The cellular uptake of pharmaceutical drugs is mainly carrier-mediated and is thus an issue not so much of biophysics but of systems biology

摘要: It is widely believed that most drug molecules are transported across the phospholipid bilayer portion of biological membranes via passive diffusion at a rate related to their lipophilicity (expressed as log P, calculated c P or D, octanol:water partition coefficient). However, studies this using purely have been very misleading since transfer these typically occurs solvent reservoirs aqueous pore defects, neither which prevalent in cells. Since types biophysical forces involved interaction drugs with lipid membrances no different from those proteins, arguments based on also apply uptake by membrane transporters carriers. A similar story attaches history mechanistic explanations mode action general anaesthetics (narcotics). Carrier-mediated and active far more common than usually assumed. This has considerable implications for design libraries discovery development, well chemical genetics/genomics systems chemistry.