PPARγ LBD (human recombinant)

Cayman Chemical Item Number 10007941

Peroxisome Proliferator-activated Receptor γ Ligand Binding Domain

Description

Source: recombinant N-terminal hexahistidine-tagged protein expressed in E. coli · M_r: ~34 kDa · The peroxisome proliferator activated receptor (PPAR) family of ligand-activated transcription factors consists of three subtypes encoded by separate genes: PPARα, PPARδ (also referred to as hNUC1, PPARβ, or FAAR), and PPARγ.¹ Among them PPARγ is the most widely studied and has been implicated in the pathology of numerous diseases including obesity, diabetes, atherosclerosis, and cancer.^1,2 Structurally, PPARγ can be described by two primary domains - a ligand binding domain (LBD) and a DNA binding domain (DBD).^2,3 Binding of activating ligands to the LBD promotes heterodimerization with retinoic acid-like receptor (RXR) resulting in the regulated expression of target genes, a significant number of which are related to lipid metabolism.¹ Select members of the thiazolidinedione class of PPARγ ligands, which includes rosiglitazone and pioglitazone, are currently used for the treatment of insulin resistance associated with type II diabetes.⁴ Cayman’s PPARγ LBD is expressed and purified from E. coli. The purity was determined using gel electrophoresis followed by coomassie staining and western blot analysis using a PPARγ polyclonal antibody. The functionality was tested using a fluorescent ligand binding assay.

1 Kersten, S., Desvergne, B., and Wahli, W. Roles of PPARs in health and disease. Nature 405 421-424 (2000).

2 Rosen, E.D., and Spiegelman, B.M. PPAR.gamma: A nuclear regulator of metabolism differentiation, and cell growth. J Biol Chem 276(1) 37731-37734 (2001).

3 Uppenberg, J., Svensson, C., Jaki, M., et al. Crystal structure of the ligand binding domain of the human nuclear receptor PPARγ. J Biol Chem 273 31108-31112 (1998).

4 Mudaliar, S., and Henry, R.R. New oral therapies for type 2 diabetes mellitus: The glitazones or insulin sensitizers. Annu Rev Med 52 239-257 (2001).

Synonyms

Peroxisome Proliferator-activated Receptor γ Ligand Binding Domain

Formulation

A solution in 50 mM sodium phosphate, pH 7.2, containing 20% glycerol, 150 mM sodium chloride, and 1 mM DTT

Purity

≥90%

Stability

6 months

Storage

-80°C

Shipping

Dry ice in continental US; may vary elsewhere

Background Reading

Kersten, S., Desvergne, B., and Wahli, W. Roles of PPARs in health and disease. Nature 405 421-424 (2000).

Rosen, E.D., and Spiegelman, B.M. PPAR.gamma: A nuclear regulator of metabolism differentiation, and cell growth. J Biol Chem 276(1) 37731-37734 (2001).

Mudaliar, S., and Henry, R.R. New oral therapies for type 2 diabetes mellitus: The glitazones or insulin sensitizers. Annu Rev Med 52 239-257 (2001).

Uppenberg, J., Svensson, C., Jaki, M., et al. Crystal structure of the ligand binding domain of the human nuclear receptor PPARγ. J Biol Chem 273 31108-31112 (1998).

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25 µg 
$118.00

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50 µg 
$224.00

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100 µg 
$425.00

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PPARγ LBD (human recombinant)