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Dale Kempf

Research Profile

Chemicals & Drugs

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HIV-1
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TOP 3
David A DeGoey; David J Grampovnik; Wenping He; Dale J Kempf; Preethi Krishnan; Dachun Liu; Kennan Marsh; Akhteruzzaman Molla; Tami Pilot-Matias; John K Pratt; Michael D Tufano; David A Betebenner; Clarence J Maring
Discovery of pyrido[2,3-d]pyrimidine-based inhibitors of HCV NS5A.
A Chris Krueger; David W A Beno; David A Betebenner; Robert Carrick; Brian E Green; Wenping He; Dachun Liu; Darold L Madigan; Clarence J Maring; Keith F McDaniel; Hongmei Mo; Akhteruzzaman Molla; Christopher E Motter; Tami Pilot-Matias; Michael D Tufano; Dale J Kempf
Novel hepatitis C virus replicon inhibitors: synthesis and structure-activity relationships of fused pyrimidine derivatives.
David A DeGoey; Tatyana Dekhtyar; William J Flosi; David J Grampovnik; Larry Klein; Mulugeta Mamo; Akhteruzzaman Molla; Vincent S Stoll; Hui-Ju Chen; Dale J Kempf
P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses.

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All Publications

2013: David A DeGoey; David J Grampovnik; Wenping He; Dale J Kempf; Preethi Krishnan; Dachun Liu; Kennan Marsh; Akhteruzzaman Molla; Tami Pilot-Matias; John K Pratt; Michael D Tufano; David A Betebenner; Clarence J Maring
Discovery of pyrido[2,3-d]pyrimidine-based inhibitors of HCV NS5A.
Bioorganic & medicinal chemistry letters 2013;23(12):3627-30.
2012: A Chris Krueger; David W A Beno; David A Betebenner; Robert Carrick; Brian E Green; Wenping He; Dachun Liu; Darold L Madigan; Clarence J Maring; Keith F McDaniel; Hongmei Mo; Akhteruzzaman Molla; Christopher E Motter; Tami Pilot-Matias; Michael D Tufano; Dale J Kempf
Novel hepatitis C virus replicon inhibitors: synthesis and structure-activity relationships of fused pyrimidine derivatives.
Bioorganic & medicinal chemistry letters 2012;22(6):2212-5.
2011: David A DeGoey; Tatyana Dekhtyar; William J Flosi; David J Grampovnik; Larry Klein; Mulugeta Mamo; Akhteruzzaman Molla; Vincent S Stoll; Hui-Ju Chen; Dale J Kempf
P1-substituted symmetry-based human immunodeficiency virus protease inhibitors with potent antiviral activity against drug-resistant viruses.
Journal of medicinal chemistry 2011;54(20):7094-104.
2011: Douglas K Hutchinson; Charles A Flentge; Pamela L Donner; Rolf Wagner; Clarence J Maring; Warren M Kati; Yaya Liu; Sherie Masse; Tim Middleton; Hongmei Mo; Debra Montgomery; Wen W Jiang; Gennadiy Koev; David W A Beno; Kent D Stewart; Vincent S Stoll; Akhteruzzaman Molla; Dale J Kempf
Hepatitis C NS5B polymerase inhibitors: functional equivalents for the benzothiadiazine moiety.
Bioorganic & medicinal chemistry letters 2011;21(6):1876-9.
2010: Thomas P Young; Neil T Parkin; Eric Stawiski; Tami Pilot-Matias; Roger Trinh; Dale J Kempf; Michael Norton
Prevalence, mutation patterns, and effects on protease inhibitor susceptibility of the L76V mutation in HIV-1 protease.
Antimicrobial agents and chemotherapy 2010;54(11):4903-6.
2010: Yi Yang; Annette J Dahly-Vernon; Eric A G Blomme; Jie Lai-Zhang; Dale J Kempf; Kennan Marsh; Yvette A Harrington; Steven H Nye; Darin L Evans; Richard J Roman; Howard J Jacob; Jeffrey F Waring
Liver transcriptomic changes associated with ritonavir-induced hyperlipidemia in sensitive and resistant strains of rats.
Veterinary journal (London, England : 1997) 2010;185(1):75-82.
2010: Jeffrey F Waring; Rita Ciurlionis; Kennan Marsh; Larry Klein; David A DeGoey; John T Randolph; Brian Spear; Dale J Kempf
Identification of proteasome gene regulation in a rat model for HIV protease inhibitor-induced hyperlipidemia.
Archives of toxicology 2010;84(4):263-70.
2010: Kent D Stewart; Jeffrey R Huth; Teresa I Ng; Keith F McDaniel; Rebecca Newlin Hutchinson; Vincent S Stoll; Renaldo R Mendoza; Edmund D Matayoshi; Robert Carrick; Hongmei Mo; Jean Severin; Karl Walter; Paul L Richardson; Leo W Barrett; Robert P Meadows; Steve Anderson; William Kohlbrenner; Clarence J Maring; Dale J Kempf; Akhter Molla; Edward T Olejniczak
Non-peptide entry inhibitors of HIV-1 that target the gp41 coiled coil pocket.
Bioorganic & medicinal chemistry letters 2010;20(2):612-7.
2009: Charles A Flentge; John T Randolph; Peggy P Huang; Larry Klein; Kennan Marsh; John Harlan; Dale J Kempf
Synthesis and evaluation of inhibitors of cytochrome P450 3A (CYP3A) for pharmacokinetic enhancement of drugs.
Bioorganic & medicinal chemistry letters 2009;19(18):5444-8.
2009: John T Randolph; Charles A Flentge; Peggy P Huang; Douglas K Hutchinson; Larry Klein; Hock Ben Lim; Rubina Mondal; Thomas Reisch; Debra A Montgomery; Wen W Jiang; Sherie Masse; Lisa E Hernandez; Rodger F Henry; Yaya Liu; Gennadiy Koev; Warren M Kati; Kent D Stewart; David W A Beno; Akhteruzzaman Molla; Dale J Kempf
Synthesis and biological characterization of B-ring amino analogues of potent benzothiadiazine hepatitis C virus polymerase inhibitors.
