gelatinase a

Neutrophil Gelatinase Associated Lipocalin (NGAL), Human (EC 6.1.1.3), is part of the lipid transport protein family and is primarily secreted by activated neutrophils. It binds to MMP-9, enhancing its activity and preventing its degradation. NGAL is mainly recognized as a biomarker for acute kidney injury and is released following renal tubular damage and during kidney regeneration.

Cipemastat is a competitive inhibitor of human collagenases 1, 2, and 3 (Kis: 3.0, 4.4, and 3.4 nM).

SB-3CT is a potent and specific gelatinase inhibitor for MMP-2 (Ki = 13.9 nM) and MMP-9 (Ki = 600 nM).

OPB-3206 is a selective inhibitor of matrix metalloproteinases (MMPs). It inhibits stromelysin, collagenase, gelatinase A (MMP-2), and gelatinase B (MMP-9) with IC50 values of 7×10^-7 M, 5×10^-6 M, 5×10^-7 M, and 2×10^-6 M, respectively. OPB-3206 reversibly binds to the zinc-binding site of MMPs, blocking the activation of MMP-9 and reducing the degradation of the extracellular matrix, thereby inhibiting tumor lung metastasis. OPB-3206 shows potential for research in osteosarcoma lung metastasis.

Siamycin I is a tricyclic peptide originally isolated from Streptomyces and has antiviral and antibacterial activities. It is active against laboratory strains and clinical isolates of HIV-1 (ED50s = 0.05-0.45 and 0.89-5.7 μM, respectively), as well as the CBL-20 strain of HIV-2 (ED50 = 0.45 μM), in vitro. Siamycin I inhibits HIV-induced fusion of C8166 T cells with HIV-1-infected CEM-SS cells with an ED50 value of 0.08 μM. It is also active against B. subtilis, M. luteus, and S. aureus (MICs = 1.6-6.3 μg/ml). Siamycin I inhibits autophosphorylation of the E. faecalis quorum sensing kinase FsrC induced by gelatinase biosynthesis-activating pheromone (GBAP).

BE-16627B is a novel metalloproteinase (MP) inhibitor isolated from Streptomyces sp. BE16627B selectively inhibited MPs such as human stromelysin and 92 kD gelatinase. After the cells were cultured with BE16627B for 5 days, BE16627B inhibited MP activity in the primary culture supernatants from synovial cells in a dose-dependent fashion without showing apparent cytotoxicity or affecting the production and secretion of MPs. Its IC50 for active collagenolysis before activation by trypsin was 25 microM.

Ambuic acid is a cyclohexanone that has phytopathogenic antifungal, quorum sensing inhibitory, and antibacterial activities. Ambuic acid inhibits the biosynthesis of cyclic peptides involved in quorum sensing, including gelatinase biosynthesis-activating pheromone (GBAP) in E. faecalis, autoinducing peptide I (AIP-I) in S. aureus, and LsrD698 and LsrD826 in L. innocua. It suppresses abcess formation in a mouse model of skin infection induced by methicillin-resistant S. aureus (MRSA) when administered at a dose of 5 µg and decreases the activity of the agr quorum sensing system in an in vivo reporter assay.

DSPE-PEG5000-CTT2 is a PEG compound composed of DSPE and the gelatinase inhibitor CTT2 (CTTHWGFTLC). CTT2 (CTTHWGFTLC) has the capability to specifically target tumors. DSPE-PEG5000-CTT2 is applicable for drug delivery purposes.

DSPE-PEG2000-CTT2 is a PEG compound consisting of DSPE and the gelatinase inhibitor CTT2 (CTTHWGFTLC). It possesses the ability to specifically target tumors. DSPE-PEG2000-CTT2 is suitable for drug delivery applications.

DSPE-PEG1000-CTT2 is a PEG compound comprised of DSPE and a gelatinase inhibitor [CTT2 (CTTHWGFTLC)]. The CTT2 (CTTHWGFTLC) peptide is capable of specifically targeting tumors. DSPE-PEG1000-CTT2 can be utilized for drug delivery.