka A Rajapakse; Philippe G Nantermet; Harold G Selnick; James C Barrow; Georgia B McGaughey; Sanjeev Munshi; Stacey R Lindsley; Mary Beth Young; Phung L Ngo; M Katharine Holloway; Ming-Tain Lai; Amy S Espeseth; Xiao-Ping Shi; Dennis Colussi; Beth L Pietrak; Ming-Chih Crouthamel; Katherine Tugusheva; Qian Huang; Min Xu; Adam J Simon; Lawrence Kuo; Daria J Hazuda; Samuel Graham; Joseph P Vacca
SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.
Bioorganic & medicinal chemistry letters 2010;20(6):1885-9.
2010: Hong Zhu; Mary Beth Young; Philippe G Nantermet; Samuel L Graham; Dennis Colussi; Ming-Tain Lai; Beth L Pietrak; Eric A Price; Sethu Sankaranarayanan; Xiao-Ping Shi; Katherine Tugusheva; Marie A Holahan; Maria S Michener; Jacquelynn J Cook; Adam Simon; Daria J Hazuda; Joseph P Vacca; Hemaka A Rajapakse
Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors.
Bioorganic & medicinal chemistry letters 2010;20(5):1779-82.
2010: Marta De Zotti; Francesca Damato; Fernando Formaggio; Marco Crisma; Elisabetta Schievano; Stefano Mammi; Bernard Kaptein; Quirinus B Broxterman; Peter J Felock; Daria J Hazuda; Sheo B Singh; Jochen Kirschbaum; Hans Brückner; Claudio Toniolo
Total synthesis, characterization, and conformational analysis of the naturally occurring hexadecapeptide integramide A and a diastereomer.
Chemistry (Weinheim an der Bergstrasse, Germany) 2010;16(1):316-27.
2010: Nigel J Liverton; Steven S Carroll; Jillian DiMuzio; Christine Fandozzi; Donald J Graham; Daria J Hazuda; M Katherine Holloway; Steven W Ludmerer; John A McCauley; Charles J McIntyre; David B Olsen; Michael T Rudd; Mark Stahlhut; Joseph P Vacca
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
Antimicrobial agents and chemotherapy 2010;54(1):305-11.
2009: Nancie M Archin; Kara S Keedy; Amy S Espeseth; Herbert Dang; Daria J Hazuda; David M Margolis
Expression of latent human immunodeficiency type 1 is induced by novel and selective histone deacetylase inhibitors.
AIDS (London, England) 2009;23(14):1799-806.
2009: Ming-Tain Lai; Vandna Munshi; Sinoeun Touch; Robert M Tynebor; Thomas J Tucker; PM McKenna; Theresa M Williams; Daniel J DiStefano; Daria J Hazuda; Michael D Miller
Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor.
Antimicrobial agents and chemotherapy 2009;53(6):2424-31.
2009: Frederic D Bushman; Nirav Malani; Jason Fernandes; Iván D'Orso; Gerard Cagney; Tracy L Diamond; Honglin Zhou; Daria J Hazuda; Amy S Espeseth; Renate König; Sourav Bandyopadhyay; Trey Ideker; Stephen P Goff; Nevan J Krogan; Alan D Frankel; John A T Young; Sumit K Chanda
Host cell factors in HIV replication: meta-analysis of genome-wide studies.
PLoS pathogens 2009;5(5):e1000437.
2009: Kara S Keedy; Nancie M Archin; Adam T Gates; Amy S Espeseth; Daria J Hazuda; David M Margolis
A limited group of class I histone deacetylases acts to repress human immunodeficiency virus type 1 expression.
Journal of virology 2009;83(10):4749-56.
2009: Jay A Grobler; Kara A Stillmock; Daria J Hazuda
Scintillation proximity assays for mechanistic and pharmacological analyses of HIV-1 integration.
Methods (San Diego, Calif.) 2009;47(4):249-53.
2009: Steven S Carroll; Steven Ludmerer; Larry Handt; Kenneth Koeplinger; Nanyan Rena Zhang; Donald Graham; Mary-Ellen Davies; Malcolm MacCoss; Daria J Hazuda; David B Olsen
Robust antiviral efficacy upon administration of a nucleoside analog to hepatitis C virus-infected chimpanzees.
Antimicrobial agents and chemotherapy 2009;53(3):926-34.
2009: Adam C Finnefrock; Aimin Tang; Fengsheng Li; Daniel C Freed; Meizhen Feng; Kara S Cox; Kara J Sykes; James P Guare; Michael D Miller; David B Olsen; Daria J Hazuda; John W Shiver; Danilo R Casimiro; Tong-Ming Fu
PD-1 blockade in rhesus macaques: impact on chronic infection and prophylactic vaccination.
Journal of immunology (Baltimore, Md. : 1950) 2009;182(2):980-7.
2009: Marta De Zotti; Fernando Formaggio; Bernard Kaptein; Quirinus B Broxterman; Peter J Felock; Daria J Hazuda; Sheo B Singh; Hans Brückner; Claudio Toniolo
Complete absolute configuration of integramide A, a natural, 16-mer peptide inhibitor of HIV-1 integrase, elucidated by total synthesis.
Chembiochem : a European journal of chemical biology 2009;10(1):87-90.
2008: Honglin Zhou; Min Xu; Qian Huang; Adam T Gates; Xiaohua D Zhang; John C Castle; Erica Stec; Marc Ferrer; Berta Strulovici; Daria J Hazuda; Amy S Espeseth
Genome-scale RNAi screen for host factors required for HIV replication.
Cell host & microbe 2008;4(5):495-504.
2008: James C Barrow; Shaun R Stauffer; Kenneth E Rittle; Phung L Ngo; ZhiQiang Yang; Harold G Selnick; Samuel L Graham; Sanjeev Munshi; Georgia B McGaughey; M Katharine Holloway; Adam J Simon; Eric A Price; Sethu Sankaranarayanan; Dennis Colussi; Katherine Tugusheva; Ming-Tain Lai; Amy S Espeseth; Min Xu; Qian Huang; Abigail Wolfe; Beth Pietrak; Paul Zuck; Dorothy A Levorse; Daria J Hazuda; Joseph P Vacca
Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase.
Journal of medicinal chemistry 2008;51(20):6259-62.
2008: Jeffrey Y Melamed; Melissa S Egbertson; Sandor L Varga; Joseph P Vacca; Gregory Moyer; Lori Gabryelski; Peter J Felock; Kara A Stillmock; Marc V Witmer; William A Schleif; Daria J Hazuda; Yvonne M Leonard; Lixia Jin; Joan D Ellis; Steven D Young
Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase.
Bioorganic & medicinal chemistry letters 2008;18(19):5307-10.
