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Andrew Combs

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Carolyn D Dzierba; Amy Galka; Paul J Gilligan; Tricia L Johnson; Padmaja Kasireddy-Polam; Nicholas J Lodge; Argyrios G Arvanitis; Joanne J Bronson; Andrew P Combs; Bireshwar Dasgupta; Thaddeus F Molski; Maria Rafalski; Thais M Sielecki; Amy Takvorian; George L Trainor; Shikha Vig; Harvey Wong; Robert Zaczek; Ge Zhang; John E Macor
Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists.
Lorin A Thompson; Jeremy H Toyn; George L Trainor; Changsheng Zheng; Jovita Marcinkeviciene; Jere E Meredith; Jodi K Muckelbauer; Richard E Olson; Jianliang Shi; Andrew J Tebben; Charles F Albright; Donna M Barten; Kenneth M Boy; Catherine R Burton; Daniel M Camac; Andrew P Combs; Robert A Copeland; Carl P Decicco; Andrew C Good; James E Grace; Jason M Guernon; Kimberley A Lentz; Ann Liauw; John E Macor
Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.
Xiangdong Liu; Niu Shin; Holly K Koblish; Gengjie Yang; Qian Wang; Kathy Wang; Lynn Leffet; Michael Hansbury; Beth Thomas; Mark Rupar; Paul Waeltz; Kevin J Bowman; Padmaja Polam; Richard B Sparks; Eddy W Yue; Yanlong Li; Richard Wynn; Jordan S Fridman; Timothy C Burn; Andrew P Combs; Robert C Newton; Peggy A Scherle
Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity.

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All Publications

2012: Carolyn D Dzierba; Amy Galka; Paul J Gilligan; Tricia L Johnson; Padmaja Kasireddy-Polam; Nicholas J Lodge; Argyrios G Arvanitis; Joanne J Bronson; Andrew P Combs; Bireshwar Dasgupta; Thaddeus F Molski; Maria Rafalski; Thais M Sielecki; Amy Takvorian; George L Trainor; Shikha Vig; Harvey Wong; Robert Zaczek; Ge Zhang; John E Macor
Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists.
Bioorganic & medicinal chemistry letters 2012;22(15):4986-9.
2011: Lorin A Thompson; Jeremy H Toyn; George L Trainor; Changsheng Zheng; Jovita Marcinkeviciene; Jere E Meredith; Jodi K Muckelbauer; Richard E Olson; Jianliang Shi; Andrew J Tebben; Charles F Albright; Donna M Barten; Kenneth M Boy; Catherine R Burton; Daniel M Camac; Andrew P Combs; Robert A Copeland; Carl P Decicco; Andrew C Good; James E Grace; Jason M Guernon; Kimberley A Lentz; Ann Liauw; John E Macor
Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.
Bioorganic & medicinal chemistry letters 2011;21(22):6909-15.
2010: Xiangdong Liu; Niu Shin; Holly K Koblish; Gengjie Yang; Qian Wang; Kathy Wang; Lynn Leffet; Michael Hansbury; Beth Thomas; Mark Rupar; Paul Waeltz; Kevin J Bowman; Padmaja Polam; Richard B Sparks; Eddy W Yue; Yanlong Li; Richard Wynn; Jordan S Fridman; Timothy C Burn; Andrew P Combs; Robert C Newton; Peggy A Scherle
Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity.
Blood 2010;115(17):3520-30.
2010: Holly K Koblish; Michael Hansbury; Kevin J Bowman; Gengjie Yang; Claire L Neilan; Patrick J Haley; Timothy C Burn; Paul Waeltz; Richard B Sparks; Eddy W Yue; Andrew P Combs; Peggy A Scherle; Kris Vaddi; Jordan S Fridman
Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors.
Molecular cancer therapeutics 2010;9(2):489-98.
2009: Eddy W Yue; Brent Douty; Brian Wayland; Michael Bower; Xiangdong Liu; Lynn Leffet; Qian Wang; Kevin J Bowman; Michael Hansbury; Changnian Liu; Min Wei; Yanlong Li; Richard Wynn; Timothy C Burn; Holly K Koblish; Jordan S Fridman; Brian Metcalf; Peggy A Scherle; Andrew P Combs
Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.
