Biological Information
Background Information:
LMPTP (low molecular weight phosphotyrosine protein phosphatase) is a ubiquitously expressed protein tyrosine phosphatase involved in the modulation of signal transduction by the insulin, platelet derived growth factor (PDGF), and T-cell receptors. The ACP-1 (acid phosphatase ) gene encodes three transcriptional variants (A, B, and C) of LMPTP; the resulting proteins of which are distinct enzyme isoforms with unique chemical properties and activity. Human LMPTP polymorphisms that confer below-normal enzyme activity (i.e. AA or AB allele carriers) are associated with allergic atopic eczema/dermatitis syndrome (AEDS), obesity, diabetes, dyslipidemia and rheumatoid arthritis. Further, total serum IgE levels are lower in carriers of the ACP-1 genotype (CB), which confers above-normal enzyme activity. Over expression of LMPTP enzyme in cells transformed by PTK oncogenes leads to decreased proliferation indicating a possible role in preventing cancer cell proliferation. Therefore, inhibition of LMPTP-B may exacerbate the above noted disease states.
Family:
Phosphatase
Sub Family:
Acid Phosphatase
Class:
Protein Tyrosine
Protein Name:
ACP1
Uniprot Number:
P24666
Protein Aliases:
acid phosphatase of erythrocyte|low molecular weight phosphotyrosine protein phosphatase|red cell acid phosphatase
Gene Name:
ACP1
Gene ID:
52
Gene Aliases:
HAAP|LMW-PTP
Accession Number:
NM_004300
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 protein phosphatase LMPTP-B expressed in E. coli is used. Test compound and/or vehicle is preincubated with 2.2 U/ml enzyme‡ for 15 minutes at 37°C in modified HEPES buffer pH 7.2. The reaction is initiated by addition of 100 µM DiFMUP for 60 minutes. Determination of the amount of DiFMU formed is read spectrofluorimetrically at 358 nm/450 nm. Compounds are screened at 10 µM.
Substrate:
100 µM DiFMUP
Incubation:
60 min at 37°C
Control Inhibitor:
(NH₄)₆Mo₇O₂₄
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:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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