Technologies to enable Aqueous Solid-Phase Peptide Synthesis (ASPPS).

The benzyloxycarbonyl (Z-) residue, an important protecting group in peptide synthesis, was introduced into the input data set o f the “Empirical Conformational Energy Program for Peptides” (ECEPP) developed by Scheraga and coworkers. With additional modifications ECEPP is now prepared for conformational analysis o f peptides containing this amino end group. Preferred conformations o f the Z-re...

The ability to speed up conventional Fmoc solid-phase peptide synthesis (SPPS) has many advantages including increased productivity. One way to speed up conventional Fmoc SPPS is the choice of activator. Recently, several new activators have been introduced into the market, and they were evaluated along with some older activators for their ability to synthesize a range of peptides with shorter ...

Key words phosphoric acid - deprotection tert-butoxycarbonyl group peptide synthesis

Objective(s): Peptide Receptor Radionuclide Therapy (PRRT) with yttrium-90 (90Y) and lutetium-177 (177Lu)-labelled SST analogues are now therapy option for patients who have failed to respond to conventional medical therapy. In-house production with automated PRRT synthesis systems have clear advantages over manual methods resulting in increasing use in hospital-based radiopharmacies. We report...

  Introduction: Radioimmunotherapy (RIT) is a very promising new therapy for the treatment of recurrent B-Cell non-Hodgkin's lymphoma (NHL). Iodine-131 is the most frequently used nuclide in clinical RIT, but its usefulness has been limited by dehalogenation of monoclonal antibodies labeled via conventional methods. To circumvent this problem, we have synthesized a tr...

Solid phase peptide synthesis method, which was introduced by Merrifield in 1963, has spawned the concept of combinatorial chemistry. In this review, we summarize the present technologies of solid phase peptide synthesis (SPPS) that are related to combinatorial chemistry. The conventional methods of peptide library synthesis on polymer support are parallel synthesis, split and mix synthesis and...

introduction: radioimmunotherapy (rit) is a very promising new therapy for the treatment of recurrent b-cell non-hodgkin's lymphoma (nhl). iodine-131 is the most frequently used nuclide in clinical rit, but its usefulness has been limited by dehalogenation of monoclonal antibodies labeled via conventional methods. to circumvent this problem, we have synthesized a tri-peptide consisting of non-m...

Solid-phase peptide synthesis in the N-to-C direction, opposite to the classical C-to-N direction of peptide synthesis, provides the synthetically versatile C-terminal carboxyl group for further modification into C-terminally modified peptide mimetics. These are of general interest as potential bioactive agents, particularly as protease inhibitors. Elaboration of peptide mimetics on the solid-p...

A novel, ultrafast, mild and scalable amide bond formation strategy in methanol using simple thioacids and amines is described. The mechanism suggests that the coupling reactions are initially mediated by CuSO(4)·5H(2)O and subsequently catalyzed by in situ generated copper sulfide. The pure peptides were isolated in satisfactory yields in less than 5 minutes.