Modulation of the sulfonylurea receptor and calcium in adipocytes for treatment of obesity/diabetes
AssigneeArtecel Sciences, Inc.
InventorsWilliam O. Wilkison, Michael B. Zemel, Naima Moustaid-Moussa
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Abstract
The invention provides methods for determining the ability of compounds to regulate lipogenesis and lipolysis by acting as a sulfonylurea-1 (SUR 1) potassium channel activator, an adipocyte potassium channel activator, an SUR 1 antagonist, and an adipocyte specific SUR 1 antagonist. The present invention recognizes the presence of the sulfonylurea receptor in adipocytes and its utility in identifying compounds and in regulating lipogenesis and lipolysis.
Claims24
A method of determining the ability of a compound to regulate lipogenesis by acting as a sulfonylurea-1 (SUR 1) potassium channel activator, comprising:
- (a) incubating cultured human adipocytes with a SUR 1 agonist in the presence and absence of said compound, and
- (b) comparing the level of at least one lipogenic or anti-lipolytic marker in said adipocytes after incubation in the presence and absence of said compound, wherein a difference in the level of said marker is correlated with the ability of the compound to regulate lipogenesis by acting as a SUR 1 potassium channel activator.
A method of determining the ability of a compound to regulate lipolysis by acing as a sulfonylurea-l (SUR 1) potassium channel activator, comprising:
- (a) incubating cultured human adipocytes with a SUR 1 agonist in the presence and absence of said compound, and
- (b) comparing the level of at least one lipogenic or anti-lipolytic marker in said adipocytes after incubation in the presence and absence of said compound, wherein a difference in the level of said marker is correlated to the ability of the compound to regulate lipolysis by acting as an (SUR 1) potassium channel activator.
A method of determining the ability of a compound to regulate lipogenesis by acting as an adipocyte potassium channel activator, comprising:
- (a) incubating cultured human adipocytes with a SUR 1 agonist in the presence and absence of said compound, and
- (b) comparing the level of at least one lipogenic or anti-lipolytic marker in said adipocytes after incubation in the presence and absence of said compound, wherein a difference in the level of said marker is correlated with the ability of the compound to regulate lipogenesis by acting as an adipocyte potassium channel activator.
A method of determining the ability of a compound to regulate lipolysis by acting as an adipocyte potassium channel activator, comprising:
- (a) incubating cultured human adipocytes with a SUR 1 agonist in the presence and absence of said compound, and
- (b) comparing the level of at least one lipogenic or anti-lipolytic marker in said adipocytes after incubation in the presence and absence of said compound, wherein a difference in the level of said marker is correlated with the ability of the compound to regulate lipolysis by acting as an adipocyte potassium channel activator.
A method of determining the ability of a compound to regulate lipogenesis by acting as an SUR 1 antagonist, comprising:
- (a) incubating cultured human adipocytes with a SUR 1 agonist in the presence and absence of said compound, and
- (b) comparing the level of at least one lipogenic or anti-lipolytic marker in said adipocytes after incubation in the presence and absence of said compound, wherein a difference in the level of said marker is correlated with the ability of the compound to regulate lipogenesis by acting as an SUR 1 antagonist.
A method of determining the ability of a compound to regulate lipolysis by acting as an SUR 1 antagonist, comprising:
- (a) incubating cultured human adipocytes with a SUR 1 agonist in the presence and absence of said compound, and
- (b) comparing the level of at least one lipogenic or anti-lipolytic marker in said adipocytes after incubation in the presence and absence of said compound, wherein a difference in the level of said marker is correlated with the ability of the compound to regulate lipolysis by acting as an SUR 1 antagonist.
A method of determining the ability of a compound to regulate lipogenesis by acting as an adipocyte specific SUR 1 antagonist, comprising:
- (a) incubating cultured human adipocytes with a SUR 1 agonist in the presence and absence of said compound, and
- (b) comparing the level of at least one lipogenic or anti-lipolytic marker in said adipocytes after incubation in the presence and absence of said compound, wherein a difference in tie level of said marker is correlated with the ability of the compound to regulate lipogenesis by acting as an adipocyte specific SUR 1 antagonist.
A method of determining the ability of a compound to regulate lipolysis by acting as an adipocyte specific SUR 1 antagonist, comprising:
- (a) incubating cultured human adipocytes with a SUR 1 agonist in the presence and absence of said compound, and
- (b) comparing the level of at least one lipogenic or anti-lipolytic marker in said adipocytes after incubation in the presence and absence of said compound, wherein a difference in the level of said marker is correlated with the ability of the compound to regulate lipolysis by acting as an adipocyte specific SUR 1 antagonist.
Dependencies are inferred from the claim text.