Phosphorothioate Analogs OF 2-5A: Activation / Inhibition of Rnase L and Inhibition of HIV-1 Reverse Transcriftase |
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Authors: | Robert J Suhadolnik Bernard Lebleu Wolfgang Pfleiderer Ramamurthy Charubala David C Montefiori William M Mitchell |
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Institution: | 1. Temple University School of Medicine, Philadelphia, Pennsylvania, USA;2. Université de Montpellier, Montpellier, France;3. Universit?t Konstanz, Konstanz, Germany;4. Vanderbilt University School of Medicine , Nashville, Tennessee, USA |
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Abstract: | Abstract Chemically and enzymatically synthesizeddiastereomeric 2′,5′- phosphorothioate dimer, trimer and tetramer cores and their 5′ - mono- and triphosphates demonstrate marked differences in their ability to bind to and activate RNase L from L929 cell extracts in radiobinding, core-cellulose and rRNA cleavage assays1,2 (Fig. 1). These are the first 2-5A cores that are able to bind to and activate Mase L. The enzymatically synthesized 2′,5′- phosphorothioate dimer and trimer 5′-triphosphates can also bind to and activate mase L1. |
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