About: The binding of palonosetron and other antiemetic drugs to the serotonin 5-HT3 receptor

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About: The binding of palonosetron and other antiemetic drugs to the serotonin 5-HT3 receptor Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

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type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
title	The binding of palonosetron and other antiemetic drugs to the serotonin 5-HT3 receptor
Creator	Cai, Wensheng Zhang, Hong Schoehn, Guy Effantin, Gregory Chipot, Christophe »more»
source	BioRxiv
abstract	Inaccurately perceived as niche drugs, antiemetics are key elements of cancer treatment alleviating the most dreaded side effect of chemotherapy. Serotonin 5-HT3 receptor antagonists are the most commonly prescribed class of drugs to control chemotherapy-induced nausea and vomiting (CINV). These antagonists have been clinically successful drugs since the 1980s, yet our understanding of how they operate at the molecular level has been hampered by the difficulty of obtaining structures of drug-receptor complexes. Here, we report the cryo-EM structure of the palonosetron-bound 5-HT3 receptor. We investigate the binding of palonosetron, granisetron, dolasetron, ondansetron, and cilansetron using molecular dynamics, covering the whole set of antagonists used in the clinical practice. The structural and computational results yield detailed atomic insight into the binding modes of the drugs. In light of our data, we establish a comprehensive framework underlying the inhibition mechanism by the -setron drug family.
has issue date	2020-02-15(xsd:dateTime)
bibo:doi	10.1101/2020.02.14.947937
has license	biorxiv
sha1sum (hex)	4b18db84c192a515cc4f74878d8a9ed807a58c25
schema:url	https://doi.org/10.1101/2020.02.14.947937
resource representing a document's title	The binding of palonosetron and other antiemetic drugs to the serotonin 5-HT3 receptor
schema:publication	bioRxiv
resource representing a document's body	covid:4b18db84c192a515cc4f74878d8a9ed807a58c25#body_text
is schema:about of	named entity 'commonly' named entity 'antagonists' named entity 'DIFFICULTY' named entity 'LIGHT' named entity 'SEROTONIN 5-HT3 RECEPTOR ANTAGONISTS' »more»

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