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How hydrogen bonds impact P-glycoprotein transport and permeability.

Bioorg Med Chem Lett. 2012 Aug 23;

Authors: Desai PV, Raub TJ, Blanco MJ


The requirement to cross a biological membrane can be a complex process especially if multidrug transporters such as P-gp must be considered. Drug partitioning into the lipid membrane and efflux by P-gp are tightly coupled processes wherein H-bonding interactions play a key role. All H-bond donors and acceptors are not equal in terms of the strength of the H-bonds that they form, hence it is important to consider their relative strength. Using various examples from literature, we illustrate the benefits of considering the relative strengths of individual H-bonds and introducing intramolecular H-bonds to increase membrane permeability and/or decrease P-gp efflux.

PMID: 23006604 [PubMed - as supplied by publisher]