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Page 1
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: xue cb. 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
Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies.
Koblish H, Li YL, Shin N, Hall L, Wang Q, Wang K, Covington M, Marando C, Bowman K, Boer J, Burke K, Wynn R, Margulis A, Reuther GW, Lambert QT, Dostalik Roman V, Zhang K, Feng H, Xue CB, Diamond S, Hollis G, Yeleswaram S, Yao W, Huber R, Vaddi K, Scherle P. Koblish H, et al. Among authors: xue cb. PLoS One. 2018 Jun 21;13(6):e0199108. doi: 10.1371/journal.pone.0199108. eCollection 2018. PLoS One. 2018. PMID: 29927999 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: xue cb. 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.
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: xue cb. 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 and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344.
Brodmerkel CM, Huber R, Covington M, Diamond S, Hall L, Collins R, Leffet L, Gallagher K, Feldman P, Collier P, Stow M, Gu X, Baribaud F, Shin N, Thomas B, Burn T, Hollis G, Yeleswaram S, Solomon K, Friedman S, Wang A, Xue CB, Newton RC, Scherle P, Vaddi K. Brodmerkel CM, et al. Among authors: xue cb. J Immunol. 2005 Oct 15;175(8):5370-8. doi: 10.4049/jimmunol.175.8.5370. J Immunol. 2005. PMID: 16210643
Identification and characterization of INCB9471, an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5 with potent inhibitory activity against monocyte migration and HIV-1 infection.
Shin N, Solomon K, Zhou N, Wang KH, Garlapati V, Thomas B, Li Y, Covington M, Baribaud F, Erickson-Viitanen S, Czerniak P, Contel N, Liu P, Burn T, Hollis G, Yeleswaram S, Vaddi K, Xue CB, Metcalf B, Friedman S, Scherle P, Newton R. Shin N, et al. Among authors: xue cb. J Pharmacol Exp Ther. 2011 Jul;338(1):228-39. doi: 10.1124/jpet.111.179531. Epub 2011 Apr 1. J Pharmacol Exp Ther. 2011. PMID: 21459966
Pharmacological characterization of INCB3344, a small molecule antagonist of human CCR2.
Shin N, Baribaud F, Wang K, Yang G, Wynn R, Covington MB, Feldman P, Gallagher KB, Leffet LM, Lo YY, Wang A, Xue CB, Newton RC, Scherle PA. Shin N, et al. Among authors: xue cb. Biochem Biophys Res Commun. 2009 Sep 18;387(2):251-5. doi: 10.1016/j.bbrc.2009.06.135. Epub 2009 Jul 1. Biochem Biophys Res Commun. 2009. PMID: 19576173
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.
Xue CB, Wang A, Meloni D, Zhang K, Kong L, Feng H, Glenn J, Huang T, Zhang Y, Cao G, Anand R, Zheng C, Xia M, Han Q, Robinson DJ, Storace L, Shao L, Li M, Brodmerkel CM, Covington M, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B. Xue CB, et al. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7473-8. doi: 10.1016/j.bmcl.2010.10.020. Epub 2010 Oct 13. Bioorg Med Chem Lett. 2010. PMID: 21036044
Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.
Zheng C, Cao G, Xia M, Feng H, Glenn J, Anand R, Zhang K, Huang T, Wang A, Kong L, Li M, Galya L, Hughes RO, Devraj R, Morton PA, Rogier DJ, Covington M, Baribaud F, Shin N, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B, Xue CB. Zheng C, et al. Among authors: xue cb. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1442-6. doi: 10.1016/j.bmcl.2011.01.015. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21295478
Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.
Xue CB, Wang A, Han Q, Zhang Y, Cao G, Feng H, Huang T, Zheng C, Xia M, Zhang K, Kong L, Glenn J, Anand R, Meloni D, Robinson DJ, Shao L, Storace L, Li M, Hughes RO, Devraj R, Morton PA, Rogier DJ, Covington M, Scherle P, Diamond S, Emm T, Yeleswaram S, Contel N, Vaddi K, Newton R, Hollis G, Metcalf B. Xue CB, et al. ACS Med Chem Lett. 2011 Oct 5;2(12):913-8. doi: 10.1021/ml200199c. eCollection 2011 Dec 8. ACS Med Chem Lett. 2011. PMID: 24900280 Free PMC article.
81 results