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Targeting the SARS-CoV-2 RNA Genome with Small Molecule Binders and Ribonuclease Targeting Chimera (RIBOTAC) Degraders

Hafeez S. Haniff, Yuquan Tong, Xiaohui Liu, Jonathan L. Chen, Blessy M. Suresh, Ryan J. Andrews, Jake M. Peterson, Collin A. O’Leary, Raphael I. Benhamou, Walter N. Moss, Matthew D. Disney

2020ACS Central Science212 citationsDOIOpen Access PDF

Abstract

) that validated direct target engagement and demonstrated its specificity for the viral RNA, as compared to highly expressed host mRNAs. The RIBOTAC lead optimization strategy improved the bioactivity of the compound at least 10-fold. Collectively, these studies demonstrate that the SARS-CoV-2 RNA genome should be considered druggable.

Topics & Concepts

RNARibonucleaseDruggabilitySmall moleculeGenomeComputational biologyChimera (genetics)BiologyRibonuclease IIIChemistryPolyadenylationCell biologyGeneticsRNA interferenceGeneSARS-CoV-2 and COVID-19 Researchinterferon and immune responsesViral Infections and Immunology Research
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