antitumor activities

S-trityl-L-Cysteine is a non-natural amino acid and an inhibitor of Eg5, also known as KSP and Kif11, a mitotic kinesin necessary for mitotic spindle formation. S-trityl-L-Cysteine inhibits the ATPase activity of Eg5 in basal and microtubule-stimulated states (IC50s = 1,000 and 140 nM, respectively). It is selective for Eg5 over nine other human kinesins in an enzyme-coupled assay. It reversibly inhibits Eg5-driven microtubule sliding velocity with an IC50 value of 500 nM using X. laevis recombinant Eg5. It induces cell cycle arrest in HeLa cells (IC50 = 700 nM), reversibly halting the cell cycle in the mitotic phase by inhibiting the separation of duplicated chromosomes and preventing bipolar spindle formation. S-trityl-L-Cysteine inhibits the growth of cancer cells in vitro when tested against the National Cancer Institute (NCI) 60 human cancer cell line panel (average GI50 = 1.3 μM) and in mouse xenograft models.

Auristatin E, a cytotoxic tubulin modifier, disrupts cell division by inhibiting tubulin polymerisation. This compound demonstrates potent and selective antitumor activities, serving as an MMAE analog and cytotoxin in antibody-drug conjugates.

Melflufen (Melphalan flufenamide), a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen exhibits significant antitumor activity against multiple myeloma (MM) cells and has been shown to inhibit angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells, thereby contributing to its antitumor efficacy. At equivalent molar concentrations, both the salt and free forms of Melflufen exhibit comparable biological activity. However, the salt form, Melflufen hydrochloride, typically demonstrates enhanced water solubility and stability, which may contribute to its increased therapeutic potential.

Lactoferricin, bovine is an iron-binding glycoprotein derived from the acidic hydrolysis of bovine lactoferrin. Lactoferricin, bovine has bactericidal, antifungal, antiparasitic, antitumor, antiviral, and immunomodulatory activities [1] .

EP3, an antimicrobial peptide, exhibits both antibacterial and antifungal activities, effectively inhibiting E. gallinarum, P. pyocyanea, A. baumanii, and K. terrigena with a minimum inhibitory concentration (MIC) of 12.85 μg/mL. Additionally, EP3 demonstrates antitumor activity against cancer cells, inducing cell apoptosis [1].