TY - JOUR
T1 - Antithrombotic P2Y 12 receptor antagonists
T2 - recent developments in drug discovery
AU - Baqi, Younis
AU - Müller, Christa E.
N1 - Publisher Copyright:
© 2018 Elsevier Ltd
PY - 2019
Y1 - 2019
N2 - The P2Y 12 receptor is one of eight known P2Y receptor subtypes, and belongs to the G-protein-coupled receptor (GPCR) family. The P2Y 12 receptor is highly expressed on blood platelets and in the brain. Potent, selective, peripherally acting antagonists for the P2Y 12 receptor are used clinically as antithrombotic drugs. Several different scaffolds have been identified as P2Y 12 receptor antagonists, including irreversibly acting thienotetrahydropyridines (prodrugs), and reversible competitive antagonists, including adenine nucleotide analogs, piperazinyl-glutamate-quinolines, -pyridines, and -pyrimidines, and anthraquinone derivatives. Here, we provide an overview of the different scaffolds that have been developed as P2Y 12 receptor antagonists, some of which have become important therapeutics.
AB - The P2Y 12 receptor is one of eight known P2Y receptor subtypes, and belongs to the G-protein-coupled receptor (GPCR) family. The P2Y 12 receptor is highly expressed on blood platelets and in the brain. Potent, selective, peripherally acting antagonists for the P2Y 12 receptor are used clinically as antithrombotic drugs. Several different scaffolds have been identified as P2Y 12 receptor antagonists, including irreversibly acting thienotetrahydropyridines (prodrugs), and reversible competitive antagonists, including adenine nucleotide analogs, piperazinyl-glutamate-quinolines, -pyridines, and -pyrimidines, and anthraquinone derivatives. Here, we provide an overview of the different scaffolds that have been developed as P2Y 12 receptor antagonists, some of which have become important therapeutics.
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U2 - 10.1016/j.drudis.2018.09.021
DO - 10.1016/j.drudis.2018.09.021
M3 - Review article
C2 - 30291899
AN - SCOPUS:85054683455
SN - 1359-6446
VL - 24
SP - 325
EP - 333
JO - Drug Discovery Today
JF - Drug Discovery Today
IS - 1
ER -