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Structure determination of GPCRs: cryo-EM compared with X-ray crystallography.


ABSTRACT: G protein-coupled receptors (GPCRs) are the largest single family of cell surface receptors encoded by the human genome and they play pivotal roles in co-ordinating cellular systems throughout the human body, making them ideal drug targets. Structural biology has played a key role in defining how receptors are activated and signal through G proteins and β-arrestins. The application of structure-based drug design (SBDD) is now yielding novel compounds targeting GPCRs. There is thus significant interest from both academia and the pharmaceutical industry in the structural biology of GPCRs as currently only about one quarter of human non-odorant receptors have had their structure determined. Initially, all the structures were determined by X-ray crystallography, but recent advances in electron

SUBMITTER: Garcia-Nafria J 

PROVIDER: S-EPMC8589417 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature