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Structure paper

TitleStructural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist.
Journal, issue, pagesScience, Vol. 350, Page aac5464-aac5464, Year 2015
Publish dateNov 3, 2015 (structure data deposition date)
AuthorsAhuja, S. / Mukund, S. / Deng, L. / Khakh, K. / Chang, E. / Ho, H. / Shriver, S. / Young, C. / Lin, S. / Johnson, J.P. ...Ahuja, S. / Mukund, S. / Deng, L. / Khakh, K. / Chang, E. / Ho, H. / Shriver, S. / Young, C. / Lin, S. / Johnson, J.P. / Wu, P. / Li, J. / Coons, M. / Tam, C. / Brillantes, B. / Sampang, H. / Mortara, K. / Bowman, K.K. / Clark, K.R. / Estevez, A. / Xie, Z. / Verschoof, H. / Grimwood, M. / Dehnhardt, C. / Andrez, J.C. / Focken, T. / Sutherlin, D.P. / Safina, B.S. / Starovasnik, M.A. / Ortwine, D.F. / Franke, Y. / Cohen, C.J. / Hackos, D.H. / Koth, C.M. / Payandeh, J.
External linksScience / PubMed:26680203
MethodsX-ray diffraction
Resolution3.53 Å
Structure data

PDB-5ek0:
Human Nav1.7-VSD4-NavAb in complex with GX-936.
Method: X-RAY DIFFRACTION / Resolution: 3.53 Å

Chemicals

ChemComp-PX4:
1,2-DIMYRISTOYL-SN-GLYCERO-3-PHOSPHOCHOLINE / DMPC, phospholipid*YM

ChemComp-5P2:
3-cyano-4-[2-[2-(1-ethylazetidin-3-yl)pyrazol-3-yl]-4-(trifluoromethyl)phenoxy]-~{N}-(1,2,4-thiadiazol-5-yl)benzenesulfonamide

Source
  • arcobacter butzleri (bacteria)
  • homo sapiens (human)
KeywordsMETAL TRANSPORT / membrane protein / ion channel / voltage-gated sodium channel / small molecule antagonist

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