11 research outputs found
Study of calix[4]resorcinarene-dopamine complextion in mixed phospholipid monolayers formed at the air-water interface
We have studied the physical properties of monolayers formed by
calix[4]resorcinarene and in mixtures with dipalmitoyl
phosphatidylcholine (DPPC) in various molar ratios formed at the
air-water interface and at presence of dopamine in water subphase by
means of measurements of surface pressure and dipole potential. We
showed that both calix[4]resorcinarene as well as its mixture with
DPPC form stable monolayers at the water subphase. The presence of
dopamine resulted in an increase of the mean molecular area and in a
decrease of the compressibility modulus of the monolayers. For mixed
monolayers at higher content of calix[4]resorcinarene (> 0.2 molar
fraction) a deviation from ideal miscibility took place especially for
monolayers in a solid state. This can be connected with formation of
aggregates of calix[4] resorcinarene. Lowest miscibility and weakest
interaction of dopamine with a monolayer was observed for
calix[4]resorcinarene molar fraction of 0.33 in the monolayer. (c)
2006 Elsevier B.V. All rights reserved
The study of the interaction of a model at-helical peptide with lipid bilayers and monolayers
The study of the interaction of a model at-helical peptide with lipid bilayers and monolayers
Functional incorporation of the pore forming segment of AChR M2 into tethered bilayer lipid membranes
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High-affinity small molecule-phospholipid complex formation: Binding of siramesine to phosphatidic acid
Siramesine (SRM) is a sigma-2 receptor agonist which has been recently shown to inhibit growth of cancer cells. Fluorescence spectroscopy experiments revealed two distinct binding sites for this drug in phospholipid membranes. More specifically, acidic phospholipids retain siramesine on the bilayer surface due to a high-affinity interaction, reaching saturation at an apparent 1:1 drug-acidic phospholipid stoichiometry, where after the drug penetrates into the hydrocarbon core of the membrane. This behavior was confirmed using Langmuir films. Of the anionic phospholipids, the highest affinity, comparable to the affinities for the binding of small molecule ligands to proteins, was measured for phosphatidic acid (PA, mole fraction Of X-PA = 0.2 in phosphatidylcholine vesicles), yielding a molecular partition coefficient of 240 +/- 80 x 10(6). An MD simulation on the siramesine:PA interaction was in agreement with the above data. Taking into account the key role of PA as a signaling molecule promoting cell growth our results suggest a new paradigm for the development of anticancer drugs, viz. design of small molecules specifically scavenging phospholipids involved in the signaling cascades controlling cell behavior