Discovery and Characterization of the Potent and Highly Selective 1,7-Naphthyridine-Based Inhibitors BAY-091 and BAY-297 of the Kinase PIP4K2A.
Animals
Apoptosis
/ drug effects
Cell Line, Tumor
Cell Proliferation
/ drug effects
Drug Discovery
Drug Screening Assays, Antitumor
Enzyme Inhibitors
/ chemistry
High-Throughput Screening Assays
Humans
Mice
Mice, Knockout
Mitochondria
/ drug effects
Naphthyridines
/ chemistry
Phosphotransferases (Alcohol Group Acceptor)
/ antagonists & inhibitors
Reactive Oxygen Species
/ metabolism
Signal Transduction
/ drug effects
Structure-Activity Relationship
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
11 11 2021
11 11 2021
Historique:
pubmed:
27
10
2021
medline:
1
2
2022
entrez:
26
10
2021
Statut:
ppublish
Résumé
PIP4K2A is an insufficiently studied type II lipid kinase that catalyzes the conversion of phosphatidylinositol-5-phosphate (PI5P) into phosphatidylinositol 4,5-bisphosphate (PI4,5P
Identifiants
pubmed: 34699202
doi: 10.1021/acs.jmedchem.1c01245
doi:
Substances chimiques
Enzyme Inhibitors
0
Naphthyridines
0
Reactive Oxygen Species
0
PIP4K2A protein, human
EC 2.7.1.-
Phosphotransferases (Alcohol Group Acceptor)
EC 2.7.1.-
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM