Protein chemical synthesis offers useful and otherwise-difficulty-to-obtain biomacromolecules for biological and pharmaceutical studies. Recently, the hydrazide chemistry has drawn attentions in this field as peptide or protein hydrazides can be used as key intermediates for different synthesis and modification purposes. Besides being a traditional bioorthogonal chemical handle, a hydrazide gro...

Chronic HBV infection is the leading cause of liver cirrhosis and hepatocellular carcinoma (HCC). Synthetic peptides derived from the N-terminus of the large HBV envelope protein (L-protein) have been shown to efficiently block HBV entry. Myr-HBVpreS/2-78, the parent compound of these drugs, inhibits human HBV infection in vitro and in vivo. An efficient synthesis is required, as these peptides...

A functional interaction between the signal sequence and the translation apparatus which may serve as a first step in chain targeting to the membrane is described. To this end, we exploited the powerful technique of molecular cloning in a procaryotic system and the well characterized translocation system of mammalian endoplasmic reticulum. The signal peptide of subunit B of the heat labile ente...

The total chemical synthesis of proteins is a tedious and time-consuming endeavour. The typical steps involve solid phase synthesis of peptide thioesters and cysteinyl peptides, native chemical ligation (NCL) in solution, desulfurization or removal of ligation auxiliaries in the case of extended NCL as well asmany intermediary and final HPLC purification steps. With an aim to facilitate and imp...

The total chemical synthesis of proteins is a tedious and time-consuming endeavour. The typical steps involve solid phase synthesis of peptide thioesters and cysteinyl peptides, native chemical ligation (NCL) in solution, desulfurization or removal of ligation auxiliaries in the case of extended NCL as well as many intermediary and final HPLC purification steps. With an aim to facilitate and im...

Antibiotic U-22,324 is a polypeptide produced by the fungus Trichoderma viride. Cycloheximide was found to block gross cellular protein synthesis of T. viride with little interference with antibiotic synthesis. No radioactive label was recovered in the ribosomes when labeled amino acids and cycloheximide were added to a culture at the onset of peptide synthesis although net antibiotic synthesis...

Novel photolabile amino acid monomers for photolithographic solid-phase peptide synthesis has been developed and a method for the maskless synthesis of individually addressable peptide microarrays using new building blocks has been described; these peptide microarrays are suitable for repetitive epitope-binding assays.

The potential of “customizable units” to generate structural diversity for biological screenings is highlighted in this proof-of-concept synthesis new peptides related the potent antitumoral Sansalvamide A. Using L-4-hydroxyproline (Hyp) as a customizable unit linear parent peptide, an improved procedure selective peptide modification was developed. A divergent Hyp scission-reductive amination ...

Repeated hourly stimulation of perfused rabbit hydronephrotic kidney (HNK) with a fixed dose of bradykinin resulted in a progressive (to-fold in 6 h) increase in prostaglandin (PG) synthesis. Inhibition of protein synthesis with cycloheximide during perfusion abolished the enhanced time-dependent responsiveness of the HNK to peptide stimulation, whereas pretreatment of rabbits with aspirin, whi...

It is shown that for carboxypeptidase Y catalyzed peptide synthesis the coupling yields using peptide esters as substrates and amino acids as nucleophiles are strongly dependent on the C-terminal amino acid residue. A dependence on the length of the acyl donating peptide chain is also observed, indicating the influence of residues other than the one directly involved in acylation of the enzyme....