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001-es BibID:	BIBFORM004868
035-os BibID:	(scopus)20144375715 (wos)000228111600008
Első szerző:	Horváth András (vegyész)
Cím:	Potent inhibition of HIV-1 entry by (s4dU)35 / Horvath, A., Tokes, S., Hartman, T., Watson, K., Turpin, J. A., Buckheit, R. W., Jr., Sebestyen, Z., Szollosi, J., Benko, I., Bardos, T. J., Dunn, J. A., Fesus, L., D. Toth, F., Aradi, J.
Dátum:	2005
ISSN:	0042-6822
Megjegyzések:	We have previously reported the potent in vitro HIV-1 anti-reverse transcriptase activity of a 35-mer of 4-thio-deoxyuridylate [(s(4)dU)(35)]. In efforts to define its activity in a more physiological system, studies were carried out to determine the stage of viral infection that this compound mediates its anti-viral effect. Results of the studies reported herein show that (s(4)dU)(35) is nontoxic and is capable of inhibiting both single and multi-drug resistant HIV strains (IC(50): 0.8-25.4 microg/ml) in vitro. Besides its previously reported anti-RT activity, (s(4)dU)(35) mediated its antiviral action by preventing virus attachment (IC(50): 0.002-0.003 microg/ml), and was stable in vitro and slowly degraded by DNAses. Competition studies and fluorescence resonance energy transfer (FRET) experiments indicated that (s(4)dU)(35) preferentially binds to CD4 receptors, but not to CD48. Confocal laser scanning microscopy (CLSM) studies showed that (s(4)dU)(35) did not penetrate into the cells and colocalized with cell surface thioredoxin. Our studies identify (s(4)dU)(35) as a potential novel HIV entry inhibitor that may have utility as either a systemic antiretroviral or as a preventing agent for HIV transmission.
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk antagonists and inhibitors Anti-HIV Agents Antigens,CD4 Cell Line Cells chemical synthesis Deoxyuracil Nucleotides drug effects Energy Transfer Fluorescence Fluorescence Resonance Energy Transfer genetics Hela Cells Hiv-1 HIV-1 Reverse Transcriptase Humans Hungary In Vitro metabolism methods Microbial Sensitivity Tests Microscopy Microscopy,Confocal pathogenicity pharmacology Research Reverse Transcriptase Inhibitors Support Thionucleotides toxicity
Megjelenés:	Virology. - 334 : 2 (2005), p. 214-223. -
További szerzők:	Tőkés Szilvia (1964-) (biológus) Hartman, Tracy Watson, Karen Turpin, Jim A. Buckheit, Robert W. Jr. Sebestyén Zsolt Szöllősi János (1953-) (biofizikus) Benkő Ilona (1954-) (orvos, farmakológus) Bardos, Thomas J. Dunn, Joseph A. Fésüs László (1947-) (orvos biokémikus) Tóth Ferenc, D. (1940-2004) (mikrobiológus, élettanász) Aradi János (1942-) (biokémikus, vegyész)
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