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Aptamer displacement identifies alternative small molecule target sites that escape viral resistance

Aptamer displacement identifies alternative small molecule target sites that escape viral resistance

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Prüfsumme: MD5:851f62dfd57d0b121be3b396e46c84c2

YAMAZAKI, Satoko, Lu TAN, Günter MAYER, Jörg HARTIG, Jin-Na SONG, Sandra REUTER, Tobias RESTLE, Sandra D. LAUFER, Dina GROHMANN, Hans-Georg KRÄUSSLICH, Jürgen BAJORATH, Michael FAMULOK, 2007. Aptamer displacement identifies alternative small molecule target sites that escape viral resistance. In: Chemistry & Biology. 14(7), pp. 804-812. ISSN 1074-5521. Available under: doi: 10.1016/j.chembiol.2007.06.003

@article{Yamazaki2007-07Aptam-15623, title={Aptamer displacement identifies alternative small molecule target sites that escape viral resistance}, year={2007}, doi={10.1016/j.chembiol.2007.06.003}, number={7}, volume={14}, issn={1074-5521}, journal={Chemistry & Biology}, pages={804--812}, author={Yamazaki, Satoko and Tan, Lu and Mayer, Günter and Hartig, Jörg and Song, Jin-Na and Reuter, Sandra and Restle, Tobias and Laufer, Sandra D. and Grohmann, Dina and Kräusslich, Hans-Georg and Bajorath, Jürgen and Famulok, Michael} }

2011-10-10T09:12:36Z Hartig, Jörg 2007-07 Aptamers targeting reverse transcriptase (RT) from HIV-1 inhibit viral replication in vitro, presumably by competing with binding of the primer/template complex. This site is not targeted by the currently available small-molecule anti-HIV-1 RT inhibitors. We have identified SY-3E4, a small-molecule inhibitor of HIV-1 RT, by applying a screening assay that utilizes a reporter-ribozyme regulated by the anti-HIV-1 RT aptamer. SY-3E4 displaces the aptamer from the protein, selectively inhibits DNA-dependent, but not RNA-dependent, polymerase activity, and inhibits the replication of both the wild-type virus and a multidrug-resistant strain. Analysis of available structural data of HIV-1 and HIV-2 RTs rationalizes many of the observed characteristics of the inhibitory profiles of SY-3E4 and the aptamer and suggests a previously not considered region in these RTs as a target for antiviral therapy. Our study reveals unexplored ways for rapidly identifying alternative small-molecule target sites in proteins and illustrates strategies for overcoming resistance-conferring mutations with small molecules. Grohmann, Dina Reuter, Sandra Reuter, Sandra Bajorath, Jürgen Restle, Tobias Famulok, Michael Hartig, Jörg Song, Jin-Na eng Famulok, Michael Laufer, Sandra D. Yamazaki, Satoko Laufer, Sandra D. deposit-license Mayer, Günter Chemistry & Biology ; 14 (2007), 7. - pp. 804-812 Tan, Lu 2011-10-10T09:12:36Z Grohmann, Dina Bajorath, Jürgen Mayer, Günter Yamazaki, Satoko Kräusslich, Hans-Georg Restle, Tobias Kräusslich, Hans-Georg Aptamer displacement identifies alternative small molecule target sites that escape viral resistance Tan, Lu Song, Jin-Na

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