Structural dynamics bridge the gap between the genetic and functional levels of GPCRs

Publikation: Bidrag til tidsskriftReviewForskningfagfællebedømt

G protein–coupled receptors (GPCRs) are implicated in nearly all physiological processes in the human body and represent an important drug targeting class. The genes encoding the different GPCR (sub)types determine their specific functionality, which can be altered by natural genetic variants and isoforms. Deciphering the molecular link between sequence diversity and its functional consequences is a current challenge and critical for the comprehension of the physiological response of GPCRs. It requires a global understanding of how protein sequence translates into protein structure, how this impacts the structural motions of the protein, and, finally, how all these factors determine the receptor functionality. Here, we discuss available resources and state-of-the-art computational approaches to address this question.

OriginalsprogEngelsk
TidsskriftCurrent Opinion in Structural Biology
Vol/bind69
Sider (fra-til)150-159
Antal sider10
ISSN0959-440X
DOI
StatusUdgivet - 2021

Bibliografisk note

Funding Information:
M.T-F. acknowledges financial support from the Spanish Ministry of Science, Innovation and Universities ( FPU16/01209 ). T.M.S. would like to acknowledge support from the National Center of Science , Poland (grant number 2017/27/N/NZ2/02571 ). D.E.G. acknowledges financial support from the Lundbeck foundation ( R163-2013-16327 ) and Novo Nordisk Foundation ( NNF18OC0031226 ). J.S. acknowledges financial support from the Instituto de Salud Carlos III FEDER ( PI15/00460 and PI18/00094 ) and the ERA-NET NEURON & Ministry of Economy, Industry and Competitiveness ( AC18/00030 ).

Funding Information:
M.T-F. acknowledges financial support from the Spanish Ministry of Science, Innovation and Universities (FPU16/01209). T.M.S. would like to acknowledge support from the National Center of Science, Poland (grant number 2017/27/N/NZ2/02571). D.E.G. acknowledges financial support from the Lundbeck foundation (R163-2013-16327) and Novo Nordisk Foundation (NNF18OC0031226). J.S. acknowledges financial support from the Instituto de Salud Carlos III FEDER (PI15/00460 and PI18/00094) and the ERA-NET NEURON & Ministry of Economy, Industry and Competitiveness (AC18/00030).

Publisher Copyright:
© 2021 Elsevier Ltd

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