Herein we present a direct label-free ultra-fast method for the identification and classification of the active members of a combinatorial library directly on the solid support used for their synthesis. The method is based on the appropriate functionalization of polyethylene glycol grafted polystyrene (TentaGel®) microbeads with Au@Ag nanoparticles, the use of these materials directly as solid-...

A system is described for solid-phase synthesis of peptides under continuous-flow conditions with liquid chromatographic equipment, conventional polystyrene supports, and well-defined chemistry. The model tetrapeptide Leu-Ala-Gly-Val was assembled in 99.3% purity in about 4 hr on microporous copoly(styrene-1% divinylbenzene). During coupling, the preformed symmetric anhydrides were conserved by...

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...

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...

The combination of solid phase peptide synthesis and endo-β-N-acetylglucosaminidase (ENGase) catalysed glycosylation is a powerful convergent synthetic method allowing access to glycopeptides bearing full-length N-glycan structures. Mannose-terminated N-glycan oligosaccharides, produced by either total or semi-synthesis, were converted into oxazoline donor substrates. A peptide from the human c...

Disulfide bonds are widespread in peptides and proteins where they strengthen conformation and lead to increased rigidity and proteolytic stability. The number of disulfide-rich therapeutics currently available is increasing, such as the FDA-approved peptide drugs Prialt (ziconotide) and Linzess (linaclotide), both of which contain 3 disulfide bonds. In order to prepare disulfide-rich peptides,...

Here we report a simple procedure for generating colorimetric histone deacetylase (HDAC) substrates by solid-phase peptide synthesis based on racemization-free couplings of amino acid chlorides. We demonstrate the applicability of these substrates in HDAC assays.

Replacing the guanidinium group in arginine (1) by a guanidiniocarbonyl pyrrole moiety provides a new class of artificial amino acids (2), that can be used as building blocks in standard solid phase peptide synthesis.

An efficient solid-phase-supported peptide synthesis (SPPS) of morpholinoglycine oligonucleotide (MorGly) mimics has been developed. The proposed strategy includes a novel specially designed labile linker group containing the oxalyl residue and the 2-aminomethylmorpholino nucleoside analogues as first subunits.