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Only FREE hormones in blood can cause action – most bound to plasma proteins (↑↑ T½ , ↓↓ metabolic clearance)
Receptor Mechanism
G-Protein Coupled Hormone binds; α, β, γ complexes assoc. w/ recepter, activated via GDP→GTP; α subunit
dissociates and binds with membrane-bound target to initiate intra-cellular signal
Enzyme-Linked Homodimer; leptin binds to extracellular part; phosphorylation and activation of JAK2; causes Leptin receptor
phosphorylation of STAT; activates tx of gene, synthesis of protein; JAK2 activates other ez
systems mediating rapid effects
G-Protein Coupled generation of G-Protein coupled mechanism activates ATP→cAMP; activated cAMP dependent protein kinase; Peptide hormone
cAMP Second Messenger phosphorylates protein; get cell response
G-Protein Coupled IP3 and DAG G-Protein coupled mechanism activates PIP2→ IP3+DAG; activates protein kinase C; Mech of angiotensin II
Second Messenger phosphrylates protein; cell response vasoconstriction
Intracellular Diffuse into cell; bind cytoplasmic or nuclear receptor; hormone-receptor complex binds hormone Steroid, T3, lipophilic hormones
response element on DNA; activates or inhibits tx, mRNA synth, protein synth