Mechanistic Basis for Ribosomal Peptide Backbone Modifications [PDF]
ACS Central Science, 2019 YcaO enzymes are known to catalyze the ATP-dependent formation of azoline heterocycles, thioamides, and (macro)lactamidines on peptide substrates. These enzymes are found in multiple biosynthetic pathways, including those for several different classes of ribosomally synthesized and post-translationally modified peptides (RiPPs).
Shi-Hui Dong +4 more
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Peptide backbone modifications of amyloid β (1–40) impact fibrillation behavior and neuronal toxicity [PDF]
Scientific Reports, 2021 Fibril formation of amyloid β (Aβ) peptides is one of the key molecular events connected to Alzheimer’s disease. The pathway of formation and mechanism of action of Aβ aggregates in biological systems is still object of very active research. To this end,
Benedikt Schwarze +6 more
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Insightful Backbone Modifications Preventing Proteolytic Degradation of Neurotensin Analogs Improve NTS1-Induced Protective Hypothermia [PDF]
Frontiers in Chemistry, 2020 Therapeutic hypothermia represents a brain-protective strategy for multiple emergency situations, such as stroke or traumatic injury. Neurotensin (NT), which exerts its effects through activation of two G protein-coupled receptors, namely NTS1 and NTS2 ...
Santo Previti +8 more
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Hydrogen Bond and Geometry Effects of Thioamide Backbone Modifications. [PDF]
J Org Chem, 2021 Thioamide substitution of backbone peptide bonds can probe interactions along the main chain of proteins. Despite theoretical predictions of the enhanced hydrogen bonding propensities of thioamides, previous studies often do not consider the geometric constraints imposed by folded peptide secondary structure.
Lampkin BJ, VanVeller B.
europepmc +3 more sources
Phosphorothioate backbone modifications of nucleotide-based drugs are potent platelet activators. [PDF]
J Exp Med, 2015 Nucleotide-based drug candidates such as antisense oligonucleotides, aptamers, immunoreceptor-activating nucleotides, or (anti)microRNAs hold great therapeutic promise for many human diseases.
Flierl U +15 more
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Influence of Combinations of Lipophilic and Phosphate Backbone Modifications on Cellular Uptake of Modified Oligonucleotides [PDF]
MoleculesNumerous types of oligonucleotide modifications have been developed since automated synthesis of DNA/RNA became a common instrument in the creation of synthetic oligonucleotides.
Timofey D. Zharkov +4 more
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Structural dynamics of therapeutic nucleic acids with phosphorothioate backbone modifications. [PDF]
NAR Genom BioinformAbstract Antisense oligonucleotides (ASOs) offer ground-breaking possibilities for selective pharmacological intervention for any gene product-related disease. Therapeutic ASOs contain extensive chemical modifications that improve stability to enzymatic cleavage and modulate binding affinity relative to natural RNA/DNA.
Carlesso A +4 more
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A Long‐Term Human Liver Spheroid Model for Assessing Silencing and Durability of GalNAc‐Conjugated siRNAs [PDF]
Clinical and Translational ScienceAdvances in RNA interference technology have established it as a powerful therapeutic tool with important future potential. The design and the chemical modifications of the siRNA nucleotide backbone have greatly enhanced stability, durability, and ...
Gijs‐Jan Scholten +8 more
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Site-selective modification of peptide backbones
Organic Chemistry Frontiers, 2021 Exciting developments in the site-selective modification of peptide backbones are allowing an outstanding fine-tuning of peptide conformation, folding ability, and physico-chemical and biological properties.
Alicia Boto +4 more
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Beilstein Journal of Organic Chemistry, 2021 Antisense oligonucleotides (ASOs) have the ability of binding to endogenous nucleic acid targets, thereby inhibiting the gene expression. Although ASOs have great potential in the treatment of many diseases, the search for favorable toxicity profiles and
Mathias B. Danielsen, Jesper Wengel
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