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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: wang x. 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: wang x. 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.
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: wang x. 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: wang x. 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. Among authors: wang x. 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.
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: wang x. 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.
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: wang x. 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.
Development of [18F]MIPS15692, a radiotracer with in vitro proof-of-concept for the imaging of MER tyrosine kinase (MERTK) in neuroinflammatory disease.
Wong SW, Vivash L, Mudududdla R, Nguyen N, Hermans SJ, Shackleford DM, Field J, Xue L, Aprico A, Hancock NC, Haskali M, Stashko MA, Frye SV, Wang X, Binder MD, Ackermann U, Parker MW, Kilpatrick TJ, Baell JB. Wong SW, et al. Among authors: wang x. Eur J Med Chem. 2021 Dec 15;226:113822. doi: 10.1016/j.ejmech.2021.113822. Epub 2021 Sep 4. Eur J Med Chem. 2021. PMID: 34563964
Use of AD Informer Set compounds to explore validity of novel targets in Alzheimer's disease pathology.
Potjewyd FM, Annor-Gyamfi JK, Aubé J, Chu S, Conlon IL, Frankowski KJ, Guduru SKR, Hardy BP, Hopkins MD, Kinoshita C, Kireev DB, Mason ER, Moerk CT, Nwogbo F, Pearce KH Jr, Richardson TI, Rogers DA, Soni DM, Stashko M, Wang X, Wells C, Willson TM, Frye SV, Young JE, Axtman AD. Potjewyd FM, et al. Among authors: wang x. Alzheimers Dement (N Y). 2022 Apr 12;8(1):e12253. doi: 10.1002/trc2.12253. eCollection 2022. Alzheimers Dement (N Y). 2022. PMID: 35434254 Free PMC article.
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