Generation and Characterization of a DNA-GCN4 Oligonucleotide-Peptide Conjugate: The Impact DNA/Protein Interactions on the Sensitization of DNA [PDF]
Radiotherapy, the most common therapy for the treatment of solid tumors, exerts its effects by inducing DNA damage. To fully understand the extent and nature of this damage, DNA models that mimic the in vivo situation should be utilized.
Paweł Wityk +3 more
doaj +5 more sources
2025 FDA TIDES (Peptides and Oligonucleotides) Harvest [PDF]
In 2025, the FDA approved 46 novel drugs, including four TIDEs (one peptide, three oligonucleotides, and one antibody drug conjugate containing peptide as a payload). The three approved oligonucleotide therapeutics—fitusiran, donidalorsen, and plozasiran—
Danah AlShaer +3 more
doaj +2 more sources
IGF1R-targeted delivery of a bridged nucleic acid oligonucleotide-peptide conjugate for microRNA-21 inhibition in triple-negative breast cancer. [PDF]
AbstractTriple-negative breast cancer (TNBC), defined by the absence of ER, PR, and Her2, impacts over 46,000 U.S. women annually, disproportionately affecting minority ethnic groups and individuals with BRCA1 mutations. Despite advancements such as PARP inhibitors, TNBC remains highly aggressive, with frequent recurrences and a 50% mortality rate ...
Jin Y +3 more
europepmc +3 more sources
Fluorescence Imaging of Extracellular Potassium Ion Using Potassium Sensing Oligonucleotide
Potassium-sensing oligonucleotide, PSO, a conjugate of a quadruplex structure-forming oligonucleotide with a peptide incorporating a Förster Resonance Energy Transfer (FRET) chromophore pair, has been developed for fluorescent detection of potassium ion (
Shinobu Sato +8 more
doaj +1 more source
Currently, oligonucleotide therapy has emerged as a new paradigm in the treatment of human diseases. In many cases, however, therapeutic oligonucleotides cannot be used directly without modification.
Irina V. Varizhuk +6 more
doaj +1 more source
A Review of Protein- and Peptide-Based Chemical Conjugates: Past, Present, and Future
Over the past few decades, the complexity of molecular entities being advanced for therapeutic purposes has continued to evolve. A main propellent fueling innovation is the perpetual mandate within the pharmaceutical industry to meet the needs of novel ...
Emily Holz +3 more
doaj +1 more source
Modular Synthesis of Trifunctional Peptide-oligonucleotide Conjugates via Native Chemical Ligation
Cell penetrating peptides (CPPs) are being increasingly used as efficient vectors for intracellular delivery of biologically active agents, such as therapeutic antisense oligonucleotides (ASOs).
Mohadeseh Dastpeyman +5 more
doaj +1 more source
Oligonucleotide‐peptide conjugates as potential antisense agents [PDF]
Oligonucleotide‐peptide conjugates have several applications, including their potential use as improved antisense agents for interfering with the RNA function within cells. In order to provide robust and generally applicable conjugation chemistry, we developed a novel approach of fragment coupling of pre‐synthesized peptides to the 2′‐position of a ...
Zubin, Eugeny M +6 more
openaire +2 more sources
The blood-brain barrier (BBB) hinders the distribution of therapeutics intended for treatment of neuroinflammation (NI) of the central nervous system. A twelve-amino acid peptide that transcytoses the BBB, termed MTfp, was chemically conjugated to siRNA ...
Brett A. Eyford +42 more
doaj +1 more source
New developments in the synthesis of oligonucleotide-peptide conjugates [PDF]
The stability of oligodeoxynucleotides to trifluoroacetic acid is studied. Pyrimidine oligonucleotides were stable in the conditions used for the removal of t-butyl groups. Oligonucleotide-3'-peptide conjugates carrying pyrimidine oligonucleotides are prepared stepwise using peptide-supports and Fmoc, t-butyl strategy.
C. Portela +7 more
openaire +4 more sources

