Novel Ridaifen-B Structure Analog Induces Apoptosis and Autophagy Depending on Pyrrolidine Side Chain.
Actins
/ genetics
Apoptosis
/ drug effects
Autophagy
/ drug effects
Caspase 3
/ genetics
Cell Line, Tumor
Gene Expression Regulation
/ drug effects
Humans
Mitochondria
/ drug effects
Mitophagy
Molecular Structure
Pyrrolidines
/ chemistry
Reactive Oxygen Species
/ metabolism
Structure-Activity Relationship
Tamoxifen
/ analogs & derivatives
apoptosis
autophagy
mitophagy
ridaifen
tamoxifen
Journal
Biological & pharmaceutical bulletin
ISSN: 1347-5215
Titre abrégé: Biol Pharm Bull
Pays: Japan
ID NLM: 9311984
Informations de publication
Date de publication:
2019
2019
Historique:
entrez:
5
3
2019
pubmed:
5
3
2019
medline:
10
7
2019
Statut:
ppublish
Résumé
Ridaifen (RID)-B is an analog derived from tamoxifen (TAM). TAM has an antitumor effect by acting as an antagonist to estrogen receptor (ER). However, TAM is known to also induces apoptosis in cancer cells that do not have ER. We clarified that RID-B induces cell death at a lower concentration than TAM, and causes ER-independent apoptosis and autophagy. Based on the results of previous studies, we assumed that RID-B had a unique target different from ER and examined structural activity correlation to determine what kinds of structural features are related to RID-B activity. As a result, we found there was activity even without one of phenyl groups (Ar
Identifiants
pubmed: 30828072
doi: 10.1248/bpb.b18-00643
doi:
Substances chimiques
Actins
0
Pyrrolidines
0
Reactive Oxygen Species
0
ridaifen-B
0
Tamoxifen
094ZI81Y45
Caspase 3
EC 3.4.22.-
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM