Project Details
Projekt
Development and characterization of heterocyclized dipeptide derivatives as inhibitors for heterotrimeric G proteins
Applicant
Professor Dr. Michael Gütschow
Subject Area
Pharmacy
Term
from 2016 to 2020
Project identifier
Deutsche Forschungsgemeinschaft (DFG) - Project number 273251628
Heterotrimeric G proteins act as molecular switches and transduce extracellular signals via G protein-coupled receptors into intracellular signal cascades. This part of the project is aimed at developing focused libraries of 5,6,7,8-tetrahydroimidazo[1,2-a]pyrazines as Ga protein subfamily selective probes. Such probes would be highly desired to understand the detailed contribution of G protein signaling under physiological and pathophysiological conditions. The design of the tool compounds is based on the structures of two low-molecular weight, cell-permeable BIM molecules. These are considered as heterocyclized dipeptide derivatives, accessible for manifold structural modifications via combinatorial chemistry. It should be investigated to what extent the selectivity and suitability of the compounds can be improved in the course of a stepwise optimization. The new compounds will be provided to the collaborators of the consortium for biochemical and pharmacological evaluation and utilization.
DFG Programme
Research Units