Journal of medicinal chemistry 2009;52(10):3174-83.
2009: David A DeGoey; David J Grampovnik; William J Flosi; Kennan Marsh; Xiu C Wang; Larry Klein; Keith F McDaniel; Yaya Liu; Michelle A Long; Warren M Kati; Akhteruzzaman Molla; Dale J Kempf
Water-soluble prodrugs of the human immunodeficiency virus protease inhibitors lopinavir and ritonavir.
Journal of medicinal chemistry 2009;52(9):2964-70.
2009: David A DeGoey; David J Grampovnik; Charles A Flentge; William J Flosi; Hui-Ju Chen; Clinton M Yeung; John T Randolph; Larry Klein; Tatyana Dekhtyar; Lynn Colletti; Kennan Marsh; Vincent S Stoll; Mulugeta Mamo; David Morfitt; Bach Nguyen; James M Schmidt; Sue J Swanson; Hongmei Mo; Warren M Kati; Akhteruzzaman Molla; Dale J Kempf
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects.
Journal of medicinal chemistry 2009;52(8):2571-86.
2009: Rolf Wagner; Daniel P Larson; David W A Beno; Todd D Bosse; John F Darbyshire; Yi Gao; Bradley D Gates; Wenping He; Rodger F Henry; Lisa E Hernandez; Douglas K Hutchinson; Wen W Jiang; Warren M Kati; Larry Klein; Gennadiy Koev; William Kohlbrenner; A Chris Krueger; Jinrong Liu; Yaya Liu; Michelle A Long; Clarence J Maring; Sherie Masse; Tim Middleton; Debra A Montgomery; John K Pratt; Patricia Stuart; Akhteruzzaman Molla; Dale J Kempf
Inhibitors of hepatitis C virus polymerase: synthesis and biological characterization of unsymmetrical dialkyl-hydroxynaphthalenoyl-benzothiadiazines.
Journal of medicinal chemistry 2009;52(6):1659-69.
2008: Douglas K Hutchinson; Teresa Rosenberg; Larry Klein; Todd D Bosse; Daniel P Larson; Wenping He; Wen W Jiang; Warren M Kati; William Kohlbrenner; Yaya Liu; Sherie Masse; Tim Middleton; Akhteruzzaman Molla; Debra A Montgomery; David W A Beno; Kent D Stewart; Vincent S Stoll; Dale J Kempf
Hepatitis C NS5B polymerase inhibitors: 4,4-Dialkyl-1-hydroxy-3-oxo-3,4-dihydronaphthalene-3-yl benzothiadiazine derivatives.
Bioorganic & medicinal chemistry letters 2008;18(14):3887-90.
2008: John T Randolph; Xiaolin Zhang; Peggy P Huang; Larry Klein; Kevin A Kurtz; Alex K Konstantinidis; Wenping He; Warren M Kati; Dale J Kempf
Synthesis, antiviral activity, and conformational studies of a P3 aza-peptide analog of a potent macrocyclic tripeptide HCV protease inhibitor.
Bioorganic & medicinal chemistry letters 2008;18(8):2745-50.
2008: Pamela L Donner; Qinghua Xie; John K Pratt; Clarence J Maring; Warren M Kati; Wen Jiang; Yaya Liu; Gennadiy Koev; Sherie Masse; Debra Montgomery; Akhteruzzaman Molla; Dale J Kempf
Des-A-ring benzothiadiazines: inhibitors of HCV genotype 1 NS5B RNA-dependent RNA polymerase.
Bioorganic & medicinal chemistry letters 2008;18(8):2735-8.
2008: Tatyana Dekhtyar; Teresa I Ng; Liangjun Lu; Sherie Masse; David A DeGoey; William J Flosi; David J Grampovnik; Larry Klein; Dale J Kempf; Akhteruzzaman Molla
Characterization of a novel human immunodeficiency virus type 1 protease inhibitor, A-790742.
Antimicrobial agents and chemotherapy 2008;52(4):1337-44.
2008: Sarah Palmer; Frank Maldarelli; Ann Wiegand; Barry Bernstein; George J Hanna; Scott C Brun; Dale J Kempf; John W Mellors; John M Coffin; Martin S King
Low-level viremia persists for at least 7 years in patients on suppressive antiretroviral therapy.
Proceedings of the National Academy of Sciences of the United States of America 2008;105(10):3879-84.
2008: A Chris Krueger; Yibo Xu; Warren M Kati; Dale J Kempf; Clarence J Maring; Keith F McDaniel; Akhteruzzaman Molla; Debra Montgomery; William Kohlbrenner
Synthesis of potent pyrrolidine influenza neuraminidase inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(5):1692-5.
2008: Christine Healan-Greenberg; Jeffrey F Waring; Dale J Kempf; Eric A G Blomme; Rommel G Tirona; Richard B Kim
A human immunodeficiency virus protease inhibitor is a novel functional inhibitor of human pregnane X receptor.
Drug metabolism and disposition: the biological fate of chemicals 2008;36(3):500-7.
2008: Yupeng He; Martin S King; Dale J Kempf; Liangjun Lu; Hock Ben Lim; Preethi Krishnan; Warren M Kati; Tim Middleton; Akhteruzzaman Molla
Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system.
Antimicrobial agents and chemotherapy 2008;52(3):1101-10.
2008: Todd D Bosse; Daniel P Larson; Rolf Wagner; Doug K Hutchinson; Todd W Rockway; Warren M Kati; Yaya Liu; Sherie Masse; Tim Middleton; Hongmei Mo; Debra Montgomery; Wen Jiang; Gennadiy Koev; Dale J Kempf; Akhteruzzaman Molla
Synthesis and SAR of novel 1,1-dialkyl-2(1H)-naphthalenones as potent HCV polymerase inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(2):568-70.
2007: Chih-Ming Chen; Yupeng He; Liangjun Lu; Hock Ben Lim; Rakesh L Tripathi; Tim Middleton; Lisa E Hernandez; David W A Beno; Michelle A Long; Warren M Kati; Todd D Bosse; Daniel P Larson; Rolf Wagner; Robert E Lanford; William Kohlbrenner; Dale J Kempf; Tami Pilot-Matias; Akhteruzzaman Molla
Activity of a potent hepatitis C virus polymerase inhibitor in the chimpanzee model.
