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Synthesis and Agonistic Activity at the GPR35 of 5,6-Dihydroxyindole-2-carboxylic Acid Analogues.


ABSTRACT: 5,6-Dihydroxyindole-2-carboxylic acid (DHICA), an intermediate of melanin synthesis and an eumelanin building block, was recently discovered to be a GPR35 agonist with moderate potency. Here, we report the synthesis and pharmacological characterization of a series of DHICA analogues against GPR35 using both label-free dynamic mass redistribution and Tango ?-arrestin translocation assays. This led to identification of novel GPR35 agonists with improved potency and/or having biased agonism.

SUBMITTER: Deng H 

PROVIDER: S-EPMC4030800 | BioStudies | 2012-01-01T00:00:00Z

REPOSITORIES: biostudies

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