A blog about conjugates.
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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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Preferential production of RNA rings by T4 RNA ligase 2 without any splint through rational design of precursor strand
Circular single-stranded RNAs (C-RNAs) are RNA rings without terminals, which are promising for many practical applications both in vivo and in vitro. Recently, for example, thousands of circular RNAs (circRNAs) have been found almost in all kingdom of organisms, and their biological roles as miRNA or RNA inhibitors have been reported. Many circRNAs have also […]
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Design of a substrate-tailored peptiligase variant for the efficient synthesis of thymosin-α1
The manufacture of long peptides using conventional chemical strategies is still very challenging and the technology used has remained almost unchanged since Merrifield developed the solid phase approach in the 1960s. Solid-phase peptide synthesis (SPPS) is characterized by an exponential decrease in the crude yield and purity as the peptide length increases: coupling and deprotection […]
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Peptiligase, an Enzyme for Efficient Chemoenzymatic Peptide Synthesis and Cyclization in Water
There is a large and growing interest in pharmaceutical peptides over the past decades, with about 60 approved peptide drugs currently on the market and some 140 candidates in different phases of clinical development. By 2018, the worldwide peptide drugs market is expected to reach $18 billion. The importance of peptides is also recognized in […]
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