Sadée W, Drübbisch V, Amidon G L
School of Pharmacy, University of California, San Francisco 94143-0446, USA.
Pharm Res. 1995 Dec;12(12):1823-37. doi: 10.1023/a:1016211015926.
Membrane transporter proteins are encoded by numerous genes that can be classified into several superfamilies, on the basis of sequence identity and biological function. Prominent examples include facilitative transporters, the secondary active symporters and antiporters driven by ion gradients, and active ABC (ATP binding cassette) transporters involved in multiple-drug resistance and targeting of antigenic peptides to MHC Class I molecules. Transported substrates range from nutrients and ions to a broad variety of drugs, peptides and proteins. Deleterious mutations of transporter genes may lead to genetic diseases or loss of cell viability. Transporter structure, function and regulation, genetic factors, and pharmaceutical implications are summarized in this review.
膜转运蛋白由众多基因编码,根据序列同一性和生物学功能,这些基因可分为几个超家族。突出的例子包括易化转运体、由离子梯度驱动的次级主动同向转运体和反向转运体,以及参与多药耐药和将抗原肽靶向主要组织相容性复合体I类分子的主动ABC(ATP结合盒)转运体。转运的底物范围从营养物质和离子到各种各样的药物、肽和蛋白质。转运体基因的有害突变可能导致遗传疾病或细胞活力丧失。本文综述了转运体的结构、功能和调节、遗传因素以及药学意义。