Department of Pharmacy, National University of Singapore, Singapore.
Curr Mol Pharmacol. 2008 Nov;1(3):213-32. doi: 10.2174/1874467210801030213.
A number of therapeutic targets have been explored for developing anticancer drugs. Continuous efforts have been directed at the discovery of new targets as well as the improvement of therapeutic efficacy of agents directed at explored targets. There are 84 and 488 targets of marketed and investigational drugs for the treatment of cancer or cancer related illness. Analysis of these targets, particularly those of drugs in clinical trials and US patents, provides useful information and perspectives about the trends, strategies and progresses in targeting key cancer-related processes and in overcoming the difficulties in developing efficacious drugs against these targets. The efficacy of anticancer drugs directed at these targets is frequently compromised by counteractive molecular interactions and network crosstalk, negative and adverse secondary effects of drugs, and undesired ADMET profiles. Multi-component therapies directed at multiple targets and improved drug targeting methods are being explored for alleviating these efficacy-reducing processes. Investigation of the modes of actions of these combinations and targeting methods offers clues to aid the development of more effective anticancer therapies.
已经探索了许多治疗靶点来开发抗癌药物。人们一直在努力发现新的靶点，并提高针对已探索靶点的药物的治疗效果。目前有 84 种和 488 种已上市和正在研究的药物靶点用于治疗癌症或与癌症相关的疾病。对这些靶点的分析，特别是对临床试验和美国专利中的药物靶点的分析，提供了有关针对关键癌症相关过程的靶向治疗趋势、策略和进展的有用信息和观点，以及克服针对这些靶点开发有效药物的困难的信息。针对这些靶点的抗癌药物的疗效经常受到拮抗分子相互作用和网络串扰、药物的负性和不良反应以及不理想的 ADMET 特征的影响。目前正在探索针对多个靶点的多组分疗法和改进的药物靶向方法，以缓解这些降低疗效的过程。对这些组合和靶向方法的作用模式的研究为辅助开发更有效的抗癌疗法提供了线索。
