Mouse farnesoid x receptor sequences for use in comparative pharmacology
OwnerJason A. Holt, Jodi Marie Maglich +1inventors
InventorsJason A. Holt, Jodi Marie Maglich, John Tomlin Moore
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Abstract
The present invention provides polynucleotides and polypeptides of the mouse Farnesoid X Receptor (FXR) as well as expression vectors and host cells for expression of the mouse FXR. Also provided are methods for screening for modulators of the mouse FXR and using these modulators in the treatment of FXR related disorders.
Claims25
An isolated farnesoid X receptor polypeptide comprising:
- (a) an amino acid sequence of SEQ ID NO:2;
- (b) a variant of SEQ ID NO:2 which is regulated by endogenous bile acids or regulates bile acid homeostasis via interaction with cytochrome P450 7a (Cyp7a) expression thereby modulating the cholesterol degradation pathway;
- or
- (c) a fragment of (a) or (b) which is regulated by endogenous bile acids or regulates bile acid homeostasis via interaction with cytochrome P450 7a (Cyp7a) expression thereby modulating the cholesterol degradation pathway.
A polynucleotide encoding a farnesoid X receptor which is regulated by endogenous bile acids or regulates bile acid homeostasis via interaction with cytochrome P450 7a (Cyp7a) expression thereby modulating the cholesterol degradation pathway, said polynucleotide comprising:
- (a) a nucleic acid sequence comprising SEQ ID NO:
- 1 or SEQ ID NO:3 or a sequence complimentary thereto;
- (b) a nucleic acid sequence which hybridizes under stringent conditions to the nucleic acid sequence as defined in (a);
- (c) a sequence that is degenerate as a result of the genetic code to a sequence as defined in (a) or (b), but which still encodes a farnesoid X receptor polypeptide which is regulated by endogenous bile acids or regulates bile acid homeostasis via interaction with cytochrome P450 7a (Cyp7a) expression thereby modulating the cholesterol degradation pathway;
- or
- (d) a sequence having at least 80% identity to a sequence as defined in (a), (b) or (c).
A method for the identification of modulators of farnesoid X receptor activity and/or expression comprising:(a) contacting a test substance and a mouse farnesoid X receptor polypeptide or polynucleotide;
- and
- (b) determining an effect of the test substance on activity and/or expression of said polypeptide or polynucleotide.
Dependencies are inferred from the claim text.