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the role of adrenergic beta receptors for skin pigmentation

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Screening <strong>of</strong> Adrenergic Receptor Beta Antagonist<br />

Using a Recombinant GPCR Cell Line<br />

• Beta-arrestin plat<strong>for</strong>m utilizing a recombinant GPCR cell line (CHO cells)<br />

• Takes advantage <strong>of</strong> <strong>the</strong> property that activated GPCRs recruit <strong>beta</strong>-arrestin a<br />

shutdown mechanism. The GPCR is expressed as a fusion protein with a small<br />

piece <strong>of</strong> <strong>beta</strong>-galactosidase on <strong>the</strong> cytoplasmic side.<br />

• Beta-arrestin is also expressed as a fusion protein with <strong>the</strong> remainder <strong>of</strong> <strong>the</strong> <strong>beta</strong><br />

galactosidase enzyme. Upon recruitment <strong>of</strong> <strong>beta</strong>-arrestin, <strong>the</strong> <strong>beta</strong>-galactosidase<br />

pieces are united to <strong>for</strong>m an active enzyme, which is detectable with a substrate<br />

mixture that produces a luminescent signal with <strong>beta</strong>-galactosidase action.

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