期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 62, 期 1, 页码 88-127出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.8b00875
关键词
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资金
- National Institutes of Health [R21 MH093844, R01 DA038446, K05 DA020087, P30 DA28821, T32 DA07287, F31 DA045511]
- R. A. Welch Foundation Chemistry and Biology Collaborative Grant from the Gulf Coast Consortia (GCC)
- Center for Addiction Research (CAR) at UTMB
- John Sealy Memorial Endowment Fund
G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR superfamily is highly represented, and continued drug discovery for this family of receptors may provide novel therapeutics for a vast range of diseases. GPCR allosteric modulation is an innovative targeting approach that broadens the available small molecule toolbox and is proving to be a viable drug discovery strategy, as evidenced by recent FDA approvals and clinical trials. Numerous class A GPCR allosteric modulators have been discovered recently, and emerging trends such as the availability of GPCR crystal structures, diverse functional assays, and structure-based computational approaches are improving optimization and development. This Perspective provides an update on allosterically targeted class A GPCRs and their disease indications and the medicinal chemistry approaches toward novel allosteric modulators and highlights emerging trends and opportunities in the field.
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