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Lipid and Carbohydrate Modifications Enhance Potency of Antisense Oligonucleotides Targeting Oncogenic KRAS

One prominent open question in the field of antisense oligonucleotide remains the intracellular delivery of active sequences. While different strategies have been developed for addressing this issue, including formulation and/or conjugation approaches, multiconjugations with both sugars and nucleolipids have not been investigated so far. In this contribution, we are interested in a new hypothesis that focuses on the double conjugation of oligonucleotides with both glucose-thymine and nucleolipid moieties. The lipid carbohydrate modified antisense oligonucleotides were the most efficient in down regulating the expression of KRAS in pancreatic cancer cells.

Abstract Image

Référence

Faith Kivunga, Virginie Baylot, Julien Verget, Helene Pereira, Brune Vialet, Patricia Korczak, Jean Dessolin and Philippe Barthélémy Bioconjugate Chem. 2026, 37, 5, 875–880 https://doi.org/10.1021/acs.bioconjchem.5c00627

Poster Price

Mathias Brouillard, 2nd year PhD., was awarded by the SCT (Société de Chimie Thérapeutique) for his poster entitled : SYNTHESIS AND FORMULATION OF ACID BASED NUCLEOLIPIDS FOR NEURODEGENERATIVE DISEASES at the international conference RICT 2021, Interfacing Chemical Biology and Drug Discovery, 56th International Conference on Medicinal Chemistry.

Congratulations to him.

Guest Editors

Tina Kauss and Philippe Barthélémy are the Guest Editors of the Pharmaceutics (IF 6.321) Special Issue on Oligonucleotides and Nucleic-Acid-Based Strategies to Address Therapeutic Challenges: From the Bench to the Bedside

The deadline for online submission is 20 November 2021.

Sylvie Crauste-Manciet is the Guest Editors of the Pharmaceutics (IF 6.321) Special Issue Nanoemulsions for drug delivery.
The deadline for online submission is 30 April 2022