The first total synthesis of Rolloamide B, a cyclic proline-enriched heptapeptide, is reported. This work features solution phase benzotriazole-mediated peptide synthesis ligating native amino acids.

Segment condensations were performed to construct peptide fragments related to Sulfolobus solifataricus Ribonuclease. At each condensation step, the new protecting groups were stable. The protected peptide fragments were treated with a low-high HF procedure to give the desired peptide fragments. These peptide fragments were also prepared by the solid-phase method, and the obtained peptides were...

Peptide-oligonucleotide conjugates (POCs) represent one of the increasingly successful albeit costly approaches to increasing cellular uptake, tissue delivery, bioavailability, and, thus, overall efficiency therapeutic nucleic acids, such as, antisense oligonucleotides and small interfering RNAs. This review puts subject chemical synthesis POCs into wider context problem acid drug cell-penetrat...

A simple acid-resistant hydrophobic tag, which can be removed rapidly in a single-step procedure after overall peptide synthesis, has been developed to accomplish practical solution-phase synthesis of a 15-mer antagonistic peptide of TNF-α (A-TNF-α). Hydrophobically tagged peptides can be separated as precipitates at each step by addition of a polar organic solvent.

Propargyl esters are employed as effective protecting groups for the carboxyl group during solution-phase peptide synthesis. The propargyl ester groups can be introduced onto free amino acids by treating them with propargyl alcohol saturated with HCl. The reaction between propargyl groups and tetrathiomolybdate is exploited to deblock the propargyl esters. The removal of the propargyl group wit...

An efficient approach for the synthesis of norbuprenorphin derivatives through coupling of enkephalins and norbuprenorphine intermediate is described. Norbuprenorphine derivative was synthesized from thebaine and then, its reaction with succinic acid and phthalic acid was also studied. Meanwhile, the synthesis of enkephalins was done using solid phase peptide synthesis approach. Furthermore, af...

introduction: bombesin (bn), a 14-amino acid neuropeptide, shows high affinity for the human grp (gastrin releasing peptide) receptors, which are overexpressed by a variety of cancers, including prostate, breast, pancreas, gastrointestinal, and small cell lung cancer. aim was to prepare [6-hydrazinopyridine-3-carboxylic acid (hynic0), d-tyr6, d-trp8] - bn [6-14] nh2 that could be easily labeled...

An efficient approach for the synthesis of norbuprenorphin derivatives through coupling of enkephalins and norbuprenorphine intermediate is described. Norbuprenorphine derivative was synthesized from thebaine and then, its reaction with succinic acid and phthalic acid was also studied. Meanwhile, the synthesis of enkephalins was done using solid phase peptide synthesis approach. Furthermore, af...