Structure-Activity Relationship and Crystallographic Studies on 4-Hydroxypyrimidine HIF Prolyl Hydroxylase Domain Inhibitors.
anaemia
hypoxia
prolyl hydroxylases
structure-activity relationships
Journal
ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013
Informations de publication
Date de publication:
05 02 2020
05 02 2020
Historique:
received:
30
09
2019
revised:
08
11
2019
pubmed:
22
11
2019
medline:
9
2
2021
entrez:
22
11
2019
Statut:
ppublish
Résumé
The 2-oxoglutarate-dependent hypoxia inducible factor prolyl hydroxylases (PHDs) are targets for treatment of a variety of diseases including anaemia. One PHD inhibitor is approved for use for the treatment of renal anaemia and others are in late stage clinical trials. The number of reported templates for PHD inhibition is limited. We report structure-activity relationship and crystallographic studies on a promising class of 4-hydroxypyrimidine-containing PHD inhibitors.
Identifiants
pubmed: 31751494
doi: 10.1002/cmdc.201900557
pmc: PMC7496690
doi:
Substances chimiques
Prolyl-Hydroxylase Inhibitors
0
Pyrimidinones
0
4-hydroxypyrimidine
4562-27-0
EGLN1 protein, human
EC 1.14.11.2
Hypoxia-Inducible Factor-Proline Dioxygenases
EC 1.14.11.29
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
270-273Subventions
Organisme : British Heart Foundation
ID : PG/12/33/29546
Pays : United Kingdom
Organisme : British Heart Foundation
ID : RG/11/1/28684
Pays : United Kingdom
Organisme : Cancer Research UK
Pays : United Kingdom
Organisme : Biotechnology and Biological Sciences Research Council
Pays : United Kingdom
Informations de copyright
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.
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