Tetraphenylporphyrin derivative specifically blocks members of the voltage-gated potassium channel subfamily Kv1

Hornig, Sönke; Ohmert, Iris; Trauner, Dirk; Ader, Christian; Baldus, Marc; Pongs, Olaf

doi:10.4161/chan.25848

Cited by 5 publications

(11 citation statements)

References 35 publications

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“…Also, for the Zn(II) complex, a higher depolarization effect was observed than in the case of the porphyrinic ligand. Our results are in accordance with those obtained by Horning et al [15], who showed that tetraphenylporphyrin derivatives can bind to potassium-voltage channel, having binding sites: one modulating the ion flow through the channel pore, the other binding targeting the voltage-sensor protein movement.…”

Section: Resultssupporting

confidence: 93%

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The Effect of Some Amphiphilic Porphyrins on the Transmembrane Potential of Cultured L929 Cells

Radulea¹,

Boscencu²,

Socoteanu³

et al. 2019

Rev. Chim.

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This study include in the same frame promising structures tailored as photoactive agents for photodynamic therapy of cancer versus one of the most versatile cell lines from experimental point of view, fibroblasts type, subcutaneous connective tissues- L929. Transmembrane potential was studied establishing important features in the behavior of chemical vectors against cultured cells via membranar media. Two amphiphilic porphyrins, 5,15-bis-(4-hydroxy-3-methoxyphenyl)-10,20-bis-(4-carboxymethylphenyl)porphyrin and Zn(II)-5,15-bis-(4-hydroxy-3-methoxyphenyl)-10,20-bis-(4-carboxymethylphenyl)porphyrin were assessed in terms of the effect on membrane potential. The comparative effect of free base porphyrin and metalloporphyrin with amphiphilic structure, reveal hyperpolarization phenomena and bring informations about consequences of active compound concentration against cell membrane.

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Section: Resultssupporting

confidence: 93%

“…Tetraphenylporphyrin derivatives have been developed as a new class of synthetic ligands for potassium channels [15], but they also can act as PDT agents.…”

mentioning

confidence: 99%

The Effect of Some Amphiphilic Porphyrins on the Transmembrane Potential of Cultured L929 Cells

Radulea¹,

Boscencu²,

Socoteanu³

et al. 2019

Rev. Chim.

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“…40,52 The porphyrin blocks the ion conduction pathway and stabilises a closed Kv channel state upon interaction with the voltage sensor domain. 44 Further studies have been directed towards inhibiting specific Kv1 channels. 53 The Yayon group studied porphyrins that bind to fibroblast growth factor (FGF) and vascular endothelial growth factor (VEGF), 45 a protein important in tumour angiogenesis and metastasis, 54 with low micromolar affinity in vitro, in cellulo, and in vivo (mouse).…”

Section: Porphyrinsmentioning

confidence: 99%

Metal complexes as “protein surface mimetics”

Hewitt

Wilson

2016

Chem. Commun.

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A key challenge in chemical biology is to identify small molecule regulators for every single protein. However, protein surfaces are notoriously difficult to recognise with synthetic molecules, often having large flat surfaces that are poorly matched to traditional small molecules. In the surface mimetic approach, a supramolecular scaffold is used to project recognition groups in such a manner as to make multivalent non-covalent contacts over a large area of protein surface. Metal based supramolecular scaffolds offer unique advantages over conventional organic molecules for protein binding, inlcuding greater steroechemcial and geometrical diversity conferred through the metal centre and the potential for direct assessment of binding properties and even visualisation in cells without recourse to further functionalisation. This feature article will highlight the current state of the art in protein surface recognition using metal complexes as surface mimetics.

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“…The function of channels is to allow selectivity and specifi city for a Variety of molecular species transport across the cell membrane (Hornig et al 2013, Rui et al 2012. These channels, included: a) ligand-gated channels, b) voltage-gated channels, c) Second messenger gated channels, d) mechanosensitive channels, e) Gap junctions: porins not gated , Lacroix et al 2014.…”

Section: Introductionmentioning

confidence: 99%

“…2004. Potassium channels are the most diverse group of the ion channel family (Hornig et al 2013). The recent determination of the crystallographic structure a bacterial K + channel from Streptomyces lividans (KcsA) (Syeda et al 2012) has provided the molecular basic for understanding the physical mechanisms controlling ionic selectivity, permeation, and transport through Various types of K + channels.…”

Section: Introductionmentioning

confidence: 99%

Amino acid binding to nanotube: Simulation of membrane protein channels by computational methods

Moghaddam¹,

Ahmadi²,

Rasoolzadeh³

2016

Biosci. Biotech. Res. Comm

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The importance of ionic channels is due to the passage of ions across the cell membrane which is based on electrochemical gradients. The structure of ionic channels often includes one or several central cores which makes up the pore. The direct electron transfer between the enzyme and unmodifi ed electrode is usually prohibited due to shielding of the redox active sites by the protein shells. Monte Carlo simulation have been used to investigate protein folding pathways with some success. Monte Carlo was originally developed for calculating equilibrium properties of physical systems .In calculations we optimized the geometry and defi ned Potential Energy of the nanotube structure by performing molecular mechanics calculation using MM+ force fi eld, if too large a time step is used in Monte Carlo simulation, it is possible to have a basic instability in the equations that result in a molecule blowing apart, we need small time steps to preserve integration accuracy, however in the Monte Carlo time step 50 femtoseconds (0.05ps) was appropriate. next step we calculated the Vibrational modes of the tube by applying the semi-empirical molecular orbital method. In this paper, we have studies the stability of CNT-Amino acids clusters using by semi-empirical method and investigation of vibrational frequencies and electrical properties. In the more the potential energy increases the more the conductivity of nanochannels decreases and we chose the least energy among nanotube and amino acid complexes. Also the more energy we use, the more conductivity we will have; therefore, we choose the complex which conducts the most current.

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Tetraphenylporphyrin derivative specifically blocks members of the voltage-gated potassium channel subfamily Kv1

Cited by 5 publications

References 35 publications

The Effect of Some Amphiphilic Porphyrins on the Transmembrane Potential of Cultured L929 Cells

The Effect of Some Amphiphilic Porphyrins on the Transmembrane Potential of Cultured L929 Cells

Metal complexes as “protein surface mimetics”

Amino acid binding to nanotube: Simulation of membrane protein channels by computational methods

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