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TitleActivation and allosteric modulation of a muscarinic acetylcholine receptor.
Journal, issue, pagesNature, Vol. 504, Page 101-106, Year 2013
Publish dateSep 16, 2013 (structure data deposition date)
AuthorsKruse, A.C. / Ring, A.M. / Manglik, A. / Hu, J. / Hu, K. / Eitel, K. / Hubner, H. / Pardon, E. / Valant, C. / Sexton, P.M. ...Kruse, A.C. / Ring, A.M. / Manglik, A. / Hu, J. / Hu, K. / Eitel, K. / Hubner, H. / Pardon, E. / Valant, C. / Sexton, P.M. / Christopoulos, A. / Felder, C.C. / Gmeiner, P. / Steyaert, J. / Weis, W.I. / Garcia, K.C. / Wess, J. / Kobilka, B.K.
External linksNature / PubMed:24256733
MethodsX-ray diffraction
Resolution3.5 - 3.7 Å
Structure data

PDB-4mqs:
Structure of active human M2 muscarinic acetylcholine receptor bound to the agonist iperoxo
Method: X-RAY DIFFRACTION / Resolution: 3.5 Å

PDB-4mqt:
Structure of active human M2 muscarinic acetylcholine receptor bound to the agonist iperoxo and allosteric modulator LY2119620
Method: X-RAY DIFFRACTION / Resolution: 3.7 Å

Chemicals

ChemComp-IXO:
4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium

ChemComp-2CU:
3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]thieno[2,3-b]pyridine-2-carboxamide

Source
  • homo sapiens (human)
  • lama glama (llama)
KeywordsSIGNALING PROTEIN / G protein-coupled receptor / Muscarinic acetylcholine receptor / allosteric modulation

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