Zheng C J, Han L Y, Yap C W, Xie B, Chen Y Z
Department of Computational Science, National University of Singapore, Blk Soc 1, Level 7, 3 Science Drive #2, Singapore 117543.
Drug News Perspect. 2005 Mar;18(2):109-27. doi: 10.1358/dnp.2005.18.2.886480.
Lead discovery against a preselected therapeutic target is a key component in modern drug development. Continuous effort and increasing interest has been directed at the search for new targets, which has led to the identification of a growing number of them. Data from the therapeutic target database, at http://bidd.nus.edu.sg/group/cjttd/ttd.asp, show that, as of July 2004, the number of documented targets of marketed and investigational drugs has reached 1,174 distinct proteins (including subtypes) and 27 nucleic acids, 239 of which are targets of the marketed drugs. Analysis of these targets, particularly those of recently approved drugs and patented investigational agents, provide useful hints about general trends of target exploration and current focus in drug discovery for the treatment of high impact diseases needing effective or more treatment options.
针对预先选定的治疗靶点进行先导化合物发现是现代药物研发的关键环节。人们持续投入精力并愈发关注寻找新的靶点,这使得已确定的靶点数量不断增加。来自治疗靶点数据库(网址:http://bidd.nus.edu.sg/group/cjttd/ttd.asp)的数据显示,截至2004年7月,已上市和正在研究的药物的已记录靶点数量已达1174种不同蛋白质(包括亚型)和27种核酸,其中239种是已上市药物的靶点。对这些靶点进行分析,尤其是对最近获批药物和已获专利的研究用药物的靶点进行分析,能为靶点探索的总体趋势以及当前治疗需要有效或更多治疗选择的重大疾病的药物研发重点提供有用线索。