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Structure-based design and discovery of protein tyrosine phosphatase inhibitors incorporating novel isothiazolidinone heterocyclic phosphotyrosine mimetics.
Combs AP, Yue EW, Bower M, Ala PJ, Wayland B, Douty B, Takvorian A, Polam P, Wasserman Z, Zhu W, Crawley ML, Pruitt J, Sparks R, Glass B, Modi D, McLaughlin E, Bostrom L, Li M, Galya L, Blom K, Hillman M, Gonneville L, Reid BG, Wei M, Becker-Pasha M, Klabe R, Huber R, Li Y, Hollis G, Burn TC, Wynn R, Liu P, Metcalf B. Combs AP, et al. Among authors: zhu w. J Med Chem. 2005 Oct 20;48(21):6544-8. doi: 10.1021/jm0504555. J Med Chem. 2005. PMID: 16220970
Potent benzimidazole sulfonamide protein tyrosine phosphatase 1B inhibitors containing the heterocyclic (S)-isothiazolidinone phosphotyrosine mimetic.
Combs AP, Zhu W, Crawley ML, Glass B, Polam P, Sparks RB, Modi D, Takvorian A, McLaughlin E, Yue EW, Wasserman Z, Bower M, Wei M, Rupar M, Ala PJ, Reid BM, Ellis D, Gonneville L, Emm T, Taylor N, Yeleswaram S, Li Y, Wynn R, Burn TC, Hollis G, Liu PC, Metcalf B. Combs AP, et al. Among authors: zhu w. J Med Chem. 2006 Jun 29;49(13):3774-89. doi: 10.1021/jm0600904. J Med Chem. 2006. PMID: 16789735
INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology.
Yue EW, Sparks R, Polam P, Modi D, Douty B, Wayland B, Glass B, Takvorian A, Glenn J, Zhu W, Bower M, Liu X, Leffet L, Wang Q, Bowman KJ, Hansbury MJ, Wei M, Li Y, Wynn R, Burn TC, Koblish HK, Fridman JS, Emm T, Scherle PA, Metcalf B, Combs AP. Yue EW, et al. Among authors: zhu w. ACS Med Chem Lett. 2017 Mar 6;8(5):486-491. doi: 10.1021/acsmedchemlett.6b00391. eCollection 2017 May 11. ACS Med Chem Lett. 2017. PMID: 28523098 Free PMC article.
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).
Yue EW, Li YL, Douty B, He C, Mei S, Wayland B, Maduskuie T, Falahatpisheh N, Sparks RB, Polam P, Zhu W, Glenn J, Feng H, Zhang K, Li Y, He X, Katiyar K, Covington M, Feldman P, Shin N, Wang KH, Diamond S, Li Y, Koblish HK, Hall L, Scherle P, Yeleswaram S, Xue CB, Metcalf B, Combs AP, Yao W. Yue EW, et al. Among authors: zhu w. ACS Med Chem Lett. 2019 Oct 17;10(11):1554-1560. doi: 10.1021/acsmedchemlett.9b00334. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749910 Free PMC article.
Discovery of INCB159020, an Orally Bioavailable KRAS G12D Inhibitor.
Ye Q, Shvartsbart A, Li Z, Gan P, Policarpo RL, Qi C, Roach JJ, Zhu W, McCammant MS, Hu B, Li G, Yin H, Carlsen P, Hoang G, Zhao L, Susick R, Zhang F, Lai CT, Allali Hassani A, Epling LB, Gallion A, Kurzeja-Lipinski K, Gallagher K, Roman V, Farren MR, Kong W, Deller MC, Zhang G, Covington M, Diamond S, Kim S, Yao W, Sokolsky A, Wang X. Ye Q, et al. Among authors: zhu w. J Med Chem. 2025 Jan 23;68(2):1924-1939. doi: 10.1021/acs.jmedchem.4c02662. Epub 2025 Jan 8. J Med Chem. 2025. PMID: 39772605
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