Article
Palonosetron-5-HT3 Receptor Interactions As Shown by a Binding Protein Cocrystal Structure.
ACS chemical neuroscience - 21 Dec 2016
Price Kerry L, Lillestol Reidun K, Ulens Chris, Lummis Sarah C R
Abstract excerpt
Palonosetron is a potent 5-HT3 receptor antagonist and an effective therapeutic agent against emesis. Here we identify the molecular determinants of compound recognition in the receptor binding site by obtaining a high resolution structure of palonosetron bound to an engineered acetylcholine binding protein that mimics the 5-HT3 receptor binding site, termed 5-HTBP, and by examining the potency of palonosetron in...
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