Discovery of nitrophenols as GPR35 agonists

H Deng, Y Fang - MedChemComm, 2012 - pubs.rsc.org
GPR35 is a family A orphan G protein-coupled receptor whose biological functions are
largely unknown. Identification of novel GPR35 ligands is essential to elucidate the biology …

High-throughput identification and characterization of novel, species-selective GPR35 agonists

Z Neetoo-Isseljee, AE MacKenzie, C Southern… - … of Pharmacology and …, 2013 - ASPET
Drugs targeting the orphan receptor GPR35 have potential therapeutic application in a
number of disease areas, including inflammation, metabolic disorders, nociception, and …

5-Nitro-2-(3-phenylpropylamino) benzoic acid is a GPR35 agonist

Y Taniguchi, H Tonai-Kachi, K Shinjo - Pharmacology, 2008 - karger.com
GPR35 is a Gi/o-and G16-coupled receptor abundantly expressed in gastrointestinal tissues
and immune cells. Kynurenic acid (a tryptophan metabolite and ionotropic glutamate …

Design and synthesis of 2-alkylpyrimidine-4, 6-diol and 6-alkylpyridine-2, 4-diol as potent GPR84 agonists

Y Liu, Q Zhang, LH Chen, H Yang, W Lu… - ACS Medicinal …, 2016 - ACS Publications
A series of alkylpyrimidine-4, 6-diol derivatives were designed and synthesized as novel
GRP84 agonists based on a high-throughput screening (HTS) hit 1. 6-Nonylpyridine-2, 4 …

[HTML][HTML] Tyrphostin analogs are GPR35 agonists

H Deng, H Hu, Y Fang - FEBS letters, 2011 - Elsevier
GPR35 is an orphan G protein-coupled receptor that is not well-characterized. Here we
employ dynamic mass redistribution (DMR) assays to discover new GPR35 agonists. DMR …

Discovery of 2-(4-Methylfuran-2(5H)-ylidene)malononitrile and Thieno[3,2-b]thiophene-2-carboxylic Acid Derivatives as G Protein-Coupled Receptor 35 (GPR35) …

H Deng, H Hu, M He, J Hu, W Niu… - Journal of medicinal …, 2011 - ACS Publications
Screening with dynamic mass redistribution (DMR) assays in a native cell line HT-29 led to
identification of two novel series of chemical compounds, 2-(4-methylfuran-2 (5 H)-ylidene) …

Therapeutic opportunities and challenges in targeting the orphan G protein-coupled receptor GPR35

T Quon, LC Lin, A Ganguly, AB Tobin… - ACS pharmacology & …, 2020 - ACS Publications
GPR35 is a class A, rhodopsin-like G protein-coupled receptor (GPCR) first identified more
than 20 years ago. In the intervening period, identification of strong expression in the lower …

[HTML][HTML] Identification of a novel scaffold for a small molecule GPR139 receptor agonist

AC Nøhr, MA Shehata, D Palmer, R Pokhrel… - Scientific Reports, 2019 - nature.com
GPR139 is an orphan G protein-coupled receptor (GPCR) that is primarily expressed in the
brain in regions known to regulate motor control and metabolism. Here, we screened a …

Structure-activity relationships of agonists for the orphan G protein-coupled receptor GPR27

T Pillaiyar, F Rosato, M Wozniak, J Blavier… - European Journal of …, 2021 - Elsevier
GPR27 belongs, with GPR85 and GPR173, to a small subfamily of three receptors called
“Super-Conserved Receptors Expressed in the Brain”(SREB). It has been postulated to …

[HTML][HTML] Crucial positively charged residues for ligand activation of the GPR35 receptor

P Zhao, TR Lane, HGL Gao, DP Hurst… - Journal of Biological …, 2014 - ASBMB
GPR35 is a G protein-coupled receptor expressed in the immune, gastrointestinal, and
nervous systems in gastric carcinomas and is implicated in heart failure and pain perception …