Amino Acid Derivatives

<p>The lipopeptide FSL-1, synthesized on the basis of the N-terminal structure of a M. salivarium lipoprotein, is capable of inducing the cell surface expression of ICAM-1 in human gingival fibroblasts. It furthermore revealed an activity to induce production of monocyte chemoattractant protein 1, interleukin-6 (IL-6), and IL-8. FSL-1 also activated macrophages to produce tumor necrosis factor alpha. Overall, results by Okusawa and coworkers suggest that the diacylglyceryl and the peptide portions of FSL-1 are indispensable for the expression of biological activities and for the recognition by Toll-like receptors 2 and 6. Furthermore, the same authors conclude that the recognition of FSL-1 by Toll-like receptors 2 and 6 apparently is hydrophobic.</p>

<p>Bachem ID: 4041119.</p>

<p>In contrast to the encephalitogenic rat homolog, myelin oligodendrocyte glycoprotein (35-55) (human) does not appear to be a major T-cell epitope in multiple sclerosis propably due to its lower amount of helical structure formed when dissolved in micellar sodium dodecyl sulfate, a membrane mimicking solvent.</p>

<p>Bachem ID: 4095528.</p>

<p>The peptide RVL-psi[CH2NH]FEA-Nle-amide containing a reduced peptide bond was found to be a competitive inhibitor of the HIV-1 protease (Ki = 50 nM).</p>

<p>Suc-AEPF-AMC, fluorogenic substrate for the peptidylprolyl isomerase Pin1.</p>

<p>Phe-CMK, inhibitor of gramicidin S synthetase 2.</p>

<p>The TNF-α antagonist WP9QY inhibited TNF-α mediated apoptosis and exhibited an IC₅₀ of 5 µM in the binding assay. YCWSQYLCY is the smallest peptidomimetic developed to date that might be used as a lead compound for the next generation of non-peptidic inhibitors. The name WP9QY arises from the binding to the site observed in the TNF-β/TNF-receptor(I) complex designated WP9 and the introduction of the amino acids Gln and Tyr.</p>

<p>Short peptides containing two disulfide bridges can form interconvertible topoisomers with the same disulfide connectivity. In case of uroguanylin (UGN), both are relatively stable and can be separated, and interconversion is slow. The topoisomers differ in biological activity: The UGN A topomer potently activates the guanylate cyclase C receptor found primarily in the intestine. The B topomer is a very weak agonist of this receptor. Moss et al. could show that UGN B has potent natriuretic activity in the kidney.</p>

<p>Degradation product of oxytocin.</p>

<p>Bachem ID: 4095648.</p>

<p>Chromogenic substrate for trypsin and papain.</p>

<p>Z-LLY-α-keto aldehyde (peptidyl glyoxal), previously shown to be an excellent inhibitor of the serine and cysteine proteases, was found to be an excellent inhibitor of the chymotryptic-like activity of proteasome exhibiting a Ki value of approximately 3.0 nM. Such inhibitor might be valuable in the characterization of the role of proteasome in normal and aberrant pathways of protein catabolism in the cell.</p>