2008: Vincenzo Summa; Alessia Petrocchi; Fabio Bonelli; Benedetta Crescenzi; Monica Donghi; Marco Ferrara; Fabrizio Fiore; Cristina Gardelli; Odalys Gonzalez Paz; Daria J Hazuda; Philip Jones; Olaf Kinzel; Ralph Laufer; Edith Monteagudo; Ester Muraglia; Emanuela Nizi; Federica Orvieto; Paola Pace; Giovanna Pescatore; Rita Scarpelli; Kara A Stillmock; Marc V Witmer; Michael Rowley
Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection.
Journal of medicinal chemistry 2008;51(18):5843-55.
2008: Jacob A Zahm; Sibes Bera; Krishan Pandey; Ajaykumar Vora; Kara A Stillmock; Daria J Hazuda; Duane P Grandgenett
Mechanisms of human immunodeficiency virus type 1 concerted integration related to strand transfer inhibition and drug resistance.
Antimicrobial agents and chemotherapy 2008;52(9):3358-68.
2008: Catherine M Wiscount; Peter D Williams; Lekhanh O Tran; Mark W Embrey; Thorsten E Fisher; Vanessa Sherman; Carl F Homnick; D Donnette Staas; Terry A Lyle; John S Wai; Joseph P Vacca; ZiQiang Wang; Peter J Felock; Kara A Stillmock; Marc V Witmer; Michael D Miller; Daria J Hazuda; Alysha M Day; Lori Gabryelski; Linda T Ecto; William A Schleif; Daniel J DiStefano; Christopher J Kochansky; M Reza Anari
10-Hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones: potent, orally bioavailable HIV-1 integrase strand-transfer inhibitors with activity against integrase mutants.
Bioorganic & medicinal chemistry letters 2008;18(16):4581-3.
2008: David A Cooper; Roy T Steigbigel; Jose M Gatell; Jurgen K Rockstroh; Christine Katlama; Patrick Yeni; Adriano Lazzarin; Bonaventura Clotet; Princy N Kumar; Joseph E Eron; Mauro Schechter; Martin Markowitz; Mona R Loutfy; Jeffrey Lennox; Jing Zhao; Joshua Chen; Desmond M Ryan; Rand R Rhodes; John A Killar; Lucinda R Gilde; Kim M Strohmaier; Anne R Meibohm; Michael D Miller; Daria J Hazuda; Michael L Nessly; Mark J DiNubile; Robin D Isaacs; Hedy Teppler; Bach-Yen Nguyen
Subgroup and resistance analyses of raltegravir for resistant HIV-1 infection.
The New England journal of medicine 2008;359(4):355-65.
2008: Roy T Steigbigel; David A Cooper; Princy N Kumar; Joseph E Eron; Mauro Schechter; Martin Markowitz; Mona R Loutfy; Jeffrey Lennox; Jose M Gatell; Jurgen K Rockstroh; Christine Katlama; Patrick Yeni; Adriano Lazzarin; Bonaventura Clotet; Jing Zhao; Joshua Chen; Desmond M Ryan; Rand R Rhodes; John A Killar; Lucinda R Gilde; Kim M Strohmaier; Anne R Meibohm; Michael D Miller; Daria J Hazuda; Michael L Nessly; Mark J DiNubile; Robin D Isaacs; Bach-Yen Nguyen; Hedy Teppler
Raltegravir with optimized background therapy for resistant HIV-1 infection.
The New England journal of medicine 2008;359(4):339-54.
2008: Vandna Munshi; Meiqing Lu; Peter J Felock; Richard J O Barnard; Daria J Hazuda; Michael D Miller; Ming-Tain Lai
Monitoring the development of non-nucleoside reverse transcriptase inhibitor-associated resistant HIV-1 using an electrochemiluminescence-based reverse transcriptase polymerase assay.
Analytical biochemistry 2008;374(1):121-32.
2008: H Marie Langford; Peter D Williams; Carl F Homnick; Joseph P Vacca; Peter J Felock; Kara A Stillmock; Marc V Witmer; Daria J Hazuda; Lori Gabryelski; William A Schleif
Design and synthesis of substituted 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxamides, novel HIV-1 integrase inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(2):721-5.
2007: Thorsten E Fisher; Boyoung Kim; Donnette D Staas; Terry A Lyle; Steven D Young; Joseph P Vacca; Matthew M Zrada; Daria J Hazuda; Peter J Felock; William A Schleif; Lori Gabryelski; M Reza Anari; Christopher J Kochansky; John S Wai
8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(23):6511-5.
2007: John M Murray; Sean Emery; Anthony D Kelleher; Matthew Law; Joshua Chen; Daria J Hazuda; Bach-Yen T Nguyen; Hedy Teppler; David A Cooper
Antiretroviral therapy with the integrase inhibitor raltegravir alters decay kinetics of HIV, significantly reducing the second phase.
AIDS (London, England) 2007;21(17):2315-21.
2007: Krishan Pandey; Sibes Bera; Jacob Zahm; Ajaykumar Vora; Kara A Stillmock; Daria J Hazuda; Duane P Grandgenett
Inhibition of human immunodeficiency virus type 1 concerted integration by strand transfer inhibitors which recognize a transient structural intermediate.
Journal of virology 2007;81(22):12189-99.
2007: John S Wai; Boyoung Kim; Thorsten E Fisher; Linghang Zhuang; Mark W Embrey; Peter D Williams; Donnette D Staas; Chris Culberson; Terry A Lyle; Joseph P Vacca; Daria J Hazuda; Peter J Felock; William A Schleif; Lori Gabryelski; Lixia Jin; I-Wu Chen; Joan D Ellis; Rama Mallai; Steven D Young
Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(20):5595-9.
2007: Cristina Gardelli; Emanuela Nizi; Ester Muraglia; Benedetta Crescenzi; Marco Ferrara; Federica Orvieto; Paola Pace; Giovanna Pescatore; Marco Poma; Maria Del Rosario Rico Ferreira; Rita Scarpelli; Carl F Homnick; Norihiro Ikemoto; Anna Alfieri; Maria Verdirame; Fabio Bonelli; Odalys Gonzalez Paz; Marina Taliani; Edith Monteagudo; Silvia Pesci; Ralph Laufer; Peter J Felock; Kara A Stillmock; Daria J Hazuda; Michael Rowley; Vincenzo Summa
Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.
Journal of medicinal chemistry 2007;50(20):4953-75.
2007: Pek Yee Lum; Yudong D He; J Greg Slatter; Jeffrey F Waring; Nicollete Zelinsky; Guy Cavet; Xudong Dai; Olivia Fong; Rebecca J Gum; Lixia Jin; Gary E Adamson; Christopher J Roberts; David B Olsen; Daria J Hazuda; Roger G Ulrich
Gene expression profiling of rat liver reveals a mechanistic basis for ritonavir-induced hyperlipidemia.
