title: 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 β-arrestin translocation assays. This led to identification of novel GPR35 agonists with improved potency and/or having biased agonism.
authors.affiliation: Biochemical Technologies, Science and Technology Division, Corning Inc. , Corning, New York 14831, United States.
authors.forename: Huayun
authors.initials: H
authors.lastname: Deng
authors.affiliation: Biochemical Technologies, Science and Technology Division, Corning Inc. , Corning, New York 14831, United States.
authors.forename: Ye
authors.initials: Y
authors.lastname: Fang
keywords: 5,6-dihydroxyindole-2-carboxylic acid; GPR35; biased agonism; melanin synthesis