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)
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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)
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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)
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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)
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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)
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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)
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Parsaclisib Is a Next-Generation Phosphoinositide 3-Kinase δ Inhibitor with Reduced Hepatotoxicity and Potent Antitumor and Immunomodulatory Activities in Models of B-Cell Malignancy
Shin, Niu, Stubbs, Matthew, Koblish, Holly, Yue, Eddy W., Soloviev, Maxim, Douty, Brent, Wang, Kathy He, Wang, Qian, Gao, Mingming, Feldman, Patricia, Yang, Gengjie, Hall, Leslie, Hansbury, Michael, O’Connor, Sybil, Leffet, Lynn, Collins, Robert, Katiyar, Kamna, He, Xin, Waeltz, Paul, Collier, Paul, Lu, Jin, Li, Yun-Long, Li, Yanlong, Liu, Phillip C.C., Burn, Timothy, Covington, Maryanne, Diamond, Sharon, Shuey, Dana, Roberts, Alan, Yeleswaram, Swamy, Hollis, Greg, Metcalf, Brian, Yao, Wenqing, Huber, Reid, Combs, Andrew, Newton, Robert, Scherle, Peggy
Published in The Journal of pharmacology and experimental therapeutics (01.07.2020)
Published in The Journal of pharmacology and experimental therapeutics (01.07.2020)
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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
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)
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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)
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Synthesis and Evaluation of Indenopyrazoles as Cyclin-Dependent Kinase Inhibitors. 3. Structure Activity Relationships at C3
Yue, Eddy W, Higley, C. Anne, DiMeo, Susan V, Carini, David J, Nugiel, David A, Benware, Carrie, Benfield, Pamela A, Burton, Catherine R, Cox, Sarah, Grafstrom, Robert H, Sharp, Diane M, Sisk, Lisa M, Boylan, John F, Muckelbauer, Jodi K, Smallwood, Angela M, Chen, Haiying, Chang, Chong-Hwan, Seitz, Steven P, Trainor, George L
Published in Journal of medicinal chemistry (21.11.2002)
Published in Journal of medicinal chemistry (21.11.2002)
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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)
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Journal Article
Structure-Based Design and Discovery of Protein Tyrosine Phosphatase Inhibitors Incorporating Novel Isothiazolidinone Heterocyclic Phosphotyrosine Mimetics
Combs, Andrew P, Yue, Eddy W, Bower, Michael, Ala, Paul J, Wayland, Brian, Douty, Brent, Takvorian, Amy, Polam, Padmaja, Wasserman, Zelda, Zhu, Wenyu, Crawley, Matthew L, Pruitt, James, Sparks, Richard, Glass, Brian, Modi, Dilip, McLaughlin, Erin, Bostrom, Lori, Li, Mei, Galya, Laurine, Blom, Karl, Hillman, Milton, Gonneville, Lucie, Reid, Brian G, Wei, Min, Becker-Pasha, Mary, Klabe, Ronald, Huber, Reid, Li, Yanlong, Hollis, Gregory, Burn, Timothy C, Wynn, Richard, Liu, Phillip, Metcalf, Brian
Published in Journal of medicinal chemistry (20.10.2005)
Published in Journal of medicinal chemistry (20.10.2005)
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In Vitro Intrinsic Clearance-Based Optimization of N 3-Phenylpyrazinones as Corticotropin-Releasing Factor-1 (CRF1) Receptor Antagonists
Hartz, Richard A, Ahuja, Vijay T, Rafalski, Maria, Schmitz, William D, Brenner, Allison B, Denhart, Derek J, Ditta, Jonathan L, Deskus, Jeffrey A, Yue, Eddy W, Arvanitis, Argyrios G, Lelas, Snjezana, Li, Yu-Wen, Molski, Thaddeus F, Wong, Harvey, Grace, James E, Lentz, Kimberley A, Li, Jianqing, Lodge, Nicholas J, Zaczek, Robert, Combs, Andrew P, Olson, Richard E, Mattson, Ronald J, Bronson, Joanne J, Macor, John E
Published in Journal of medicinal chemistry (23.07.2009)
Published in Journal of medicinal chemistry (23.07.2009)
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Isothiazolidinone heterocycles as inhibitors of protein tyrosine phosphatases: Synthesis and structure–activity relationships of a peptide scaffold
Yue, Eddy W., Wayland, Brian, Douty, Brent, Crawley, Matthew L., McLaughlin, Erin, Takvorian, Amy, Wasserman, Zelda, Bower, Michael J., Wei, Min, Li, Yanlong, Ala, Paul J., Gonneville, Lucie, Wynn, Richard, Burn, Timothy C., Liu, Phillip C.C., Combs, Andrew P.
