RTU Research Information System
Latviešu English

Publikācija: A Novel Matrix Metalloproteinase-2 Inhibitor Triazolylmethyl Aziridine Reduces Melanoma Cell Invasion

Publication Type Scientific article indexed in SCOPUS or WOS database
Funding for basic activity Unknown
Defending: ,
Publication language English (en)
Title in original language A Novel Matrix Metalloproteinase-2 Inhibitor Triazolylmethyl Aziridine Reduces Melanoma Cell Invasion, Angiogenesis and Targets ERK1/2 Phosphorylation
Field of research 1. Natural sciences
Sub-field of research 1.4 Chemical sciences
Authors Nadežda Romančikova
Peteris Trapencieris
Jānis Zemītis
Māris Turks
Keywords Angiogenesis, aziridine-triazole conjugate, drug discovery, invasion, matrix metalloproteinase inhibitor, melanoma
Abstract A novel matrix metalloproteinase-2 (MMP-2) inhibitor JaZ-30, which belongs to the class of C(2)-monosubstituted aziridine – aryl-1,2,3-triazole conjugates, was developed. MTT and crystal violet assays were used to determine cytotoxicity- IC(50) values of compound JaZ-30 on melanoma cell line B16 4A5. Our study proves the anti-cancer properties of JaZ-30 with a wide spectrum of activities. JaZ-30 was revealed as selective inhibitor of matrix metalloproteinase-2. JaZ-30-mediated decrease of Vascular Endothelial Growth Factor (VEGF) secretion results in inhibition of angiogenesis, performed with the human umbilical vein endothelial cell line (HUVEC-2) on Matrigel. A novel inhibitor decreases invasive properties of melanoma cells measured in Matrigel chambers assay. JaZ-30 downregulates phosphorylation of the extracellular signal-regulated kinases 1 and 2 (ERK1/2) in melanoma cells stimulated by phorbol-12-myristate-13-acetate (PMA). Our findings propose a novel MMP-2 inhibitor JaZ-30 as an attractive potential agent for melanoma treatment.
DOI: 10.3109/14756366.2013.855207
Hyperlink: http://informahealthcare.com/doi/abs/10.3109/14756366.2013.855207 
Reference Romančikova, N., Trapencieris, P., Zemītis, J., Turks, M. A Novel Matrix Metalloproteinase-2 Inhibitor Triazolylmethyl Aziridine Reduces Melanoma Cell Invasion, Angiogenesis and Targets ERK1/2 Phosphorylation. Journal of Enzyme Inhibition and Medicinal Chemistry, 2014, Vol.29, No.6 , pp.765-772. ISSN 1475-6366. e-ISSN 1475-6374. Available from: doi:10.3109/14756366.2013.855207
Additional information Citation count:
ID 19601