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Resumo

The human CDC42 binding protein kinase gamma (MRCKγ), a serine/threonine kinase remains unexplored. However their isoforms MRCKα and MRCKβ are involved in the regulation of actomyosin cytoskeleton, required for the process associated with invasion and metastasis. The high degree of homology among the MRCKs family and the lack of structural information become a challenge in the development of selective MRCKγ inhibitor that can modulate this kinase. Here we report the docking studies, synthesis and selectivity profile with score S(35) of 0.013 of pteridine scaffolds as a novel class of potent MRCKγ inhibitor.

Palavras-chave
kinase inhibitor
MRCK
pteridine
CDC42BP
molecular docking