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001-es BibID:	BIBFORM067230
035-os BibID:	(Cikkazonosító)41376 (WOS)000393137000001 (Scopus)85011264087
Első szerző:	Tarapcsák Szabolcs (Molekuláris biológus)
Cím:	Interactions of retinoids with the ABC transporters P-glycoprotein and Breast Cancer Resistance Protein / Szabolcs Tarapcsák, Gábor Szalóki, Ágnes Telbisz, Zsuzsanna Gyöngy, Krisztina Matúz, Éva Csősz, Péter Nagy, Imre J. Holb, Ralph Rühl, László Nagy, Gábor Szabó, Goda Katalin
Dátum:	2017
ISSN:	2045-2322
Megjegyzések:	Retinoids - derivatives of vitamin A - are important cell permeant signaling molecules that regulate gene expression through activation of nuclear receptors. P-glycoprotein (Pgp) and ABCG2 are plasma membrane efflux transporters affecting the tissue distribution of numerous structurally unrelated lipophilic compounds. In the present work we aimed to study the interaction of the above ABC transporters with retinoid derivatives. We have found that 13-cis-retinoic acid, retinol and retinyl-acetate inhibited the Pgp and ABCG2 mediated substrate transport as well as the substrate stimulated ATPase activity of these transporters. Interestingly, 9-cis-retinoic acid and ATRA (all-trans retinoic acid), both are stereoisomers of 13-cis-retinoic acid, did not have any effect on the transporters' activity. Our fluorescence anisotropy measurements revealed that 13-cis-retinoic acid, retinol and retinyl-acetate selectively increase the viscosity and packing density of the membrane. Thus, the mixed-type inhibition of both transporters by retinol and ABCG2 by 13-cis-retinoic acid may be the collective result of direct interactions of these retinoids with the substrate binding site(s) and of indirect interactions mediated by their membrane rigidifying effects.
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk retinoid derivatives P-glycoprotein ABCG2 ABC transporter membrane fluidity intramembrane localization
Megjelenés:	Scientific Reports. - 7 : 41376 (2017), p. 1-31. -
További szerzők:	Szalóki Gábor (1986-) (molekuláris biológus) Telbisz Ágnes Gyöngy Zsuzsanna (1991-) (molekuláris biológus) Matúz Krisztina (1980-) (vegyész, biokémikus) Csősz Éva (1977-) (biokémikus, molekuláris biológus) Nagy Péter (1971-) (biofizikus) Holb Imre (1973-) (agrármérnök) Rühl, Ralph (1969-) (vegyész) Nagy László (1966-) (molekuláris sejtbiológus, biokémikus) Szabó Gábor (1953-) (biofizikus) Goda Katalin (1969-) (biofizikus)
Internet cím:	DOI Intézményi repozitóriumban (DEA) tárolt változat
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001-es BibID:	BIBFORM043017
035-os BibID:	PMID:22115866
Első szerző:	Telbisz Ágnes
Cím:	Antibody binding shift assay for rapid screening of drug interactions with the human ABCG2 multidrug transporter / Ágnes Telbisz, Csilla Hegedüs, Csilla Özvegy-Laczka, Katalin Goda, György Várady, Zoltán Takáts, Eszter Szabó, Brian P. Sorrentino, András Váradi, Balázs Sarkadi
Dátum:	2012
Megjegyzések:	The ABCG2 multidrug transporter protein has been identified as a key player in cancer drug resistance and xenobiotic elimination, as its actively transported substrates include anticancer drugs, intermediates of heme metabolism, xenobiotics, and also drug conjugates. Several transported substrates at higher concentrations, and some anticancer agents even at low concentrations directly inhibit the ABCG2 transporter, thus it is difficult to provide estimation for pharmacologically important ABCG2-dependent interactions. In addition, as documented here, in mutant variants of the transporter, inhibitors of the wild-type ABCG2 may become actively transported substrates. In this paper we describe a rapid in vitro assay to identify transport modulation by measuring the cell surface interaction of a conformation sensitive monoclonal antibody (5D3) with ABCG2 in intact cells. As documented, in conjunction with membrane ATPase, transport and cytotoxicity measurements, this assay provides a reliable estimate of concentration-dependent modulation of ABCG2 by newly emerging pharmacophores. A high-throughput, 96-well plate assay platform is also provided
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban antagonists & inhibitors Antibodies Antibodies,Monoclonal Antigen-Antibody Reactions Antineoplastic Agents article ATP-Binding Cassette Transporters Biophysics blood Cell Line,Tumor cell surface Cells Drug Discovery drug effects Drug Interactions Drug Resistance Drug Resistance,Neoplasm genetics High-Throughput Screening Assays Human Humans Hungary In Vitro ligand Ligands Membrane Transport Modulators metabolism methods monoclonal antibody Mutant Proteins Neoplasm Proteins Osmolar Concentration pharmacology Proteins Recombinant Proteins Research Research Support Support Xenobiotics egyetemen (Magyarországon) készült közlemény
Megjelenés:	European Journal of Pharmaceutical Sciences. - 45 : 1-2 (2012), p. 101-109. -
További szerzők:	Hegedűs Csilla Özvegy-Laczka Csilla Goda Katalin (1969-) (biofizikus) Várady György Takáts Zoltán Szabó Eszter Sorrentino, Brian P. Váradi András Sarkadi Balázs
Internet cím:	DOI Intézményi repozitóriumban (DEA) tárolt változat
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