Agonist Activation of GPCR - answer-Ligand binds
Promotes conformational changes
Increase in R
Inverse Agonist Inhibition of GPCR - answer-Ligand binds
Stabilizes inactive receptor conformations
Antagonist Inhibition of GPCR - answer-Do not effect basal constitutive signaling
Do not affec...
Receptor tyrosine kinases - answer-Receptor tyrosine kinases (RTKs) consist
of an extracellular ligand
binding and dimerization domain, a single hydrophobic
transmembrane a-helix and a cytosolic domain with intrinsic
tyrosine kinase activity
Two types of RTKs - answer-Single transmembrane spanning proteins that
dimerize when ligand binds (EGF receptor, PGDF receptor)
Covalently linked dimers (insulin receptor, IGF-1 receptor)
PKB/Akt - answer-phosphorylate multiple proteins which regulate a wide
variety of intracellular events
Steroid class receptors - answer-GR, MR, PR, AR, ER
RXR partnered receptors - answer-TR, RAR, VDR, PPAR, a, b, y
Orphan receptors - answer-COUP-TF, HNF-4
Steroid receptor ligands - answer-Steroids
RXR partnered ligands - answer-9-Cis RA + X
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