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The small-molecule MERTK inhibitor UNC2025 decreases platelet activation and prevents thrombosis.
Branchford BR, Stalker TJ, Law L, Acevedo G, Sather S, Brzezinski C, Wilson KM, Minson K, Lee-Sherick AB, Davizon-Castillo P, Ng C, Zhang W, Neeves KB, Lentz SR, Wang X, Frye SV, Shelton Earp H 3rd, DeRyckere D, Brass LF, Graham DK, Di Paola JA. Branchford BR, et al. Among authors: zhang w. J Thromb Haemost. 2018 Feb;16(2):352-363. doi: 10.1111/jth.13875. Epub 2018 Jan 12. J Thromb Haemost. 2018. PMID: 29045015 Free PMC article.
UNC1062, a new and potent Mer inhibitor.
Liu J, Zhang W, Stashko MA, Deryckere D, Cummings CT, Hunter D, Yang C, Jayakody CN, Cheng N, Simpson C, Norris-Drouin J, Sather S, Kireev D, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X. Liu J, et al. Among authors: zhang w. Eur J Med Chem. 2013 Jul;65:83-93. doi: 10.1016/j.ejmech.2013.03.035. Epub 2013 Apr 2. Eur J Med Chem. 2013. PMID: 23693152 Free PMC article.
Pseudo-cyclization through intramolecular hydrogen bond enables discovery of pyridine substituted pyrimidines as new Mer kinase inhibitors.
Zhang W, Zhang D, Stashko MA, DeRyckere D, Hunter D, Kireev D, Miley MJ, Cummings C, Lee M, Norris-Drouin J, Stewart WM, Sather S, Zhou Y, Kirkpatrick G, Machius M, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X. Zhang W, et al. Among authors: zhang d. J Med Chem. 2013 Dec 12;56(23):9683-92. doi: 10.1021/jm401387j. Epub 2013 Nov 20. J Med Chem. 2013. PMID: 24195762 Free PMC article.
Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis.
Zhang W, McIver AL, Stashko MA, DeRyckere D, Branchford BR, Hunter D, Kireev D, Miley MJ, Norris-Drouin J, Stewart WM, Lee M, Sather S, Zhou Y, Di Paola JA, Machius M, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X. Zhang W, et al. J Med Chem. 2013 Dec 12;56(23):9693-700. doi: 10.1021/jm4013888. Epub 2013 Nov 20. J Med Chem. 2013. PMID: 24219778 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: zhang d. 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.
Efficacy of a Mer and Flt3 tyrosine kinase small molecule inhibitor, UNC1666, in acute myeloid leukemia.
Lee-Sherick AB, Zhang W, Menachof KK, Hill AA, Rinella S, Kirkpatrick G, Page LS, Stashko MA, Jordan CT, Wei Q, Liu J, Zhang D, DeRyckere D, Wang X, Frye S, Earp HS, Graham DK. Lee-Sherick AB, et al. Among authors: zhang w, zhang d. Oncotarget. 2015 Mar 30;6(9):6722-36. doi: 10.18632/oncotarget.3156. Oncotarget. 2015. PMID: 25762638 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: zhang w. 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.
Discovery of Macrocyclic Pyrimidines as MerTK-Specific Inhibitors.
McIver AL, Zhang W, Liu Q, Jiang X, Stashko MA, Nichols J, Miley MJ, Norris-Drouin J, Machius M, DeRyckere D, Wood E, Graham DK, Earp HS, Kireev D, Frye SV, Wang X. McIver AL, et al. Among authors: zhang w. ChemMedChem. 2017 Feb 3;12(3):207-213. doi: 10.1002/cmdc.201600589. Epub 2017 Jan 9. ChemMedChem. 2017. PMID: 28032464 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: zhang w, zhang d, zhang y. 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
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