Design of bivalent ligands targeting putative GPCR dimers
| Autor: | Boshi Huang, Yan Zhang, Celsey M. St. Onge, Hongguang Ma |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
0301 basic medicine
Pharmacology Chemistry Drug discovery Computational biology Ligands Bivalent (genetics) Article Receptors G-Protein-Coupled 03 medical and health sciences 030104 developmental biology 0302 clinical medicine 030220 oncology & carcinogenesis Drug Design Drug Discovery Humans Technology Pharmaceutical Pharmacophore Protein Multimerization Disease treatment G protein-coupled receptor |
| Zdroj: | Drug Discov Today |
| ISSN: | 1878-5832 |
| Popis: | G protein-coupled receptors (GPCRs) have been exploited as primary targets for drug discovery, and GPCR dimerization offers opportunities for drug design and disease treatment. An important strategy for targeting putative GPCR dimers is the use of bivalent ligands, which are single molecules that contain two pharmacophores connected through a spacer. Here, we discuss the selection of pharmacophores, the optimal length and chemical composition of the spacer, and the choice of spacer attachment points to the pharmacophores. Furthermore, we review the most recent advances (from 2018 to the present) in the design, discovery and development of bivalent ligands. We aim to reveal the state-of-the-art design strategy for bivalent ligands and provide insights into future opportunities in this promising field of drug discovery. |
| Databáze: | OpenAIRE |
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