Phosphodiesterase Type-5 Inhibitor Tadalafil Modulates Steroid Hormones Signaling in a Prostate Cancer Cell Line.
Biomarkers
Cell Line, Tumor
Cell Proliferation
/ drug effects
Cell Survival
/ drug effects
Drug Resistance, Neoplasm
Gene Expression Profiling
Gene Expression Regulation, Neoplastic
Hormones
/ metabolism
Humans
Male
Phosphodiesterase 5 Inhibitors
/ pharmacology
Prostatic Neoplasms
/ drug therapy
Protein Transport
Receptors, Androgen
/ genetics
Signal Transduction
/ drug effects
Steroids
/ metabolism
Tadalafil
/ pharmacology
androgen resistance
aromatase
bicalutamide
prostate cancer
tadalafil
Journal
International journal of molecular sciences
ISSN: 1422-0067
Titre abrégé: Int J Mol Sci
Pays: Switzerland
ID NLM: 101092791
Informations de publication
Date de publication:
13 Jan 2021
13 Jan 2021
Historique:
received:
15
12
2020
revised:
07
01
2021
accepted:
08
01
2021
entrez:
16
1
2021
pubmed:
17
1
2021
medline:
10
4
2021
Statut:
epublish
Résumé
The androgen receptor (AR) plays a key role in normal prostate homeostasis and in prostate cancer (PCa) development, while the role of aromatase (Cyp19a1) is still unclear. We evaluated the effects of a treatment with Tadalafil (TAD) on both these proteins. Androgen-sensitive human PCa cell line (LnCAP) was incubated with/without TAD (10 TAD increased early AR nuclear translocation ( We demonstrate for the first time that TAD can significantly modulate AR expression and activity, Cyp19a1 and ERβ expression in PCa cells, suggesting a specific effect of these proteins. In addition, TAD potentiates the antiproliferative activity of BCT, opening a new clinical scenario in the treatment of PCa.
Sections du résumé
BACKGROUND
BACKGROUND
The androgen receptor (AR) plays a key role in normal prostate homeostasis and in prostate cancer (PCa) development, while the role of aromatase (Cyp19a1) is still unclear. We evaluated the effects of a treatment with Tadalafil (TAD) on both these proteins.
METHODS
METHODS
Androgen-sensitive human PCa cell line (LnCAP) was incubated with/without TAD (10
RESULTS
RESULTS
TAD increased early AR nuclear translocation (
CONCLUSION
CONCLUSIONS
We demonstrate for the first time that TAD can significantly modulate AR expression and activity, Cyp19a1 and ERβ expression in PCa cells, suggesting a specific effect of these proteins. In addition, TAD potentiates the antiproliferative activity of BCT, opening a new clinical scenario in the treatment of PCa.
Identifiants
pubmed: 33451122
pii: ijms22020754
doi: 10.3390/ijms22020754
pmc: PMC7828628
pii:
doi:
Substances chimiques
AR protein, human
0
Biomarkers
0
Hormones
0
Phosphodiesterase 5 Inhibitors
0
Receptors, Androgen
0
Steroids
0
Tadalafil
742SXX0ICT
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Agenzia Italiana del Farmaco, Ministero della Salute
ID : 2015XCR88M_008
Organisme : Agenzia Italiana del Farmaco, Ministero della Salute
ID : 2017HBHA98
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