PMID- 24900508
OWN - NLM
STAT- PubMed-not-MEDLINE
DCOM- 20140605
LR  - 20211021
IS  - 1948-5875 (Print)
IS  - 1948-5875 (Electronic)
IS  - 1948-5875 (Linking)
VI  - 3
IP  - 7
DP  - 2012 Jul 12
TI  - Synthesis and Agonistic Activity at the GPR35 of 5,6-Dihydroxyindole-2-carboxylic 
      Acid Analogues.
PG  - 550-4
LID - 10.1021/ml300076u [doi]
AB  - 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 beta-arrestin translocation assays. 
      This led to identification of novel GPR35 agonists with improved potency and/or 
      having biased agonism.
FAU - Deng, Huayun
AU  - Deng H
AD  - Biochemical Technologies, Science and Technology Division, Corning Inc. , 
      Corning, New York 14831, United States.
FAU - Fang, Ye
AU  - Fang Y
AD  - Biochemical Technologies, Science and Technology Division, Corning Inc. , 
      Corning, New York 14831, United States.
LA  - eng
PT  - Journal Article
DEP - 20120606
PL  - United States
TA  - ACS Med Chem Lett
JT  - ACS medicinal chemistry letters
JID - 101521073
PMC - PMC4030800
OTO - NOTNLM
OT  - 5,6-dihydroxyindole-2-carboxylic acid
OT  - GPR35
OT  - biased agonism
OT  - melanin synthesis
EDAT- 2012/07/12 00:00
MHDA- 2012/07/12 00:01
PMCR- 2013/07/12
CRDT- 2014/06/06 06:00
PHST- 2012/04/01 00:00 [received]
PHST- 2012/06/06 00:00 [accepted]
PHST- 2014/06/06 06:00 [entrez]
PHST- 2012/07/12 00:00 [pubmed]
PHST- 2012/07/12 00:01 [medline]
PHST- 2013/07/12 00:00 [pmc-release]
AID - 10.1021/ml300076u [doi]
PST - epublish
SO  - ACS Med Chem Lett. 2012 Jun 6;3(7):550-4. doi: 10.1021/ml300076u. eCollection 
      2012 Jul 12.