کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1375285 | 981936 | 2009 | 5 صفحه PDF | دانلود رایگان |
We report synthesis and properties of a pair of new potent inhibitors of translation, namely two diastereomers of 7-methylguanosine 5′-(1-thiotriphosphate). These new analogs of mRNA 5′cap (referred to as m7GTPαS (D1) and (D2)) are recognized by translational factor eIF4E with high affinity and are not susceptible to hydrolysis by Decapping Scavenger pyrophosphatase (DcpS). The more potent of diastereomers, m7GTPαS (D1), inhibited cap-dependent translation in rabbit reticulocyte lysate ∼8-fold and ∼15-fold more efficiently than m7GTP and m7GpppG, respectively. Both analogs were also significantly more stable in RRL than unmodified ones.
The synthesis and properties of new potent inhibitors of translation, two diastereomers of 7-methylguanosine 5′-(1-thiotriphosphate), are reported. These analogs of mRNA 5′cap are recognized by translational factor eIF4E with high affinity and are resistant to hydrolysis by Decapping Scavenger pyrophosphatase.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 7, 1 April 2009, Pages 1921–1925