Mechanically activated channel blocker

Details Mechanically activated channel blocker Mechanically activated channel blocker

2007-08-21

2007-08-21

Russel, Jeffrey Edwin (Department: 1654)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

C530S324000, C530S858000

Reexamination Certificate

active

11176745

ABSTRACT:
The present invention discloses a peptide of SEQ ID NO:1 and its variants that blocks stretch-activated ion channels. All amino acids in this peptide are D-amino acids. The peptide, designated as D-GsMTx4, is an enantiomer of a peptide GsMTX-4 present in the venom of the spiderGrammostola spatulata. The present invention also discloses a method for inhibition of stretch activated ion channels in a cell. This peptide can be used for the treatment of cardiac arrhythmias and other pathologies that involve alterations in mechanical stress.

REFERENCES:
patent: 5756663 (1998-05-01), Lampe et al.
patent: 6261569 (2001-07-01), Comis et al.
patent: WO 01/76618 (2001-10-01), None
patent: WO 2004/085647 (2004-10-01), None
Suchyna, Thomas M. et. al., Bilayer-dependent inhibition of mechanosensitive channels by neuroactive peptide enantiomers; Nature, vol. 430 (6996) Jul. 8, 2004, pp. 235-240.
Gottlieb, Philip A., et. al., Mechanosensitive Ion Channels as Drug Targets; Current Drug Targets, CNS & Neurological Disorders, vol. 3 (4), Aug. 2004, p. 287-295.

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