2014
DOI: 10.1016/j.bbamem.2014.06.003
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The application of solid-state NMR spectroscopy to study candesartan cilexetil (TCV-116) membrane interactions. Comparative study with the AT1R antagonist drug olmesartan

Abstract: AT1 receptor (AT1R) antagonists exert their antihypertensive effects by preventing the vasoconstrictive hormone AngII to bind to the AT1 receptor. It has been proposed that these biological effects are mediated through a two-step mechanism reaction. In the first step, they are incorporated in the core of the lipid bilayers and in the second step they reach the active site of the receptor through lateral diffusion. In this model, drug/membrane interactions are key elements for the drugs achieving inhibition at … Show more

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Cited by 17 publications
(7 citation statements)
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“…The data suggest that each AT 1 R antagonist has a unique action on the membrane [95,96,97,98,99,100,101,102,103,104,105,106,107]. In the following figure, the interactions of candesartan cilexetil and olmesartan are illustrated as revealed from a combination of NMR spectroscopy, molecular modeling, Raman spectroscopy and Differential Scanning Calorimetry [108]. The study of the mechanism of losartan as it embeds in the lipid bilayers and approaches the AT 1 R has been recently studied [109].…”
Section: Resultsmentioning
confidence: 99%
“…The data suggest that each AT 1 R antagonist has a unique action on the membrane [95,96,97,98,99,100,101,102,103,104,105,106,107]. In the following figure, the interactions of candesartan cilexetil and olmesartan are illustrated as revealed from a combination of NMR spectroscopy, molecular modeling, Raman spectroscopy and Differential Scanning Calorimetry [108]. The study of the mechanism of losartan as it embeds in the lipid bilayers and approaches the AT 1 R has been recently studied [109].…”
Section: Resultsmentioning
confidence: 99%
“…Similar spectra can be also obtained for other labeling schemes at different positions and thus this could reveal the selectivity of the drug to participate in specific topographic position in DPPC bilayers. In addition, comparative studies with other prodrugs or AT1R antagonists can be established using specific deuteration [45].…”
Section: At1r Antagonists: Membrane Bilayer Interactionsmentioning
confidence: 99%
“…2 H solid-state NMR spectra were recorded on a BrukerAvance 600 MHz WB spectrometer equipped with a 4 mm HX double resonance MAS probe. Spectra were recorded without spinning the 4 mm MAS rotor using a solid echo sequence with an echo delay of 35 µs and a pulse length of 2.5 µs [45]. Reprinted from Biochimica et Biophysica Acta (BBA)-Biomembranes, 1838, Dimitrios Ntountaniotis, Tahsin Kellici, Andreas Tzakos, Pinelopi Kolokotroni, Theodore Tselios, Johanna Becker-Baldus, Clemens Glaubitz, Sonyan Lin, Alexandros Makriyannis, Thomas Mavromoustakos, The application of solid-state NMR spectroscopy to study candesartan cilexetil (TCV-116) membrane interactions.…”
Section: At1r Antagonists: Membrane Bilayer Interactionsmentioning
confidence: 99%
“…The possibility of the drug to act through both mechanisms can be also considered. We have previously studied the effects of various sartans on lipid bilayers. These investigations combined several complementary biophysical techniques [differential scanning calorimetry (DSC), Raman spectroscopy, small-angle X-ray scattering (SAXS), wide-angle X-ray scattering (WAXS), solid-state nuclear magnetic resonance (ssNMR), and molecular dynamics (MD) simulations] to reveal the complexity of the interaction of AT1 antagonists, when all of them were accommodated in the polar–nonpolar interface of the lipid bilayers. Each sartan is characterized by a unique “fingerprint” in terms of perturbation, orientation, and localization in lipid bilayers.…”
Section: Introductionmentioning
confidence: 99%