Pharmacology of voltage-gated and calcium-activated potassium channels

Pharmacology of voltage-gated and calcium-activated potassium channels Several important new findings have furthered the development of voltage-gated and calcium-activated potassium channel pharmacology. The molecular constituents of several members of these large ion channel families were identified. Small-molecule modulators of some of these channels were reported, including correolide, the first potent, small-molecule, natural product inhibitor of the Shaker family of voltage-gated potassium channels to be disclosed. The initial crystal structure of a bacterial potassium channel was determined; this work gives a physical basis for understanding the mechanisms of ion selectivity and ion conduction. With the recent molecular characterization of a potassium channel structure and the discovery of new templates for channel modulatory agents, the ability to rationally identify and develop potassium channel agonists and antagonists may become a reality in the near future. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Current Opinion in Chemical Biology Elsevier

Pharmacology of voltage-gated and calcium-activated potassium channels

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Publisher
Elsevier
Copyright
Copyright © 1999 Elsevier Science Ltd
ISSN
1367-5931
DOI
10.1016/S1367-5931(99)80066-0
pmid
10419851
Publisher site
See Article on Publisher Site

Abstract

Several important new findings have furthered the development of voltage-gated and calcium-activated potassium channel pharmacology. The molecular constituents of several members of these large ion channel families were identified. Small-molecule modulators of some of these channels were reported, including correolide, the first potent, small-molecule, natural product inhibitor of the Shaker family of voltage-gated potassium channels to be disclosed. The initial crystal structure of a bacterial potassium channel was determined; this work gives a physical basis for understanding the mechanisms of ion selectivity and ion conduction. With the recent molecular characterization of a potassium channel structure and the discovery of new templates for channel modulatory agents, the ability to rationally identify and develop potassium channel agonists and antagonists may become a reality in the near future.

Journal

Current Opinion in Chemical BiologyElsevier

Published: Aug 1, 1999

References

  • Voltage-gated potassium channels regulate calcium-dependent pathways involved in human T lymphocyte activation
    Lin, CS; Boltz, RC; Blake, JT; Nguyen, M; Talento, A; Fischer, PA; Springer, MS; Sigal, NH; Slaughter, RS; Garcia, ML
  • Effects of the K + channel blockers paspalitrem C and paxilline on mammalian smooth muscle
    DeFarias, FP; Carvalho, MF; Lee, SH; Kaczorowski, GJ; Suarez-Kurtz, G
  • Mechanism of maxi-K channel activation by dehydrosoyasaponin-I
    Giangiacomo, KM; Kamassah, A; Harris, G; McManus, OB
  • Novel and potent BK channel openers: CGS 7181 and its analogs
    Hu, S; Fink, CA; Kim, HS; Lappe, RW
  • Discovery of a novel class of BK channel openers: enantiospecific synthesis and BK channel opening activity of 3- (5-chloro-2-hydroxyphenyl) -1,3-dihydro-3-hydroxy-6- (trifluoromethyl) -2 H -indol-2-one
    Hewawasam, P; Meanwell, NA; Gribkoff, VK; Dworetzky, SI; Boissard, CG
  • The discovery of novel openers of Ca 2+ -dependent large-conductance potassium channels: pharmacophore search and physiological evaluation of flavonoids
    Li, Y; Starrett, JE; Meanwell, NA; Johnson, G; Harte, WE; Dworetzky, SI; Boissard, CG; Gribkoff, VK

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