Antimicrobial agents and chemotherapy 2007;51(12):4290-6.
2007: Sherie Masse; Xiaozhi Lu; Tatyana Dekhtyar; Liangjun Lu; Gennadiy Koev; Feng Gao; Hongmei Mo; Dale J Kempf; Barry Bernstein; George J Hanna; Akhteruzzaman Molla
In vitro selection and characterization of human immunodeficiency virus type 2 with decreased susceptibility to lopinavir.
Antimicrobial agents and chemotherapy 2007;51(9):3075-80.
2007: Martin S King; Richard Rode; Isabelle Cohen-Codar; Vincent Calvez; Anne-Geneviève Marcelin; George J Hanna; Dale J Kempf
Predictive genotypic algorithm for virologic response to lopinavir-ritonavir in protease inhibitor-experienced patients.
Antimicrobial agents and chemotherapy 2007;51(9):3067-74.
2007: A Chris Krueger; Darold L Madigan; Brian E Green; Douglas K Hutchinson; Wen W Jiang; Warren M Kati; Yaya Liu; Clarence J Maring; Sherie Masse; Keith F McDaniel; Tim Middleton; Hongmei Mo; Akhteruzzaman Molla; Debra A Montgomery; Teresa I Ng; Dale J Kempf
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of unsymmetrical 1-hydroxy-4,4-dialkyl-3-oxo-3,4-dihydronaphthalene benzothiadiazine derivatives.
Bioorganic & medicinal chemistry letters 2007;17(8):2289-92.
2007: Frank Maldarelli; Sarah Palmer; Martin S King; Ann Wiegand; Michael A Polis; JoAnn M Mican; Joseph A Kovacs; Richard Davey; Diane Rock Kress; Robin L Dewar; Shuying Liu; Julia A Metcalf; Catherine A Rehm; Scott C Brun; George J Hanna; Dale J Kempf; John M Coffin; John W Mellors
ART suppresses plasma HIV-1 RNA to a stable set point predicted by pretherapy viremia.
PLoS pathogens 2007;3(4):e46.
2007: Hongmei Mo; Neil Parkin; Kent D Stewart; Liangjun Lu; Tatyana Dekhtyar; Dale J Kempf; Akhteruzzaman Molla
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
Antimicrobial agents and chemotherapy 2007;51(2):732-5.
2007: Dale J Kempf; Cheri Klein; Hui-Ju Chen; Larry Klein; Clinton Yeung; John T Randolph; Yau Yi Lau; Linda E Chovan; Zhiwen Guan; Lisa Hernandez; Teresa M Turner; Peter Dandliker; Kennan Marsh
Pharmacokinetic enhancement of the hepatitis C virus protease inhibitors VX-950 and SCH 503034 by co-dosing with ritonavir.
Antiviral chemistry & chemotherapy 2007;18(3):163-7.
2007: Kent D Stewart; Kevin Steffy; Kevin Harris; John Harlan; Vincent S Stoll; Jeffrey R Huth; Karl A Walter; Emily Gramling-Evans; Renaldo Mendoza; Jean M Severin; Paul L Richardson; Leo W Barrett; Edmund D Matayoshi; Kerry M Swift; Stephen F Betz; Steven W Muchmore; Dale J Kempf; Akhteruzzaman Molla
Design and characterization of an engineered gp41 protein from human immunodeficiency virus-1 as a tool for drug discovery.
Journal of computer-aided molecular design 2007;21(1-3):121-30.
2006: William J Flosi; David A DeGoey; David J Grampovnik; Hui-ju Chen; Larry Klein; Tatyana Dekhtyar; Sherie Masse; Kennan Marsh; Hong Mei Mo; Dale J Kempf
Discovery of imidazolidine-2,4-dione-linked HIV protease inhibitors with activity against lopinavir-resistant mutant HIV.
Bioorganic & medicinal chemistry 2006;14(19):6695-712.
2006: Todd W Rockway; Rong Zhang; Dachun Liu; David A Betebenner; Keith F McDaniel; John K Pratt; David W A Beno; Debra Montgomery; Wen W Jiang; Sherie Masse; Warren M Kati; Tim Middleton; Akhteruzzaman Molla; Clarence J Maring; Dale J Kempf
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-benzyl and N-1-[3-methylbutyl]-4-hydroxy-1,8-naphthyridon-3-yl benzothiadiazine analogs containing substituents on the aromatic ring.
Bioorganic & medicinal chemistry letters 2006;16(14):3833-8.
2006: A Chris Krueger; Darold L Madigan; Wen W Jiang; Warren M Kati; Dachun Liu; Yaya Liu; Clarence J Maring; Sherie Masse; Keith F McDaniel; Tim Middleton; Hongmei Mo; Akhteruzzaman Molla; Debra Montgomery; John K Pratt; Todd W Rockway; Rong Zhang; Dale J Kempf
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-alkyl-4-hydroxyquinolon-3-yl-benzothiadiazine sulfamides.
Bioorganic & medicinal chemistry letters 2006;16(13):3367-70.
2006: John T Randolph; Peggy P Huang; William J Flosi; David A DeGoey; Larry Klein; Clinton M Yeung; Charles A Flentge; Mingua Sun; Chen Zhao; Tatyana Dekhtyar; Hongmei Mo; Lynn Colletti; Warren M Kati; Kennan Marsh; Akhteruzzaman Molla; Dale J Kempf
Synthesis, antiviral activity, and pharmacokinetic evaluation of P3 pyridylmethyl analogs of oximinoarylsulfonyl HIV-1 protease inhibitors.
Bioorganic & medicinal chemistry 2006;14(12):4035-46.
2006: Dale J Kempf; Jeffrey F Waring; David Morfitt; Paige Werner; Brian Ebert; Michael J Mitten; Bach Nguyen; John T Randolph; David A DeGoey; Larry Klein; Kennan Marsh
Practical preclinical model for assessing the potential for unconjugated hyperbilirubinemia produced by human immunodeficiency virus protease inhibitors.
