INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology
Yue, Eddy W, Sparks, Richard, Polam, Padmaja, Modi, Dilip, Douty, Brent, Wayland, Brian, Glass, Brian, Takvorian, Amy, Glenn, Joseph, Zhu, Wenyu, Bower, Michael, Liu, Xiangdong, Leffet, Lynn, Wang, Qian, Bowman, Kevin J, Hansbury, Michael J, Wei, Min, Li, Yanlong, Wynn, Richard, Burn, Timothy C, Koblish, Holly K, Fridman, Jordan S, Emm, Tom, Scherle, Peggy A, Metcalf, Brian, Combs, Andrew P
Published in ACS medicinal chemistry letters (11.05.2017)
Published in ACS medicinal chemistry letters (11.05.2017)
Get full text
Journal Article
Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity
Liu, Xiangdong, Shin, Niu, Koblish, Holly K., Yang, Gengjie, Wang, Qian, Wang, Kathy, Leffet, Lynn, Hansbury, Michael J., Thomas, Beth, Rupar, Mark, Waeltz, Paul, Bowman, Kevin J., Polam, Padmaja, Sparks, Richard B., Yue, Eddy W., Li, Yanlong, Wynn, Richard, Fridman, Jordan S., Burn, Timothy C., Combs, Andrew P., Newton, Robert C., Scherle, Peggy A.
Published in Blood (29.04.2010)
Published in Blood (29.04.2010)
Get full text
Journal Article
Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors
Koblish, Holly K, Hansbury, Michael J, Bowman, Kevin J, Yang, Gengjie, Neilan, Claire L, Haley, Patrick J, Burn, Timothy C, Waeltz, Paul, Sparks, Richard B, Yue, Eddy W, Combs, Andrew P, Scherle, Peggy A, Vaddi, Kris, Fridman, Jordan S
Published in Molecular cancer therapeutics (01.02.2010)
Published in Molecular cancer therapeutics (01.02.2010)
Get full text
Journal Article
INCB16562, a JAK1/2 Selective Inhibitor, Is Efficacious against Multiple Myeloma Cells and Reverses the Protective Effects of Cytokine and Stromal Cell Support
Li, Jun, Favata, Margaret, Kelley, Jennifer A., Caulder, Eian, Thomas, Beth, Wen, Xiaoming, Sparks, Richard B., Arvanitis, Ari, Rogers, James D., Combs, Andrew P., Vaddi, Kris, Solomon, Kimberly A., Scherle, Peggy A., Newton, Robert, Fridman, Jordan S.
Published in Neoplasia (New York, N.Y.) (01.01.2010)
Published in Neoplasia (New York, N.Y.) (01.01.2010)
Get full text
Journal Article
Structural Basis for Inhibition of Protein-tyrosine Phosphatase 1B by Isothiazolidinone Heterocyclic Phosphonate Mimetics
Ala, Paul J., Gonneville, Lucie, Hillman, Milton C., Becker-Pasha, Mary, Wei, Min, Reid, Brian G., Klabe, Ronald, Yue, Eddy W., Wayland, Brian, Douty, Brent, Polam, Padmaja, Wasserman, Zelda, Bower, Michael, Combs, Andrew P., Burn, Timothy C., Hollis, Gregory F., Wynn, Richard
Published in The Journal of biological chemistry (27.10.2006)
Published in The Journal of biological chemistry (27.10.2006)
Get full text
Journal Article
Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines
Douty, Brent, Wayland, Brian, Ala, Paul J., Bower, Michael J., Pruitt, James, Bostrom, Lori, Wei, Min, Klabe, Ronald, Gonneville, Lucie, Wynn, Richard, Burn, Timothy C., Liu, Phillip C.C., Combs, Andrew P., Yue, Eddy W.