Published in Bioorganic & medicinal chemistry (01.09.2006)
Published in Bioorganic & medicinal chemistry (01.09.2006)
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Synthesis, Structure−Activity Relationships, and In Vivo Evaluation of N 3-Phenylpyrazinones as Novel Corticotropin-Releasing Factor-1 (CRF1) Receptor Antagonists
Hartz, Richard A, Ahuja, Vijay T, Arvanitis, Argyrios G, Rafalski, Maria, Yue, Eddy W, Denhart, Derek J, Schmitz, William D, Ditta, Jonathan L, Deskus, Jeffrey A, Brenner, Allison B, Hobbs, Frank W, Payne, Joseph, Lelas, Snjezana, Li, Yu-Wen, Molski, Thaddeus F, Mattson, Gail K, Peng, Yong, Wong, Harvey, Grace, James E, Lentz, Kimberley A, Qian-Cutrone, Jingfang, Zhuo, Xiaoliang, Shu, Yue-Zhong, Lodge, Nicholas J, Zaczek, Robert, Combs, Andrew P, Olson, Richard E, Bronson, Joanne J, Mattson, Ronald J, Macor, John E
Published in Journal of medicinal chemistry (23.07.2009)
Published in Journal of medicinal chemistry (23.07.2009)
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포스포이노시티드 3-키나아제 (PI3K) 억제제의 결정질 형태
BURNS DAVID M, COMBS ANDREW P, YUE EDDY W, DOUTY BRENT, JIA ZHONGJIANG, LEVY DANIEL
Year of Publication 21.07.2021
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Year of Publication 21.07.2021
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HETEROCYCLYLAMINES AS PI3K INHIBITORS
ANDREW P COMBS, YAO WENQING, HE CHUNHONG, MADUSKUIE JR THOMAS P, SPARKS RICHARD B, MEI SONG, YUE EDDY W, ZHU WENYU, LI YUN-LONG, GLENN JOSEPH, BRENT DOUTY
Year of Publication 28.12.2023
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Year of Publication 28.12.2023
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PI3K USE OF PYRAZOLOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PI3K RELATED DISORDERS
YAO WENQING, HE CHUNHONG, SPARKS RICHARD B, MEI SONG, LI YUN LONG, COMBS ANDREW P, MADUSKUIE JR. THOMAS P, YUE EDDY W, ZHU WENYU, DOUTY BRENT, GLENN JOSEPH
Year of Publication 17.10.2023
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Year of Publication 17.10.2023
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CONDENSED IMIDAZOLE DERIVATIVES SUBSTITUTED WITH TERTIARY HYDROXY GROUPS AS PI3K-γ INHIBITORS
JALLURI RAVI KUMAR, ANDREW P COMBS, FALAHATPISHEH NIKOO, SPARKS RICHARD B, SHEPARD STACEY, ARTEM SHVARTSBART, DAVID M BURNS, ANDREW W BUESKING, DANIEL LEVY, PADMAJA POLAM, SHAO LIXIN, YUE EDDY W, BRENT DOUTY
Year of Publication 20.06.2023
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Year of Publication 20.06.2023
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HETEROCYCLYLAMINES AS PI3K INHIBITORS
YAO WENQING, HE CHUNHONG, SPARKS RICHARD B, MEI SONG, LI YUN LONG, COMBS ANDREW P, YUE EDDY W, ZHU WENYU, DOUTY BRENT, MADUSKUIE THOMAS P. JR, GLENN JOSEPH
Year of Publication 20.03.2023
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Year of Publication 20.03.2023
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