Multi-Leu peptide

Multi-Leu peptide

• Handling and Storage of Synthetic Peptides
• Material Safety Data Sheets (MSDS)

Ac-LLLLRVKR-NH2

Ac-Leu-Leu-Leu-Leu-Arg-Val-Lys-Arg-NH2

8

95.1%

C₄₉H₉₄N₁₆O₉

1051.37

Synthetic

Powder

Multi-Leu peptide is a peptide identified from a partial combinatorial library that is selective for the proprotein convertase PACE4, notably being 20 fold selective over furin, a closely related enzyme with similar structural characteristics. Proprotein convertases play an important role in protein precursor activation through processing at paired basic residues and PACE4 specifically has an important role in prostate cancer. Consistent with inhibition of PACE4, Multi-Leu peptide significantly reduces the proliferation of DU145 and LNCaP prostate cancer derived cell lines and induces G0/G1 cell cycle arrest.

Normally, this peptide will be delivered in lyophilized form and should be stored in a freezer at or below -20 °C. For more details, please refer to the manual:Handling and Storage of Synthetic Peptides

• Levesque et al (2012) The Multi-Leu peptide inhibitor discriminates between PACE4 and furin and exhibits antiproliferative effects on prostate cancer cells. J Med Chem. 55(23) 10501 PMID: 23126600
• Kwiatkowska et al (2019) Enhanced anti-tumor activity of the Multi-Leu peptide PACE4 inhibitor transformed into an albumin-bound tumor-targeting prodrug. Sci Rep. 9(1) 2118 PMID: 30765725

Trifluoroacetic acid (TFA) has a significant impact on peptides due to its role in the peptide synthesis process.

TFA is essential for the protonation of peptides that lack basic amino acids such as Arginine (Arg), Histidine (His), and Lysine (Lys), or ones that have blocked N-termini. As a result, peptides often contain TFA salts in the final product.

TFA residues, when present in custom peptides, can cause unpredictable fluctuations in experimental data. At a nanomolar (nM) level, TFA can influence cell experiments, hindering cell growth at low concentrations (as low as 10 nM) and promoting it at higher doses (0.5–7.0 mM). It can also serve as an allosteric regulator on the GlyR of glycine receptors, thereby increasing receptor activity at lower glycine concentrations.

In an in vivo setting, TFA can trifluoroacetylate amino groups in proteins and phospholipids, inducing potentially unwanted antibody responses. Moreover, TFA can impact structure studies as it affects spectrum absorption.