A new series of peptide-like derivatives containing different aromatic amino acids andpossessing pharmacophores of COX-2 inhibitors as SO2Me or N3 attached to the para positionof an end phenyl ring was synthesized for evaluation as selective cyclooxygenase-2 (COX-2)inhibitors. The synthetic reactions were based on the solid phase peptide synthesis methodusing Wang resin. One of the analogues, i...

background: migraine is a prevalent disease which is classified into two groups of migraine with aura and without aura. eighteen percent of women and 6.5 percent of men in united states have migraine headache. migraine headache is prevalent in all age groups but it usually subsides in adults above fifty. migraine has many risk factors such as stress, light, tiredness, special foods and beverage...

pegylation is a well-established technique utilized to overcome the problems related to the therapeutic applications of peptides and proteins. reasons for the pegylation of these biological macromolecules include reducing immunogenicity, proteolytic degradation and rapid clearance from blood circulation. octreotide is an octapeptide analogue of naturally-occurred somatostatin. this peptide has ...

When examining the effects of peptide analogues without proliferation-inducing activity on three human CD4+ T cell clones with distinct TCRbeta recognizing a nonself mycobacterial bacillus Calmette-Guerin a (BCGa) peptide fragment (EEYLILSARDVLAVVSK)/HLA-DR14 complex, we found that 1) stimulation of T cells with a one-residue-substituted analogue or a minimally homologous self peptide fragment ...

An obese lady of 51 year with Type 2 Diabetes Mellitus for 13 years was prescribed Liraglutide, a glucagon like peptide (GLP-1) analogue (Victoza) for glycaemic control and reduction of weight. She was on gliclazide and Insulin prior to initiation of Liraglutide. Eight weeks after initiation of GLP -1 analogue, she developed severe abdominal pain, nausea and vomiting. She was admitted to a priv...

Triazolo-β-aza-ε-amino acid and its aromatic analogue ((Al)TAA/(Ar)TAA) in the peptide backbone mark a novel class of conformationally constrained molecular scaffolds to induce β-turn conformations. This was demonstrated for (Al)TAA in a Leu-enkephalin analogue and in a designed pentapeptide wherein the FRET process was established. Restricted rotation induced chirality and turn conformation in...

The 4-chlorophenylthio analogue of cyclic AMP evoked profound and long-lasting changes in cytosolic [Ca2+] ([Ca2+]i) in pituitary-derived GH3 cells. However, vasoactive intestinal peptide (VIP), a hormone considered to act via cyclic AMP, was ineffective in modulating [Ca2+]i. The ability of VIP to modulate [Ca2+]i was enhanced by treatments that increased intracellular cyclic AMP. Much greater...

Upon entering the host cell's cytoplasm, the pathogen Listeria monocytogenes can subvert the normal contractile system of the host cell; subsequent assembly of polar actin-filament structures is likely to provide the force for rapid intracellular bacterial movement and its cell-to-cell spread. We have now investigated the functional consequences of microinjecting Listeria-infected PtK2 cells wi...