[HTML][HTML] Internalization of the human nicotinic acid receptor GPR109A is regulated by Gi, GRK2, and arrestin3

G Li, Y Shi, H Huang, Y Zhang, K Wu, J Luo… - Journal of biological …, 2010 - ASBMB
Nicotinic acid (niacin) has been widely used as a favorable lipid-lowering drug for several
decades, and the orphan G protein-coupled receptor GPR109A has been identified to be a
receptor for niacin. Mechanistic investigations have shown that as a G i-coupled receptor,
GPR109A inhibits adenylate cyclase activity upon niacin activation, thereby inhibiting free
fatty acid liberation. However, the underlying molecular mechanisms that regulate signaling
and internalization of GPR109A remain largely unknown. To further characterize GPR109A …