Počet záznamů: 1
Point mutations in human guanylate kinase account for acquired resistance to anticancer nucleotide analogue PMEG
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SYSNO ASEP 0360711 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Point mutations in human guanylate kinase account for acquired resistance to anticancer nucleotide analogue PMEG Tvůrce(i) Mertlíková-Kaiserová, Helena (UOCHB-X) RID, ORCID
Rumlová, Michaela (UOCHB-X) RID
Tloušťová, Eva (UOCHB-X) RID, ORCID
Procházková, Eliška (UOCHB-X) RID, ORCID
Holý, Antonín (UOCHB-X)
Votruba, Ivan (UOCHB-X) RIDCelkový počet autorů 6 Zdroj.dok. Biochemical Pharmacology. - : Elsevier - ISSN 0006-2952
Roč. 82, č. 2 (2011), s. 131-138Poč.str. 8 s. Jazyk dok. eng - angličtina Země vyd. US - Spojené státy americké Klíč. slova resistance ; acyclic nucleoside phosphonates ; PMEG ; PMEDAP Vědní obor RIV CE - Biochemie CEP 1M0508 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy CEZ AV0Z40550506 - UOCHB-X (2005-2011) UT WOS 000291760700005 DOI 10.1016/j.bcp.2011.04.002 Anotace The ability of a nucleotide analogue PMEG to induce resistance and the mechanisms involved were adressed. CCRF-CEM cells resistant to either PMEG or its congener PMEDAP were assayed for the expression of membrane transporters, PMEG and PMEDAP uptake and metabolism. PMEG phosphorylation to PMEG mono- and diphosphate was completely impaired in resistant cells. Guanylate kinase (GUK) obtained from PMEG-resistant cells revealed two point mutations S(35)N V(168)F that significantly suppressed its catalytic activity. Transfection with wtGUK led to the recovery of phosphorylating activity and sensitivity towards PMEG cytotoxicity. Primary sequence of adenylate kinase (AK) from PMEDAP resistant cells was unaffected. Resistance induced by PMEDAP is thus conferred by other mechanisms. No differences in PMEG uptake have been found between sensitive and resistant cells. GUK was identified as the sole molecular target for the development of resistance to PMEG. Pracoviště Ústav organické chemie a biochemie Kontakt asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Rok sběru 2012
Počet záznamů: 1