The metabolic processing of dehydrophos, a broad-spectrum peptide antibiotic containing an unusual vinyl-phosphonate moiety, was examined by using a panel of Salmonella enterica mutants deficient in peptide uptake and catabolism. Dehydrophos bioactivity is lost in opp tpp double mutants, demonstrating a requirement for uptake via nonspecific oligopeptide permeases. Dehydrophos bioactivity is al...

Protein farnesytransferase (PFTase) catalyzes the farnesylation of proteins with a carboxy-terminal tetrapeptide sequence denoted as a Ca1a2X box. To explore the specificity of this enzyme, an important therapeutic target, solid-phase peptide synthesis in concert with a peptide inversion strategy was used to prepare two libraries, each containing 380 peptides. The libraries were screened using ...

The increasing problem of antibiotic resistance among pathogenic bacteria requires development of new antimicrobial agents. Synthesis and experimental application of the hybrids peptides may be one of the interesting possibilities in antimicrobial treatment. The aim of the present investigation is to determinate in vitro activities of two synthetic peptide amides: cecropin-melittin hybrid pepti...

To evaluate the role of aromatic amino-acids residues, four analogues of the -selective opioid peptide agonist DALDA (H-Tyr-D-Arg-Phe-Lys-NH2) containing the amphiphilic, , -disubstituted amino acid (R)or (S)-hydroxymethyltyrosine (HmTyr) in position 1 and (R)or (S)-hydroxymethylphenylalanine (HmPhe) in position 3 of the peptide sequence were synthesized. Only the [(R)-HmPhe 3 )]DALDA analogue ...

A 75 year old woman was treated for over three years with the somatostatin analogue, octreotide for an insulinoma. She had presented in a hypoglycaemic coma. C-peptide and insulin concentrations were both raised and an area of increased vascularity within the pancreas was shown by angiography. No lesion was found at laparotomy and no resection was performed. After over three years of octreotide...

The requirement for GTP in the initiation process on reticulocyte ribosomes and ribosomal subunits has been examined by studying Met-tRNA(F) binding, ribosome-dependent [gamma-(32)P]GTP hydrolysis, and peptide-bond formation with puromycin. Met-tRNA(F) binding can be obtained with the methylene analogue, 5'-guanylylmethylene diphosphonate, as well as GTP, and it is not inhibited by fusidic acid...

OBJECTIVE The authors have conjugated chelating agents (DOTA and NODAGA) with a peptide (pituitary adenylate cyclase-activating peptide [PACAP] analogue) that has a high affinity for VPAC1 receptors expressed on cancer cells. To determine a suitable chelating agent for labeling with (68)Ga, they have compared the labeling kinetics and stability of these peptide conjugates. METHODS For labelin...

The formation of a carboxylate anion binding pocket in the antibiotics of the vancomycin group is made energetically more favorable by the S stereochemistry of residue 3 relative to the R stereochemistries of residues 1, 2 , and 4 . Pocket formation is further favoured by the covalent cross-linking of the sidechains of residues 2 and 4 , and in some cases, also of residues 1 and 3 . In the abse...

AIM Glucose-dependent insulinotropic peptide (GIP) is an incretin hormone that is released from intestinal K cells in response to nutrient ingestion. We aimed to investigate the therapeutic potential of the novel N- and C-terminally modified GIP analogue AC163794. METHODS AC163794 was synthesized by solid-phase peptide synthesis. Design involved the substitution of the C-terminus tail region ...