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TitleTrelagliptin (SYR-472, Zafatek), Novel Once-Weekly Treatment for Type 2 Diabetes, Inhibits Dipeptidyl Peptidase-4 (DPP-4) via a Non-Covalent Mechanism.
Journal, issue, pagesPlos One, Vol. 11, Page e0157509-e0157509, Year 2016
Publish dateJun 3, 2016 (structure data deposition date)
AuthorsGrimshaw, C.E. / Jennings, A. / Kamran, R. / Ueno, H. / Nishigaki, N. / Kosaka, T. / Tani, A. / Sano, H. / Kinugawa, Y. / Koumura, E. ...Grimshaw, C.E. / Jennings, A. / Kamran, R. / Ueno, H. / Nishigaki, N. / Kosaka, T. / Tani, A. / Sano, H. / Kinugawa, Y. / Koumura, E. / Shi, L. / Takeuchi, K.
External linksPlos One / PubMed:27328054
MethodsX-ray diffraction
Resolution2.24 Å
Structure data

PDB-5kby:
Crystal structure of dipeptidyl peptidase IV in complex with SYR-472
Method: X-RAY DIFFRACTION / Resolution: 2.24 Å

Chemicals

ChemComp-NAG:
2-acetamido-2-deoxy-beta-D-glucopyranose

ChemComp-6RL:
2-[[6-[(3~{R})-3-azanylpiperidin-1-yl]-3-methyl-2,4-bis(oxidanylidene)pyrimidin-1-yl]methyl]-4-fluoranyl-benzenecarboni

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsHYDROLASE/HYDROLASE INHIBITOR / peptidase / glp-1 / metabolic disease / co-complex / HYDROLASE-HYDROLASE INHIBITOR complex

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