Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Tobias, Linder"'
Publikováno v:
PLoS Computational Biology, Vol 9, Iss 5, p e1003058 (2013)
The bacterial potassium channel KcsA, which has been crystallized in several conformations, offers an ideal model to investigate activation gating of ion channels. In this study, essential dynamics simulations are applied to obtain insights into the
Externí odkaz:
https://doaj.org/article/71a3f063ff8645a1aaff80e3a1c33299
Publikováno v:
PLoS ONE, Vol 6, Iss 12, p e28778 (2011)
Pharmacological inhibition of cardiac hERG K(+) channels is associated with increased risk of lethal arrhythmias. Many drugs reduce hERG current by directly binding to the channel, thereby blocking ion conduction. Mutation of two aromatic residues (F
Externí odkaz:
https://doaj.org/article/bc466ea9fbd24dde873fbbe4f17382a0
Autor:
Igor, Baburin, Rosanne, Varkevisser, Anja, Schramm, Priyanka, Saxena, Stanislav, Beyl, Phillip, Szkokan, Tobias, Linder, Anna, Stary-Weinzinger, Marcel A G, van der Heyden, Marien, Houtman, Hiroki, Takanari, Malin, Jonsson, Jet H D, Beekman, Matthias, Hamburger, Marc A, Vos, Steffen, Hering
Publikováno v:
Pharmacological research. 131
Evodiae fructus is a widely used herbal drug in traditional Chinese medicine. Evodia extract was found to inhibit hERG channels. The aim of the current study was to identify hERG inhibitors in Evodia extract and to investigate their potential proarrh
Autor:
Adriaan P. IJzerman, M. Houtman, M A Vos, Anna Stary-Weinzinger, H D M Beekman, Rosanne Varkevisser, Tobias Linder, M. A. G. van der Heyden, K. C. G. de Git, Richard R. Tidwell
Publikováno v:
British Journal of Pharmacology
Background and Purpose Drug interference with normal hERG protein trafficking substantially reduces the channel density in the plasma membrane and thereby poses an arrhythmic threat. The chemical substructures important for hERG trafficking inhibitio
Autor:
Kathy C G de Git, Teun P. de Boer, Richard R. Tidwell, Lukas Nalos, Maaike Peschar, Hiroki Takanari, Marcel A.G. van der Heyden, Martin B. Rook, Anna Stary-Weinzinger, Tobias Linder, Marien J C Houtman, Marc A. Vos, Rosanne Varkevisser
Publikováno v:
Cardiovascular Research. 99:203-214
Aims In excitable cells, KIR2.x ion-channel-carried inward rectifier current ( I K1) is thought to set the negative and stable resting membrane potential, and contributes to action potential repolarization. Loss- or gain-of-function mutations correla
Autor:
Tobias, Linder, Harald, Bernsteiner, Priyanka, Saxena, Florian, Bauer, Thomas, Erker, Eugen, Timin, Steffen, Hering, Anna, Stary-Weinzinger
Publikováno v:
Medchemcomm
The hERG cavity can trap very bulky compounds, without perturbing normal gate closure.
Inhibition of hERG K+ channels by structurally diverse drugs prolongs the ventricular action potential and increases the risk of torsade de pointes arrhythmia
Inhibition of hERG K+ channels by structurally diverse drugs prolongs the ventricular action potential and increases the risk of torsade de pointes arrhythmia
Publikováno v:
Journal of chemical information and modeling. 54(11)
K(+) channels play a critical role in numerous physiological and pathophysiological processes rendering them an attractive target for therapeutic intervention. However, the hERG K(+) channel poses a special challenge in drug discovery, since block of
Autor:
Adriaan P. IJzerman, Gerhard F. Ecker, Eugen Timin, Tobias Linder, Priyanka Saxena, Steffen Hering, Anna Stary-Weinzinger
Publikováno v:
Biophysical Journal. 106(2)
Understanding the molecular basis of hERG (Kv11.1) inhibition is essential for drug development. Here we systematically analyzed the mechanism and potency of hERG inhibition by a library of 13 dofetilide derivatives1. Currents through hERG channels s
Autor:
Tobias Linder, Steffen Hering, Anna Stary-Weinzinger, Florian Bauer, Priyanka Saxena, Thomas Erker, Eugen Timin
Publikováno v:
Biophysical Journal. 104(2)
Human ether-a-go-go related gene (hERG) channel inhibitors can be trapped in the channels at rest. The structural peculiarities of hERG blockers that enable trapping or alternatively resting state dissociation are currently unknown. Propafenone (smal
Autor:
Tobias Linder, Anna Stary-Weinzinger
Publikováno v:
Biophysical Journal. 102(3)
Voltage gated K+ channels open and close in response to voltage changes. While crystal structures capture a limited number of gating conformations (open, closed), the transition steps and mechanism are still unknown. A limited number of voltage gated