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Updated: Jan 25, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Recent progress on the discovery of P2Y14 receptor antagonists
Ran Lu1, Zhenguo Zhang1, Cheng Jiang1
1Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China.
Abstract:
The P2Y14 receptor (P2Y14R), a G protein-coupled receptor (GPCR), is activated by extracellular nucleotides. P2Y14R is involved in inflammatory, diabetes, immune processes and other related complications, and is therefore an attractive therapeutic target. As the three-dimensional structure of the P2Y14R has not yet been elucidated, homology modeling based on the crystallography of the closely related P2Y12R have been used in the structure-based design of P2Y14R ligands. Several P2Y14R antagonists with excellent potency and high subtype-selectivity have been discovered in recent years. In this review, development of novel small molecules as antagonists of P2Y14R was described.
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