UGT1A1 Human Glycosyltransferase Enzymatic LeadHunter Assay - TW

Item: 196000

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

UDP-glucuronosyltransferases (UGT) represents a family of enzymes which catalyze the linkage of glucuronic acid with endobiotic (e.g. steroids and bilirubin) and exobiotic (e.g. drugs and carcinogens) chemical compounds. Glucuronidation is a major Phase II metabolic pathway for the inactivation and excretion of many of the pharmaceutical products currently in use. To date, at least 16 human UGT enzymes have been cloned and sequenced. Like the P450s, individual UGT's have unique, yet overlapping substrate specificities. UGT1A1 (UGT1A) has been reported as specific for estradiol and bilirubin glucuronidation.

Family:

Glycosyltransferase

Sub Family:

UDP Glucuronosyltransferase

Protein Name:

UGT1A1

Uniprot Number:

P22309

Gene Name:

UGT1A1

Gene ID:

54658

Gene Aliases:

UGT1A

Accession Number:

NM_000463

Organism:

Human

Construct Details:

Full Length, Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Spectrofluorimetry

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Human recombinant UDP-glucuronosyltransferases μgT1A1 expressed in insect cells is used. Test compound and/or vehicle is preincubated with 10 μM scopoletin in modified Tris-HCl buffer pH 7.5 for 15 minutes at 25°C. The reaction is initiated by addition of 50 μg/ml enzyme for another 30 minute incubation period. Determination of the amount of scopoletin remained is read spectrofluorimetrically with excitation at 360 nm and emission at 460 nm. Compounds are screened at 10 μM.

Substrate:

10 µM Scopoletin

Incubation:

30 min at 25°C

Control Inhibitor:

Estradiol

Criteria For Significance:

≥ 50% of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 uM

Test Sample Requirements:

Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).

Minimum Order Quantity:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

5757

Name

Estradiol

Measurement

20μM - IC50

Clinical Relevance

Adverse / Beneficial Action:

Inhibition of bilirubin glucuronidation may cause chronic hyperbilirubinemia that can lead to nervous system damage and death; inhibition may also interfere with glucoronidation and elimation of some drugs.

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei