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Cryo-EM of GLP-1 receptor bound to GLP-1 and Gs protein

ABSTRACT:

SUBMITTER: Radostin Danev

PROVIDER: EMPIAR-10673 | biostudies-other |

REPOSITORIES: biostudies-other

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Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists.

Zhang Xin X Belousoff Matthew J MJ Zhao Peishen P Kooistra Albert J AJ Truong Tin T TT Ang Sheng Yu SY Underwood Christina Rye CR Egebjerg Thomas T Šenel Petr P Stewart Gregory D GD Liang Yi-Lynn YL Glukhova Alisa A Venugopal Hari H Christopoulos Arthur A Furness Sebastian G B SGB Miller Laurence J LJ Reedtz-Runge Steffen S Langmead Christopher J CJ Gloriam David E DE Danev Radostin R Sexton Patrick M PM Wootten Denise D

Molecular cell 20201006 3

Peptide drugs targeting class B1 G-protein-coupled receptors (GPCRs) can treat multiple diseases; however, there remains substantial interest in the development of orally delivered non-peptide drugs. Here, we reveal unexpected overlap between signaling and regulation of the glucagon-like peptide-1 (GLP-1) receptor by the non-peptide agonist PF 06882961 and GLP-1 that was not observed for another compound, CHU-128. Compounds from these patent series, including PF 06882961, are currently in clinic ...[more]

PMID: 33027691

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