The Gq and G12 families of heterotrimeric G proteins report functional selectivity.

ABSTRACT: Receptors coupled to the G(q) and G(12) families of heterotrimeric G proteins have surfaced rarely in the context of functional selectivity and always indirectly. We explore here the differential engagement of G(q) and G(13) (of the G(12) family) by the thromboxane A(2) receptor alpha (TPalpha), via agonist-effected [(35)S]-guanosine 5'-O-(3-thio)triphosphate binding when the G proteins themselves are used as reporters. We find for TPalpha introduced into human embryonic kidney 293 cells and for the receptor expressed normally in human platelets an agonist-selective engagement of G(q) versus G(13). Pinane thromboxane A(2) (PTA(2)) activates G(q) in preference to G(13), whereas 8-iso-prostaglandin F(2alpha) activates G(13) in preference to G(q). 9,11-Dideoxy-9alpha,11alpha-methanoepoxy-pros

SUBMITTER: Zhang L 

PROVIDER: S-EPMC2685064 | biostudies-literature | 2009 Jan

REPOSITORIES: biostudies-literature