Genomics 2007;90(4):464-73.
2007: Guochun Jiang; Amy S Espeseth; Daria J Hazuda; David M Margolis
c-Myc and Sp1 contribute to proviral latency by recruiting histone deacetylase 1 to the human immunodeficiency virus type 1 promoter.
Journal of virology 2007;81(20):10914-23.
2007: Agata Czyz; Kara A Stillmock; Daria J Hazuda; William S Reznikoff
Dissecting Tn5 transposition using HIV-1 integrase diketoacid inhibitors.
Biochemistry 2007;46(38):10776-89.
2007: Stacey R Lindsley; Keith P Moore; Hemaka A Rajapakse; Harold G Selnick; Mary Beth Young; Hong Zhu; Sanjeev Munshi; Lawrence Kuo; Georgia B McGaughey; Dennis Colussi; Ming-Chih Crouthamel; Ming-Tain Lai; Beth L Pietrak; Eric A Price; Sethu Sankaranarayanan; Adam J Simon; Guy R Seabrook; Daria J Hazuda; Nicole T Pudvah; Jerome H Hochman; Samuel L Graham; Joseph P Vacca; Philippe G Nantermet
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(14):4057-61.
2007: Paola Pace; M Emilia Di Francesco; Cristina Gardelli; Steven Harper; Ester Muraglia; Emanuela Nizi; Federica Orvieto; Alessia Petrocchi; Marco Poma; Michael Rowley; Rita Scarpelli; Ralph Laufer; Odalys Gonzalez Paz; Edith Monteagudo; Fabio Bonelli; Daria J Hazuda; Kara A Stillmock; Vincenzo Summa
Dihydroxypyrimidine-4-carboxamides as novel potent and selective HIV integrase inhibitors.
Journal of medicinal chemistry 2007;50(9):2225-39.
2007: Jay A Grobler; Geethanjali Dornadula; Michele R Rice; Amy L Simcoe; Daria J Hazuda; Michael D Miller
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
The Journal of biological chemistry 2007;282(11):8005-10.
2007: Melissa S Egbertson; H Marie Moritz; Jeffrey Y Melamed; Wei Han; Debra S Perlow; Michelle Kuo; Mark W Embrey; Joseph P Vacca; Matthew M Zrada; Amanda R Cortes; Audrey Wallace; Yvonne M Leonard; Daria J Hazuda; Michael D Miller; Peter J Felock; Kara A Stillmock; Marc V Witmer; William A Schleif; Lori Gabryelski; Gregory Moyer; Joan D Ellis; Lixia Jin; Wei Xu; Matthew P Braun; Kelem Kassahun; Nancy N Tsou; Steven D Young
A potent and orally active HIV-1 integrase inhibitor.
Bioorganic & medicinal chemistry letters 2007;17(5):1392-8.
2006: Hemaka A Rajapakse; Philippe G Nantermet; Harold G Selnick; Sanjeev Munshi; Georgia B McGaughey; Stacey R Lindsley; Mary Beth Young; Ming-Tain Lai; Amy S Espeseth; Xiao-Ping Shi; Dennis Colussi; Beth L Pietrak; Ming-Chih Crouthamel; Katherine Tugusheva; Qian Huang; Min Xu; Adam J Simon; Lawrence Kuo; Daria J Hazuda; Samuel Graham; Joseph P Vacca
Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).
Journal of medicinal chemistry 2006;49(25):7270-3.
2006: John Majercak; William Ray; Amy S Espeseth; Adam Simon; Xiao-Ping Shi; Carrie Wolffe; Krista Getty; Shane Marine; Erica Stec; Marc Ferrer; Berta Strulovici; Steven Bartz; Adam Gates; Min Xu; Qian Huang; Lei Ma; Paul J Shughrue; Julja Burchard; Dennis Colussi; Beth L Pietrak; Jason Kahana; Dirk Beher; Thomas W Rosahl; Mark S Shearman; Daria J Hazuda; Alan B Sachs; Kenneth S Koblan; Guy R Seabrook; David J Stone
LRRTM3 promotes processing of amyloid-precursor protein by BACE1 and is a positional candidate gene for late-onset Alzheimer's disease.
Proceedings of the National Academy of Sciences of the United States of America 2006;103(47):17967-72.
2006: Amy S Espeseth; Qian Huang; Adam Gates; Min Xu; Yuanjiang Yu; Adam J Simon; Xiao-Ping Shi; Xiaohua Zhang; Paul Hodor; David J Stone; Julja Burchard; Guy Cavet; Steven Bartz; Peter Linsley; William Ray; Daria J Hazuda
A genome wide analysis of ubiquitin ligases in APP processing identifies a novel regulator of BACE1 mRNA levels.
Molecular and cellular neurosciences 2006;33(3):227-35.
2006: Shawn J Stachel; Craig A Coburn; Sethu Sankaranarayanan; Eric A Price; Guoxin Wu; Ming-Chih Crouthamel; Beth L Pietrak; Qian Huang; Janet Lineberger; Amy S Espeseth; Lixia Jin; Joan Ellis; M Katharine Holloway; Sanjeev Munshi; Timothy Allison; Daria J Hazuda; Adam J Simon; Samuel L Graham; Joseph P Vacca
Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.
Journal of medicinal chemistry 2006;49(21):6147-50.
2006: Craig A Coburn; Shawn J Stachel; Kristen G Jones; Thomas G Steele; Diane M Rush; Jillian DiMuzio; Beth L Pietrak; Ming-Tain Lai; Qian Huang; Janet Lineberger; Lixia Jin; Sanjeev Munshi; M Katharine Holloway; Amy S Espeseth; Adam Simon; Daria J Hazuda; Samuel L Graham; Joseph P Vacca
BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.
Bioorganic & medicinal chemistry letters 2006;16(14):3635-8.
2006: James P Guare; John S Wai; Robert P Gomez; Neville J Anthony; Samson M Jolly; Amanda R Cortes; Joseph P Vacca; Peter J Felock; Kara A Stillmock; William A Schleif; Gregory Moyer; Lori Gabryelski; Lixia Jin; I-Wu Chen; Daria J Hazuda; Steven D Young
A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(11):2900-4.
2006: Daria J Hazuda
Inhibitors of human immunodeficiency virus type I integration.
Current opinion in HIV and AIDS 2006;1(3):212-7.
2006: Ming-Tain Lai; Ming-Chih Crouthamel; Jillian DiMuzio; Beth L Pietrak; Dorit B Donoviel; alan bernstein; Stephen J Gardell; Yueming Li; Daria J Hazuda
A presenilin-independent aspartyl protease prefers the gamma-42 site cleavage.