Antimicrobial agents and chemotherapy 2006;50(2):762-4.
2005: Chen Zhao; Hing L Sham; Minghua Sun; Vincent S Stoll; Kent D Stewart; Shuqun Lin; Hongmei Mo; Sudthida Vasavanonda; Ayda Saldivar; Chang Park; Edith J McDonald; Kennan Marsh; Larry Klein; Dale J Kempf; Daniel W Norbeck
Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains.
Bioorganic & medicinal chemistry letters 2005;15(24):5499-503.
2005: Clarence J Maring; Vincent S Stoll; Chen Zhao; Minghua Sun; Allan C Krueger; Kent D Stewart; Darold L Madigan; Warren M Kati; Yibo Xu; Robert Carrick; Debra A Montgomery; Anita J Kempf-Grote; Kennan Marsh; Akhteruzzaman Molla; Kevin Steffy; Hing L Sham; W Graeme Laver; Yu Gui Gu; Dale J Kempf; William Kohlbrenner
Structure-based characterization and optimization of novel hydrophobic binding interactions in a series of pyrrolidine influenza neuraminidase inhibitors.
Journal of medicinal chemistry 2005;48(12):3980-90.
2005: Martin S King; Scott C Brun; Dale J Kempf
Relationship between adherence and the development of resistance in antiretroviral-naive, HIV-1-infected patients receiving lopinavir/ritonavir or nelfinavir.
The Journal of infectious diseases 2005;191(12):2046-52.
2005: Clinton M Yeung; Larry Klein; Charles A Flentge; John T Randolph; Chen Zhao; MingHua Sun; Tatyana Dekhtyar; Vincent S Stoll; Dale J Kempf
Oximinoarylsulfonamides as potent HIV protease inhibitors.
Bioorganic & medicinal chemistry letters 2005;15(9):2275-8.
2005: Anne-Geneviève Marcelin; Isabelle Cohen-Codar; Martin S King; Philippe Colson; Emmanuel Guillevic; Diane Descamps; Claire Lamotte; Véronique Schneider; Jacques Ritter; MICHEL SEGONDY; Hélène Peigue-Lafeuille; Laurence Morand-Joubert; Anne Schmuck; Annick Ruffault; Pierre Palmer; Marie-Laure Chaix; Vincent Mackiewicz; Véronique Brodard; Jacques Izopet; Jacqueline Cottalorda; Evelyne Kohli; Jean-Pierre Chauvin; Dale J Kempf; Gilles Peytavin; Vincent Calvez
Virological and pharmacological parameters predicting the response to lopinavir-ritonavir in heavily protease inhibitor-experienced patients.
Antimicrobial agents and chemotherapy 2005;49(5):1720-6.
2005: John K Pratt; Pamela Donner; Keith F McDaniel; Clarence J Maring; Warren M Kati; Hongmei Mo; Tim Middleton; Yaya Liu; Teresa Ng; Qinghua Xie; Rong Zhang; Debra Montgomery; Akhteruzzaman Molla; Dale J Kempf; William Kohlbrenner
Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines.
Bioorganic & medicinal chemistry letters 2005;15(6):1577-82.
2005: Hongmei Mo; Martin S King; Kathryn King; Akhteruzzaman Molla; Scott C Brun; Dale J Kempf
Selection of resistance in protease inhibitor-experienced, human immunodeficiency virus type 1-infected subjects failing lopinavir- and ritonavir-based therapy: mutation patterns and baseline correlates.
Journal of virology 2005;79(6):3329-38.
2005: Gary T Wang; Sheldon Wang; Robert Gentles; Thomas J Sowin; Clarence J Maring; Dale J Kempf; Warren M Kati; Vincent S Stoll; Kent D Stewart; Graeme Laver
Design, synthesis, and structural analysis of inhibitors of influenza neuraminidase containing a 2,3-disubstituted tetrahydrofuran-5-carboxylic acid core.
Bioorganic & medicinal chemistry letters 2005;15(1):125-8.
2004: Kent D Stewart; Dale J Kempf
An 'inside-the-box' approach to drug resistance.
Chemistry & biology 2004;11(10):1327-8.
2004: Gondi N Kumar; Venkata K Jayanti; Marianne K Johnson; John T Uchic; Samuel Thomas; Ronald D Lee; Brian A Grabowski; Hing L Sham; Dale J Kempf; Jon F Denissen; Kennan Marsh; Eugene Sun; Stanley A Roberts
Metabolism and disposition of the HIV-1 protease inhibitor lopinavir (ABT-378) given in combination with ritonavir in rats, dogs, and humans.
Pharmaceutical research 2004;21(9):1622-30.
2004: Hongmei Mo; Liangjun Lu; Ron Pithawalla; Dale J Kempf; Akhteruzzaman Molla
Complementation in cells cotransfected with a mixture of wild-type and mutant human immunodeficiency virus (HIV) influences the replication capacities and phenotypes of mutant variants in a single-cycle HIV resistance assay.
Journal of clinical microbiology 2004;42(9):4169-74.
2004: Peggy P Huang; John T Randolph; Larry Klein; Sudthida Vasavanonda; Tatyana Dekhtyar; Vincent S Stoll; Dale J Kempf
Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(15):4075-8.
2004: Françoise Brun-Vézinet; Dominique Costagliola; Mounir Ait Khaled; Vincent Calvez; François Clavel; Bonaventura Clotet; Richard Haubrich; Dale J Kempf; Marty King; Daniel R Kuritzkes; Randall Lanier; M Miller; Veronica Miller; Andrews Phillips; Deenan Pillay; Jonathan M Schapiro; Janna Scott; Robert Shafer; Maurizio Zazzi; Andrew R Zolopa; Victor DeGruttola
Clinically validated genotype analysis: guiding principles and statistical concerns.
Antiviral therapy 2004;9(4):465-78.
2004: Dean Hickman; Sudthida Vasavanonda; George Nequist; Lynn Colletti; Warren M Kati; Richard Bertz; Ann Hsu; Dale J Kempf
Estimation of serum-free 50-percent inhibitory concentrations for human immunodeficiency virus protease inhibitors lopinavir and ritonavir.
