This week in techniques



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Crystal structure of corticotropin-releasing factor receptor 1 (CRHR1; CRFR1) bound to a small molecule antagonist

A crystal structure of an antagonist-bound CRHR1 could help inform the development of compounds targeting class B
GPCRs. Researchers solved the structure of the transmembrane region of CRHR1 in an inactive conformation bound to a small molecule antagonist at 3.0 Å resolution. The structure showed that the antagonist binding site is in a deep hydrophobic pocket ~13-23 Å away from ligands that bind class A GPCRs. Next steps include combining these and other structural data to build a model of another GPCR, glucagon-like peptide-1 receptor (GLP-1R; GLP1R), to aid the development of therapeutics to treat diabetes (see Deep pockets, page 1).

SciBX 6(32); doi:10.1038/scibx.2013.875
Published online Aug. 22, 2013

Patented; unavailable for licensing

Hollenstein, K. et al. Nature; published online July 17, 2013;
Contact: Fiona H. Marshall, Heptares Therapeutics Ltd., Welwyn Garden City, U.K.