Onvansertib, a polo-like kinase 1 inhibitor, inhibits prostate stromal cell growth and prostate smooth muscle contraction, which is additive to inhibition by α
Adrenergic alpha-2 Receptor Antagonists
/ pharmacology
Cell Cycle Proteins
/ antagonists & inhibitors
Cell Proliferation
/ drug effects
Cell Survival
/ drug effects
Cells, Cultured
Drug Synergism
Humans
In Vitro Techniques
Male
Muscle Contraction
/ drug effects
Muscle, Smooth
/ drug effects
Piperazines
/ pharmacology
Prostate
/ cytology
Protein Kinase Inhibitors
/ pharmacology
Protein Serine-Threonine Kinases
/ antagonists & inhibitors
Proto-Oncogene Proteins
/ antagonists & inhibitors
Pyrazoles
/ pharmacology
Quinazolines
/ pharmacology
Stromal Cells
/ drug effects
Tumor Stem Cell Assay
Polo-Like Kinase 1
Benign prostatic hyperplasia (BPH)
Human endothelin-1 (PubChem CID 16212950)
Lower urinary tract symptoms (LUTS)
Methoxamine (PubChem CID 6081)
Noradrenaline (PubChem CID 439260)
Onvansertib
Onvansertib (PCM-075) (PubChem CID 49792852)
Phenylephrine (PubChem CID 5284443)
Polo-like kinase (PLK)
Prostate smooth muscle contraction
Silodosin (PubChem CID 5312125)
Tamsulosin (PubChem CID 5362376)
U46619 (PubChem CID 16760624)
Journal
European journal of pharmacology
ISSN: 1879-0712
Titre abrégé: Eur J Pharmacol
Pays: Netherlands
ID NLM: 1254354
Informations de publication
Date de publication:
15 Apr 2020
15 Apr 2020
Historique:
received:
23
07
2019
revised:
15
01
2020
accepted:
31
01
2020
pubmed:
6
2
2020
medline:
28
11
2020
entrez:
5
2
2020
Statut:
ppublish
Résumé
Prostate smooth muscle contraction and prostate enlargement contribute to lower urinary tract symptoms suggestive of benign prostatic hyperplasia. Recent evidence demonstrated that inhibitors for polo-like kinases (PLKs) inhibit smooth muscle contraction of human prostate tissues. However, their additive effects to α
Identifiants
pubmed: 32017934
pii: S0014-2999(20)30077-7
doi: 10.1016/j.ejphar.2020.172985
pii:
doi:
Substances chimiques
Adrenergic alpha-2 Receptor Antagonists
0
Cell Cycle Proteins
0
Piperazines
0
Protein Kinase Inhibitors
0
Proto-Oncogene Proteins
0
Pyrazoles
0
Quinazolines
0
onvansertib
67RM91WDHQ
Protein Serine-Threonine Kinases
EC 2.7.11.1
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
172985Informations de copyright
Copyright © 2020 Elsevier B.V. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest This project was supported in part by a research grant from Trovagene Inc. (San Diego, CA, USA), which was provided to the Department of Urology, University Hospital Munich to perform this project. The opinions expressed in this article are those of the authors and do not necessarily represent those of Trovagene Inc. The study design was based on a contract between University Hospital Munich and Trovagene. Trovagene was not involved in the collection, analysis, and interpretation of data. The manuscript has been approved by all authors. The decision to submit the article for publication was made by Martin Hennenberg. The DFG had no role in study design, in the collection, analysis and interpretation of data, in writing of the report, and in the decision to submit the article for publication.