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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: deryckere d. 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.
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: deryckere d. 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: deryckere 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.
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
Liu J, Yang C, Simpson C, Deryckere D, Van Deusen A, Miley MJ, Kireev D, Norris-Drouin J, Sather S, Hunter D, Korboukh VK, Patel HS, Janzen WP, Machius M, Johnson GL, Earp HS, Graham DK, Frye SV, Wang X. Liu J, et al. Among authors: deryckere d. ACS Med Chem Lett. 2012 Feb 9;3(2):129-134. doi: 10.1021/ml200239k. ACS Med Chem Lett. 2012. PMID: 22662287 Free PMC article.
Design and Synthesis of Novel Macrocyclic Mer Tyrosine Kinase Inhibitors.
Wang X, Liu J, Zhang W, Stashko MA, Nichols J, Miley MJ, Norris-Drouin J, Chen Z, Machius M, DeRyckere D, Wood E, Graham DK, Earp HS, Kireev D, Frye SV. Wang X, et al. Among authors: deryckere d. ACS Med Chem Lett. 2016 Sep 13;7(12):1044-1049. doi: 10.1021/acsmedchemlett.6b00221. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994735 Free PMC article.
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: deryckere d. 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.
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: deryckere d. 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: deryckere d. 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
72 results