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Structure paper

TitleStructure-Activity Relationship and Crystallographic Studies on 4-Hydroxypyrimidine HIF Prolyl Hydroxylase Domain Inhibitors.
Journal, issue, pagesChemmedchem, Vol. 15, Page 270-273, Year 2020
Publish dateSep 10, 2019 (structure data deposition date)
AuthorsHolt-Martyn, J.P. / Chowdhury, R. / Tumber, A. / Yeh, T.L. / Abboud, M.I. / Lippl, K. / Lohans, C.T. / Langley, G.W. / Figg Jr., W. / McDonough, M.A. ...Holt-Martyn, J.P. / Chowdhury, R. / Tumber, A. / Yeh, T.L. / Abboud, M.I. / Lippl, K. / Lohans, C.T. / Langley, G.W. / Figg Jr., W. / McDonough, M.A. / Pugh, C.W. / Ratcliffe, P.J. / Schofield, C.J.
External linksChemmedchem / PubMed:31751494
MethodsX-ray diffraction
Resolution2.426 Å
Structure data

PDB-6st3:
HIF prolyl hydroxylase 2 (PHD2/ EGLN1) in complex with 4-hydroxy-N-(4-phenoxybenzyl)-2-(1H-pyrazol-1-yl)pyrimidine-5-carboxamide
Method: X-RAY DIFFRACTION / Resolution: 2.426 Å

Chemicals

ChemComp-LUW:
4-oxidanyl-~{N}-[(4-phenoxyphenyl)methyl]-2-pyrazol-1-yl-pyrimidine-5-carboxamide

ChemComp-FMT:
FORMIC ACID

ChemComp-MN:
Unknown entry

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsOXIDOREDUCTASE / NON-HEME DIOXYGENASE / IRON / 2-OXOGLUTARATE / HYPOXIA-INDUCIBLE FACTOR / HIF / HIF PROLYL HYDROXYLASE DOMAIN 2 / PHD2 / EGLN1 / OXYGENASE / HYPOXIA / DNA-BINDING / METAL-BINDING / TRANSCRIPTION / HELIX-LOOP-HELIX-BETA / DSBH / FACIAL TRIAD / CYTOPLASM / TRANSCRIPTION/EPIGENETIC REGULATION / SIGNALING / DEVELOPMENT / CELL STRUCTURE / BETA-HYDROXYLATION / TRANSCRIPTION ACTIVATOR/INHIBITOR / UBL CONJUGATION / POLYMORPHISM / VITAMIN C / ZINC-FINGER / FAMILIAL ERYTHROCYTOSIS / BREAST CANCER / TRANSCRIPTION COMPLEX

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