Docherty A J, O'Connell J, Crabbe T, Angal S, Murphy G
Celltech Ltd, Slough, UK.
Trends Biotechnol. 1992 Jun;10(6):200-7. doi: 10.1016/0167-7799(92)90214-g.
Uncontrolled matrix metalloproteinase activity is thought to be a cause of the tissue damage observed in many disease processes. None of the drugs currently in use can prevent tissue destruction, and strategies for the development of synthetic inhibitors have been hampered by a poor understanding of the biochemistry of matrix metalloproteinases. Recent cDNA cloning efforts and characterization of recombinant human matrix metalloproteinases have permitted structure-function analysis of the enzymes and their inhibitors. Progress in this area should help indicate a route to rational strategies for designing lead therapeutic compounds.
不受控制的基质金属蛋白酶活性被认为是许多疾病过程中所观察到的组织损伤的一个原因。目前使用的药物都无法预防组织破坏，而合成抑制剂的开发策略因对基质金属蛋白酶生物化学的了解不足而受到阻碍。最近的cDNA克隆工作以及重组人基质金属蛋白酶的特性分析使得对这些酶及其抑制剂进行结构-功能分析成为可能。该领域的进展应有助于指明设计先导治疗化合物合理策略的途径。
