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MERTK inhibition alters the PD-1 axis and promotes anti-leukemia immunity.
Lee-Sherick AB, Jacobsen KM, Henry CJ, Huey MG, Parker RE, Page LS, Hill AA, Wang X, Frye SV, Earp HS, Jordan CT, DeRyckere D, Graham DK. Lee-Sherick AB, et al. Among authors: earp hs. JCI Insight. 2018 Nov 2;3(21):e97941. doi: 10.1172/jci.insight.97941. JCI Insight. 2018. PMID: 30385715 Free PMC article.
Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group.
Zhao J, Zhang D, Zhang W, Stashko MA, DeRyckere D, Vasileiadi E, Parker RE, Hunter D, Liu Q, Zhang Y, Norris-Drouin J, Li B, Drewry DH, Kireev D, Graham DK, Earp HS, Frye SV, Wang X. Zhao J, et al. Among authors: earp hs. J Med Chem. 2018 Nov 21;61(22):10242-10254. doi: 10.1021/acs.jmedchem.8b01229. Epub 2018 Nov 5. J Med Chem. 2018. PMID: 30347155
UNC5293, a potent, orally available and highly MERTK-selective inhibitor.
Zheng H, Zhao J, Li B, Zhang W, Stashko MA, Minson KA, Huey MG, Zhou Y, Earp HS, Kireev D, Graham DK, DeRyckere D, Frye SV, Wang X. Zheng H, et al. Among authors: earp hs. Eur J Med Chem. 2021 Aug 5;220:113534. doi: 10.1016/j.ejmech.2021.113534. Epub 2021 May 17. Eur J Med Chem. 2021. PMID: 34038857
MERTK receptor tyrosine kinase is a therapeutic target in melanoma.
Schlegel J, Sambade MJ, Sather S, Moschos SJ, Tan AC, Winges A, DeRyckere D, Carson CC, Trembath DG, Tentler JJ, Eckhardt SG, Kuan PF, Hamilton RL, Duncan LM, Miller CR, Nikolaishvili-Feinberg N, Midkiff BR, Liu J, Zhang W, Yang C, Wang X, Frye SV, Earp HS, Shields JM, Graham DK. Schlegel J, et al. Among authors: earp hs. J Clin Invest. 2013 May;123(5):2257-67. doi: 10.1172/JCI67816. Epub 2013 Apr 15. J Clin Invest. 2013. PMID: 23585477 Free PMC article.
Molecular pathways: MERTK signaling in cancer.
Cummings CT, Deryckere D, Earp HS, Graham DK. Cummings CT, et al. Among authors: earp hs. Clin Cancer Res. 2013 Oct 1;19(19):5275-80. doi: 10.1158/1078-0432.CCR-12-1451. Epub 2013 Jul 5. Clin Cancer Res. 2013. PMID: 23833304 Free PMC article. Review.
UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with Methotrexate in Leukemia Models.
DeRyckere D, Lee-Sherick AB, Huey MG, Hill AA, Tyner JW, Jacobsen KM, Page LS, Kirkpatrick GG, Eryildiz F, Montgomery SA, Zhang W, Wang X, Frye SV, Earp HS, Graham DK. DeRyckere D, et al. Among authors: earp hs. Clin Cancer Res. 2017 Mar 15;23(6):1481-1492. doi: 10.1158/1078-0432.CCR-16-1330. Epub 2016 Sep 20. Clin Cancer Res. 2017. PMID: 27649555 Free PMC article.
212 results