Published in Bioorganic & medicinal chemistry letters (2008)
Published in Bioorganic & medicinal chemistry letters (2008)
Get full text
Journal Article
Structural Insights into the Design of Nonpeptidic Isothiazolidinone-containing Inhibitors of Protein-tyrosine Phosphatase 1B
Ala, Paul J., Gonneville, Lucie, Hillman, Milton, Becker-Pasha, Mary, Yue, Eddy W., Douty, Brent, Wayland, Brian, Polam, Padmaja, Crawley, Matthew L., McLaughlin, Erin, Sparks, Richard B., Glass, Brian, Takvorian, Amy, Combs, Andrew P., Burn, Timothy C., Hollis, Gregory F., Wynn, Richard
Published in The Journal of biological chemistry (08.12.2006)
Published in The Journal of biological chemistry (08.12.2006)
Get full text
Journal Article
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
Liu, Phillip C C, Caulder, Eian, Li, Jun, Waeltz, Paul, Margulis, Alex, Wynn, Richard, Becker-Pasha, Mary, Li, Yanlong, Crowgey, Erin, Hollis, Gregory, Haley, Patrick, Sparks, Richard B, Combs, Andrew P, Rodgers, James D, Burn, Timothy C, Vaddi, Kris, Fridman, Jordan S
Published in Clinical cancer research (15.11.2009)
Published in Clinical cancer research (15.11.2009)
Get full text
Journal Article
Discovery of Potent Competitive Inhibitors of Indoleamine 2,3-Dioxygenase with in Vivo Pharmacodynamic Activity and Efficacy in a Mouse Melanoma Model
Yue, Eddy W, Douty, Brent, Wayland, Brian, Bower, Michael, Liu, Xiangdong, Leffet, Lynn, Wang, Qian, Bowman, Kevin J, Hansbury, Michael J, Liu, Changnian, Wei, Min, Li, Yanlong, Wynn, Richard, Burn, Timothy C, Koblish, Holly K, Fridman, Jordan S, Metcalf, Brian, Scherle, Peggy A, Combs, Andrew P
Published in Journal of medicinal chemistry (10.12.2009)
Published in Journal of medicinal chemistry (10.12.2009)
Get full text
Journal Article
The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies
Stubbs, Matthew C, Burn, Timothy C, Sparks, Richard, Maduskuie, Thomas, Diamond, Sharon, Rupar, Mark, Wen, Xiaoming, Volgina, Alla, Zolotarjova, Nina, Waeltz, Paul, Favata, Margaret, Jalluri, Ravi, Liu, Huiqing, Liu, Xuesong Mike, Li, Jun, Collins, Robert, Falahatpisheh, Nikoo, Polam, Padmaja, DiMatteo, Darlise, Feldman, Patricia, Dostalik, Valerie, Thekkat, Pramod, Gardiner, Christine, He, Xin, Li, Yanlong, Covington, Maryanne, Wynn, Richard, Ruggeri, Bruce, Yeleswaram, Swamy, Xue, Chu-Biao, Yao, Wenqing, Combs, Andrew P, Huber, Reid, Hollis, Gregory, Scherle, Peggy, Liu, Phillip C C
Published in Clinical cancer research (01.01.2019)
Published in Clinical cancer research (01.01.2019)
Get full text
Journal Article
Parallel Synthesis of Potent, Pyrazole-Based Inhibitors of Helicobacter pylori Dihydroorotate Dehydrogenase
HAQUE, Tasir S., TADESSE, Seifu, MARCINKEVICIENE, Jovita, ROGERS, M. John, SIZEMORE, Christine, KOPCHO, Lisa M., AMSLER, Karen, ECRET, Lisa D., ZHAN, Dong Liang, HOBBS, Frank, SLEE, Andrew, TRAINOR, George L., STERN, Andrew M., COPELAND, Robert A., COMBS, Andrew P.