Journal of medicinal chemistry 2009;52(23):7364-7.
2009: Phillip C C Liu; Eian Caulder; Jun Li; Paul Waeltz; Alex Margulis; Richard Wynn; Mary Becker-Pasha; Yanlong Li; Erin Crowgey; Gregory F Hollis; Patrick Haley; Richard B Sparks; Andrew P Combs; James D Rodgers; Timothy C Burn; Kris Vaddi; Jordan S Fridman
Combined inhibition of Janus kinase 1/2 for the treatment of JAK2V617F-driven neoplasms: selective effects on mutant cells and improvements in measures of disease severity.
Clinical cancer research : an official journal of the American Association for Cancer Research 2009;15(22):6891-900.
2009: Richard A Hartz; Vijay T Ahuja; Argyrios G Arvanitis; Maria Rafalski; Eddy W Yue; Derek J Denhart; William D Schmitz; Jonathan L Ditta; Jeffrey A Deskus; Allison B Brenner; Frank W Hobbs; Joseph Payne; Snjezana Lelas; Yu-Wen Li; Thaddeus F Molski; Gail K Mattson; Yong Peng; Harvey Wong; James E Grace; Kimberley A Lentz; Jingfang Qian-Cutrone; Xiaoliang Zhuo; Yue-Zhong Shu; Nicholas J Lodge; Robert Zaczek; Andrew P Combs; Richard E Olson; Joanne J Bronson; Ronald J Mattson; John E Macor
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Journal of medicinal chemistry 2009;52(14):4173-91.
2009: Richard A Hartz; Vijay T Ahuja; Maria Rafalski; William D Schmitz; Allison B Brenner; Derek J Denhart; Jonathan L Ditta; Jeffrey A Deskus; Eddy W Yue; Argyrios G Arvanitis; Snjezana Lelas; Yu-Wen Li; Thaddeus F Molski; Harvey Wong; James E Grace; Kimberley A Lentz; Jianqing Li; Nicholas J Lodge; Robert Zaczek; Andrew P Combs; Richard E Olson; Ronald J Mattson; Joanne J Bronson; John E Macor
In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Journal of medicinal chemistry 2009;52(14):4161-72.
2008: Brent Douty; Brian Wayland; Paul J Ala; Michael J Bower; James Pruitt; Lori Bostrom; Min Wei; Ronald Klabe; Lucie Gonneville; Richard Wynn; Timothy C Burn; Phillip C C Liu; Andrew P Combs; Eddy W Yue
Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines.
Bioorganic & medicinal chemistry letters 2008;18(1):66-71.
2007: Carolyn D Dzierba; Andrew J Tebben; Richard G Wilde; Amy Takvorian; Maria Rafalski; Padmaja Kasireddy-Polam; John D Klaczkiewicz; Anthony D Pechulis; Amy L Davis; Mark P Sweet; Alex M Woo; Zhicai Yang; Sarah M Ebeltoft; Thaddeus F Molski; Ge Zhang; Robert Zaczek; George L Trainor; Andrew P Combs; Paul J Gilligan
Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling.
Journal of medicinal chemistry 2007;50(9):2269-72.
2007: Andrew P Combs; Brian Glass; Laurine G Galya; Mei Li
Asymmetric synthesis of the (S)-1,1-dioxido-isothiazolidin-3-one phosphotyrosine mimetic via reduction of a homochiral (R)-oxido-isothiazolidin-3-one.
Organic letters 2007;9(7):1279-82.
2007: Richard B Sparks; Padmaja Polam; Wenyu Zhu; Matthew L Crawley; Amy Takvorian; Erin McLaughlin; Min Wei; Paul J Ala; Lucie Gonneville; Nancy Taylor; Yanlong Li; Richard Wynn; Timothy C Burn; Phillip C C Liu; Andrew P Combs
Benzothiazole benzimidazole (S)-isothiazolidinone derivatives as protein tyrosine phosphatase-1B inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(3):736-40.
