Compositions and methods for inhibiting inward-rectifier...

Chemistry: analytical and immunological testing – Biospecific ligand binding assay

Reexamination Certificate

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C514S002600, C514S013800, C530S300000, C530S326000

Reexamination Certificate

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06979572

ABSTRACT:
The present invention provides compounds and methods of identifying and designing compounds which inhibit activity of inward-rectifier K+channels. In particular, compounds having a tertiapin-like α helix, such as a stable tertiapin derivative wherein the methionine residue in position 13 of tertiapin is replaced by glutamine, are described. Methods of using these compounds to control insulin secretion, and cardiac rhythm and electrical conduction, to modulate neurotransmissions of neurons, and to induce diuresis in mammals are also provided.

REFERENCES:
patent: 3878297 (1975-04-01), Vick
Hider et al., Biochimica Biophysica Acta, vol. 667 (1981) pp. 197-208.
Jin et al., Biochemistry vol. 38 (Oct. 8, 1999) pp. 14286-14293.
Hider et al. Biochim. Et Biophys. Acta vol. 667 (1981) pp. 197-208.
Habermann (1972) Science vol. 177 pp. 314-322.
Biosequence Searching For The USPO@ (STN International, May 1996) pp. 30-31.
Hider et al., “A comparative Stgructural Study of Apamin and Releated Bee Venom Peptides”,Biochemica Biophysica Acta.1981 667:197-208 [0006-3002].

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