Published in Journal of medicinal chemistry (10.10.2002)
Published in Journal of medicinal chemistry (10.10.2002)
Get full text
Journal Article
Roles of UGT, P450, and Gut Microbiota in the Metabolism of Epacadostat in Humans
Boer, Jason, Young-Sciame, Ruth, Lee, Fiona, Bowman, Kevin J, Yang, Xiaoqing, Shi, Jack G, Nedza, Frank M, Frietze, William, Galya, Laurine, Combs, Andrew P, Yeleswaram, Swamy, Diamond, Sharon
Published in Drug metabolism and disposition (01.10.2016)
Published in Drug metabolism and disposition (01.10.2016)
Get full text
Journal Article
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3‑Kinase Delta (PI3Kδ)
Yue, Eddy W, Li, Yun-Long, Douty, Brent, He, Chunhong, Mei, Song, Wayland, Brian, Maduskuie, Thomas, Falahatpisheh, Nikoo, Sparks, Richard B, Polam, Padmaja, Zhu, Wenyu, Glenn, Joseph, Feng, Hao, Zhang, Ke, Li, Yanlong, He, Xin, Katiyar, Kamna, Covington, Maryanne, Feldman, Patricia, Shin, Niu, Wang, Kathy He, Diamond, Sharon, Li, Yu, Koblish, Holly K, Hall, Leslie, Scherle, Peggy, Yeleswaram, Swamy, Xue, Chu-Biao, Metcalf, Brian, Combs, Andrew P, Yao, Wenqing
Published in ACS medicinal chemistry letters (14.11.2019)
Published in ACS medicinal chemistry letters (14.11.2019)
Get full text
Journal Article
Efficacy of the JAK2 inhibitor INCB16562 in a murine model of MPLW515L-induced thrombocytosis and myelofibrosis
Koppikar, Priya, Abdel-Wahab, Omar, Hedvat, Cyrus, Marubayashi, Sachie, Patel, Jay, Goel, Aviva, Kucine, Nicole, Gardner, Jeffrey R., Combs, Andrew P., Vaddi, Kris, Haley, Patrick J., Burn, Timothy C., Rupar, Mark, Bromberg, Jacqueline F., Heaney, Mark L., de Stanchina, Elisa, Fridman, Jordan S., Levine, Ross L.
Published in Blood (08.04.2010)
Published in Blood (08.04.2010)
Get full text
Journal Article
Abstract 3780: Activity of the BET inhibitor INCB054329 in models of lymphoma
Stubbs, Matthew, Collins, Robert, Volgina, Alla, Liu, Mike, Favata, Margaret, Rupar, Mark, Wen, Xiaomng, Sparks, Richard, Maduskuie, Thomas, Covington, Maryanne, Burn, Timothy, Ruggeri, Bruce, Combs, Andrew P., Yao, Wenqing, Huber, Reid, Hollis, Gregory, Scherle, Peggy, Liu, Phillip CC
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Get full text
Journal Article
Multiple-Component Condensation Strategies for Combinatorial Library Synthesis
Armstrong, Robert W, Combs, Andrew P, Tempest, Paul A, Brown, S. David, Keating, Thomas A
Published in Accounts of chemical research (13.03.1996)
Published in Accounts of chemical research (13.03.1996)
Get full text
Journal Article
Potent Benzimidazole Sulfonamide Protein Tyrosine Phosphatase 1B Inhibitors Containing the Heterocyclic (S)-Isothiazolidinone Phosphotyrosine Mimetic
Combs, Andrew P, Zhu, Wenyu, Crawley, Matthew L, Glass, Brian, Polam, Padmaja, Sparks, Richard B, Modi, Dilip, Takvorian, Amy, McLaughlin, Erin, Yue, Eddy W, Wasserman, Zelda, Bower, Michael, Wei, Min, Rupar, Mark, Ala, Paul J, Reid, Brian M, Ellis, Dawn, Gonneville, Lucie, Emm, Thomas, Taylor, Nancy, Yeleswaram, Swamy, Li, Yanlong, Wynn, Richard, Burn, Timothy C, Hollis, Gregory, Liu, Phillip C. C, Metcalf, Brian
Published in Journal of medicinal chemistry (29.06.2006)
Published in Journal of medicinal chemistry (29.06.2006)
Get full text
Journal Article
N-Arylation of α-aminoesters with p-tolylboronic acid promoted by copper(II) acetate
Lam, Patrick Y.S, Bonne, Damien, Vincent, Guillaume, Clark, Charles G, Combs, Andrew P
Published in Tetrahedron letters (17.02.2003)
Published in Tetrahedron letters (17.02.2003)
Get full text
Journal Article