作者: Mark L. Sundermeyer , Alfonso Bellacosa , Neal J. Meropol
DOI: 10.1007/978-1-59745-337-0_7
关键词: Vascular endothelial growth factor 、 Thymidylate synthase 、 Medicine 、 Mechanism of action 、 Drug development 、 Current generation 、 Oncology 、 Colorectal cancer 、 Cancer 、 Molecular targeting 、 Internal medicine
摘要: Colorectal cancer is the fourth most common worldwide and cause of mortality, with approximately 529,000 deaths annually (1). The concept molecular targeting in colorectal not new. After all, 5-fluorouracil (5-FU), standard bearer “old school” treatment continued mainstay colon systemic therapy, was developed as a “targeted” agent. In this case, primary target thymidylate synthase, key enzyme DNA synthesis, mechanism action competitive inhibition by false substrate. Whereas 5-FU clearly targeted, it lacks specificity, therapeutic window therefore narrow. past decade, advances understanding biology well technology drug development have permitted identification new targets inhibitory pharmaceuticals high specificity favorable toxicity profiles. It regard to both tissue that characterizes current generation targeted therapeutics.