2006: Paul J Ala; Lucie Gonneville; Milton C Hillman; Mary Becker-Pasha; Eddy W Yue; Brent Douty; Brian Wayland; Padmaja Polam; Matthew L Crawley; Erin McLaughlin; Richard B Sparks; Brian Glass; Amy Takvorian; Andrew P Combs; Timothy C Burn; Gregory F Hollis; Richard Wynn
Structural insights into the design of nonpeptidic isothiazolidinone-containing inhibitors of protein-tyrosine phosphatase 1B.
The Journal of biological chemistry 2006;281(49):38013-21.
2006: Paul J Ala; Lucie Gonneville; Milton C Hillman; Mary Becker-Pasha; Min Wei; Brian G Reid; Ronald Klabe; Eddy W Yue; Brian Wayland; Brent Douty; Padmaja Polam; Zelda R Wasserman; Michael Bower; Andrew P Combs; Timothy C Burn; Gregory F Hollis; Richard Wynn
Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics.
The Journal of biological chemistry 2006;281(43):32784-95.
2006: Eddy W Yue; Brian Wayland; Brent Douty; Matthew L Crawley; Erin McLaughlin; Amy Takvorian; Zelda R Wasserman; Michael J Bower; Min Wei; Yanlong Li; Paul J Ala; Lucie Gonneville; Richard Wynn; Timothy C Burn; Phillip C C Liu; Andrew P Combs
Isothiazolidinone heterocycles as inhibitors of protein tyrosine phosphatases: synthesis and structure-activity relationships of a peptide scaffold.
Bioorganic & medicinal chemistry 2006;14(17):5833-49.
2006: Andrew P Combs; Wenyu Zhu; Matthew L Crawley; Brian Glass; Padmaja Polam; Richard B Sparks; Dilip Modi; Amy Takvorian; Erin McLaughlin; Eddy W Yue; Zelda R Wasserman; Michael Bower; Min Wei; Mark J Rupar; Paul J Ala; Brian M Reid; Dawn Ellis; Lucie Gonneville; Thomas Emm; Nancy Taylor; Swamy Yeleswaram; Yanlong Li; Richard Wynn; Timothy C Burn; Gregory F Hollis; Phillip C C Liu; Brian Metcalf
Potent benzimidazole sulfonamide protein tyrosine phosphatase 1B inhibitors containing the heterocyclic (S)-isothiazolidinone phosphotyrosine mimetic.
Journal of medicinal chemistry 2006;49(13):3774-89.
2006: Lorin A Thompson; Ann Y Liauw; Mercy M Ramanjulu; Padmaja Kasireddy-Polam; Stephen E Mercer; Thomas Maduskuie; Marcie Glicksman; Arthur H Roach; Jere E Meredith; Rui-Qin Liu; Andrew P Combs; Jeffrey N Higaki; Barbara Cordell; Dietmar Seiffert; Robert Zaczek; David W Robertson; Richard E Olson
Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(9):2357-63.
2005: Matthew L Crawley; Erin McLaughlin; Wenyu Zhu; Andrew P Combs
Concise approach to novel isothiazolidinone phosphotyrosine mimetics: microwave-assisted addition of bisulfite to activated olefins.
Organic letters 2005;7(22):5067-9.
2005: Charles F Albright; Nilsa Graciani; Wei Han; Eddy Yue; Ross Stein; Zhihong Lai; Melody Diamond; Randine Dowling; Lisa Grimminger; Shu-Yun Zhang; Davette Behrens; Amy Musselman; Robert Bruckner; Mingzhu Zhang; Xiang Jiang; Daniel Hu; Anne Higley; Susan Dimeo; Maria Rafalski; Sandya Mandlekar; Bruce Car; Swamy Yeleswaram; Andrew Stern; Robert Copeland; Andrew P Combs; Steven P Seitz; George L Trainor; Rebecca A Taub; Pearl Huang; Allen Oliff
Matrix metalloproteinase-activated doxorubicin prodrugs inhibit HT1080 xenograft growth better than doxorubicin with less toxicity.
