A blog about conjugates.
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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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A traceless linker for aliphatic aminesA traceless linker for aliphatic amines
Reduction sensitive linkers (RSLs) have the potential to transform the field of drug delivery due to their ease of use and selective cleavage in intracellular environments. However, despite their compelling attributes, developing reduction sensitive self-immolative linkers for aliphatic amines has been challenging due to their poor leaving group ability and high pKa values. Here a traceless…
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Perspectives in Peptide-Based Vaccination Strategies
Peptide-Based Vaccines in Diseases An innovative approach is represented by peptide-based prototypes (Skwarczynski and Toth, 2016; Malonis et al., 2020) that are often able to overcome disadvantages encountered by other strategies as a more safe profile since for easiness of purification (Marasco et al., 2008; Marasco and Scognamiglio, 2015). Their chemical synthesis renders them suitable for large…
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Peptides as Pharmacological Carriers to the Brain: Promises, Shortcomings and Challenges
Central nervous system (CNS) diseases are among the most difficult to treat, mainly because the vast majority of the drugs fail to cross the blood-brain barrier (BBB) or to reach the brain at concentrations adequate to exert a pharmacological activity. The obstacle posed by the BBB has led to the in-depth study of strategies allowing…
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