Journal of neurochemistry 2006;96(1):118-25.
2006: Donald J Graham; Mark Stahlhut; Osvaldo A Flores; David B Olsen; Daria J Hazuda; Robert L LaFemina; Steven W Ludmerer
A genotype 2b NS5B polymerase with novel substitutions supports replication of a chimeric HCV 1b:2b replicon containing a genotype 1b NS3-5A background.
Antiviral research 2006;69(1):24-30.
2005: Mark W Embrey; John S Wai; Timothy W Funk; Carl F Homnick; Debra S Perlow; Steven D Young; Joseph P Vacca; Daria J Hazuda; Peter J Felock; Kara A Stillmock; Marc V Witmer; Gregory Moyer; William A Schleif; Lori Gabryelski; Lixia Jin; I-Wu Chen; Joan D Ellis; Bradley K Wong; Jiunn H Lin; Yvonne M Leonard; Nancy N Tsou; Linghang Zhuang
A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells.
Bioorganic & medicinal chemistry letters 2005;15(20):4550-4.
2005: Beth L Pietrak; Ming-Chih Crouthamel; Katherine Tugusheva; Janet Lineberger; Min Xu; Jillian DiMuzio; Thomas G Steele; Amy S Espeseth; Shawn J Stachel; Craig A Coburn; Samuel L Graham; Joseph P Vacca; Xiao-Ping Shi; Adam J Simon; Daria J Hazuda; Ming-Tain Lai
Biochemical and cell-based assays for characterization of BACE-1 inhibitors.
Analytical biochemistry 2005;342(1):144-51.
2005: Amy S Espeseth; Min Xu; Qian Huang; Craig A Coburn; Kristen L G Jones; Marc Ferrer; Paul Zuck; Berta Strulovici; Eric A Price; Guoxin Wu; Abigail L Wolfe; Janet Lineberger; Mohinder K Sardana; Katherine Tugusheva; Beth L Pietrak; Ming-Chih Crouthamel; Ming-Tain Lai; Elizabeth Chen Dodson; Renzo Bazzo; Xiao-Ping Shi; Adam J Simon; Yueming Li; Daria J Hazuda
Compounds that bind APP and inhibit Abeta processing in vitro suggest a novel approach to Alzheimer disease therapeutics.
The Journal of biological chemistry 2005;280(18):17792-7.
2005: Steven W Ludmerer; Donald J Graham; Evelyn Boots; Edward M Murray; Amy L Simcoe; Eric J Markel; Jay A Grobler; Osvaldo A Flores; David B Olsen; Daria J Hazuda; Robert L LaFemina
Replication fitness and NS5B drug sensitivity of diverse hepatitis C virus isolates characterized by using a transient replication assay.
Antimicrobial agents and chemotherapy 2005;49(5):2059-69.
2005: Dooseop Kim; Liping Wang; Jeffrey J Hale; Christopher L Lynch; Richard J Budhu; Malcolm MacCoss; Sander G Mills; Lorraine Malkowitz; Sandra L Gould; Julie A DeMartino; Martin S Springer; Daria J Hazuda; Michael Miller; Joseph Kessler; Renee C Hrin; Gwen Carver; Anthony Carella; Karen Henry; Janet Lineberger; William A Schleif; Emilio A Emini
Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties.
Bioorganic & medicinal chemistry letters 2005;15(8):2129-34.
2005: Xiao-Ping Shi; Katherine Tugusheva; James E Bruce; Adam Lucka; Elizabeth Chen-Dodson; Binghua Hu; Guo-Xin Wu; Eric Price; Robert B Register; Janet Lineberger; Ron Miller; Mei-Jy Tang; Amy S Espeseth; Jason Kahana; Abigail Wolfe; Ming-Chih Crouthamel; Sethu Sankaranarayanan; Adam Simon; Lin Chen; Ming-Tain Lai; Beth L Pietrak; Jillian DiMuzio; Yueming Li; Min Xu; Qian Huang; Victor M Garsky; Mohinder K Sardana; Daria J Hazuda
Novel mutations introduced at the beta-site of amyloid beta protein precursor enhance the production of amyloid beta peptide by BACE1 in vitro and in cells.
Journal of Alzheimer's disease : JAD 2005;7(2):139-48; discussion 173-80.
2005: Shrenik K Shah; Natalie Chen; Ravindra N Guthikonda; Sander G Mills; Lorraine Malkowitz; Martin S Springer; Sandra L Gould; Julie A DeMartino; Anthony Carella; Gwen Carver; Karen Holmes; William A Schleif; Renee Danzeisen; Daria J Hazuda; Joseph Kessler; Janet Lineberger; Michael Miller; Emilio A Emini; Malcolm MacCoss
Synthesis and evaluation of CCR5 antagonists containing modified 4-piperidinyl-2-phenyl-1-(phenylsulfonylamino)-butane.
Bioorganic & medicinal chemistry letters 2005;15(4):977-82.
2005: Cathryn A Shaw-Reid; Bradley P Feuston; Vandna Munshi; Krista Getty; Julie Krueger; Daria J Hazuda; Michael A Parniak; Michael D Miller; Dale Lewis
Dissecting the effects of DNA polymerase and ribonuclease H inhibitor combinations on HIV-1 reverse-transcriptase activities.
Biochemistry 2005;44(5):1595-606.
2004: David B Olsen; Anne B Eldrup; Linda Bartholomew; Balkrishen Bhat; Michele Bosserman; Alessandra Ceccacci; Lawrence F Colwell; John F Fay; Osvaldo A Flores; Krista Getty; Jay A Grobler; Robert L LaFemina; Eric J Markel; Giovanni Migliaccio; Marija Prhavc; Mark Stahlhut; Joanne E Tomassini; Malcolm MacCoss; Daria J Hazuda; Steven S Carroll
A 7-deaza-adenosine analog is a potent and selective inhibitor of hepatitis C virus replication with excellent pharmacokinetic properties.
Antimicrobial agents and chemotherapy 2004;48(10):3944-53.
2004: Daria J Hazuda; Steven D Young; James P Guare; Neville J Anthony; Robert P Gomez; John S Wai; Joseph P Vacca; Larry Handt; Sherri L Motzel; Hilton J Klein; Geethanjali Dornadula; Robert M Danovich; Marc V Witmer; Keith A Wilson; Lynda Tussey; William A Schleif; Lori S Gabryelski; Lixia Jin; Michael D Miller; Danilo R Casimiro; Emilio A Emini; John W Shiver
Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaques.
Science (New York, N.Y.) 2004;305(5683):528-32.
