5-hydroxytryptamine receptor: Difference between revisions
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< | <StructureSection load='4iar' size='350' side='right' scene='' caption='Human 5-hydroxytryptamine receptor 1B chimera with E. coli cytochrome B562 complex with ergotamine (PDB code [[4iar]]) '> | ||
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== Function == | == Function == | ||
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5-HT3 antagonists have been predominantly used as an antiemetic drug in relieving treating symptoms such as nausea and vomiting for a cancer patient receiving chemotherapy. Three high affinity antagonist often used are granisetron, tropisteron and ondansetron. The common structure shared among 5-HT3 antagonists contains an amine with an aromatic ring system and a carbonyl group. <ref name = "two" /> Experimental homology modeling suggests that 5-HT3 antagonists have aromatic rings that form π-π interactions with the tyrosine, Y143 and tryptophan, W183, side chains of the 5-HT3 receptor. It is also theorized that the antagonist contain carbonyl groups which accept hydrogen bonds from serine, S227, side chain of the 5-HT3 receptor.<ref>Maksay G, Zsolt B, Miklós S. ''Binding Interactions of Antagonists with 5‐Hydroxytryptamine 3A Receptor Models.'' Journal of Receptors and Signal Transduction 23.2-3 (2003): 255-70. [http://www.tandfonline.com/doi/full/10.1081/RRS-120025568 DOI:10.1081/RRS-120025568]</ref> During the binding of granisteron to the 5-HT3 receptor, the aromatic rings sit within W183 and Y234 and an azabicyclic ring within W90 and F226 of the binding pocket.<ref name = "two" /> Once a 5-HT3 antagonist has bound to a 5-HT3 receptor, serotonin binding is inhibited.<ref>Brunton LL, Lazo JS, Parker KL. (2006). Goddman & Gilman's The Pharmacological Basis of Therapeutics. New York: McGraw-Hill. pp. 1000–3. ISBN 978-0-07-142280-2.</ref><br /> | 5-HT3 antagonists have been predominantly used as an antiemetic drug in relieving treating symptoms such as nausea and vomiting for a cancer patient receiving chemotherapy. Three high affinity antagonist often used are granisetron, tropisteron and ondansetron. The common structure shared among 5-HT3 antagonists contains an amine with an aromatic ring system and a carbonyl group. <ref name = "two" /> Experimental homology modeling suggests that 5-HT3 antagonists have aromatic rings that form π-π interactions with the tyrosine, Y143 and tryptophan, W183, side chains of the 5-HT3 receptor. It is also theorized that the antagonist contain carbonyl groups which accept hydrogen bonds from serine, S227, side chain of the 5-HT3 receptor.<ref>Maksay G, Zsolt B, Miklós S. ''Binding Interactions of Antagonists with 5‐Hydroxytryptamine 3A Receptor Models.'' Journal of Receptors and Signal Transduction 23.2-3 (2003): 255-70. [http://www.tandfonline.com/doi/full/10.1081/RRS-120025568 DOI:10.1081/RRS-120025568]</ref> During the binding of granisteron to the 5-HT3 receptor, the aromatic rings sit within W183 and Y234 and an azabicyclic ring within W90 and F226 of the binding pocket.<ref name = "two" /> Once a 5-HT3 antagonist has bound to a 5-HT3 receptor, serotonin binding is inhibited.<ref>Brunton LL, Lazo JS, Parker KL. (2006). Goddman & Gilman's The Pharmacological Basis of Therapeutics. New York: McGraw-Hill. pp. 1000–3. ISBN 978-0-07-142280-2.</ref><br /> | ||
For more details see [[5-ht3a receptor]]. | For more details see [[5-ht3a receptor]]. | ||
</StructureSection> | |||
==3D structures of 5-hydroxytryptamine receptor== | ==3D structures of 5-hydroxytryptamine receptor== | ||
Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}} | Updated on {{REVISIONDAY2}}-{{MONTHNAME|{{REVISIONMONTH}}}}-{{REVISIONYEAR}} | ||
