US2015072940A1PendingUtilityA1

Treatment of Obesity and Obesity-Related Disorders by Pharmalogical Targeting of Kv 1.3 Potassium Channels

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Assignee: KINETA ONE LLCPriority: Oct 3, 2011Filed: Oct 2, 2012Published: Mar 12, 2015
Est. expiryOct 3, 2031(~5.2 yrs left)· nominal 20-yr term from priority
Inventors:K. George ChandySanjeev Kumar UpadhayayPing WangPaolo Sassone-CorsiKristin Lynn Eckel-MahanShawn P. IadonatoJogesh MukherjeeM. Reza Mirbolooki
A61P 43/00A61P 3/00A61P 3/04C07K 14/43595A61K 38/17A61K 38/1767A61K 38/00A61K 38/16
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Claims

Abstract

Activation of brown adipose tissue, treatment of obesity and/or treatment of obesity-related disorders in human or non-human animal subjects by administering to the subject a potassium channel inhibiting agent. The potassium channel inhibiting agent may comprise ShK toxin or a modified ShK toxin. Examples of modified ShK toxins include ShK-186.

Claims

exact text as granted — not AI-modified
1 - 48 . (canceled) 
     
     
         49 . A method for activation of brown adipose tissue, treating obesity or treating an obesity-related disorder in a human or animal subject, said method comprising the steps of administering to the subject an agent which inhibits potassium channels. 
     
     
         50 . A method according to  claim 49  wherein the agent comprises the ShK toxin (SEQ ID NO:1) 
     
     
         51 . A method according to  claim 49  wherein the agent comprises a modified ShK toxin selected from: SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO:4, SEQ ID NO:5, SEQ ID NO:6 or SEQ ID NO:7. 
     
     
         52 . A method according to  claim 49  wherein the agent comprises an ShK toxin attached to a chemical entity. 
     
     
         53 . A method according to  claim 52  wherein the chemical entity attached to ShK toxin is selected from: AEEAc-L-Tyr(PO 3 H 2 ), AEEAc-L-Pmp(OH 2 ), AEEAc-D-Pmp(OH 2 ), AEEAc-D-Pmp(OH, Et), AEEAc-L-Pmp(Et 2 ), AEEAc-D-Pmp(Et 2 ), AEEAc-L-Tyr, AEEAc-L-Phe(p-NH 2 ), AEEAc-L-Phe(p-CO 2 H), AEEAc-L-Aspartate, AEEAc-D-Aspartate, AEEAc-L-Glutamate, or AEEAc-D-Glutamate 
     
     
         54 . A method according to  claim 49  wherein said chemical entity is attached to the N-terminal residue of ShK. 
     
     
         55 . A method according to  claim 49  wherein the ShK toxin is obtained from a natural source. 
     
     
         56 . A method according to  claim 49  wherein the ShK toxin is synthetic. 
     
     
         57 . A method according to  claim 52  wherein the chemical entity includes a fluorophore tag. 
     
     
         58 . A method according to  claim 52  wherein the chemical entity attached to ShK toxin comprises AEEAc-L-Pmp(OH 2 ). 
     
     
         59 . A method according to  claim 52  wherein the chemical entity attached to ShK toxin comprises AEEAc-D-Pmp(OH 2 ). 
     
     
         60 . A method according to  claim 52  wherein the chemical entity attached to ShK toxin comprises AEEAc-D-Pmp(OH, Et). 
     
     
         61 . A method according to  claim 52  wherein the chemical entity attached to ShK toxin comprises AEEAc-L-Pmp(Et 2 ). 
     
     
         62 . A method according to  claim 52  wherein the chemical entity attached to ShK toxin comprises AEEAc-D-Pmp(Et 2 ). 
     
     
         63 . A method according to  claim 52  wherein the chemical entity attached to ShK toxin comprises AEEAc-L-Tyr. 
     
     
         64 . A method according to  claim 52  wherein the chemical entity attached to ShK toxin comprises AEEAc-L-Phe(p-NH 2 ). 
     
     
         65 . A method according to  claim 52  wherein the chemical entity attached to ShK toxin comprises AEEAc-L-Phe(p-CO 2 H). 
     
     
         66 . A method according to  claim 52  wherein the chemical entity attached to ShK toxin comprises AEEAc-L-Aspartate. 
     
     
         67 . A method according to  claim 52  wherein the chemical entity attached to ShK toxin comprises AEEAc-D-Aspartate. 
     
     
         68 . A method according to  claim 52  wherein the chemical entity attached to ShK toxin comprises AEEAc-L-Glutamate. 
     
     
         69 . A method according to  claim 52  wherein the chemical entity attached to ShK toxin AEEAc-D-Glutamate. 
     
     
         70 . A method according to  claim 49  wherein the agent inhibits Kv1.3 potassium channels. 
     
     
         71 . A method according to  claim 49  wherein the agent selectively inhibits Kv1.3 more than Kv1.1 potassium channels. 
     
     
         72 . A method according to  claim 49  wherein the chemical entity attached to ShK toxin further comprises proteins in-frame or polyethylene glycols of differing sizes.

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