Aromatase Inhibitor Screening Kit ab284522 enables rapid screening of drugs and other small molecules for compound-Aromatase interaction in a reliable, high-throughput fluorescence-based assay.
Individual kit components also available for purchase with a minimum order of 20 units. Contact us to discuss your needs.
Images
Key facts
- Detection method
Fluorescent
- Sample types
Inhibitor compounds
- Assay type
Enzyme activity (quantitative)
Target data
Function
A cytochrome P450 monooxygenase that catalyzes the conversion of C19 androgens, androst-4-ene-3,17-dione (androstenedione) and testosterone to the C18 estrogens, estrone and estradiol, respectively (PubMed:27702664, PubMed:2848247). Catalyzes three successive oxidations of C19 androgens: two conventional oxidations at C19 yielding 19-hydroxy and 19-oxo/19-aldehyde derivatives, followed by a third oxidative aromatization step that involves C1-beta hydrogen abstraction combined with cleavage of the C10-C19 bond to yield a phenolic A ring and formic acid (PubMed:20385561). Alternatively, the third oxidative reaction yields a 19-norsteroid and formic acid. Converts dihydrotestosterone to delta1,10-dehydro 19-nordihydrotestosterone and may play a role in homeostasis of this potent androgen (PubMed:22773874). Also displays 2-hydroxylase activity toward estrone (PubMed:22773874). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (CPR; NADPH-ferrihemoprotein reductase) (PubMed:20385561, PubMed:22773874).
Alternative names
Aromatase, CYPXIX, Cytochrome P-450AROM, Cytochrome P450 19A1, Estrogen synthase, CYP19, CYP19A1, ARO1, CYAR
What's included?
Recommended products
Aromatase Inhibitor Screening Kit ab284522 enables rapid screening of drugs and other small molecules for compound-Aromatase interaction in a reliable, high-throughput fluorescence-based assay.
Individual kit components also available for purchase with a minimum order of 20 units. Contact us to discuss your needs.
Alternative names
Aromatase, CYPXIX, Cytochrome P-450AROM, Cytochrome P450 19A1, Estrogen synthase, CYP19, CYP19A1, ARO1, CYAR
Key facts
- Detection method
Fluorescent
- Sample types
Inhibitor compounds
- Assay type
Enzyme activity (quantitative)
- Assay Platform
Microplate reader, Fluorescence microscope
Storage
- Shipped at conditions
Blue Ice
- Appropriate short-term storage conditions
-20°C
- Appropriate long-term storage conditions
-20°C
- Storage information
-20°C
Notes
The Aromatase Inhibitor Screening Kit (ab284522) (K984) 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.
This product is manufactured by BioVision, an Abcam company and was previously called K984 Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric). K984-100 is the same size as the 100 test size of ab284522.
Supplementary info
This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
Aromatase also known as CYP19A is an enzyme responsible for the conversion of androgens into estrogens. It is a member of the cytochrome P450 superfamily and has a molecular mass of approximately 58 kDa. Aromatase is mainly expressed in the gonads brain adipose tissue and placenta. The activity of this enzyme is important for estrogen biosynthesis which is especially important in postmenopausal women where adipose tissue becomes an important estrogen source.
- Biological function summary
The enzyme catalyzes the aromatization of androgens aiding in the production of estrogens like estradiol. This process is essential for maintaining estrogen levels in the human body. Aromatase operates as a monomer and does not form part of any larger complex. The balance of androgens and estrogens maintained by aromatase activity plays a significant role in reproductive functions and other physiological processes.
- Pathways
Aromatase enzyme activity plays a pivotal role in the steroidogenesis pathway which involves the biosynthesis of steroid hormones. It is also a part of the estrogen signaling pathway interacting with other proteins like estrogen receptors. These pathways help regulate gene expression and are important in processes such as cell proliferation and differentiation linking aromatase function to broader metabolic and developmental effects.
- Associated diseases and disorders
Aromatase has a significant role in conditions such as hormone receptor-positive breast cancer and endometriosis. In breast cancer increased aromatase activity elevates estrogen levels promoting cancer cell growth. Anti-aromatase drugs like aromatase inhibitors target this enzyme to lower estrogen production. Additionally defects in aromatase activity can lead to disorders like aromatase deficiency resulting in an imbalance in sex hormone levels. Understanding its function aids in the development of therapies targeting proteins like the estrogen receptor which interacts with products of aromatase activity.
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3 product images
Functional Studies - Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric) (ab284522)
Functional Studies - Aromatase standard curve.
Aromatase Substrate metabolite fluorescence standard curve. One mole of fluorescence standard corresponds to the metabolism of one mole of Aromatase Substrate.
Functional Studies - Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric) (ab284522)
Functional Studies - Reaction kinetics of recombinant human aromatase.
Reaction kinetics of recombinant human aromatase enzyme at 37°C in the presence and absence of the indicated aromatase inhibitors. The solvent control reaction contained assay buffer with 0.2% acetonitrile.
Functional Studies - Aromatase (CYP19A) Inhibitor Screening Kit (Fluorometric) (ab284522)
Functional studies - Dose-response curves for various aromatase ligands.
Dose-response curves for various aromatase ligands of differing structural and mechanistic classes. The potent competitive inhibitor letrozole, the mechanism-based irreversible inhibitor exemestane, the phytoestrogen-like synthetic flavonoid α-naphthoflavone and the antifungal ketoconazole (a competitive inhibitor of several CYP isoforms) are plotted in the graph. For dose-response curves, percent activity was calculated for each concentration of inhibitor by comparison to activity of reactions containing no inhibitor. For each inhibitor, IC50 values were derived by 4-parameter logistic curve fitting with each point representing the mean ± SEM of at least four replicates. Assays were performed according to the kit protocol.
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