2004: K Shankaran; Karla L Donnelly; Shrenik K Shah; Charles G Caldwell; Ping Chen; Paul E Finke; Bryan Oates; Malcolm MacCoss; Sander G Mills; Julie A DeMartino; Sandra L Gould; Lorraine Malkowitz; Salvatore J Siciliano; Martin S Springer; Gloria Y Kwei; Anthony Carella; Gwen Carver; Renee Danzeisen; Daria J Hazuda; Karen Holmes; Joseph Kessler; Janet Lineberger; Michael D Miller; Emilio A Emini; William A Schleif
Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists.
Bioorganic & medicinal chemistry letters 2004;14(13):3589-93.
2004: K Shankaran; Karla L Donnelly; Shrenik K Shah; Ravindra N Guthikonda; Malcolm MacCoss; Sander G Mills; Sandra L Gould; Lorraine Malkowitz; Salvatore J Siciliano; Martin S Springer; Anthony Carella; Gwen Carver; Daria J Hazuda; Karen Holmes; Joseph Kessler; Janet Lineberger; Michael D Miller; Emilio A Emini; William A Schleif
Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor.
Bioorganic & medicinal chemistry letters 2004;14(13):3419-24.
2004: Kithsiri B Herath; Hiranthi Jayasuriya; Gerald F Bills; Jon D Polishook; Anne W Dombrowski; Ziqiang Guan; Peter J Felock; Daria J Hazuda; Sheo B Singh
Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide.
Journal of natural products 2004;67(5):872-4.
2004: Michael D Miller; Daria J Hazuda
HIV resistance to the fusion inhibitor enfuvirtide: mechanisms and clinical implications.
Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy 2004;7(2):89-95.
2004: Min Shu; Jennifer L Loebach; Kerry A Parker; Sander G Mills; Kevin Chapman; Dong-Ming Shen; Lorraine Malkowitz; Martin S Springer; Sandra L Gould; Julie A DeMartino; Salvatore J Siciliano; Jerry Di Salvo; Kathryn Lyons; James V Pivnichny; Gloria Y Kwei; Anthony Carella; Gwen Carver; Karen Holmes; William A Schleif; Renee Danzeisen; Daria J Hazuda; Joseph Kessler; Janet Lineberger; Michael D Miller; Emilio A Emini
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.
Bioorganic & medicinal chemistry letters 2004;14(4):947-52.
2004: Dong-Ming Shen; Min Shu; Christopher A Willoughby; Shrenik Shah; Christopher L Lynch; Jeffrey J Hale; Sander G Mills; Kevin Chapman; Lorraine Malkowitz; Martin S Springer; Sandra L Gould; Julie A DeMartino; Salvatore J Siciliano; Kathryn Lyons; James V Pivnichny; Gloria Y Kwei; Anthony Carella; Gwen Carver; Karen Holmes; William A Schleif; Renee Danzeisen; Daria J Hazuda; Joseph Kessler; Janet Lineberger; Michael D Miller; Emilio A Emini
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.
Bioorganic & medicinal chemistry letters 2004;14(4):941-5.
2004: Dong-Ming Shen; Min Shu; Sander G Mills; Kevin Chapman; Lorraine Malkowitz; Martin S Springer; Sandra L Gould; Julie A DeMartino; Salvatore J Siciliano; Gloria Y Kwei; Anthony Carella; Gwen Carver; Karen Holmes; William A Schleif; Renee Danzeisen; Daria J Hazuda; Joseph Kessler; Janet Lineberger; Michael D Miller; Emilio A Emini
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains.
Bioorganic & medicinal chemistry letters 2004;14(4):935-9.
2004: Stephen F Brady; Satendra Singh; Ming-Chih Crouthamel; M Katharine Holloway; Craig A Coburn; Victor M Garsky; Michael J Bogusky; Michael Pennington; Joseph P Vacca; Daria J Hazuda; Ming-Tain Lai
Rational design and synthesis of selective BACE-1 inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(3):601-4.
2003: Giovanni Migliaccio; Joanne E Tomassini; Steven S Carroll; Licia tomei; Sergio Altamura; Balkrishen Bhat; Linda Bartholomew; Michele Bosserman; Alessandra Ceccacci; Lawrence F Colwell; Riccardo Cortese; Raffaele De Francesco; Anne B Eldrup; Krista Getty; Xiaoli S Hou; Robert L LaFemina; Steven W Ludmerer; Malcolm MacCoss; Daniel R McMasters; Mark Stahlhut; David B Olsen; Daria J Hazuda; Osvaldo A Flores
Characterization of resistance to non-obligate chain-terminating ribonucleoside analogs that inhibit hepatitis C virus replication in vitro.
The Journal of biological chemistry 2003;278(49):49164-70.
2003: John G Ondeyka; Deborah L Zink; Anne W Dombrowski; Jon D Polishook; Peter J Felock; Daria J Hazuda; Sheo B Singh
Isolation, structure and HIV-1 integrase inhibitory activity of exophillic acid, a novel fungal metabolite from Exophiala pisciphila.
The Journal of antibiotics 2003;56(12):1018-23.
2003: Sheo B Singh; Hiranthi Jayasuriya; Raymond Dewey; Jon D Polishook; Anne W Dombrowski; Deborah L Zink; Ziqiang Guan; Javier Collado; Gonzalo Platas; Fernando Pelaez; Peter J Felock; Daria J Hazuda
Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites.
Journal of industrial microbiology & biotechnology 2003;30(12):721-31.
2003: Sheo B Singh; John G Ondeyka; William A Schleif; Peter J Felock; Daria J Hazuda
Chemistry and structure-activity relationship of HIV-1 integrase inhibitor integracide B and related natural products.
Journal of natural products 2003;66(10):1338-44.
2003: Christopher L Lynch; Jeffrey J Hale; Richard J Budhu; Amy L Gentry; Paul E Finke; Charles G Caldwell; Sander G Mills; Malcolm MacCoss; Dong-Ming Shen; Kevin Chapman; Lorraine Malkowitz; Martin S Springer; Sandra L Gould; Julie A DeMartino; Salvatore J Siciliano; Margaret A Cascieri; Anthony Carella; Gwen Carver; Karen Holmes; William A Schleif; Renee Danzeisen; Daria J Hazuda; Joseph Kessler; Janet Lineberger; Michael Miller; Emilio A Emini
CCR5 antagonists: 3-(pyrrolidin-1-yl)propionic acid analogues with potent anti-HIV activity.
Organic letters 2003;5(14):2473-5.
2003: Ming-Tain Lai; Elizabeth Chen; Ming-Chih Crouthamel; Jillian DiMuzio-Mower; Min Xu; Qian Huang; Eric Price; Robert B Register; Xiao-Ping Shi; Dorit B Donoviel; alan bernstein; Daria J Hazuda; Stephen J Gardell; Yueming Li
Presenilin-1 and presenilin-2 exhibit distinct yet overlapping gamma-secretase activities.
