Amino Acid Derivatives

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.

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).

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).

Bachem ID: 4096115.

Phe-CMK, inhibitor of gramicidin S synthetase 2.

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.

This biotinylated LHRH derivative has been used in a functional analysis of the LHRH receptor ligand binding.

Degradation product of oxytocin.

Bachem ID: 4095528.

Suc-AEPF-AMC, fluorogenic substrate for the peptidylprolyl isomerase Pin1.

A highly amyloidogenic region of lactoferrin.

CA074, a potent inhibitor specific for cathepsin B in vitro (IC₅₀= 2.24 nM for rat liver cathepsin B) and in vivo.