Peptide synthesis has been developed into one of the most efficient synthetic procedures in organic chemistry. The problems of orthogonal functional group protection and amide bond formation without racemization have been developed in a number of ingenious strategies. Optimization, in particular, has been achieved in stepwise solid phase synthesis. This in turn made possible the development of ...

  Introduction: It has been shown that some primary human tumors and their metastases, including prostate and breast tumors, over-express gastrin-releasing peptide (GRP) receptors. Bombesin is a neuropeptide with a high affinity for these GRP receptors. The purpose of this study was to prepare and evaluate the characteristics of a new Freeze-dried kit, [6-hydrazinopyr...

The observation that thyroxine stimulated in vitro protein synthesis in the absence of mitochondria (Carter, W.J., Faas, F.H., and Wynn, J (1971) J. Biol. Chem. 246, 4973-4977) has been disputed on the basis that radioactivity incorporated into protein did not represent peptide synthesis but incorporation of labeled contaminants present in the L-(U-14C) valine precursor (Sokoloff, L., and Rober...

Despite the great advances in solid-phase peptide synthesis (SPPS), incorporation of certain functional groups into sequences is restricted by compatibility building blocks with conditions used during SPPS. In particular, introduction highly reactive modern bioorthogonal reactions peptides remains elusive. Here, we present an optimized synthetic protocol enabling installation two strained dieno...

In the course of a study in protease-controlled peptide synthesis, several promising pathways to synthetic enkephalins had to be discarded or modified because they failed to give the required products. Partial deprotection of peptide fragments prior to chain elongation resulted in an enhanced susceptibility of scissile bonds to proteolysis. The use of proteases, the specificity of which was not...

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...

This communication reports a new technology platform that advantageously combines organic solvent nanofiltration (a newly emerging technology capable of molecular separations in organic solvents) with solution phase peptide synthesis-Membrane Enhanced Peptide Synthesis (MEPS).