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10.1111/bph.12689

http://scihub22266oqcxt.onion/10.1111/bph.12689
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C4080969!4080969!24628305
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suck abstract from ncbi


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pmid24628305      Br+J+Pharmacol 2014 ; 171 (13): 3132-45
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  • Structure of Class B GPCRs: new horizons for drug discovery #MMPMID24628305
  • Bortolato A; Doré AS; Hollenstein K; Tehan BG; Mason JS; Marshall FH
  • Br J Pharmacol 2014[Jul]; 171 (13): 3132-45 PMID24628305show ga
  • 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.
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