Sixteen different types of lipid-conjugated siRNAs containing saturated and unsaturated fatty acids and exhibiting enhanced RNAi potency

T Kubo, Y Nishimura, Y Sato, K Yanagihara… - ACS chemical …, 2020 - ACS Publications
SiRNAs are strong gene-silencing agents that function in a target sequence-specific
manner. Although siRNAs might one day be used in therapy for intractable diseases such as …

Preparation of Lipid-Conjugated SiRNA Oligonucleotides for Enhanced Gene Inhibition in Mammalian Cells

S Grijalvo, SM Ocampo, JC Perales, R Eritja - Design and Delivery of …, 2021 - Springer
Nucleic acid conjugates are promising drugs for treating gene-related diseases.
Conjugating specific units like lipids, cell-penetrating peptides, polymers, antibodies, and …

The valency of fatty acid conjugates impacts siRNA pharmacokinetics, distribution, and efficacy in vivo

A Biscans, A Coles, D Echeverria… - Journal of controlled …, 2019 - Elsevier
Lipid-conjugated small-interfering RNAs (siRNAs) exhibit accumulation and gene silencing
in extrahepatic tissues, providing an opportunity to expand therapeutic siRNA utility beyond …

Multifunctional pH-sensitive amino lipids for siRNA delivery

M Gujrati, A Vaidya, ZR Lu - Bioconjugate chemistry, 2016 - ACS Publications
RNA interference (RNAi) represents a powerful modality for human disease therapy that can
regulate gene expression signature using small interfering RNA (siRNA). Successful …

Diverse lipid conjugates for functional extra-hepatic siRNA delivery in vivo

A Biscans, A Coles, R Haraszti… - Nucleic acids …, 2019 - academic.oup.com
Small interfering RNA (siRNA)-based therapies are proving to be efficient for treating liver-
associated disorders. However, extra-hepatic delivery remains challenging, limiting …

Combinatorial approach to determine functional group effects on lipidoid-mediated siRNA delivery

KP Mahon, KT Love, KA Whitehead, J Qin… - Bioconjugate …, 2010 - ACS Publications
The application of RNA interference (RNAi), either in the clinic or in the laboratory, requires
safe and effective delivery methods. Here, we develop a combinatorial approach to …

Gene-silencing potency of symmetric and asymmetric lipid-conjugated siRNAs and its correlation with dicer recognition

T Kubo, K Yanagihara, Y Sato, Y Nishimura… - Bioconjugate …, 2013 - ACS Publications
Three types of siRNAs and three types of left-overhang siRNAs (LoRNAs) were synthesized
along with their conjugations with palmitic acid (C16) to investigate the correlation between …

Effective carrier-free gene-silencing activity of sphingosine-modified siRNAs

C Fernandez, I Giorgees, E Goss… - Organic & Biomolecular …, 2023 - pubs.rsc.org
RNA interference (RNAi) is a natural cellular process that silences the expression of target
genes in a sequence-specific way by mediating targeted mRNA degradation. One of the …

[HTML][HTML] Engineered ionizable lipid siRNA conjugates enhance endosomal escape but induce toxicity in vivo

A Biscans, S Ly, N McHugh, DA Cooper… - Journal of Controlled …, 2022 - Elsevier
Lipid conjugation supports delivery of small interfering RNAs (siRNAs) to extrahepatic
tissues, expanding the therapeutic potential of siRNAs beyond liver indications. However …

Carrier-free cellular uptake and the gene-silencing activity of the lipophilic siRNAs is strongly affected by the length of the linker between siRNA and lipophilic group

NS Petrova, IV Chernikov… - Nucleic acids …, 2012 - academic.oup.com
The conjugation of siRNA to molecules, which can be internalized into the cell via natural
transport mechanisms, can result in the enhancement of siRNA cellular uptake. Herein, the …