Evidence map›Paper›PMID 24946142›Full record

ArticleBiochimica et biophysica acta2014

The application of solid-state NMR spectroscopy to study candesartan cilexetil (TCV-116) membrane interactions. Comparative study with the AT1R antagonist drug olmesartan.

Dimitrios Ntountaniotis, Tahsin Kellici, Andreas Tzakos, Pinelopi Kolokotroni, Theodore Tselios, Johanna Becker-Baldus, Clemens Glaubitz, Sonyan Lin, Alexandros Makriyannis, Thomas Mavromoustakos

Open access · greenAbstract readComparative Study
PubMed Full text at PMC Publisher
In one paragraph

Article in Biochimica et biophysica acta, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
1.1field-weighted citation impact, top 25% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

4 citing papers in PubMed, 17 citations in OpenAlex.

  1. Review
  2. Lipophilicity Modulations by Fluorination Correlate with Membrane Partitioning.Angewandte Chemie (International ed. in English) · 2023
    Article
  3. Review
  4. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors at 6 institutions in 3 countries.

Dimitrios NtountaniotisNational and Kapodistrian University of Athens, Department of Chemistry, Panepistimioupolis Zografou 15771, Athens, Greece. Electronic address: doudaniotis@yahoo.gr.
Tahsin KelliciNational and Kapodistrian University of Athens, Department of Chemistry, Panepistimioupolis Zografou 15771, Athens, Greece; University of Ioannina, Department of Chemistry, 45110 Ioannina, Greece.
Andreas TzakosUniversity of Ioannina, Department of Chemistry, 45110 Ioannina, Greece.
Pinelopi KolokotroniUniversity of Patras, Department of Chemistry, Patras 26500, Greece.
Theodore TseliosUniversity of Patras, Department of Chemistry, Patras 26500, Greece.
Johanna Becker-BaldusGoethe University Frankfurt, Institute of Biophysical Chemistry, Max-von-Laue-Str. 9, 60438 Frankfurt, Germany.
Clemens GlaubitzGoethe University Frankfurt, Institute of Biophysical Chemistry, Max-von-Laue-Str. 9, 60438 Frankfurt, Germany.
Sonyan LinUniversity of Connecticut, School of Pharmacy, Storrs, CT 06269, USA.
Alexandros MakriyannisNortheastern University, Center for Drug Discovery, Boston, MA 02115, USA.
Thomas MavromoustakosNational and Kapodistrian University of Athens, Department of Chemistry, Panepistimioupolis Zografou 15771, Athens, Greece. Electronic address: tmavrom@chem.uoa.gr.
Goethe University Frankfurt · DENational and Kapodistrian University of Athens · GRUniversity of Ioannina · GRUniversity of Patras · GRNortheastern University · USUniversity of Connecticut · US

Funding

MOLECULAR BASIS OF CANNABINOID ACTIVITYR01DA003801 · NIDA · UNIVERSITY OF CONNECTICUT STORRS · PI MAKRIYANNIS, ALEXANDROS · 1985 to 2017
$2.5M
NIDA NIH HHS R01 DA003801
6 · The paper itself

Abstract

ΑΤ1 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 the AT1 receptor. In this work, the interactions of the prodrug candesartan cilexetil (TCV-116) with lipid bilayers are studied at molecular detail. Solid-state (13)C-CP/MAS, 2D (1)H-(1)H NOESY NMR spectroscopy and in silico calculations are used. TCV-116 and olmesartan, another drug which acts as an AT1R antagonist are compared for their dynamic effects in lipid bilayers using solid-state (2)H-NMR. We find a similar localization of TCV-116 compared to other AT1 antagonists in the intermediate polar region. In addition, we can identify specific local interactions. These interactions may be associated in part with the discrete pharmacological profiles observed for different antagonists.

Indexed as

Membranes, ArtificialModels, ChemicalMolecular Dynamics SimulationAngiotensin II Type 1 Receptor BlockersBenzimidazolesBiphenyl CompoundsHumansMagnetic Resonance SpectroscopyTetrazolesAngiotensin II Type 1 Receptor BlockersBenzimidazolesBiphenyl Compoundscandesartan cilexetilMembranes, ArtificialTetrazolesCandesartan cilexetil (TCV-116)Drug/membrane interactionsIn silico calculationsLipid bilayersOlmesartanSolid-state NMR spectroscopy

Identifiers

PMID24946142
PMCPMC4321718
OpenAlexW2037803157

What OpenQuestion holds

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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.