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Structure paper

Title5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology.
Journal, issue, pagesCell, Vol. 172, Page 719-730.e14, Year 2018
Publish dateNov 27, 2017 (structure data deposition date)
AuthorsPeng, Y. / McCorvy, J.D. / Harpsoe, K. / Lansu, K. / Yuan, S. / Popov, P. / Qu, L. / Pu, M. / Che, T. / Nikolajsen, L.F. ...Peng, Y. / McCorvy, J.D. / Harpsoe, K. / Lansu, K. / Yuan, S. / Popov, P. / Qu, L. / Pu, M. / Che, T. / Nikolajsen, L.F. / Huang, X.P. / Wu, Y. / Shen, L. / Bjorn-Yoshimoto, W.E. / Ding, K. / Wacker, D. / Han, G.W. / Cheng, J. / Katritch, V. / Jensen, A.A. / Hanson, M.A. / Zhao, S. / Gloriam, D.E. / Roth, B.L. / Stevens, R.C. / Liu, Z.J.
External linksCell / PubMed:29398112
MethodsX-ray diffraction
Resolution2.7 - 3 Å
Structure data

PDB-6bqg:
Crystal structure of 5-HT2C in complex with ergotamine
Method: X-RAY DIFFRACTION / Resolution: 3 Å

PDB-6bqh:
Crystal structure of 5-HT2C in complex with ritanserin
Method: X-RAY DIFFRACTION / Resolution: 2.7 Å

Chemicals

ChemComp-ERM:
Ergotamine / neurotransmitter, alkaloid*YM

ChemComp-OLC:
(2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate

ChemComp-E2J:
6-(2-{4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl}ethyl)-7-methyl-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one / medication, antidepressant, antagonist*YM

ChemComp-PEG:
DI(HYDROXYETHYL)ETHER

ChemComp-OLA:
OLEIC ACID

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
  • escherichia coli (E. coli)
KeywordsMEMBRANE PROTEIN / human 5-HT2C receptor / GPCR / ergotamine / polypharmacology / BRIL / LCP / ritanserin / selectivity

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