Ward C M
CRC Institute for Cancer Studies, University of Birmingham, Vincent Drive, Birmingham, B15 2TA, UK.
Curr Opin Mol Ther. 2000 Apr;2(2):182-7.
The vitamin folic acid exhibits high affinity for the endocytosed, membrane-bound folate receptor. Conjugation of folic acid via its gamma-carboxyl group to various macromolecules results in binding to, and endocytosis into, cells expressing the folate receptor. The folate receptor is overexpressed on a wide range of cancers, therefore folic acid has been investigated as a targeting ligand for the specific delivery of therapeutic compounds to cancer cells. This review will introduce folate-targeting of macromolecules to cancer cells in vitro and in vivo, and discuss the accumulation of such compounds in non-target tissues in vivo. Folate-targeting of non-viral DNA vectors in vitro and in vivo will be discussed in detail, with particular emphasis on the recent advances in this field.
维生素叶酸对胞吞作用的膜结合叶酸受体具有高亲和力。通过其γ-羧基将叶酸与各种大分子共轭，会导致与表达叶酸受体的细胞结合并被内吞。叶酸受体在多种癌症中过度表达，因此叶酸已被研究作为一种靶向配体，用于将治疗性化合物特异性递送至癌细胞。本综述将介绍大分子在体外和体内对癌细胞的叶酸靶向作用，并讨论此类化合物在体内非靶组织中的蓄积情况。将详细讨论非病毒DNA载体在体外和体内的叶酸靶向作用，尤其着重于该领域的最新进展。
