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212 results

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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.
MerTK inhibition in tumor leukocytes decreases tumor growth and metastasis.
Cook RS, Jacobsen KM, Wofford AM, DeRyckere D, Stanford J, Prieto AL, Redente E, Sandahl M, Hunter DM, Strunk KE, Graham DK, Earp HS 3rd. Cook RS, et al. Among authors: earp hs 3rd. J Clin Invest. 2013 Aug;123(8):3231-42. doi: 10.1172/JCI67655. Epub 2013 Jul 8. J Clin Invest. 2013. PMID: 23867499 Free PMC article.
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.
MERTK Mediates Intrinsic and Adaptive Resistance to AXL-targeting Agents.
McDaniel NK, Cummings CT, Iida M, Hülse J, Pearson HE, Vasileiadi E, Parker RE, Orbuch RA, Ondracek OJ, Welke NB, Kang GH, Davies KD, Wang X, Frye SV, Earp HS, Harari PM, Kimple RJ, DeRyckere D, Graham DK, Wheeler DL. McDaniel NK, et al. Among authors: earp hs. Mol Cancer Ther. 2018 Nov;17(11):2297-2308. doi: 10.1158/1535-7163.MCT-17-1239. Epub 2018 Aug 9. Mol Cancer Ther. 2018. PMID: 30093568 Free PMC article.
212 results