Trends in GPCR drug discovery: new agents, targets and indications

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Trends in GPCR drug discovery : new agents, targets and indications

G protein-coupled receptors (GPCRs) are the most intensively studied drug targets, mostly due to their substantial involvement in human pathophysiology and their pharmacological tractability. Here, we report an up-to-date analysis of all GPCR drugs and agents in clinical trials, which reveals current trends across molecule types, drug targets and therapeutic indications, including showing that 475 drugs (~34% of all drugs approved by the US Food and Drug Administration (FDA)) act at 108 unique GPCRs. Approximately 321 agents are currently in clinical trials, of which ~20% target 66 potentially novel GPCR targets without an approved drug, and the number of biological drugs, allosteric modulators and biased agonists has increased. The major disease indications for GPCR modulators show a shift towards diabetes, obesity and Alzheimer disease, although several central nervous system disorders are also highly represented. The 224 (56%) non-olfactory GPCRs that have not yet been explored in clinical trials have broad untapped therapeutic potential, particularly in genetic and immune system disorders. Finally, we provide an interactive online resource to analyse and infer trends in GPCR drug discovery.

Attwood, Misty M.Uppsala universitet,Funktionell farmakologi(Swepub:uu)misat949 (författare)
Rask-Andersen, Mathias,1979-Uppsala universitet,Science for Life Laboratory, SciLifeLab,Medicinsk genetik och genomik(Swepub:uu)matra895 (författare)
Schiöth, Helgi B.Uppsala universitet,Funktionell farmakologi(Swepub:uu)helgschi (författare)
Gloriam, David E (författare)
Uppsala universitetFunktionell farmakologi (creator_code:org_t)

Ingår i:Nature reviews. Drug discovery: Springer Science and Business Media LLC16:12, s. 829-8421474-17761474-1784

Av författaren/redakt...: Hauser, Alexande ...; Attwood, Misty M ...; Rask-Andersen, M ...; Schiöth, Helgi B ...; Gloriam, David E

Om ämnet

MEDICIN OCH HÄLSOVETENSKAP: MEDICIN OCH HÄLS ...; och Medicinska och f ...; och Farmakologi och ...

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