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TitlePotent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain.
Journal, issue, pagesPlos One, Vol. 10, Page 32004-, Year 2015
Publish dateJun 3, 2015 (structure data deposition date)
AuthorsChan, M.C. / Atasoylu, O. / Hodson, E. / Tumber, A. / Leung, I.K.H. / Chowdhury, R. / Gomez-Perez, V. / Demetriades, M. / Rydzik, A.M. / Holt-Martyn, J. ...Chan, M.C. / Atasoylu, O. / Hodson, E. / Tumber, A. / Leung, I.K.H. / Chowdhury, R. / Gomez-Perez, V. / Demetriades, M. / Rydzik, A.M. / Holt-Martyn, J. / Tian, Y. / Bishop, T. / Claridge, T.D.W. / Kawamura, A. / Pugh, C.W. / Ratcliffe, P.J. / Schofield, C.J.
External linksPlos One / PubMed:26147748
MethodsX-ray diffraction
Resolution3.3 Å
Structure data

PDB-5a3u:
HIF prolyl hydroxylase 2 (PHD2/EGLN1) in complex with 6-(5-oxo-4-(1H- 1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinic acid
Method: X-RAY DIFFRACTION / Resolution: 3.3 Å

Chemicals

ChemComp-MN:
Unknown entry

ChemComp-R8J:
6-(5-oxo-4-(1H-1,2,3-triazol-1-yl)-2,5-dihydro-1H-pyrazol-1-yl)nicotinic acid

Source
  • homo sapiens (human)
KeywordsOXIDOREDUCTASE / NON-HEME / IRON / 2-OXOGLUTARATE / DIOXYGENASE / HYPOXIA-INDUCIBLE FACTOR / HIF / HIF PROLYL HYDROXYLASE DOMAIN 2 / PHD2 / EGLN / OXYGENASE / HYPOXIA / DNA-BINDING / METAL-BINDING / TRANSCRIPTION / HELIX-LOOP-HELIX-BETA / DSBH / FACIAL TRIAD / ASPARAGINYL/ ASPARTYL HYDROXYLASE / TRANSCRIPTION AND EPIGENETIC REGULATION / SIGNALING / DEVELOPMENT / CELL STRUCTURE / ANKYRIN REPEAT DOMAIN / ARD / BETA-HYDROXYLATION / TRANSCRIPTION ACTIVATOR/INHIBITOR / PHOSPHORYLATION / S-NITROSYLATION

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