The Journal of biological chemistry 2003;278(25):22475-81.
2003: Xiao-Ping Shi; Katherine Tugusheva; James E Bruce; Adam Lucka; Guo-Xin Wu; Elizabeth Chen-Dodson; Eric Price; Yueming Li; Min Xu; Qian Huang; Mohinder K Sardana; Daria J Hazuda
Beta-secretase cleavage at amino acid residue 34 in the amyloid beta peptide is dependent upon gamma-secretase activity.
The Journal of biological chemistry 2003;278(23):21286-94.
2003: Sheo B Singh; Deborah L Zink; Anne W Dombrowski; Jon D Polishook; John G Ondeyka; Jorden Hirshfield; Peter J Felock; Daria J Hazuda
Integracides: tetracyclic triterpenoid inhibitors of HIV-1 integrase produced by Fusarium sp.
Bioorganic & medicinal chemistry 2003;11(7):1577-82.
2003: Hiranthi Jayasuriya; Ziqiang Guan; Jon D Polishook; Anne W Dombrowski; Peter J Felock; Daria J Hazuda; Sheo B Singh
Isolation, structure, and HIV-1 integrase inhibitory activity of Cytosporic acid, a fungal metabolite produced by a Cytospora sp.
Journal of natural products 2003;66(4):551-3.
2003: Sheo B Singh; Deborah L Zink; Gerald F Bills; Ana Teran; Keith C Silverman; Russell Lingham; Peter J Felock; Daria J Hazuda
Four novel bis-(naphtho-gamma-pyrones) isolated from Fusarium species as inhibitors of HIV-1 integrase.
Bioorganic & medicinal chemistry letters 2003;13(4):713-7.
2003: Linghang Zhuang; John S Wai; Mark W Embrey; Thorsten E Fisher; Melissa S Egbertson; Linda S Payne; James P Guare; Joseph P Vacca; Daria J Hazuda; Peter J Felock; Abigail L Wolfe; Kara A Stillmock; Marc V Witmer; Gregory Moyer; William A Schleif; Lori Gabryelski; Yvonne M Leonard; Joseph J Lynch; Stuart R Michelson; Steven D Young
Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.
Journal of medicinal chemistry 2003;46(4):453-6.
2003: Christopher A Willoughby; Keith G Rosauer; Jeffrey J Hale; Richard J Budhu; Sander G Mills; Kevin Chapman; Malcolm MacCoss; Lorraine Malkowitz; Martin S Springer; Sandra L Gould; Julie A DeMartino; Salvatore J Siciliano; Margaret A Cascieri; Anthony Carella; Gwen Carver; Karen Holmes; William A Schleif; Renee Danzeisen; Daria J Hazuda; Joseph Kessler; Janet Lineberger; Michael Miller; Emilio A Emini
1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.
Bioorganic & medicinal chemistry letters 2003;13(3):427-31.
2003: Cathryn A Shaw-Reid; Vandna Munshi; Pia Graham; Abigail Wolfe; Marc V Witmer; Renee Danzeisen; David B Olsen; Steven S Carroll; Mark W Embrey; John S Wai; Michael D Miller; James L Cole; Daria J Hazuda
Inhibition of HIV-1 ribonuclease H by a novel diketo acid, 4-[5-(benzoylamino)thien-2-yl]-2,4-dioxobutanoic acid.
The Journal of biological chemistry 2003;278(5):2777-80.
2003: Christopher L Lynch; Christopher A Willoughby; Jeffrey J Hale; Edward J Holson; Richard J Budhu; Amy L Gentry; Keith G Rosauer; Charles G Caldwell; Ping Chen; Sander G Mills; Malcolm MacCoss; Scott Berk; Liya Chen; Kevin Chapman; Lorraine Malkowitz; Martin S Springer; Sandra L Gould; Julie A DeMartino; Salvatore J Siciliano; Margaret A Cascieri; Anthony Carella; Gwen Carver; Karen Holmes; William A Schleif; Renee Danzeisen; Daria J Hazuda; Joseph Kessler; Janet Lineberger; Michael Miller; Emilio A Emini
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.
Bioorganic & medicinal chemistry letters 2003;13(1):119-23.
2002: Christopher L Lynch; Jeffrey J Hale; Richard J Budhu; Amy L Gentry; Sander G Mills; Kevin Chapman; Malcolm MacCoss; Lorraine Malkowitz; Martin S Springer; Sandra L Gould; Julie A DeMartino; Salvatore J Siciliano; Margaret A Cascieri; Anthony Carella; Gwen Carver; Karen Holmes; William A Schleif; Renee Danzeisen; Daria J Hazuda; Joseph Kessler; Janet Lineberger; Michael Miller; Emilio A Emini
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.
Bioorganic & medicinal chemistry letters 2002;12(20):3001-4.
2002: Jeffrey J Hale; Richard J Budhu; Sander G Mills; Malcolm MacCoss; Sandra L Gould; Julie A DeMartino; Martin S Springer; Salvatore J Siciliano; Lorraine Malkowitz; William A Schleif; Daria J Hazuda; Michael Miller; Joseph Kessler; Renee Danzeisen; Karen Holmes; Janet Lineberger; Anthony Carella; Gwen Carver; Emilio A Emini
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity.
Bioorganic & medicinal chemistry letters 2002;12(20):2997-3000.
2002: Jay A Grobler; Kara A Stillmock; Binghua Hu; Marc V Witmer; Peter J Felock; Amy S Espeseth; Abigail Wolfe; Melissa S Egbertson; Michele Bourgeois; Jeffrey Y Melamed; John S Wai; Steve Young; Joseph P Vacca; Daria J Hazuda
Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymes.
Proceedings of the National Academy of Sciences of the United States of America 2002;99(10):6661-6.
2002: Sheo B Singh; Kithsiri B Herath; Ziqiang Guan; Deborah L Zink; Anne W Dombrowski; Jon D Polishook; Keith C Silverman; Russell Lingham; Peter J Felock; Daria J Hazuda
Integramides A and B, two novel non-ribosomal linear peptides containing nine C(alpha)-methyl amino acids produced by fungal fermentations that are inhibitors of HIV-1 integrase.
Organic letters 2002;4(9):1431-4.
2002: Sheo B Singh; Deborah L Zink; Brian Heimbach; Olga Genilloud; Ana Teran; Keith C Silverman; Russell Lingham; Peter J Felock; Daria J Hazuda
Structure, stereochemistry, and biological activity of integramycin, a novel hexacyclic natural product produced by Actinoplanes sp. that inhibits HIV-1 integrase.
