Biology 3355A/B Lecture Notes - Lecture 18: Rgs4, Thapsigargin, Pentamer

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Normally g proteins are found in gdp-bound state which is inactivate. Gdp can dissociate; since there"s more gtp in the cell, it can bind to g protein and cause effector interaction. It is selective for gq and interacts poorly with gi. Rgs proteins bind to galpha and promote gtp hydrolysis (gap effect) and/or impede ga-effector coupling (effector antagonism: decrease gpcr agonist potency/efficacy. Rgs2 selectively inhibits gq and gs signaling. Rgs2 is not a gap for galphas, but it can bind to both galphas and adenylyl cyclase. Rgs2 is widely expressed and implicated in many physiological and pathophysiological processes: cv and cns func and dysfunc. Immune func: renal func, adipose func, circadian rhythm, cell differentiation, cell stress response. Dynamically expressed and upregulated by a # of things. Highest expression in lung, heart, and lymphocytes. Rgs2 is upregulated by gq and gs-mediated signals to attenuate gpcr signaling.

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