Molecular cancer therapeutics 2005;4(5):751-60.
2004: Carolyn D Dzierba; Amy Takvorian; Maria Rafalski; Padmaja Kasireddy-Polam; Harvey Wong; Thaddeus F Molski; Ge Zhang; Yu-Wen Li; Snjezana Lelas; Yong Peng; John F McElroy; Robert Zaczek; Rebecca A Taub; Andrew P Combs; Paul J Gilligan; George L Trainor
Synthesis, structure-activity relationships, and in vivo properties of 3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-ones as corticotropin-releasing factor-1 receptor antagonists.
Journal of medicinal chemistry 2004;47(23):5783-90.
2004: Richard B Sparks; Andrew P Combs
Microwave-assisted synthesis of 2,4,5-triaryl-imidazole; a novel thermally induced N-hydroxyimidazole N-O bond cleavage.
Organic letters 2004;6(14):2473-5.
2004: Amy Takvorian; Andrew P Combs
Microwave-assisted organic synthesis using minivials to optimize and expedite the synthesis of diverse purine libraries.
Journal of combinatorial chemistry 2004;6(2):171-4.
2003: Andrew P Combs; Brian Glass; Sharon A Jackson
Microwave-assisted solid-phase organic synthesis (MA-SPOS) of oxazolidinone antimicrobials.
Methods in enzymology 2003;369():223-31.
2002: Tasir S Haque; Seifu Tadesse; Jovita Marcinkeviciene; Martin Rogers; Christine F Sizemore; Lisa M Kopcho; Karen M Amsler; Lisa D Ecret; Dong Liang Zhan; Frank Hobbs; Andrew Slee; George L Trainor; Andrew M Stern; Robert Copeland; Andrew P Combs
Parallel synthesis of potent, pyrazole-based inhibitors of Helicobacter pylori dihydroorotate dehydrogenase.
Journal of medicinal chemistry 2002;45(21):4669-78.
2002: Jovita Marcinkeviciene; Lisa M Kopcho; Tao Yang; Robert Copeland; Brian Glass; Andrew P Combs; Nikoo Falahatpisheh; Lorin Thompson
Novel inhibition of porcine pepsin by a substituted piperidine. Preference for one of the enzyme conformers.
The Journal of biological chemistry 2002;277(32):28677-82.
2002: Andrew P Combs; Seifu Tadesse; Maria Rafalski; Tasir S Haque; Patrick Y S Lam
N-arylation of primary and secondary aliphatic amines on solid supports.
Journal of combinatorial chemistry 2002;4(2):179-82.
2001: Jovita Marcinkeviciene; Y Luo; N R Graciani; Andrew P Combs; Robert Copeland
Mechanism of Inhibition of beta-site amyloid precursor protein-cleaving enzyme (BACE) by a statine-based peptide.
The Journal of biological chemistry 2001;276(26):23790-4.
2000: Dietmar Seiffert; Jodi D Bradley; Cynthia M Rominger; David H Rominger; F Yang; Jere E Meredith; Qian Wang; Arthur H Roach; Lorin A Thompson; Susan M Spitz; Jeffrey N Higaki; Shimoga R Prakash; Andrew P Combs; Robert Copeland; Stephen P Arneric; Paul R Hartig; David W Robertson; Barbara Cordell; Andrew M Stern; Richard E Olson; Robert Zaczek
Presenilin-1 and -2 are molecular targets for gamma-secretase inhibitors.
The Journal of biological chemistry 2000;275(44):34086-91.
2000: Robert Copeland; Jovita Marcinkeviciene; Tasir S Haque; Lisa M Kopcho; Wenjun Jiang; K Wang; L D Ecret; Christine F Sizemore; K A Amsler; L Foster; Seifu Tadesse; Andrew P Combs; Andrew M Stern; George L Trainor; Andrew Slee; Martin Rogers; Frank Hobbs
Helicobacter pylori-selective antibacterials based on inhibition of pyrimidine biosynthesis.
The Journal of biological chemistry 2000;275(43):33373-8.