Position 4 analogues of d-alanine in the peptide subunit of uridine 5'-diphosphate-N-acetylmuramyl-Ala(1)-dGlu(2)- Lys(3)-dAla(4)-dAla(5) have a significant inhibitory effect on penicillin-sensitive peptidoglycan synthesis in Gaffkya homari (C. V. Carpenter, S. Goyer, and F. C. Neuhaus, 1976). The specificity profile of this in vitro system has been used as a basis for designing analogues with ...

The self-peptide MART1(27-35) derives from the melanocyte/melanoma protein Melan A/MART1 and is a target epitope of CD8+ T cells, commonly recovered from tumor-infiltrating lymphocytes of HLA-A2.1+ melanoma patients. Despite their prevalence in such patients, these CTLs generally appear to be ineffective in mediating tumor regression in vivo. We have noted previously that numerous peptides from...

The melanocortin system is a complex control center that regulates various physiological pathways, which include skin pigmentation, steroidogenesis, sexual function, sebaceous lipid production, energy and weight homeostasis, and food satiety. [1,2] This system consists of five G-protein coupled receptors (MC1R-MC5R), four known endogenous agonists, and two known endogenous antagonists. [2, 3] T...

The frog skin host-defense peptide esculentin-2CHa (GFSSIFRGVA10KFASKGLGK D20LAKLGVDLVA30CKISKQC) displays antimicrobial, antitumor, and immunomodulatory properties. This study investigated the antidiabetic actions of the peptide and selected analogues. Esculentin-2CHa stimulated insulin secretion from rat BRIN-BD11 clonal pancreatic β-cells at concentrations greater than 0.3 nM without cytotox...

AIMS To investigate the effect of Glu-3 OXM-like analogues on food intake and bodyweight in male rats. BACKGROUND Oxyntomodulin (OXM) is a natural agonist at both the glucagon receptor (GCGr) and the glucagon-like peptide 1 receptor (GLP-1r), and peripheral administration reduces food intake and increases energy expenditure in rodents and humans. Substituting the native glutamine (Gln) at ami...

Echinomycin producing Streptomyces cultures (X-53 or X-63) grown in the presence of quinazol-4-one-3-acetic acid yield an analogue in which one of the two quinoxaline-2-carboxyl residues is replaced by a quinazol-4-one-3acetyl moiety. This analogue has been designated quinazomycin. Cell-free extracts of culture X-63 .synthesize echinomycin in the presence of precursors, ATP, Mg2 + and mercaptoe...

Previous investigations indicate that α-melanocyte-stimulating hormone (α-MSH) and certain synthetic analogues of it exert antimicrobial effects against bacteria and yeasts. However, these molecules have weak activity in standard microbiology conditions and this hampers a realistic clinical use. The aim in the present study was to identify novel peptides with broad-spectrum antimicrobial activi...

Heparin-binding proteins may contain specific patterns of basic amino acids, called consensus sequences, that interact with heparin. Small peptides were synthesized that contained consensus sequences (i.e. FAKLNCRLYRKANKSSK) or disrupted consensus sequences (i.e. K136-->A) based on the known sequence of antithrombin III (amino acid residues 123-139). These peptides were then examined in both co...

Analogues of fatty acids have been synthesized which contain an S-S bridge in the aliphatic chain and at the omega-carbon the photoactivatable p-(3-trifluoromethyldiazirino)phenyl or p-azidophenyl group as a carbene and nitrene precursor, respectively. These acids were used to acylate 1-palmitoyl phosphatidylcholine by the procedure described by Gupta et al. (Gupta, C.M., Radhakrishnan, R., and...

BACKGROUND Lipodystrophic syndromes are uncommon medical conditions which are normally associated with metabolic disorders, such as diabetes mellitus, dyslipidemia, and fatty liver disease. These complications are generally difficult to treat, particularly diabetes, due to severe insulin resistance. We present two case reports of successful treatment of diabetes with glucagon-like peptide-1 ana...