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Isoxazole-containing 5′ mRNA cap analogues as inhibitors of the translation initiation process

Journal

BIOORGANIC CHEMISTRY
Volume 96, Issue -, Pages -

Publisher

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.103583

Keywords

Cap analogue; mRNA; Translation initiation; Isoxazol; Cycloaddition reaction

Funding

  1. National Science Centre, Poland [2016/21/D/ST501654, 2018/31/B/ST5/03544, 2013/08/A/NZ1/00866]

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Herein we describe a synthesis of new isoxazole-containing 5' mRNA cap analogues via a cycloaddition reaction. The obtained analogues show a capability to inhibit cap-dependent translation in vitro and are characterized by a new binding mode in which an isoxazolic ring, instead of guanine, is involved in the stacking effect. Our study provides valuable information toward designing new compounds that can be potentially used as anticancer therapeutics.

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