Albany College of Pharmacy and Health Sciences, Vermont Campus, Department of Pharmaceutical Sciences, Colchester, VT 05446, USA.
Drug Discov Today. 2012 Oct;17(19-20):1079-87. doi: 10.1016/j.drudis.2012.06.003. Epub 2012 Jun 15.
The existing consensus on coexistence of transbilayer diffusion and carrier-mediated transport as two main mechanisms for drugs crossing biological membranes was recently challenged by a systems biology group. Their transporters-only hypothesis is examined in this article using published experimental evidence. The main focus is on the key claim of their hypothesis, stating that 'the drug molecules cross pure phospholipid bilayers through transient pores that cannot form in the bilayers of cell membranes, and thus transbilayer drug transport does not exist in cells'. The analysis shows that the prior consensus remains a valid scientific view of the membrane transport of drugs.
最近,一个系统生物学小组对跨生物膜药物转运的两种主要机制(跨膜扩散和载体介导转运)共存的现有共识提出了质疑。本文利用已发表的实验证据对他们的仅转运体假说进行了检验。本文的主要重点是他们假说的关键主张,即“药物分子通过不能在细胞膜双层中形成的瞬时孔穿过纯磷脂双层,因此跨膜药物转运在细胞中不存在”。分析表明,先前的共识仍然是药物跨膜转运的有效科学观点。