Amino Acid Derivatives

<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>

<p>This 25 residue peptide was completely resistant to proteolysis by cathepsin B even after incubation overnight. It inhibited human cathepsin B with Ki = 2.8 µM and rat cathepsin B with Ki = 2 µM.</p>

<p>(Leu¹³)-Motilin (human, porcine) has been shown to produce an excitory response in the chicken gastrointestinal tract with a different sensitivity from region to region. The mechanisms of action were different between the proventriculus and the intestinal segments. The motilin analog contracted the intestinal segments by direct action on the smooth muscle cells whereas in the proventriculus it caused contraction and enhancement of electrical field stimulation-induced response through an action on the intramural cholinergic neurons.</p>

<p>Bachem ID: 4097460.</p>

<p>Potential impurity of exenatide.</p>

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

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

<p>Bachem ID: 4099858.</p>

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

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

<p>Bachem ID: 4097932.</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>Bachem ID: 4011240.</p>

<p>WFYpSPR-pNA, chromogenic substrate for Pin1, an essential and conserved mitotic peptidyl-prolyl isomerase (PPIase), that specifically recognizes the phosphoserine-proline bonds present in mitotic phosphoproteins (kcat/Km = 20160 mM⁻¹s⁻¹).</p>

<p>Bachem ID: 4012218.</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>Main degradation product of NPY in serum and Y2/Y5 receptor agonist.</p>