Organic letters 2002;4(7):1123-6.
2002: Janet Lineberger; Renee Danzeisen; Daria J Hazuda; Adam J Simon; Michael D Miller
Altering expression levels of human immunodeficiency virus type 1 gp120-gp41 affects efficiency but not kinetics of cell-cell fusion.
Journal of virology 2002;76(7):3522-33.
2002: Christopher L Lynch; Amy L Gentry; Jeffrey J Hale; Sander G Mills; Malcolm MacCoss; Lorraine Malkowitz; Martin S Springer; Sandra L Gould; Julie A DeMartino; Salvatore J Siciliano; Margaret A Cascieri; George A Doss; Anthony Carella; Gwen Carver; Karen Holmes; William A Schleif; Renee Danzeisen; Daria J Hazuda; Joseph Kessler; Janet Lineberger; Michael Miller; Emilio A Emini
CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines.
Bioorganic & medicinal chemistry letters 2002;12(4):677-9.
2002: Jon H Condra; Michael D Miller; Daria J Hazuda; Emilio A Emini
Potential new therapies for the treatment of HIV-1 infection.
Annual review of medicine 2002;53():541-55.
2001: Christopher A Willoughby; Scott Berk; Keith G Rosauer; SJ Degrado; Kevin Chapman; Sandra L Gould; Martin S Springer; Lorraine Malkowitz; William A Schleif; Daria J Hazuda; Michael Miller; Joseph Kessler; Renee Danzeisen; Karen Holmes; Janet Lineberger; Anthony Carella; Gwen Carver; Emilio A Emini
Combinatorial synthesis of CCR5 antagonists.
Bioorganic & medicinal chemistry letters 2001;11(24):3137-41.
2001: Dooseop Kim; Liping Wang; Charles G Caldwell; Ping Chen; Paul E Finke; Bryan Oates; Malcolm MacCoss; Sander G Mills; Lorraine Malkowitz; Sandra L Gould; Julie A DeMartino; Martin S Springer; Daria J Hazuda; Michael Miller; Joseph Kessler; Renee Danzeisen; Gwen Carver; Anthony Carella; Karen Holmes; Janet Lineberger; William A Schleif; Emilio A Emini
Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection.
Bioorganic & medicinal chemistry letters 2001;11(24):3103-6.
2001: Dooseop Kim; Liping Wang; Charles G Caldwell; Ping Chen; Paul E Finke; Bryan Oates; Malcolm MacCoss; Sander G Mills; Lorraine Malkowitz; Sandra L Gould; Julie A DeMartino; Martin S Springer; Daria J Hazuda; Michael Miller; Joseph Kessler; Renee Danzeisen; Gwen Carver; Anthony Carella; Karen Holmes; Janet Lineberger; William A Schleif; Emilio A Emini
Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection.
Bioorganic & medicinal chemistry letters 2001;11(24):3099-102.
2001: Jeffrey J Hale; Richard J Budhu; E B Holson; Paul E Finke; Bryan Oates; Sander G Mills; Malcolm MacCoss; Sandra L Gould; Julie A DeMartino; Martin S Springer; Salvatore J Siciliano; Lorraine Malkowitz; William A Schleif; Daria J Hazuda; Michael Miller; Joseph Kessler; Renee Danzeisen; Karen Holmes; Janet Lineberger; Anthony Carella; Gwen Carver; Emilio A Emini
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity.
Bioorganic & medicinal chemistry letters 2001;11(20):2741-5.
2001: Michael D Miller; Daria J Hazuda
New antiretroviral agents: looking beyond protease and reverse transcriptase.
Current opinion in microbiology 2001;4(5):535-9.
2001: Paul E Finke; Bryan Oates; Sander G Mills; Malcolm MacCoss; Lorraine Malkowitz; Martin S Springer; Sandra L Gould; Julie A DeMartino; Anthony Carella; Gwen Carver; Karen Holmes; Renee Danzeisen; Daria J Hazuda; Joseph Kessler; Janet Lineberger; Michael Miller; William A Schleif; Emilio A Emini
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes.
Bioorganic & medicinal chemistry letters 2001;11(18):2475-9.
2001: Sheo B Singh; Hiranthi Jayasuriya; Gino M Salituro; Deborah L Zink; A Shafiee; B Heimbuch; Keith C Silverman; Russell Lingham; Olga Genilloud; Ana Teran; D Vilella; Peter J Felock; Daria J Hazuda
The complestatins as HIV-1 integrase inhibitors. Efficient isolation, structure elucidation, and inhibitory activities of isocomplestatin, chloropeptin I, new complestatins, A and B, and acid-hydrolysis products of chloropeptin I.
Journal of natural products 2001;64(7):874-82.
2001: Paul E Finke; Laura C Meurer; Bryan Oates; Sander G Mills; Malcolm MacCoss; Lorraine Malkowitz; Martin S Springer; Bruce L Daugherty; Sandra L Gould; Julie A DeMartino; Salvatore J Siciliano; Anthony Carella; Gwen Carver; Karen Holmes; Renee Danzeisen; Daria J Hazuda; Joseph Kessler; Janet Lineberger; Michael Miller; William A Schleif; Emilio A Emini
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes.
Bioorganic & medicinal chemistry letters 2001;11(2):265-70.
2001: C P Dorn; Paul E Finke; Bryan Oates; Richard J Budhu; Sander G Mills; Malcolm MacCoss; Lorraine Malkowitz; Martin S Springer; Bruce L Daugherty; Sandra L Gould; Julie A DeMartino; Salvatore J Siciliano; Anthony Carella; Gwen Carver; Karen Holmes; Renee Danzeisen; Daria J Hazuda; Joseph Kessler; Janet Lineberger; Michael Miller; William A Schleif; Emilio A Emini
Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes.
Bioorganic & medicinal chemistry letters 2001;11(2):259-64.
2000: John S Wai; Melissa S Egbertson; L S Payne; Thorsten E Fisher; Mark W Embrey; L O Tran; Jeffrey Y Melamed; H M Langford; James P Guare; Linghang Zhuang; V E Grey; Joseph P Vacca; M Katharine Holloway; Adel M Naylor-Olsen; Daria J Hazuda; Peter J Felock; Abigail L Wolfe; Kara A Stillmock; William A Schleif; Lori Gabryelski; Steven D Young
4-Aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells.
Journal of medicinal chemistry 2000;43(26):4923-6.
2000: Amy S Espeseth; Peter J Felock; Abigail Wolfe; Marc V Witmer; Jay A Grobler; Neville J Anthony; Melissa S Egbertson; Jeffrey Y Melamed; S Young; Terence G Hamill; James L Cole; Daria J Hazuda
HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase.
