Functional characteristic of snake venom disintegrins: potential therapeutic implication.
Functional characteristic of snake venom disintegrins: potential therapeutic implication.
复制标题
DOI：
10.2174/1381612053381765
复制
发表时间：
2005-02
影响因子：
3.1
通讯作者：
C. Marcinkiewicz
中科院分区：
文献类型：
--
作者：
C. Marcinkiewicz
蛇毒去整合素是天然产物，已被研究为各种整合素的有效抑制剂。在功能上，去整合素可根据其整合素选择性和特异性活性基序的存在分为三组。该分类包括RGD-去整合素、MLD-去整合素和KTS-去整合素。RGD-去整合素已经被最深入地研究，并且它们的研究导致了新的药物化合物依替巴肽和替罗非班的设计和合成，这些药物化合物目前正在评估用于治疗急性冠状动脉缺血综合征。MLD-和KTS-去整合素分别对白细胞整合素和胶原受体具有特异性，并且正在药物研究的新领域中进行研究。本文综述了蛇毒去整合素的生物学活性，并讨论了其在各种人类疾病药理学研究中的潜力。
Snake venom disintegrins are the natural products that have been investigated as potent inhibitors of various integrins. Functionally, disintegrins can be divided into three groups according to their integrin selectivity and presence of specific, active motifs. This classification includes RGD-disintegrins, MLD-disintegrins, and KTS-disintegrins. RGD-disintegrins have been the most intensively investigated, and their research resulted in design and synthesis of new pharmaceutical compounds, eptifibatide and tirofiban that are currently being evaluated for the therapy of acute coronary ischaemic syndrome. MLD- and KTS-disintegrins are specific for leukocyte integrins and collagen receptors, respectively, and are being investigated in the new fields of pharmaceutical research. This review summarizes the biological activities of snake venom disintegrins, as well as discusses their potential in the study of the pharmacology of various human diseases.