Antimicrobial agents and chemotherapy 2004;48(8):2911-7.
2004: Dale J Kempf; Martin S King; Barry Bernstein; Paul Cernohous; Eric Bauer; Jennifer Moseley; Kai Gu; Ann Hsu; Scott C Brun; Eugene Sun
Incidence of resistance in a double-blind study comparing lopinavir/ritonavir plus stavudine and lamivudine to nelfinavir plus stavudine and lamivudine.
The Journal of infectious diseases 2004;189(1):51-60.
2003: Xiaoqi Chen; Dale J Kempf; Lin Li; Hing L Sham; Sudthida Vasavanonda; Norman E Wideburg; Ayda Saldivar; Kennan Marsh; Edith McDonald; Daniel W Norbeck
Synthesis and SAR studies of potent HIV protease inhibitors containing novel dimethylphenoxyl acetates as P2 ligands.
Bioorganic & medicinal chemistry letters 2003;13(21):3657-60.
2003: Hongmei Mo; Liangjun Lu; Tatyana Dekhtyar; Kent D Stewart; Eugene Sun; Dale J Kempf; Akhteruzzaman Molla
Characterization of resistant HIV variants generated by in vitro passage with lopinavir/ritonavir.
Antiviral research 2003;59(3):173-80.
2003: Xavier Sáez-Llorens; Avyi Violari; Carl O Deetz; Richard Rode; Perry Gomez; Edward Handelsman; Stephen I Pelton; Octavio Ramilo; Pedro Cahn; Ellen Chadwick; Upton Allen; Stephen Arpadi; Maria Mercedes Castrejón; Renee S Heuser; Dale J Kempf; Richard Bertz; Ann F Hsu; Barry Bernstein; Cheryl L Renz; Eugene Sun
Forty-eight-week evaluation of lopinavir/ritonavir, a new protease inhibitor, in human immunodeficiency virus-infected children.
The Pediatric infectious disease journal 2003;22(3):216-24.
2003: Vincent S Stoll; Kent D Stewart; Clarence J Maring; Steven W Muchmore; Vincent L Giranda; Yu Gui Gu; Gary Wang; Yuanwei Chen; Minghua Sun; Chen Zhao; April L Kennedy; Darold L Madigan; Yibo Xu; Ayda Saldivar; Warren M Kati; Graeme Laver; Thomas J Sowin; Hing L Sham; Jonathan Greer; Dale J Kempf
Influenza neuraminidase inhibitors: structure-based design of a novel inhibitor series.
Biochemistry 2003;42(3):718-27.
2003: Ann Hsu; Jeffrey D Isaacson; Scott C Brun; Barry Bernstein; Wayne Lam; Richard Bertz; Cheryl Foit; Karen Rynkiewicz; Bruce Richards; Martin King; Richard Rode; Dale J Kempf; G Richard Granneman; Eugene Sun
Pharmacokinetic-pharmacodynamic analysis of lopinavir-ritonavir in combination with efavirenz and two nucleoside reverse transcriptase inhibitors in extensively pretreated human immunodeficiency virus-infected patients.
Antimicrobial agents and chemotherapy 2003;47(1):350-9.
2002: Stephen Hanessian; Jianchio Wang; Debra Montgomery; Vincent S Stoll; Kent D Stewart; Warren M Kati; Clarence J Maring; Dale J Kempf; Charles W Hutchins; W Graeme Laver
Design, synthesis, and neuraminidase inhibitory activity of GS-4071 analogues that utilize a novel hydrophobic paradigm.
Bioorganic & medicinal chemistry letters 2002;12(23):3425-9.
2002: Nancy S Shulman; Andrew R Zolopa; Diane V Havlir; Ann Hsu; Cheryl Renz; Sheila Boller; Ping Jiang; Richard Rode; Joel E Gallant; Elizabeth Race; Dale J Kempf; Eugene Sun
Virtual inhibitory quotient predicts response to ritonavir boosting of indinavir-based therapy in human immunodeficiency virus-infected patients with ongoing viremia.
Antimicrobial agents and chemotherapy 2002;46(12):3907-16.
2002: Hing L Sham; Chen Zhao; Leping Li; David A Betebenner; Ayda Saldivar; Sudthida Vasavanonda; Dale J Kempf; Jacob J Plattner; Daniel W Norbeck
Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships.
Bioorganic & medicinal chemistry letters 2002;12(21):3101-3.
2002: Dale J Kempf; Jeffrey D Isaacson; Martin S King; Scott C Brun; Jacquelyn Sylte; Bruce Richards; Barry Bernstein; Richard Rode; Eugene Sun
Analysis of the virological response with respect to baseline viral phenotype and genotype in protease inhibitor-experienced HIV-1-infected patients receiving lopinavir/ritonavir therapy.
Antiviral therapy 2002;7(3):165-74.
2002: David A DeGoey; Hui-Ju Chen; William J Flosi; David J Grampovnik; Clinton M Yeung; Larry Klein; Dale J Kempf
Enantioselective synthesis of antiinfluenza compound A-315675.
The Journal of organic chemistry 2002;67(16):5445-53.
2002: Vincent S Stoll; Wenying Qin; Kent D Stewart; Clarissa Jakob; Chang Park; K Walter; Robert L Simmer; Rosalind J Helfrich; Dirk Bussiere; J Kao; Dale J Kempf; Hing L Sham; Daniel W Norbeck
X-ray crystallographic structure of ABT-378 (lopinavir) bound to HIV-1 protease.
Bioorganic & medicinal chemistry 2002;10(8):2803-6.
2002: Akhteruzzaman Molla; Hongmei Mo; Sudthida Vasavanonda; Lixin Han; C Thomas Lin; Ann Hsu; Dale J Kempf
In vitro antiviral interaction of lopinavir with other protease inhibitors.
Antimicrobial agents and chemotherapy 2002;46(7):2249-53.
