Elucidation of G-protein and β-arrestin functional selectivity at the dopamine D2 receptor.

ABSTRACT: The neuromodulator dopamine signals through the dopamine D2 receptor (D2R) to modulate central nervous system functions through diverse signal transduction pathways. D2R is a prominent target for drug treatments in disorders where dopamine function is aberrant, such as schizophrenia. D2R signals through distinct G-protein and β-arrestin pathways, and drugs that are functionally selective for these pathways could have improved therapeutic potential. How D2R signals through the two pathways is still not well defined, and efforts to elucidate these pathways have been hampered by the lack of adequate tools for assessing the contribution of each pathway independently. To address this, Evolutionary Trace was used to produce D2R mutants with strongly biased signal transduction for either the G-pr

SUBMITTER: Peterson SM 

PROVIDER: S-EPMC4460444 | biostudies-literature | 2015 Jun

REPOSITORIES: biostudies-literature