Article
A small molecule ligand of the glucagon-like peptide 1 receptor targets its amino-terminal hormone binding domain.
The Journal of biological chemistry - 12 Oct 2001
Tibaduiza E C, Chen C, Beinborn M
Abstract excerpt
The glucagon-like peptide 1 receptor (GLP-1R) belongs to a distinct subgroup of G protein-coupled peptide hormone receptors (class B) that has been difficult to target by small molecule drugs. Here, we report that a non-peptide compound, T-0632, binds with micromolar affinity to the human GLP-1R and blocks GLP-1-induced cAMP production. Furthermore, the observation that T-0632 has almost 100-fold selectivity for...
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