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Structure of Class B GPCRs: new horizons for drug discovery.


ABSTRACT: Class B GPCRs of the secretin family are important drug targets in many human diseases including diabetes, neurodegeneration, cardiovascular disease and psychiatric disorders. X-ray crystal structures for the glucagon receptor and corticotropin-releasing factor receptor 1 have now been published. In this review, we analyse the new structures and how they compare with each other and with Class A and F receptors. We also consider the differences in druggability and possible similarity in the activation mechanisms. Finally, we discuss the potential for the design of small-molecule modulators for these important targets in drug discovery. This new structural insight allows, for the first time, structure-based drug design methods to be applied to Class B GPCRs.

SUBMITTER: Bortolato A 

PROVIDER: S-EPMC4080969 | biostudies-literature | 2014 Jul

REPOSITORIES: biostudies-literature

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Structure of Class B GPCRs: new horizons for drug discovery.

Bortolato Andrea A   Doré Andrew S AS   Hollenstein Kaspar K   Tehan Benjamin G BG   Mason Jonathan S JS   Marshall Fiona H FH  

British journal of pharmacology 20140701 13


Class B GPCRs of the secretin family are important drug targets in many human diseases including diabetes, neurodegeneration, cardiovascular disease and psychiatric disorders. X-ray crystal structures for the glucagon receptor and corticotropin-releasing factor receptor 1 have now been published. In this review, we analyse the new structures and how they compare with each other and with Class A and F receptors. We also consider the differences in druggability and possible similarity in the activ  ...[more]

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