(1 Signal transduction pathway introduced by GP receptor GP DG-PKC PLCB AC IP3、Ca2-CaK
(1) Signal transduction pathway introduced by GP receptor GP IP3、Ca2 + -CaK DG-PKC AC PLC β
阝R W2-R, M-R Cori. 1947 Gsa Gilman 1994 AC 、cAMP CGMP? Sutherland PKA 1998 ro Krebs Edmond H glycogenolysis 1992 Fischer GPCR signal pathway
β-R α2-R，M-R α1-R，ET-R Gsα Gi Gqα AC PLCβ cAMP PIP2 IP3 PKA DAG(DG) gene PKC - + Pro* Sutherland 1971 Krebs 1992 Gilman 1994 Murad 1998 cGMP? ? Cori, 1947 GPCR signal pathway Edmond H. glycogenolysis Fischer
Mechanism of gp GP(Ga)=GTPase GTP GDP on off GEF+ Small GP(Ga) GAP guanine-nucleotide exchange factor GTPase activating protein
GDP GP(G) = GTPase GEF GAP Small GP (G) + - Mechanism of GP GTPase activating protein guanine-nucleotide exchange factor GTP on off
GTP-BINDING PROTEIN SUPERFAMILY HETEROTRIMERIC(afy) SMALL GTP-BINDING PROTEINS Gs Gi Gq G12 RAS RHO RAB RAN ARF Gas Ga1 Gaq Ga12 H-Ras RhoA Rab1A TC4 ARF1 Gaolf Go2 Gal1 Ga13 K-Ras RhoB Rab1B Rab2 R an ARF2 Gai3 Ga14 N-Ras Rhoc Rab3A ARF3 R-Ras Gao Ga15 RhoG Rab3B ARF4 RaplA Rabic Got Ga16 Rap1B Rac1 Rab4 ARF5 Go Rac2 Baba ARF6 Rap2B CDC42Rabe ARLS Ral A TC10 Rab7 Rab8 RalB Rabg TC21 Rab10 Rab11 Rem
signal transduction pathway introduced by GP-R R a2-R, M-R a1-R, ET-R Gsa L AC βy CAMP PIP2 IP3 PKA DAGODG) Target Pro Ca2+ released phospho Targetgene transcription PKC Target pro phospho
signal transduction pathway introduced by GP -R - + + + β-R α2-R，M-R α1-R，ET-R Gqα Gsα Gi AC cAMP PKA PLCβ PKC PIP2 IP3 Ca2+ released DAG(DG) Target Pro phospho Targetgene transcription Target Pro phospho