Pharmacological characterization of five cloned voltage-gated K+ channels, types Kv1.1, 1.2, 1.3, 1.5, and 3.1, stably expressed in mammalian cell lines.
We have analyzed the biophysical and pharmacological properties of five cloned K+ (Kv) channels (Kv1.1, Kv1.2, Kv1.3, Kv1.5, and Kv3.1) stably expressed in mammalian cell lines. Kv1.1 is…
Design of a potent and selective inhibitor of the intermediate-conductance Ca2+-activated K+ channel, IKCa1: a potential immunosuppressant.
- H. Wulff, M. Miller, W. Hansel, S. Grissmer, M. Cahalan, K. Chandy
- Biology, ChemistryProceedings of the National Academy of Sciences…
- 5 July 2000
TRAM-34 (1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole) inhibits the cloned and the native IKCa1 channel in human T lymphocytes with a K(d) of 20-25 nM and is 200- to 1,500-fold selective over other ion channels, suggesting that TRAM- 34 and related compounds may hold therapeutic promise as immunosuppressants.
International Union of Pharmacology. LII. Nomenclature and Molecular Relationships of Calcium-Activated Potassium Channels
- A. Wei, G. Gutman, R. Aldrich, K. Chandy, S. Grissmer, H. Wulff
- BiologyPharmacological Reviews
- 1 December 2005
The first cloned potassium channel gene was the Drosophila voltage-gated shaker channel, and this was rapidly followed by the identification of other potassium channel genes.
International Union of Pharmacology. LII. Nomenclature and molecular relationships of calcium-activated potassium channels.
Department of Anatomy and Neurobiology, Washington University School of Medicine, St. Louis, Missouri (A.D.A.G.) and Physiology and Biophysics (K.W.G).
International Union of Pharmacology. LIII. Nomenclature and Molecular Relationships of Voltage-Gated Potassium Channels
Department of Microbiology and Molecular Genetics (G.A.G.) and Physiology and Biophysics (K.R.C.) and Institute of Materia Medica, Chinese Academy of Medical Sciences, and Peking Union Medical College, Beijing, China.
Calcium-activated potassium channels in resting and activated human T lymphocytes. Expression levels, calcium dependence, ion selectivity, and pharmacology
While K(Ca) and voltage-gated K+ channels in the same cells share similarities in ion permeation, Cs+ and Ba2+ block, and sensitivity to CTX, the underlying proteins differ in structural characteristics that determine channel gating and block by NTX and TEA.
International Union of Pharmacology. XLI. Compendium of Voltage-Gated Ion Channels: Potassium Channels
An overview of the molecular relationships among the voltage-gated potassium channels and a standard nomenclature for them is presented, which is derived from the IUPHAR Compendium of Voltage-Gated Ion Channels.
TEA prevents inactivation while blocking open K+ channels in human T lymphocytes.
Regulation of a mammalian Shaker‐related potassium channel, hKv1.5, by extracellular potassium and pH
Blockage of intermediate-conductance Ca2+-activated K+ channels inhibit human pancreatic cancer cell growth in vitro.
- H. Jäger, Tobias Dreker, Anita Buck, K. Giehl, T. Gress, S. Grissmer
- BiologyMolecular Pharmacology
- 1 March 2004
The blockade of IK channels may ultimately prove useful as a therapeutic option for some patients with ductal adenocarcinoma of the pancreas with an up-regulated IK channel expression.