Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-
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:
09 06 2022
09 06 2022
Historique:
pubmed:
25
5
2022
medline:
11
6
2022
entrez:
24
5
2022
Statut:
ppublish
Résumé
Serine/threonine kinase 17A (death-associated protein kinase-related apoptosis-inducing protein kinase 1─DRAK1) is a part of the death-associated protein kinase (DAPK) family and belongs to the so-called dark kinome. Thus, the current state of knowledge of the cellular function of DRAK1 and its involvement in pathophysiological processes is very limited. Recently, DRAK1 has been implicated in tumorigenesis of glioblastoma multiforme (GBM) and other cancers, but no selective inhibitors of DRAK1 are available yet. To this end, we optimized a pyrazolo[1,5-
Identifiants
pubmed: 35608370
doi: 10.1021/acs.jmedchem.2c00173
doi:
Substances chimiques
Apoptosis Regulatory Proteins
0
Protein Kinase Inhibitors
0
Pyrimidines
0
Serine
452VLY9402
Death-Associated Protein Kinases
EC 2.7.11.1
Protein Serine-Threonine Kinases
EC 2.7.11.1
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM