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Merck

Use of X-ray scattering to aid the design and delivery of membrane-active drugs.

European biophysics journal : EBJ (2012-06-05)
G Pabst, D Zweytick, R Prassl, K Lohner
RESUMEN

Biological membranes can be targets for compounds that either disrupt their barrier function or affect protein function via membrane-mediated processes. Biophysical studies on membrane-mimetic systems composed of membrane lipids have contributed substantially to our knowledge on the pertaining membrane physics and aid the development of membrane-specific drugs. Moreover, lipid membranes and, in particular, liposomes are convenient systems for drug delivery. We review some of our recent work that demonstrates the applicability of X-ray scattering to understanding the molecular mechanisms of drug-membrane interactions. In particular we focus on effects of anesthetics, sphingomyelinase, and antimicrobial peptides. We further discuss X-ray scattering as a quality-control tool for liposomal drug-delivery systems.

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Sphingomyelinase from Bacillus cereus, buffered aqueous glycerol solution, ≥100 units/mg protein (Lowry)