Publications by authors named "Andrew P Combs"

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INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).
Eddy W Yue, Yun-Long Li, Brent Douty, Chunhong He, Song Mei, Andrew P Combs

ACS Med Chem Lett· November 2019

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The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies.
Matthew C Stubbs, Timothy C Burn, Richard Sparks, Thomas Maduskuie, Sharon Diamond, Andrew P Combs

Clin Cancer Res· January 2019

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INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology.
Eddy W Yue, Richard Sparks, Padmaja Polam, Dilip Modi, Brent Douty, Andrew P Combs

ACS Med Chem Lett· May 2017

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Roles of UGT, P450, and Gut Microbiota in the Metabolism of Epacadostat in Humans.
Jason Boer, Ruth Young-Sciame, Fiona Lee, Kevin J Bowman, Xiaoqing Yang, Andrew P Combs

Drug Metab Dispos· October 2016

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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.
Carolyn D Dzierba, Thais M Sielecki, Argyrios G Arvanitis, Amy Galka, Tricia L Johnson, Andrew P Combs

Bioorg Med Chem Lett· August 2012

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Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.
Lorin A Thompson, Jianliang Shi, Carl P Decicco, Andrew J Tebben, Richard E Olson, Andrew P Combs

Bioorg Med Chem Lett· November 2011

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Efficacy of the JAK2 inhibitor INCB16562 in a murine model of MPLW515L-induced thrombocytosis and myelofibrosis.
Priya Koppikar, Omar Abdel-Wahab, Cyrus Hedvat, Sachie Marubayashi, Jay Patel, Andrew P Combs

Blood· April 2010

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Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity.
Xiangdong Liu, Niu Shin, Holly K Koblish, Gengjie Yang, Qian Wang, Andrew P Combs

Blood· April 2010

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Recent advances in the discovery of competitive protein tyrosine phosphatase 1B inhibitors for the treatment of diabetes, obesity, and cancer.
Andrew P Combs

J Med Chem· March 2010

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Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors.
Holly K Koblish, Michael J Hansbury, Kevin J Bowman, Gengjie Yang, Claire L Neilan, Andrew P Combs

Mol Cancer Ther· February 2010

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INCB16562, a JAK1/2 selective inhibitor, is efficacious against multiple myeloma cells and reverses the protective effects of cytokine and stromal cell support.
Jun Li, Margaret Favata, Jennifer A Kelley, Eian Caulder, Beth Thomas, Andrew P Combs

Neoplasia· January 2010

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Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.
Eddy W Yue, Brent Douty, Brian Wayland, Michael Bower, Xiangdong Liu, Andrew P Combs

J Med Chem· December 2009

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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.
Phillip C C Liu, Eian Caulder, Jun Li, Paul Waeltz, Alex Margulis, Andrew P Combs

Clin Cancer Res· November 2009

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In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Richard A Hartz, Vijay T Ahuja, Maria Rafalski, William D Schmitz, Allison B Brenner, Andrew P Combs

J Med Chem· July 2009

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Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.
Richard A Hartz, Vijay T Ahuja, Argyrios G Arvanitis, Maria Rafalski, Eddy W Yue, Andrew P Combs

J Med Chem· July 2009

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Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines.
Brent Douty, Brian Wayland, Paul J Ala, Michael J Bower, James Pruitt, Andrew P Combs

Bioorg Med Chem Lett· January 2008

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Dihydropyridopyrazinones and dihydropteridinones as corticotropin-releasing factor-1 receptor antagonists: structure-activity relationships and computational modeling.
Carolyn D Dzierba, Andrew J Tebben, Richard G Wilde, Amy G Takvorian, Maria Rafalski, Andrew P Combs

J Med Chem· May 2007

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Asymmetric synthesis of the (S)-1,1-dioxido-isothiazolidin-3-one phosphotyrosine mimetic via reduction of a homochiral (R)-oxido-isothiazolidin-3-one.
Andrew P Combs, Brian Glass, Laurine G Galya, Mei Li

Org Lett· March 2007

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Benzothiazole benzimidazole (S)-isothiazolidinone derivatives as protein tyrosine phosphatase-1B inhibitors.
Richard B Sparks, Padmaja Polam, Wenyu Zhu, Matthew L Crawley, Amy Takvorian, Andrew P Combs

Bioorg Med Chem Lett· February 2007

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Structure-based drug design of new leads for phosphatase research.
Andrew P Combs

IDrugs· February 2007

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Structural insights into the design of nonpeptidic isothiazolidinone-containing inhibitors of protein-tyrosine phosphatase 1B.
Paul J Ala, Lucie Gonneville, Milton Hillman, Mary Becker-Pasha, Eddy W Yue, Andrew P Combs

J Biol Chem· December 2006

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Structural basis for inhibition of protein-tyrosine phosphatase 1B by isothiazolidinone heterocyclic phosphonate mimetics.
Paul J Ala, Lucie Gonneville, Milton C Hillman, Mary Becker-Pasha, Min Wei, Andrew P Combs

J Biol Chem· October 2006

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Isothiazolidinone heterocycles as inhibitors of protein tyrosine phosphatases: synthesis and structure-activity relationships of a peptide scaffold.
Eddy W Yue, Brian Wayland, Brent Douty, Matthew L Crawley, Eric McLaughlin, Andrew P Combs

Bioorg Med Chem· September 2006

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Potent benzimidazole sulfonamide protein tyrosine phosphatase 1B inhibitors containing the heterocyclic (S)-isothiazolidinone phosphotyrosine mimetic.
Andrew P Combs, Wenyu Zhu, Matthew L Crawley, Brian Glass, Padmaja Polam

J Med Chem· June 2006

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Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.
Lorin A Thompson, Ann Y Liauw, Mercy M Ramanjulu, Padmaja Kasireddy-Polam, Stephen E Mercer, Andrew P Combs

Bioorg Med Chem Lett· May 2006

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