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INCB040093 Is a Novel PI3Kδ Inhibitor for the Treatment of B Cell Lymphoid Malignancies.
Shin N, Li YL, Mei S, Wang KH, Hall L, Katiyar K, Wang Q, Yang G, Rumberger B, Leffet L, He X, Rupar M, Bowman K, Favata M, Li J, Liu M, Li Y, Covington M, Koblish H, Soloviev M, Shuey D, Burn T, Diamond S, Fridman J, Combs A, Yao W, Yeleswaram S, Hollis G, Vaddi K, Huber R, Newton R, Scherle P. Shin N, et al. Among authors: he x. J Pharmacol Exp Ther. 2018 Jan;364(1):120-130. doi: 10.1124/jpet.117.244947. Epub 2017 Nov 10. J Pharmacol Exp Ther. 2018. PMID: 29127109
INCB38579, a novel and potent histamine H₄ receptor small molecule antagonist with anti-inflammatory pain and anti-pruritic functions.
Shin N, Covington M, Bian D, Zhuo J, Bowman K, Li Y, Soloviev M, Qian DQ, Feldman P, Leffet L, He X, He Wang K, Krug K, Bell D, Czerniak P, Hu Z, Zhao H, Zhang J, Yeleswaram S, Yao W, Newton R, Scherle P. Shin N, et al. Among authors: he x, he wang k. Eur J Pharmacol. 2012 Jan 30;675(1-3):47-56. doi: 10.1016/j.ejphar.2011.11.027. Epub 2011 Nov 27. Eur J Pharmacol. 2012. PMID: 22155710
The Novel Bromodomain and Extraterminal Domain Inhibitor INCB054329 Induces Vulnerabilities in Myeloma Cells That Inform Rational Combination Strategies.
Stubbs MC, Burn TC, Sparks R, Maduskuie T, Diamond S, Rupar M, Wen X, Volgina A, Zolotarjova N, Waeltz P, Favata M, Jalluri R, Liu H, Liu XM, Li J, Collins R, Falahatpisheh N, Polam P, DiMatteo D, Feldman P, Dostalik V, Thekkat P, Gardiner C, He X, Li Y, Covington M, Wynn R, Ruggeri B, Yeleswaram S, Xue CB, Yao W, Combs AP, Huber R, Hollis G, Scherle P, Liu PCC. Stubbs MC, et al. Among authors: he x. Clin Cancer Res. 2019 Jan 1;25(1):300-311. doi: 10.1158/1078-0432.CCR-18-0098. Epub 2018 Sep 11. Clin Cancer Res. 2019. PMID: 30206163
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: he c, he x. 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.
INCB054828 (pemigatinib), a potent and selective inhibitor of fibroblast growth factor receptors 1, 2, and 3, displays activity against genetically defined tumor models.
Liu PCC, Koblish H, Wu L, Bowman K, Diamond S, DiMatteo D, Zhang Y, Hansbury M, Rupar M, Wen X, Collier P, Feldman P, Klabe R, Burke KA, Soloviev M, Gardiner C, He X, Volgina A, Covington M, Ruggeri B, Wynn R, Burn TC, Scherle P, Yeleswaram S, Yao W, Huber R, Hollis G. Liu PCC, et al. Among authors: he x. PLoS One. 2020 Apr 21;15(4):e0231877. doi: 10.1371/journal.pone.0231877. eCollection 2020. PLoS One. 2020. PMID: 32315352 Free PMC article.
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 N, Stubbs M, Koblish H, Yue EW, Soloviev M, Douty B, Wang KH, Wang Q, Gao M, Feldman P, Yang G, Hall L, Hansbury M, O'Connor S, Leffet L, Collins R, Katiyar K, He X, Waeltz P, Collier P, Lu J, Li YL, Li Y, Liu PCC, Burn T, Covington M, Diamond S, Shuey D, Roberts A, Yeleswaram S, Hollis G, Metcalf B, Yao W, Huber R, Combs A, Newton R, Scherle P. Shin N, et al. Among authors: he x. J Pharmacol Exp Ther. 2020 Jul;374(1):211-222. doi: 10.1124/jpet.120.265538. Epub 2020 Apr 28. J Pharmacol Exp Ther. 2020. PMID: 32345620
Preclinical characterization of itacitinib (INCB039110), a novel selective inhibitor of JAK1, for the treatment of inflammatory diseases.
Covington M, He X, Scuron M, Li J, Collins R, Juvekar A, Shin N, Favata M, Gallagher K, Sarah S, Xue CB, Peel M, Burke K, Oliver J, Fay B, Yao W, Huang T, Scherle P, Diamond S, Newton R, Zhang Y, Smith P. Covington M, et al. Among authors: he x. Eur J Pharmacol. 2020 Oct 15;885:173505. doi: 10.1016/j.ejphar.2020.173505. Epub 2020 Aug 28. Eur J Pharmacol. 2020. PMID: 32861662
Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.
Shvartsbart A, Roach JJ, Witten MR, Koblish H, Harris JJ, Covington M, Hess R, Lin L, Frascella M, Truong L, Leffet L, Conlen P, Beshad E, Klabe R, Katiyar K, Kaldon L, Young-Sciame R, He X, Petusky S, Chen KJ, Horsey A, Lei HT, Epling LB, Deller MC, Vechorkin O, Yao W. Shvartsbart A, et al. Among authors: he x. J Med Chem. 2022 Nov 24;65(22):15433-15442. doi: 10.1021/acs.jmedchem.2c01366. Epub 2022 Nov 10. J Med Chem. 2022. PMID: 36356320
Discovery of Pyrazolopyridine Derivatives as HPK1 Inhibitors.
Ye Q, Liu K, Ye HF, Pan J, Sokolsky A, Wang A, Zhang K, Hummel JR, Kong L, Behshad E, He X, Conlen P, Stump K, Ye M, Diamond S, Covington M, Yeleswaram S, Atasoylu O, Vechorkin O, Yao W. Ye Q, et al. Among authors: he x. ACS Med Chem Lett. 2022 Dec 12;14(1):5-10. doi: 10.1021/acsmedchemlett.2c00238. eCollection 2023 Jan 12. ACS Med Chem Lett. 2022. PMID: 36655125 Free PMC article.
Potent and Selective Biaryl Amide Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).
Sokolsky A, Vechorkin O, Hummel JR, Styduhar ED, Wang A, Nguyen MH, Ye HF, Liu K, Zhang K, Pan J, Ye Q, Atasoylu O, Behshad E, He X, Conlen P, Stump K, Ye M, Diamond S, Covington M, Yeleswaram S, Yao W. Sokolsky A, et al. Among authors: he x. ACS Med Chem Lett. 2022 Dec 13;14(1):116-122. doi: 10.1021/acsmedchemlett.2c00241. eCollection 2023 Jan 12. ACS Med Chem Lett. 2022. PMID: 36655134 Free PMC article.
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