Inhibitors of g-protein-beta/gamma subunit function

摘要

G-protein beta gamma -subunits (G beta gamma ) act as active transmembrane signaling components. It is shown here that the high affinity and inhibitory action of phosducin for G beta gamma is largely due to a small region (amino acids 217-231) in its C-terminus. Corresponding peptides including this region disrupt G beta gamma -G alpha -interactions, but also other G beta gamma -mediated functions. This region represents a model switch that can turn off G beta gamma . The knowledge of the region in phosducin and the part of G beta gamma interacting with this region of phosducin enables the design of small compounds which act as G beta gamma antagonists.