Display Settings:

Format

Send to:

Choose Destination
See comment in PubMed Commons below
Toxicon. 2012 Mar 15;59(4):529-46. doi: 10.1016/j.toxicon.2011.07.016. Epub 2011 Aug 12.

Development of a sea anemone toxin as an immunomodulator for therapy of autoimmune diseases.

Author information

  • 1Department of Physiology and Biophysics, UC Irvine, Irvine, CA 92697, USA.

Abstract

Electrophysiological and pharmacological studies coupled with molecular identification have revealed a unique network of ion channels--Kv1.3, KCa3.1, CRAC (Orai1 + Stim1), TRPM7, Cl(swell)--in lymphocytes that initiates and maintains the calcium signaling cascade required for activation. The expression pattern of these channels changes during lymphocyte activation and differentiation, allowing the functional network to adapt during an immune response. The Kv1.3 channel is of interest because it plays a critical role in subsets of T and B lymphocytes implicated in autoimmune disorders. The ShK toxin from the sea anemone Stichodactyla helianthus is a potent blocker of Kv1.3. ShK-186, a synthetic analog of ShK, is being developed as a therapeutic for autoimmune diseases, and is scheduled to begin first-in-man phase-1 trials in 2011. This review describes the journey that has led to the development of ShK-186.

Copyright © 2011 Elsevier Ltd. All rights reserved.

PMID:
21867724
[PubMed - indexed for MEDLINE]
PMCID:
PMC3397671
Free PMC Article

Images from this publication.See all images (10)Free text

Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
Figure 6
Figure 7
Figure 8
Figure 9
Figure 10
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Icon for Elsevier Science Icon for PubMed Central
    Loading ...
    Write to the Help Desk