Inhibition of Invasion and Capillary-like Tube Formation by Retrohydroxamate-based MMP Inhibitors
- Authors
- Choi, Seung-Su; Ji, Ae-Ri; Yu, Seung-Woo; Cho, Bong-Hwan; Park, Jung Dae; Park, Jun Hyoung; Lee, Hyun Soo; Ryu, Seong Eon; Kim, Dong Han; Kang, Jae-Hoon; Lee, Seung-Taek
- Issue Date
- Jun-2011
- Publisher
- Korean Chemical Society
- Keywords
- Inhibitor; Invasion; Matrix metalloproteinase (MMP); N-Formylhydroxylamine; Retrohydroxamate
- Citation
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.32, no.6, pp.2032 - 2038
- Indexed
- SCIE
SCOPUS
KCI
- Journal Title
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- Volume
- 32
- Number
- 6
- Start Page
- 2032
- End Page
- 2038
- URI
- https://scholarworks.bwise.kr/hanyang/handle/2021.sw.hanyang/168347
- DOI
- 10.5012/bkcs.2011.32.6.2032
- ISSN
- 0253-2964
- Abstract
- Matrix metalloproteinases (MMPs), a family of zinc-containing endopeptidases, participate in many normal processes such as embryonic development and wound repair, and in many pathological situations such as cancer, atherosclerosis, and arthritis. Peptidomimetic MIMP inhibitors were designed and synthesized with N-formylhydroxylamine (retrohydroxamate) as a zinc-binding group and various side chains on the alpha, P1', and P2' positions. Using in vitro MMP assays with purified MMPs (MMP-1, MMP-2, MMP-3, MMP-9, and MMP-14) and fluorogenic peptide substrates, it was found that compounds 2d and 2g selectively inhibit gelatinases (MMP-2 and MMP-9) and interstitial collagenase (MMP-1). They also inhibited the chemo-invasion of fibrosarcoma HT-1080 cells and tube formation of human umbilical vascular endothelial cells in a dose-dependent manner. Our results suggest that retrohydroxamate-based MMP inhibitors, especially compounds 2d and 2g, have the potential to be used as therapeutic drugs for cancer and other MMP-related diseases.
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