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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: sparks r. 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. 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.
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: sparks r. 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: sparks rb. J Med Chem. 2006 Jun 29;49(13):3774-89. doi: 10.1021/jm0600904. J Med Chem. 2006. PMID: 16789735
Structural insights into the design of nonpeptidic isothiazolidinone-containing inhibitors of protein-tyrosine phosphatase 1B.
Ala PJ, Gonneville L, Hillman M, Becker-Pasha M, Yue EW, Douty B, Wayland B, Polam P, Crawley ML, McLaughlin E, Sparks RB, Glass B, Takvorian A, Combs AP, Burn TC, Hollis GF, Wynn R. Ala PJ, et al. Among authors: sparks rb. J Biol Chem. 2006 Dec 8;281(49):38013-21. doi: 10.1074/jbc.M607913200. Epub 2006 Oct 6. J Biol Chem. 2006. PMID: 17028182 Free article.
Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity.
Liu X, Shin N, Koblish HK, Yang G, Wang Q, Wang K, Leffet L, Hansbury MJ, Thomas B, Rupar M, Waeltz P, Bowman KJ, Polam P, Sparks RB, Yue EW, Li Y, Wynn R, Fridman JS, Burn TC, Combs AP, Newton RC, Scherle PA. Liu X, et al. Among authors: sparks rb. Blood. 2010 Apr 29;115(17):3520-30. doi: 10.1182/blood-2009-09-246124. Epub 2010 Mar 2. Blood. 2010. PMID: 20197554 Free 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 J, Favata M, Kelley JA, Caulder E, Thomas B, Wen X, Sparks RB, Arvanitis A, Rogers JD, Combs AP, Vaddi K, Solomon KA, Scherle PA, Newton R, Fridman JS. Li J, et al. Among authors: sparks rb. Neoplasia. 2010 Jan;12(1):28-38. doi: 10.1593/neo.91192. Neoplasia. 2010. PMID: 20072651 Free PMC article.
435 results