Proceedings of the National Academy of Sciences of the United States of America 2000;97(21):11244-9.
2000: Zhongguo Chen; Youwei Yan; Sanjeev Munshi; Yueming Li; Joan Zugay-Murphy; Bei Xu; Marc V Witmer; Peter J Felock; Abigail Wolfe; Vinod Sardana; Emilio A Emini; Daria J Hazuda; Lawrence C Kuo
X-ray structure of simian immunodeficiency virus integrase containing the core and C-terminal domain (residues 50-293)--an initial glance of the viral DNA binding platform.
Journal of molecular biology 2000;296(2):521-33.
2000: Sheo B Singh; Peter J Felock; Daria J Hazuda
Chemical and enzymatic modifications of integric acid and HIV-1 integrase inhibitory activity.
Bioorganic & medicinal chemistry letters 2000;10(3):235-8.
2000: Daria J Hazuda; Peter J Felock; Marc V Witmer; Abigail Wolfe; Kara A Stillmock; Jay A Grobler; Amy S Espeseth; Lori Gabryelski; William A Schleif; CU Blau; Michael D Miller
Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells.
Science (New York, N.Y.) 2000;287(5453):646-50.
1999: Yueming Li; Youwei Yan; Joan Zugay-Murphy; Bei Xu; James L Cole; Marc V Witmer; Peter J Felock; Abigail Wolfe; Daria J Hazuda; Mohinder K Sardana; Zhongguo Chen; Lawrence C Kuo; Vinod Sardana
Purification, solution properties and crystallization of SIV integrase containing a continuous core and C-terminal domain.
Acta crystallographica. Section D, Biological crystallography 1999;55(Pt 11):1906-10.
1999: G Goodarzi; M Pursley; Peter J Felock; Marc V Witmer; Daria J Hazuda; K Brackmann; Duane P Grandgenett
Efficiency and fidelity of full-site integration reactions using recombinant simian immunodeficiency virus integrase.
Journal of virology 1999;73(10):8104-11.
1999: O Flores; G Lee; J Kessler; M Miller; W Schlief; Joanne E Tomassini; Daria J Hazuda
Host-cell positive transcription elongation factor b kinase activity is essential and limiting for HIV type 1 replication.
Proceedings of the National Academy of Sciences of the United States of America 1999;96(13):7208-13.
1999: Daria J Hazuda; CU Blau; Peter J Felock; J Hastings; B Pramanik; Abigail Wolfe; Frederic D Bushman; Chris Farnet; M Goetz; M Williams; Keith C Silverman; Russell Lingham; S Singh
Isolation and characterization of novel human immunodeficiency virus integrase inhibitors from fungal metabolites.
Antiviral chemistry & chemotherapy 1999;10(2):63-70.
1997: H S Mancebo; G Lee; J Flygare; Joanne E Tomassini; P Luu; Y Zhu; Junmin Peng; CU Blau; Daria J Hazuda; D Price; O Flores
P-TEFb kinase is required for HIV Tat transcriptional activation in vivo and in vitro.
Genes & development 1997;11(20):2633-44.
1997: Daria J Hazuda; Peter J Felock; J C Hastings; B Pramanik; Abigail L Wolfe
Differential divalent cation requirements uncouple the assembly and catalytic reactions of human immunodeficiency virus type 1 integrase.
Journal of virology 1997;71(9):7005-11.
1997: Daria J Hazuda; Peter J Felock; J C Hastings; B Pramanik; Abigail L Wolfe
Discovery and analysis of inhibitors of the human immunodeficiency integrase.
Drug design and discovery 1997;15(1):17-24.
1997: Daria J Hazuda; Peter J Felock; J Hastings; B Pramanik; Abigail Wolfe; G Goodarzi; Ajaykumar Vora; K Brackmann; Duane P Grandgenett
Equivalent inhibition of half-site and full-site retroviral strand transfer reactions by structurally diverse compounds.
Journal of virology 1997;71(1):807-11.
1996: R L LaFemina; K Bakshi; W J Long; B Pramanik; C A Veloski; B S Wolanski; A I Marcy; Daria J Hazuda
Characterization of a soluble stable human cytomegalovirus protease and inhibition by M-site peptide mimics.
Journal of virology 1996;70(7):4819-24.
1996: A L Wolfe; Peter J Felock; J C Hastings; C U Blau; Daria J Hazuda
The role of manganese in promoting multimerization and assembly of human immunodeficiency virus type 1 integrase as a catalytically active complex on immobilized long terminal repeat substrates.
Journal of virology 1996;70(3):1424-32.
1996: V Byrnes; Daria J Hazuda
A system to analyze and identify inhibitors of HIV-1 gene regulation using a defective integrated provirus.
Methods in enzymology 1996;275():348-61.
1995: R L LaFemina; P L Graham; K LeGrow; J C Hastings; A Wolfe; S D Young; Emilio A Emini; Daria J Hazuda
Inhibition of human immunodeficiency virus integrase by bis-catechols.
Antimicrobial agents and chemotherapy 1995;39(2):320-4.
1994: Joanne E Tomassini; Harold G Selnick; Mary-Ellen Davies; M E Armstrong; J Baldwin; M Bourgeois; J Hastings; Daria J Hazuda; J Lewis; William L McClements
Inhibition of cap (m7GpppXm)-dependent endonuclease of influenza virus by 4-substituted 2,4-dioxobutanoic acid compounds.
Antimicrobial agents and chemotherapy 1994;38(12):2827-37.
1994: Daria J Hazuda; J C Hastings; A L Wolfe; Emilio A Emini
A novel assay for the DNA strand-transfer reaction of HIV-1 integrase.
Nucleic acids research 1994;22(6):1121-2.
1994: Daria J Hazuda; A L Wolfe; J C Hastings; H L Robbins; P L Graham; R L LaFemina; Emilio A Emini
Viral long terminal repeat substrate binding characteristics of the human immunodeficiency virus type 1 integrase.
The Journal of biological chemistry 1994;269(6):3999-4004.
1993: Helen C Perry; Daria J Hazuda; William L McClements
The DNA binding domain of herpes simplex virus type 1 origin binding protein is a transdominant inhibitor of virus replication.
Virology 1993;193(1):73-9.
1992: Daria J Hazuda; Helen C Perry; William L McClements
Cooperative interactions between replication origin-bound molecules of herpes simplex virus origin-binding protein are mediated via the amino terminus of the protein.
The Journal of biological chemistry 1992;267(20):14309-15.
1991: Daria J Hazuda; Helen C Perry; A M Naylor; William L McClements
Characterization of the herpes simplex virus origin binding protein interaction with OriS.
The Journal of biological chemistry 1991;266(36):24621-6.