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Cancer; thrombosis

c-Mer proto-oncogene tyrosine kinase (MERTK)

In vitro studies suggest a new class of MERTK inhibitors could help treat cancer or thrombosis. Chemical synthesis, SAR and in vitro testing of pyridinepyrimidine analogs identified several compounds as selective, low nanomolar inhibitors of MERTK. In different blood and solid cancer cell lines, one lead compound inhibited MERTK phosphorylation and cellular proliferation at low nanomolar IC50 values. In ex vivo, platelet-rich human plasma, another lead compound decreased platelet aggregation compared with vehicle. Ongoing work includes optimizing the compounds and testing them in animal models of cancer and thrombosis.

SciBX 6(48); doi:10.1038/scibx.2013.1400
Published online Dec. 19, 2013

Patented by The University of North Carolina; licensed to Meryx Inc.

Zhang, W. et al. J. Med. Chem.;
published online Nov. 6, 2013;
Zhang, W. et al. J. Med. Chem.;
published online Nov. 12, 2013;
Contact: Xiaodong Wang, The University of North Carolina at Chapel Hill, Chapel Hill, N.C.