A blog about conjugates.
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Cell cycle arrest through indirect transcriptional repression by p53: I have a DREAM
Activation of the p53 tumor suppressor can lead to cell cycle arrest. The key mechanism of p53-mediated arrest is transcriptional downregulation of many cell cycle genes. In recent years it has become evident that p53-dependent repression is controlled by the p53-p21-DREAM-E2F/CHR pathway (p53-DREAM pathway). DREAM is a transcriptional repressor that binds to E2F or CHR…
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Mechanism of DNA Binding and Cleavage
The necessity for cellular regulation of DNA led to the development of metallonucleases to catalyze and repair DNA strand breaks. Due to cationic character, three-dimensional structural profiles, and propensity for performing hydrolysis, redox, or photoreactions of metal ions and complexes, have a natural ability for interacting with DNA. Since binding and cleavage of DNA is…
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G-Quadruplexes in Nuclear Biomolecular Condensates
G-quadruplexes (G4s) have long been implicated in the regulation of chromatin packaging and gene expression. These processes require or are accelerated by the separation of related proteins into liquid condensates on DNA/RNA matrices. While cytoplasmic G4s are acknowledged scaffolds of potentially pathogenic condensates, the possible contribution of G4s to phase transitions in the nucleus has…
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Cyclodipeptides: From Their Green Synthesis to Anti-Age Activity
Cyclodipeptides (CDPs) or 2,5-diketopiperazines (DKPs) are naturally occurring biomolecules that have increasingly attracted researchers’ attention for a variety of reasons, as evident from the many recent reviews that cover aspects ranging from their sustainable production via enzymatic catalysis to all the possible methods for their preparation and self-assembly into gels and their biological activities, including…
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Gemdimethyl Peptide Nucleic Acids (α/β/γ-gdm-PNA): E/Z-Rotamers Influence the Selectivity in the Formation of Parallel/Antiparallel gdm-PNA:DNA/RNA Duplexes
Peptide nucleic acids (PNAs) consist of an aminoethylglycine (aeg) backbone to which the nucleobases are linked through a tertiary amide group and bind to complementary DNA/RNA in a sequence-specific manner. The flexible aeg backbone has been the target for several chemical modifications of the PNA to improve its properties such as specificity, solubility, etc. PNA monomers exhibit…
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Novel branched amphiphilic peptides for nucleic acids delivery
Branched peptides are a new type of peptide-based nucleic acid delivery vectors. It has been reported that branched and dendrimeric cationic peptides have better transfection efficiencies than linear peptides due to their superior capacity for DNA condensation (Ageitos et al., 2015, Luo et al., 2011). Ageitos et al. synthesized linear cationic peptides and branched cationic peptide…
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Disulfide based prodrugs for cancer therapy
Advances in the tumor microenvironment have facilitated the development of novel anticancer drugs and delivery vehicles for improved therapeutic efficacy and decreased side effects. Disulfide bonds with unique chemical and biophysical properties can be used as cleavable linkers for the delivery of chemotherapeutic drugs. Accordingly, small molecule-, peptide-, polymer- and protein-based multifunctional prodrugs bearing cleavable…
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SPARC: a key player in the pathologies associated with obesity and diabetes
SPARC (secreted protein acidic and rich in cysteine, also known as osteonectin or BM-40) is a widely expressed profibrotic protein with pleiotropic roles, which have been studied in a variety of conditions. Notably, SPARC is linked to human obesity; SPARC derived from adipose tissue is associated with insulin resistance and secretion of SPARC by adipose…
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Proteolytic Characteristics of Cathepsin D Related to the Recognition and Cleavage of Its Target Proteins
Cathepsin D (CD) plays an important role in both biological and pathological processes, although the cleavage characteristics and substrate selection of CD have yet to be fully explored. We employed liquid chromatography-tandem mass spectrometry (LC-MS/MS) to identify the CD cleavage sites in bovine serum albumin (BSA). We found that the hydrophobic residues at P1 were…
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The Discovery and Development of Liraglutide and Semaglutide
The discovery of glucagon-like peptide-1 (GLP-1), an incretin hormone with important effects on glycemic control and body weight regulation, led to efforts to extend its half-life and make it therapeutically effective in people with type 2 diabetes (T2D). The development of short- and then long-acting GLP-1 receptor agonists (GLP-1RAs) followed. Our article charts the discovery…
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