Design, synthesis, and evaluation of novel stilbene derivatives that degrade acidic nucleoplasmic DNA-binding protein 1 (And1) and synergize with PARP1 inhibitor in NSCLC cells.
Humans
Structure-Activity Relationship
Cell Proliferation
/ drug effects
Drug Screening Assays, Antitumor
Drug Design
Molecular Structure
Antineoplastic Agents
/ pharmacology
Dose-Response Relationship, Drug
Lung Neoplasms
/ drug therapy
Poly (ADP-Ribose) Polymerase-1
/ antagonists & inhibitors
Carcinoma, Non-Small-Cell Lung
/ drug therapy
Stilbenes
/ pharmacology
Poly(ADP-ribose) Polymerase Inhibitors
/ pharmacology
DNA-Binding Proteins
/ metabolism
Cell Line, Tumor
And-1(WDHD1)
DNA damage response
antitumor
synthetic lethal
Journal
Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203
Informations de publication
Date de publication:
Dec 2024
Dec 2024
Historique:
medline:
29
7
2024
pubmed:
29
7
2024
entrez:
29
7
2024
Statut:
ppublish
Résumé
Specifically inducing the degradation of acidic nucleoplasmic DNA-binding protein 1 (And1) is a promising antitumor strategy. Our previous study identified Bazedoxifene (BZA) and CH3 as specific And1 degraders and validated their activity in reversing radiotherapy resistance
Identifiants
pubmed: 39072709
doi: 10.1080/14756366.2024.2383886
doi:
Substances chimiques
Antineoplastic Agents
0
Poly (ADP-Ribose) Polymerase-1
EC 2.4.2.30
Stilbenes
0
PARP1 protein, human
EC 2.4.2.30
Poly(ADP-ribose) Polymerase Inhibitors
0
DNA-Binding Proteins
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM