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Structure paper

TitleMechanism of inhibition of human glucose transporter GLUT1 is conserved between cytochalasin B and phenylalanine amides.
Journal, issue, pagesProc. Natl. Acad. Sci. USA, Vol. 113, Page 4711-4716, Year 2016
Publish dateNov 12, 2015 (structure data deposition date)
AuthorsKapoor, K. / Finer-Moore, J.S. / Pedersen, B.P. / Caboni, L. / Waight, A. / Hillig, R.C. / Bringmann, P. / Heisler, I. / Muller, T. / Siebeneicher, H. / Stroud, R.M.
External linksProc. Natl. Acad. Sci. USA / PubMed:27078104
MethodsX-ray diffraction
Resolution2.9 - 3.002 Å
Structure data

PDB-5eqg:
Human GLUT1 in complex with inhibitor (2~{S})-3-(4-fluorophenyl)-2-[2-(3-hydroxyphenyl)ethanoylamino]-~{N}-[(1~{S})-1-phenylethyl]propanamide
Method: X-RAY DIFFRACTION / Resolution: 2.9 Å

PDB-5eqh:
Human GLUT1 in complex with inhibitor (2~{S})-3-(2-bromophenyl)-2-[2-(4-methoxyphenyl)ethanoylamino]-~{N}-[(1~{S})-1-phenylethyl]propanamide
Method: X-RAY DIFFRACTION / Resolution: 2.99 Å

PDB-5eqi:
Human GLUT1 in complex with Cytochalasin B
Method: X-RAY DIFFRACTION / Resolution: 3.002 Å

Chemicals

ChemComp-5RE:
(2~{S})-3-(4-fluorophenyl)-2-[2-(3-hydroxyphenyl)ethanoylamino]-~{N}-[(1~{S})-1-phenylethyl]propanamide

ChemComp-5RF:
(2~{S})-3-(2-bromophenyl)-2-[2-(4-methoxyphenyl)ethanoylamino]-~{N}-[(1~{S})-1-phenylethyl]propanamide

ChemComp-5RH:
Cytochalasin B / toxin*YM

Source
  • homo sapiens (human)
KeywordsTRANSPORT PROTEIN/INHIBITOR / MFS transporter / glucose transporter / TRANSPORT PROTEIN-INHIBITOR complex

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