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Selective inhibition reveals cyclin-dependent kinase 2 as another kinase that phosphorylates the androgen receptor at serine 81

SYSNO ASEP	0488706
Document Type	J - Journal Article
R&D Document Type	Journal Article
Subsidiary J	Článek ve WOS
Title	Selective inhibition reveals cyclin-dependent kinase 2 as another kinase that phosphorylates the androgen receptor at serine 81
Author(s)	Jorda, Radek (UEB-Q)_{ORCID, RID} Bučková, Zuzana (UEB-Q) Řezníčková, Eva (UEB-Q)_{RID, ORCID} Bouchal, J. (CZ) Kryštof, Vladimír (UEB-Q)_{RID, ORCID}
Number of authors	5
Source Title	Biochimica Et Biophysica Acta-Molecular Cell Research. - : Elsevier - ISSN 0167-4889 Roč. 1865, č. 2 (2018), s. 354-363
Number of pages	10 s.
Language	eng - English
Country	NL - Netherlands
Keywords	Androgen receptor ; Cyclin-dependent kinase ; Inhibitor ; Phosphorylation ; Serine 81
Subject RIV	EB - Genetics ; Molecular Biology
OECD category	Biochemistry and molecular biology
R&D Projects	LO1204 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
	LO1304 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
Institutional support	UEB-Q - RVO:61389030
UT WOS	000423893100013
EID SCOPUS	85034845471
DOI	10.1016/j.bbamcr.2017.11.011
Annotation	Several studies have revealed that cyclin-dependent kinases (CDK) can mediate phosphorylation of steroid receptors at multiple sites, including serine 81 of the androgen receptor (AR). Phosphorylation of S81 is required for AR nuclear translocation, an association with chromatin and also regulates endogenous AR-regulated transcription in response to hormones. Up to date, S81-phosphorylation has been studied using different CDK inhibitors. Nevertheless, most inhibitors are non-selective or have unknown selectivity. We investigated the selectivity of commercially available CDK inhibitors and identified compounds that will be suitable for further studies to identify the CDKs responsible for S81-AR phosphorylation. We confirmed the positive impact of CDK1 and CDK9 on phosphorylation of S81-AR and its transcriptional activity. Although CDK1-mediated phosphorylation was previously shown to occur during mitosis, our experiments did not confirm this finding. By using chemical and genetic inhibition techniques, we identified that CDK2 contributes to S81-AR phosphorylation and transactivation while CDK4 was not shown to be involved in this process.
Workplace	Institute of Experimental Botany
Contact	David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469
Year of Publishing	2019

Number of the records: 1