ZYBT1, a potent, irreversible Bruton's Tyrosine Kinase (BTK) inhibitor that inhibits the C481S BTK with profound efficacy against arthritis and cancer.
Bruton's tyrosine kinase
cancer
irreversible inhibitor
rheumatoid arthritis
xenograft
Journal
Pharmacology research & perspectives
ISSN: 2052-1707
Titre abrégé: Pharmacol Res Perspect
Pays: United States
ID NLM: 101626369
Informations de publication
Date de publication:
08 2020
08 2020
Historique:
received:
27
11
2019
revised:
18
01
2020
accepted:
20
01
2020
entrez:
14
8
2020
pubmed:
14
8
2020
medline:
4
6
2021
Statut:
ppublish
Résumé
Bruton's tyrosine kinase (BTK) plays a central and pivotal role in controlling the pathways involved in the pathobiology of cancer, rheumatoid arthritis (RA), and other autoimmune disorders. ZYBT1 is a potent, irreversible, specific BTK inhibitor that inhibits the ibrutinib-resistant C481S BTK with nanomolar potency. ZYBT1 is found to be a promising molecule to treat both cancer and RA. In the present report we profiled the molecule for in-vitro, in-vivo activity, and pharmacokinetic properties. ZYBT1 inhibits BTK and C481S BTK with an IC
Identifiants
pubmed: 32790160
doi: 10.1002/prp2.565
pmc: PMC7424564
doi:
Substances chimiques
Protein Kinase Inhibitors
0
Agammaglobulinaemia Tyrosine Kinase
EC 2.7.10.2
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
e00565Informations de copyright
© 2020 The Authors. Pharmacology Research & Perspectives published by John Wiley & Sons Ltd, British Pharmacological Society and American Society for Pharmacology and Experimental Therapeutics.
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