GPR109a agonists. Part 2: Pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a

被引：10

作者：

Imbriglio, Jason E. ^{[1
]}

Chang, Sookhee ^{[1
]}

Liang, Rui ^{[1
]}

Raghavan, Subharekha ^{[1
]}

Schmidt, Darby ^{[1
]}

Smenton, Abby ^{[1
]}

Tria, Scott ^{[1
]}

Schrader, Thomas O. ^{[4
]}

Jung, Jae-Kyu ^{[4
]}

Esser, Craig ^{[1
]}

Holt, Tom G. ^{[2
]}

Wolff, Michael S. ^{[2
]}

Taggart, Andrew K. P. ^{[3
]}

Cheng, Kang ^{[3
]}

Carballo-Jane, Ester ^{[3
]}

Waters, M. Gerard ^{[3
]}

Tata, James R. ^{[1
]}

Colletti, Steven L. ^{[1
]}

机构：

[1] Merck & Co Inc, Dept Med Chem, Merck Res Labs, Rahway, NJ 07065 USA

[2] Merck & Co Inc, Dept Drug Metab, Merck Res Labs, Rahway, NJ 07065 USA

[3] Merck & Co Inc, Dept Cardiovasc Dis, Merck Res Labs, Rahway, NJ 07065 USA

[4] Arena Pharmaceut, Dept Med Chem, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 15期

关键词：

Niacin; GPR109a; Agonists; NICOTINIC-ACID; MOLECULAR-IDENTIFICATION;

D O I：

10.1016/j.bmcl.2010.06.041

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5-Alkyl and aryl-pyrazole-acids have been identified as a new class of selective, small-molecule, agonists of the human orphan G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：4472 / 4474

页数：3

共 34 条

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Wu, Kuangpei
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[22] Expression and localization of GPR109A (PUMA-G/HM74A) mRNA and protein in mammalian retinal pigment epithelium
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[23] Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A)
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[24] Niacin receptor GPR109A inhibits insulin secretion and is down-regulated in type 2 diabetic islet beta-cells
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[25] Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control
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[26] Discovery of Novel and Selective G-Protein Coupled Receptor 120 (GPR120) Agonists for the Treatment of Type 2 Diabetes Mellitus
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[27] Aromatic D-amino acids act as chemoattractant factors for human leukocytes through a G protein-coupled receptor, GPR109B
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[28] 4-Hydroxynonenal-induced GPR109A (HCA2 receptor) activation elicits bipolar responses, Gαi-mediated anti-inflammatory effects and Gβγ-mediated cell death
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[29] Distinct Kinetic and Spatial Patterns of Protein Kinase C (PKC)- and Epidermal Growth Factor Receptor (EGFR)-dependent Activation of Extracellular Signal-regulated Kinases 1 and 2 by Human Nicotinic Acid Receptor GPR109A
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[30] The Specificity and Broad Multitarget Properties of Ligands for the Free Fatty Acid Receptors FFA3/GPR41 and FFA2/GPR43 and the Related Hydroxycarboxylic Acid Receptor HCA2/GPR109A
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