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Description
High-throughput compatible, quick and easy screening for Aromatase inhibitors or ligands; Includes human Aromatase.
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Summary
• Detection method - Fluorescence (Ex/Em 488/527 nm) • Species reactivity - Eukaryotes • Applications - • Rapid assessment of native/recombinant Aromatase activity in lysates or microsomal fractions prepared from tissues, cells. • Development of structure-activity relationship (SAR) models to predict aromatase inhibition liability of novel compounds and analogues. • Prediction of aromatase-dependent endocrine disruption potential for novel compounds.
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Detection Method
Fluorescence (Ex/Em 488/527 nm)
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Species Reactivity
Eukaryotes
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Applications
Rapid, high-throughput screening of drugs and novel ligands. Development of structure-activity relationship (SAR) models to predict Aromatase inhibition liability of novel compounds. Prediction of adverse drug-drug interaction potential and bioavailability for compounds metabolized by Aromatase.
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Sample Type
Samples containing drugs, inhibitors or ligands (compounds that can interact and affect Aromatase activity)
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Features Benefits
• Simple, highly sensitive, high-throughput compatible • Rapid screening of Aromatase inhibitors or ligands • Kit includes the Aromatase inhibitor (Letrozole) and a stable, recombinant human Aromatase
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Storage Conditions
-20°C
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Shipping Conditions
gel pack
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Shelf life
12 months
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Background
Aromatase (CYP19A, EC 1.14.14.14) is a member of the cytochrome P450 monooxidase (CYP) family of microsomal xenobiotic metabolism enzymes. Aromatase plays a critical role in steroidogenesis, catalyzing the conversion of androgenic hormones into estrogens. The enzyme is expressed in high levels in reproductive tissues, placenta, brain and adipose tissue and is responsible for mammalian sexual dimorphism and development of secondary sexual characteristics. Inhibitors of aromatase are used to treat estrogen-dependent breast cancer, as estrogens promote the expression of peptide growth factors responsible for tumorigenesis. Aromatase activity and expression can be affected by many organic environmental pollutants such as pesticides and plasticizers. Such compounds, known as endocrine disruptors, are suspected of causing precocious puberty, obesity, infertility and various cancers. BioVision’s Aromatase Inhibitor Screening Kit enables rapid screening of drugs and other small molecules for compound-Aromatase interaction in a reliable, high-throughput fluorescence-based assay. The assay utilizes a fluorogenic substrate that is converted into a highly fluorescent metabolite detected in the visible range (Ex/Em = 488/527 nm), ensuring a high signal-to-background ratio with little interference by autofluorescence. The kit contains a complete set of reagents sufficient for performing 100 reactions in a 96-well plate format.
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Additional description
Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.
