Molecular Mechanism of Action of Phorbol Ester

$610,815ZIAFY2018CANIH

Division Of Basic Sciences - Nci

Investigators

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Abstract

Due to Dr. Blumberg's retirement, this project was completed in January 2018. The lab described the critical role of Trp-588 of presynaptic Munc13-1 played for ligand binding and membrane translocation. In addition, they found that the deletion of the C26 methyl substituent from the bryostatin analogue Merle 23 has negligible impact on its biological profile and potency. The team described the potential for the design of custom C1 domain targeted molecules selective for the atypical C1 domains of Vav family proteins. Finally, they showed the importance of the REM (Ras exchange) domain for membrane interactions by RasGRP3.

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