Prevention of Skin Carcinogenesis by the Non-β-blocking R-carvedilol Enantiomer.
Animals
Carcinogenesis
/ chemically induced
Carvedilol
/ administration & dosage
Epidermal Cells
Epidermal Growth Factor
/ toxicity
Epidermis
/ drug effects
Female
HEK293 Cells
Humans
Mice
Neoplasms, Experimental
/ etiology
Skin Neoplasms
/ etiology
Stereoisomerism
Ultraviolet Rays
/ adverse effects
Journal
Cancer prevention research (Philadelphia, Pa.)
ISSN: 1940-6215
Titre abrégé: Cancer Prev Res (Phila)
Pays: United States
ID NLM: 101479409
Informations de publication
Date de publication:
05 2021
05 2021
Historique:
received:
23
11
2020
revised:
22
01
2021
accepted:
25
02
2021
pubmed:
3
3
2021
medline:
11
3
2022
entrez:
2
3
2021
Statut:
ppublish
Résumé
Skin cancer is the most common malignancy worldwide and is rapidly rising in incidence, representing a significant public health challenge. The β-blocker, carvedilol, has shown promising effects in preventing skin cancer. However, as a potent β-blocker, repurposing carvedilol to an anticancer agent is limited by cardiovascular effects. Carvedilol is a racemic mixture consisting of equimolar S- and R-carvedilol, whereas the R-carvedilol enantiomer does not possess β-blocking activity. Because previous studies suggest that carvedilol's cancer preventive activity is independent of β-blockade, we examined the skin cancer preventive activity of R-carvedilol compared with S-carvedilol and the racemic carvedilol. R- and S-carvedilol were equally effective in preventing EGF-induced neoplastic transformation of the mouse epidermal JB6 Cl 41-5a (JB6 P+) cells and displayed similar attenuation of EGF-induced ELK-1 activity. R-carvedilol appeared slightly better than S-carvedilol against UV-induced intracellular oxidative stress and release of prostaglandin E
Identifiants
pubmed: 33648941
pii: 1940-6207.CAPR-20-0609
doi: 10.1158/1940-6207.CAPR-20-0609
pmc: PMC8102373
mid: NIHMS1680452
doi:
Substances chimiques
Carvedilol
0K47UL67F2
Epidermal Growth Factor
62229-50-9
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
527-540Subventions
Organisme : NCI NIH HHS
ID : R15 CA227946
Pays : United States
Informations de copyright
©2021 American Association for Cancer Research.
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