A potentiator of orthosteric ligand activity at GLP-1R acts via covalent modification

NATURE CHEMICAL BIOLOGY(2014)

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摘要
BETP, a positive allosteric modulator of GLP-1R, a class B GPCR and an important therapeutic target for type II diabetes, covalently modifies two cysteine residues at the receptor's cytoplasmic face, where one of these enhances agonist-induced signaling. [In the version of the Table of Contents initially published, the labels for the BETP conditions were swapped in graphical abstract of the Nolte et al . article. The error has been corrected in the HTML and PDF versions of the Table of Contents.]
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nature chemical biology, science
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