untitled
<OAI-PMH schemaLocation=http://www.openarchives.org/OAI/2.0/ http://www.openarchives.org/OAI/2.0/OAI-PMH.xsd>
<responseDate>2018-01-15T18:25:43Z</responseDate>
<request identifier=oai:HAL:hal-01216205v1 verb=GetRecord metadataPrefix=oai_dc>http://api.archives-ouvertes.fr/oai/hal/</request>
<GetRecord>
<record>
<header>
<identifier>oai:HAL:hal-01216205v1</identifier>
<datestamp>2017-12-21</datestamp>
<setSpec>type:ART</setSpec>
<setSpec>subject:sdv</setSpec>
<setSpec>collection:UNIV-RENNES1</setSpec>
<setSpec>collection:UNIV-AG</setSpec>
<setSpec>collection:IRSET</setSpec>
<setSpec>collection:U991</setSpec>
<setSpec>collection:IRSET-CCII</setSpec>
<setSpec>collection:IFR140</setSpec>
<setSpec>collection:BIOSIT</setSpec>
<setSpec>collection:NUMECAN</setSpec>
<setSpec>collection:INSERM</setSpec>
<setSpec>collection:UR1-UFR-SVE</setSpec>
<setSpec>collection:STATS-UR1</setSpec>
<setSpec>collection:UR1-HAL</setSpec>
<setSpec>collection:EHESP</setSpec>
<setSpec>collection:USPC</setSpec>
<setSpec>collection:UR1-SDV</setSpec>
<setSpec>collection:IRSET-1</setSpec>
<setSpec>collection:UNIV-ANGERS</setSpec>
<setSpec>collection:IRSET-EHESP</setSpec>
</header>
<metadata><dc>
<publisher>HAL CCSD</publisher>
<title lang=en>Protein kinase C-dependent regulation of human hepatic drug transporter expression</title>
<creator>Mayati, Abdullah</creator>
<creator>Le Vee, Marc</creator>
<creator>Moreau, Amélie</creator>
<creator>Jouan, Elodie</creator>
<creator>Bucher, Simon</creator>
<creator>Stieger, Bruno</creator>
<creator>Denizot, Claire</creator>
<creator>Parmentier, Yannick</creator>
<creator>FARDEL, Olivier</creator>
<contributor>Institut de recherche, santé, environnement et travail [Rennes] (Irset) ; Université d'Angers (UA) - Université des Antilles et de la Guyane (UAG) - Université de Rennes 1 (UR1) - École des Hautes Études en Santé Publique [EHESP] (EHESP) - Institut National de la Santé et de la Recherche Médicale (INSERM) - Structure Fédérative de Recherche en Biologie et Santé de Rennes ( Biosit : Biologie - Santé - Innovation Technologique )</contributor>
<contributor>Laboratoire Pharmaceutique ; Technologie Servier</contributor>
<contributor>Foie, métabolismes et cancer ; Université de Rennes 1 (UR1) - Institut National de la Santé et de la Recherche Médicale (INSERM) - Structure Fédérative de Recherche en Biologie et Santé de Rennes ( Biosit : Biologie - Santé - Innovation Technologique )</contributor>
<contributor>Division of Clinical Pharmacology and Toxicology ; University hospital of Zurich [Zurich]</contributor>
<description>International audience</description>
<source>ISSN: 0006-2952</source>
<source>Biochemical Pharmacology</source>
<publisher>Elsevier</publisher>
<identifier>hal-01216205</identifier>
<identifier>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01216205</identifier>
<identifier>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01216205/document</identifier>
<identifier>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01216205/file/Protein%20kinase%20C-dependent%20regulation.pdf</identifier>
<source>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01216205</source>
<source>Biochemical Pharmacology, Elsevier, 2015, 98 (4), pp.703-717. 〈10.1016/j.bcp.2015.10.007〉</source>
<identifier>DOI : 10.1016/j.bcp.2015.10.007</identifier>
<relation>info:eu-repo/semantics/altIdentifier/doi/10.1016/j.bcp.2015.10.007</relation>
<identifier>PUBMED : 26462574</identifier>
<relation>info:eu-repo/semantics/altIdentifier/pmid/26462574</relation>
<language>en</language>
<subject lang=en>Drug transporter</subject>
<subject lang=en>hepatocyte</subject>
<subject lang=en>phorbol ester</subject>
<subject lang=en>protein kinase C</subject>
<subject lang=en>regulation</subject>
<subject>[SDV] Life Sciences [q-bio]</subject>
<subject>[SDV.SP] Life Sciences [q-bio]/Pharmaceutical sciences</subject>
<type>info:eu-repo/semantics/article</type>
<type>Journal articles</type>
<description lang=en>Hepatic drug transporters are now recognized as major actors of hepatobiliary elimination of drugs. Characterization of their regulatory pathways is therefore an important issue. In this context, the present study was designed to analyze the potential regulation of human hepatic transporter expression by protein kinase C (PKC) activation. Treatment by the reference PKC activator phorbol 12-myristate 13-acetate (PMA) for 48 h was shown to decrease mRNA expression of various sinusoidal transporters, including OATP1B1, OATP2B1, NTCP, OCT1 and MRP3, but to increase that of OATP1B3, whereas mRNA expression of canalicular transporters was transiently enhanced (MDR1), decreased (BSEP and MRP2) or unchanged (BCRP) in human hepatoma HepaRG cells. The profile of hepatic transporter mRNA expression changes in PMA-treated HepaRG cells was correlated to that found in PMA-exposed primary human hepatocytes and was similarly observed in response to the PKC-activating marketed drug ingenol mebutate. It was associated with concomitant repression of OATP1B1 and OATP2B1 protein expression and reduction of OATP, OCT1, NTCP and MRP2 activity. The use of chemical PKC inhibitors further suggested a contribution of novel PKCs isoforms to PMA-mediated regulations of transporter mRNA expression. PMA was finally shown to cause epithelial-mesenchymal transition (EMT) in HepaRG cells and exposure to various additional EMT inducers, i.e., hepatocyte growth factor, tumor growth factor-β1 or the HNF4α inhibitor ≡I6015, led to transporter expression alterations highly correlated to those triggered by PMA. Taken together, these data highlight PKC-dependent regulation of human hepatic drug transporter expression, which may be closely linked to EMT triggered by PKC activation</description>
<date>2015</date>
</dc>
</metadata>
</record>
</GetRecord>
</OAI-PMH>