2002: Akhteruzzaman Molla; Warren M Kati; Robert Carrick; Kevin Steffy; Yan Shi; Debra Montgomery; Nanette Gusick; Vincent S Stoll; Kent D Stewart; Teresa I Ng; Clarence J Maring; Dale J Kempf; William Kohlbrenner
In vitro selection and characterization of influenza A (A/N9) virus variants resistant to a novel neuraminidase inhibitor, A-315675.
Journal of virology 2002;76(11):5380-6.
2002: Hing L Sham; David A Betebenner; Xiaoqi Chen; Ayda Saldivar; Sudthida Vasavanonda; Dale J Kempf; Jacob J Plattner; Daniel W Norbeck
Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir).
Bioorganic & medicinal chemistry letters 2002;12(8):1185-7.
2002: Warren M Kati; Debra Montgomery; Robert Carrick; Larisa V Gubareva; Clarence J Maring; Keith F McDaniel; Kevin Steffy; Akhteruzzaman Molla; Frederick G Hayden; Dale J Kempf; William Kohlbrenner
In vitro characterization of A-315675, a highly potent inhibitor of A and B strain influenza virus neuraminidases and influenza virus replication.
Antimicrobial agents and chemotherapy 2002;46(4):1014-21.
2002: Constance A Benson; Steven G Deeks; Scott C Brun; Roy M Gulick; Joseph J Eron; Harold A Kessler; Robert L Murphy; Charles Hicks; Martin King; David Wheeler; Judith Feinberg; Richard Stryker; Paul E Sax; Sharon A Riddler; Melanie Thompson; Kathryn Real; Ann Hsu; Dale J Kempf; Anthony J Japour; Eugene Sun
Safety and antiviral activity at 48 weeks of lopinavir/ritonavir plus nevirapine and 2 nucleoside reverse-transcriptase inhibitors in human immunodeficiency virus type 1-infected protease inhibitor-experienced patients.
The Journal of infectious diseases 2002;185(5):599-607.
2001: Dale J Kempf; Jeffrey D Isaacson; Martin S King; Scott C Brun; Y Xu; K Real; Barry Bernstein; Anthony J Japour; Eugene Sun; Richard Rode
Identification of genotypic changes in human immunodeficiency virus protease that correlate with reduced susceptibility to the protease inhibitor lopinavir among viral isolates from protease inhibitor-experienced patients.
Journal of virology 2001;75(16):7462-9.
2001: Hing L Sham; David A Betebenner; T Herrin; G Kumar; Ayda Saldivar; Sudthida Vasavanonda; Akhteruzzaman Molla; Dale J Kempf; Jacob J Plattner; Daniel W Norbeck
Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir).
Bioorganic & medicinal chemistry letters 2001;11(11):1351-3.
2001: Gary T Wang; Yuanwei Chen; Sanyi Wang; Robert Gentles; Thomas J Sowin; Warren M Kati; Steven W Muchmore; Vincent L Giranda; Kent Stewart; Hing L Sham; Dale J Kempf; W Graeme Laver
Design, synthesis, and structural analysis of influenza neuraminidase inhibitors containing pyrrolidine cores.
Journal of medicinal chemistry 2001;44(8):1192-201.
1999: William Cameron; Anthony J Japour; Y Xu; Ann Hsu; J Mellors; C Farthing; C Cohen; D Poretz; M Markowitz; S Follansbee; Jonathan B Angel; D McMahon; D Ho; V Devanarayan; Richard Rode; M Salgo; Dale J Kempf; Richard G Granneman; JM Leonard; Eugene Sun
Ritonavir and saquinavir combination therapy for the treatment of HIV infection.
AIDS (London, England) 1999;13(2):213-24.
1999: Gondi N Kumar; Venkata K Jayanti; R D Lee; D N Whittern; John T Uchic; Samuel Thomas; P Johnson; Brian A Grabowski; Hing L Sham; David A Betebenner; Dale J Kempf; Jon F Denissen
In vitro metabolism of the HIV-1 protease inhibitor ABT-378: species comparison and metabolite identification.
Drug metabolism and disposition: the biological fate of chemicals 1999;27(1):86-91.
1998: Xiaoqi Chen; Dale J Kempf; Hing L Sham; Brian E Green; Akhteruzzaman Molla; M Korneyeva; Sudthida Vasavanonda; Norman E Wideburg; Ayda Saldivar; Kennan Marsh; Edith McDonald; Daniel W Norbeck
Potent piperazine hydroxyethylamine HIV protease inhibitors containing novel P3 ligands.
Bioorganic & medicinal chemistry letters 1998;8(24):3531-6.
1998: Hing L Sham; Dale J Kempf; Akhteruzzaman Molla; Kennan Marsh; Gondi N Kumar; Chih-Ming Chen; Warren M Kati; K Stewart; R Lal; Ann Hsu; David A Betebenner; M Korneyeva; Sudthida Vasavanonda; Edith McDonald; Ayda Saldivar; Norman E Wideburg; Xiaoqi Chen; P Niu; Chang Park; Venkata K Jayanti; Brian A Grabowski; G Richard Granneman; Eugene Sun; Anthony J Japour; JM Leonard; Jacob J Plattner; Daniel W Norbeck
ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease.
Antimicrobial agents and chemotherapy 1998;42(12):3218-24.
1998: Akhteruzzaman Molla; Sudthida Vasavanonda; G Kumar; Hing L Sham; M Johnson; Brian A Grabowski; Jon F Denissen; William Kohlbrenner; Jacob J Plattner; JM Leonard; Daniel W Norbeck; Dale J Kempf
Human serum attenuates the activity of protease inhibitors toward wild-type and mutant human immunodeficiency virus.
Virology 1998;250(2):255-62.
1998: A Carrillo; Kent D Stewart; Hing L Sham; Daniel W Norbeck; William Kohlbrenner; JM Leonard; Dale J Kempf; Akhteruzzaman Molla
In vitro selection and characterization of human immunodeficiency virus type 1 variants with increased resistance to ABT-378, a novel protease inhibitor.
Journal of virology 1998;72(9):7532-41.
1998: Akhteruzzaman Molla; G Richard Granneman; Eugene Sun; Dale J Kempf
Recent developments in HIV protease inhibitor therapy.
Antiviral research 1998;39(1):1-23.
