Amino Acid Derivatives

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.

Bachem ID: 4099858.

Bachem ID: 4095648.

Bachem ID: 4030725.

Cyclolinopeptide B has been isolated from the seeds of Linum usitatissimum. It showed potent immunosuppressive activity comparable with that of cyclosporin A.

Main degradation product of NPY in serum and Y2/Y5 receptor agonist.

Bachem ID: 4011240.

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).

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

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.

Bachem ID: 4095647.

This NPY analog is a highly potent and selective ligand for Y₁ receptors in different cell lines and tissues. It has therefore been used to detect the NPY/PYY receptor subtype distribution, e.g., in rat brain. The peptide is also active in vivo, showing an even higher potency than NPY in increasing blood pressure in anesthetized rats.

A highly amyloidogenic region of lactoferrin.

Potential impurity of exenatide.

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.

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

Bachem ID: 4097932.

Bachem ID: 4096115.

Bachem ID: 4012218.

Degradation product of oxytocin.