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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.
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.
UNC569, a novel small-molecule mer inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo.
Christoph S, Deryckere D, Schlegel J, Frazer JK, Batchelor LA, Trakhimets AY, Sather S, Hunter DM, Cummings CT, Liu J, Yang C, Kireev D, Simpson C, Norris-Drouin J, Hull-Ryde EA, Janzen WP, Johnson GL, Wang X, Frye SV, Earp HS 3rd, Graham DK. Christoph S, et al. Among authors: earp hs 3rd. Mol Cancer Ther. 2013 Nov;12(11):2367-77. doi: 10.1158/1535-7163.MCT-13-0040. Epub 2013 Aug 30. Mol Cancer Ther. 2013. PMID: 23997116 Free PMC article.
UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor.
Zhang W, DeRyckere D, Hunter D, Liu J, Stashko MA, Minson KA, Cummings CT, Lee M, Glaros TG, Newton DL, Sather S, Zhang D, Kireev D, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X. Zhang W, et al. Among authors: earp hs. J Med Chem. 2014 Aug 28;57(16):7031-41. doi: 10.1021/jm500749d. Epub 2014 Aug 6. J Med Chem. 2014. PMID: 25068800 Free PMC article.
The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia.
Minson KA, Smith CC, DeRyckere D, Libbrecht C, Lee-Sherick AB, Huey MG, Lasater EA, Kirkpatrick GD, Stashko MA, Zhang W, Jordan CT, Kireev D, Wang X, Frye SV, Earp HS, Shah NP, Graham DK. Minson KA, et al. Among authors: earp hs. JCI Insight. 2016 Mar;1(3):e85630. doi: 10.1172/jci.insight.85630. JCI Insight. 2016. PMID: 27158668 Free PMC article.
212 results