1998: Dale J Kempf; Richard Rode; Y Xu; Eugene Sun; ME Heath-Chiozzi; J Valdes; Anthony J Japour; S Danner; C Boucher; Akhteruzzaman Molla; JM Leonard
The duration of viral suppression during protease inhibitor therapy for HIV-1 infection is predicted by plasma HIV-1 RNA at the nadir.
AIDS (London, England) 1998;12(5):F9-14.
1998: Dale J Kempf; Hing L Sham; Kennan Marsh; Charles A Flentge; David A Betebenner; Brian E Green; Edith McDonald; Sudthida Vasavanonda; Ayda Saldivar; Norman E Wideburg; Warren M Kati; L Ruiz; Chen Zhao; L Fino; J Patterson; Akhteruzzaman Molla; Jacob J Plattner; Daniel W Norbeck
Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical efficacy.
Journal of medicinal chemistry 1998;41(4):602-17.
1997: Philip J Hajduk; Jurgen Dinges; G F Miknis; M Merlock; John Harlan; Dale J Kempf; David A Egan; Karl A Walter; T S Robins; Suzanne B Shuker; Thomas F Holzman; Stephen W Fesik
NMR-based discovery of lead inhibitors that block DNA binding of the human papillomavirus E2 protein.
Journal of medicinal chemistry 1997;40(20):3144-50.
1997: Jon F Denissen; Brian A Grabowski; M K Johnson; Alex M Buko; Dale J Kempf; S B Thomas; Bruce W Surber
Metabolism and disposition of the HIV-1 protease inhibitor ritonavir (ABT-538) in rats, dogs, and humans.
Drug metabolism and disposition: the biological fate of chemicals 1997;25(4):489-501.
1997: Dale J Kempf; Kennan Marsh; G Kumar; A David Rodrigues; Jon F Denissen; Edith McDonald; M J Kukulka; Ann Hsu; G Richard Granneman; PA Baroldi; Eugene Sun; DJ Pizzuti; Jacob J Plattner; Daniel W Norbeck; JM Leonard
Pharmacokinetic enhancement of inhibitors of the human immunodeficiency virus protease by coadministration with ritonavir.
Antimicrobial agents and chemotherapy 1997;41(3):654-60.
1996: Hing L Sham; C Zhao; Kennan Marsh; David A Betebenner; S Lin; W Rosenbrook; T Herrin; L Li; D Madigan; Sudthida Vasavanonda; Akhteruzzaman Molla; Ayda Saldivar; Edith McDonald; Norman E Wideburg; Dale J Kempf; Daniel W Norbeck; Jacob J Plattner
Novel azacyclic ureas that are potent inhibitors of HIV-1 protease.
Biochemical and biophysical research communications 1996;225(2):436-40.
1996: Akhteruzzaman Molla; M Korneyeva; Q Gao; Sudthida Vasavanonda; P J Schipper; H M Mo; Martin Markowitz; T Chernyavskiy; P Niu; N Lyons; Ann Hsu; G Richard Granneman; David D Ho; Charles A B Boucher; J M Leonard; Daniel W Norbeck; Dale J Kempf
Ordered accumulation of mutations in HIV protease confers resistance to ritonavir.
Nature medicine 1996;2(7):760-6.
1996: John Bilello; P A Bilello; K Stellrecht; J Leonard; Daniel W Norbeck; Dale J Kempf; T Robins; George L Drusano
Human serum alpha 1 acid glycoprotein reduces uptake, intracellular concentration, and antiviral activity of A-80987, an inhibitor of the human immunodeficiency virus type 1 protease.
Antimicrobial agents and chemotherapy 1996;40(6):1491-7.
1996: A Hsu; Dale J Kempf; J Leonard; R Mills
Letter to the editor. [letter].
Journal of the International Association of Physicians in AIDS Care 1996;2(4):60.
1996: Hing L Sham; C Zhao; Kent D Stewart; David A Betebenner; S Lin; C H Park; X P Kong; W Rosenbrook; T Herrin; D Madigan; Sudthida Vasavanonda; N Lyons; Akhteruzzaman Molla; Ayda Saldivar; Kennan Marsh; Edith McDonald; Norman E Wideburg; Jon F Denissen; T Robins; Dale J Kempf; Jacob J Plattner; Daniel W Norbeck
A novel, picomolar inhibitor of human immunodeficiency virus type 1 protease.
Journal of medicinal chemistry 1996;39(2):392-7.
1995: G T Wang; S Li; Norman E Wideburg; Grant A Krafft; Dale J Kempf
Synthetic chemical diversity: solid phase synthesis of libraries of C2 symmetric inhibitors of HIV protease containing diamino diol and diamino alcohol cores.
Journal of medicinal chemistry 1995;38(16):2995-3002.
1995: Dale J Kempf; Kennan Marsh; Jon F Denissen; Edith McDonald; Sudthida Vasavanonda; C A Flentge; Brian E Green; L Fino; C H Park; X P Kong
ABT-538 is a potent inhibitor of human immunodeficiency virus protease and has high oral bioavailability in humans.
Proceedings of the National Academy of Sciences of the United States of America 1995;92(7):2484-8.
1995: Martin Markowitz; H Mo; Dale J Kempf; Daniel W Norbeck; T N Bhat; John W Erickson; David D Ho
Selection and analysis of human immunodeficiency virus type 1 variants with increased resistance to ABT-538, a novel protease inhibitor.
Journal of virology 1995;69(2):701-6.
1994: Andrew H Kaplan; Paul Krogstad; Dale J Kempf; Daniel W Norbeck; Ronald Swanstrom
Human immunodeficiency virus type 1 virions composed of unprocessed Gag and Gag-Pol precursors are capable of reverse transcribing viral genomic RNA.
Antimicrobial agents and chemotherapy 1994;38(12):2929-33.
1994: Dale J Kempf; Kennan Marsh; L C Fino; P Bryant; A Craig-Kennard; Hing L Sham; C Zhao; Sudthida Vasavanonda; William Kohlbrenner; Norman E Wideburg
Design of orally bioavailable, symmetry-based inhibitors of HIV protease.
