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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: burn tc. 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. 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
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: burn tc. 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
Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.
Wu L, Zhang C, He C, Qian D, Lu L, Sun Y, Xu M, Zhuo J, Liu PCC, Klabe R, Wynn R, Covington M, Gallagher K, Leffet L, Bowman K, Diamond S, Koblish H, Zhang Y, Soloviev M, Hollis G, Burn TC, Scherle P, Yeleswaram S, Huber R, Yao W. Wu L, et al. Among authors: burn tc. J Med Chem. 2021 Aug 12;64(15):10666-10679. doi: 10.1021/acs.jmedchem.1c00713. Epub 2021 Jul 16. J Med Chem. 2021. PMID: 34269576
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. J Immunol. 2005 Oct 15;175(8):5370-8. doi: 10.4049/jimmunol.175.8.5370. J Immunol. 2005. PMID: 16210643
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. 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
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.
Yao W, Zhuo J, Burns DM, Xu M, Zhang C, Li YL, Qian DQ, He C, Weng L, Shi E, Lin Q, Agrios C, Burn TC, Caulder E, Covington MB, Fridman JS, Friedman S, Katiyar K, Hollis G, Li Y, Liu C, Liu X, Marando CA, Newton R, Pan M, Scherle P, Taylor N, Vaddi K, Wasserman ZR, Wynn R, Yeleswaram S, Jalluri R, Bower M, Zhou BB, Metcalf B. Yao W, et al. Among authors: burn tc. J Med Chem. 2007 Feb 22;50(4):603-6. doi: 10.1021/jm061344o. Epub 2007 Jan 26. J Med Chem. 2007. PMID: 17256836
Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.
Fridman JS, Scherle PA, Collins R, Burn TC, Li Y, Li J, Covington MB, Thomas B, Collier P, Favata MF, Wen X, Shi J, McGee R, Haley PJ, Shepard S, Rodgers JD, Yeleswaram S, Hollis G, Newton RC, Metcalf B, Friedman SM, Vaddi K. Fridman JS, et al. Among authors: burn tc. J Immunol. 2010 May 1;184(9):5298-307. doi: 10.4049/jimmunol.0902819. Epub 2010 Apr 2. J Immunol. 2010. PMID: 20363976
Preclinical evaluation of local JAK1 and JAK2 inhibition in cutaneous inflammation.
Fridman JS, Scherle PA, Collins R, Burn T, Neilan CL, Hertel D, Contel N, Haley P, Thomas B, Shi J, Collier P, Rodgers JD, Shepard S, Metcalf B, Hollis G, Newton RC, Yeleswaram S, Friedman SM, Vaddi K. Fridman JS, et al. J Invest Dermatol. 2011 Sep;131(9):1838-44. doi: 10.1038/jid.2011.140. Epub 2011 Jun 16. J Invest Dermatol. 2011. PMID: 21677670 Free article.
80 results