page_title: Metalloprotease inhibitor
section_title: Hydroxypyrone-based inhibitors
hierarchical_section_title: Metalloprotease inhibitor / Drug development / Hydroxypyrone-based inhibitors
context_page_description: Metalloprotease inhibitors are cellular inhibitors of the Matrix metalloproteinases. MMPs belong to a family of zinc-dependent neutral endopeptidases. These enzymes have the ability to break down connective tissue. The expression of MMPs is increased in various pathological conditions like inflammatory conditions, metabolic bone disease, to cancer invasion, metastasis and angiogenesis.
  Examples of diseases are periodontitis, hepatitis, glomerulonephritis, atherosclerosis, emphysema, asthma, autoimmune disorders of skin and dermal photoaging, rheumatoid arthritis, osteoarthritis, multiple sclerosis, Alzheimer's disease, chronic ulcerations, uterine involution, corneal epithelial defects, bone resorption and tumor progression and metastasis. Due to the role of MMPs in pathological conditions, inhibitors of MMPs may have therapeutic potential. Several other proteins have similar inhibitory effects, however none as effective. They might have other biological activities which have yet been fully characterised.
  MMP inhibitors can broadly be subdivided into non-synthetic or synthetic.
context_section_description: Potent and selective MMP-3 inhibitors have been developed by using a hydroxypyrone as the zinc binding group. By attaching an aryl backbone to the 2-position of the pyrone ring, more selectivity was gained. On the hydroxypyrone ring, three positions are available to attach backbones, position 2-, 5- and 6-.
  Hydroxypyrone-based MMP inhibitors are structurally corresponding to the pyrimidinetriones. A recent inhibitor is the compound 3-hydroxypyran-4-one nominated 868368-30-3. It is MMP-3 selective and its 0,0-bidentate chelation of zinc is the structural part proposed to be responsible for the MMP recognition.
caption: Compound 868368-30-3