Bioorganic & medicinal chemistry 1994;2(9):847-58.
1994: Andrew H Kaplan; S F Michael; R S Wehbie; MF Knigge; D A Paul; L Everitt; Dale J Kempf; Daniel W Norbeck; J W Erickson; Ronald Swanstrom
Selection of multiple human immunodeficiency virus type 1 variants that encode viral proteases with decreased sensitivity to an inhibitor of the viral protease.
Proceedings of the National Academy of Sciences of the United States of America 1994;91(12):5597-601.
1994: S Kageyama; D T Hoekzema; Y Murakawa; Eiji Kojima; T Shirasaka; Dale J Kempf; Daniel W Norbeck; J Erickson; Hiroaki Mitsuya
A C2 symmetry-based HIV protease inhibitor, A77003, irreversibly inhibits infectivity of HIV-1 in vitro.
AIDS research and human retroviruses 1994;10(6):735-43.
1994: David D Ho; T Toyoshima; H Mo; Dale J Kempf; Daniel W Norbeck; Chih-Ming Chen; Norman E Wideburg; S K Burt; John W Erickson; M K Singh
Characterization of human immunodeficiency virus type 1 variants with increased resistance to a C2-symmetric protease inhibitor.
Journal of virology 1994;68(3):2016-20.
1994: J Erickson; Dale J Kempf
Structure-based design of symmetric inhibitors of HIV-1 protease.
Archives of virology. Supplementum 1994;9():19-29.
1993: Hing L Sham; David A Betebenner; Norman E Wideburg; Ayda Saldivar; William Kohlbrenner; A Craig-Kennard; Sudthida Vasavanonda; Dale J Kempf; J J Clement; J E Erickson
Pseudo-symmetrical difluoroketones. Highly potent and specific inhibitors of HIV-1 protease.
FEBS letters 1993;329(1-2):144-6.
1993: Andrew H Kaplan; Jerome A Zack; MF Knigge; D A Paul; Dale J Kempf; Daniel W Norbeck; Ronald Swanstrom
Partial inhibition of the human immunodeficiency virus type 1 protease results in aberrant virus assembly and the formation of noninfectious particles.
Journal of virology 1993;67(7):4050-5.
1993: Dale J Kempf; L Codacovi; X C Wang; William Kohlbrenner; Norman E Wideburg; Ayda Saldivar; Sudthida Vasavanonda; Kennan Marsh; P Bryant; Hing L Sham
Symmetry-based inhibitors of HIV protease. Structure-activity studies of acylated 2,4-diamino-1,5-diphenyl-3-hydroxypentane and 2,5-diamino-1,6-diphenylhexane-3,4-diol.
Journal of medicinal chemistry 1993;36(3):320-30.
1992: S Kageyama; John N Weinstein; T Shirasaka; Dale J Kempf; Daniel W Norbeck; Jacob J Plattner; J Erickson; Hiroaki Mitsuya
In vitro inhibition of human immunodeficiency virus (HIV) type 1 replication by C2 symmetry-based HIV protease inhibitors as single agents or in combinations.
Antimicrobial agents and chemotherapy 1992;36(5):926-33.
1991: Dale J Kempf; Kennan Marsh; D A Paul; MF Knigge; Daniel W Norbeck; William Kohlbrenner; L Codacovi; Sudthida Vasavanonda; P Bryant; X C Wang
Antiviral and pharmacokinetic properties of C2 symmetric inhibitors of the human immunodeficiency virus type 1 protease.
Antimicrobial agents and chemotherapy 1991;35(11):2209-14.
1991: Thomas F Holzman; William Kohlbrenner; Weigl Debra; J Rittenhouse; Dale J Kempf; J Erickson
Inhibitor stabilization of human immunodeficiency virus type-2 proteinase dimer formation.
The Journal of biological chemistry 1991;266(29):19217-20.
1991: Dale J Kempf; X C Wang; S G Spanton
Stereocontrolled synthesis of psi[CH = CH] dipeptide isosteres.
International journal of peptide and protein research 1991;38(3):237-41.
1991: Hing L Sham; David A Betebenner; Norman E Wideburg; Ayda Saldivar; William Kohlbrenner; Sudthida Vasavanonda; Dale J Kempf; Daniel W Norbeck; C Zhao; J J Clement
Potent HIV-1 protease inhibitors with antiviral activities in vitro.
Biochemical and biophysical research communications 1991;175(3):914-9.
1990: Dale J Kempf; Daniel W Norbeck; L Codacovi; X C Wang; William Kohlbrenner; Norman E Wideburg; D A Paul; MF Knigge; Sudthida Vasavanonda; A Craig-Kennard
Structure-based, C2 symmetric inhibitors of HIV protease.
Journal of medicinal chemistry 1990;33(10):2687-9.
1990: J Erickson; D J Neidhart; J VanDrie; Dale J Kempf; X C Wang; Daniel W Norbeck; Jacob J Plattner; J W Rittenhouse; M Turon; Norman E Wideburg
Design, activity, and 2.8 A crystal structure of a C2 symmetric inhibitor complexed to HIV-1 protease.
Science (New York, N.Y.) 1990;249(4968):527-33.
1990: Saul H Rosenberg; J F Dellaria; Dale J Kempf; Charles W Hutchins; K W Woods; R G Maki; E de Lara; K P Spina; H H Stein; Jerry Cohen
Potent, low molecular weight renin inhibitors containing a C-terminal heterocycle: hydrogen bonding at the active site.
Journal of medicinal chemistry 1990;33(6):1582-90.
1990: Dale J Kempf; E de Lara; H H Stein; Jerry Cohen; David A Egan; Jacob J Plattner
Renin inhibitors based on dipeptide analogues. Incorporation of the hydroxyethylene isostere at the P2/P3 sites.
Journal of medicinal chemistry 1990;33(1):371-4.
1987: Dale J Kempf; E de Lara; H H Stein; Jerry Cohen; Jacob J Plattner
Renin inhibitors based on novel dipeptide analogues. Incorporation of the dehydrohydroxyethylene isostere at the scissile bond.
Journal of medicinal chemistry 1987;30(11):1978-83.