Kowalska Joanna, Zuberek Joanna, Darzynkiewicz Zbigniew M, Lukaszewicz Maciej, Darzynkiewicz Edward, Jemielity Jacek
Division of Biophysics, Institute of Experimental Physics, University of Warsaw, 02-089 Warsaw, Poland.
Nucleic Acids Symp Ser (Oxf). 2008(52):289-90. doi: 10.1093/nass/nrn146.
The syntheses of mRNA cap analogs modified with boranophosphate moiety at either the alpha or beta-position of the 5', 5'-triphosphate bridge (m(7)Gppp(BH3)G, m(7)Gpp(BH3)pG and m(7)Gpp(BH3)pm(7)G) are described. The preliminary biological characterization of these compounds revealed that they have high affinity for translational factor eIF4E and high potency to inhibit cap-dependent translation in cell free system. The analogs modified at the beta-position were also found to be resistant to DcpS decapping pyrophosphatase.
描述了在5',5'-三磷酸桥的α或β位用硼磷酸部分修饰的mRNA帽类似物的合成(m(7)Gppp(BH3)G、m(7)Gpp(BH3)pG和m(7)Gpp(BH3)pm(7)G)。这些化合物的初步生物学特性表明,它们对翻译因子eIF4E具有高亲和力,并且在无细胞系统中具有高效抑制帽依赖性翻译的能力。还发现β位修饰的类似物对DcpS去帽焦磷酸酶具有抗性。