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BioAssay: AID 2818

Summary assay for identification of inhibitors of mouse intestinal alkaline phosphatase

Alkaline phosphatase (EC 3.1.3.1) (APs) catalyze the hydrolysis of phosphomonoesters, releasing inorganic phosphate and alcohol. APs are dimeric enzymes found in most organisms. In human, four isozymes of APs have been identified. One isozyme is tissue-nonspecific (designated TNAP) and three other isozymes are tissue-specific and named according to the tissue of their predominant expression: more ..
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AID: 2818
Data Source: Burnham Center for Chemical Genomics (BCCG-A357-Mouse_IAP_Inhibitor-Summary-Assay)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2010-05-07
Modify Date: 2011-02-03
Target
Depositor Specified Assays
Show more
AIDNameTypeComment
2806uHTS Luminescent assay for identification of inhibitors of mouse intestinal alkaline phosphatasescreeningPrimary Screen
493135SAR analysis of small molecule inhibitors of mouse intestinal alkaline phosphatase via a luminescent assayconfirmatory
493136SAR analysis of small molecule inhibitors of Mouse Intestinal Alkaline Phosphatase using Placental Alkaline Phosphataseconfirmatory
493144SAR analysis of small molecule inhibitors of Mouse Intestinal Alkaline Phosphatase using Human Intestinal Alkaline Phosphataseconfirmatory
493148SAR analysis of small molecule inhibitors of Mouse Intestinal Alkaline Phosphatase using Tissue Nonspecific Alkaline Phosphatase.confirmatory
434971Single concentration confirmation of uHTS hits from a small molecule inhibitors of mouse intestinal alkaline phosphatase via a luminescent assayscreening
488785Dose Response confirmation of uHTS hits from a small molecule inhibitors of mouse intestinal alkaline phosphatase via a luminescent assayconfirmatory
488876Dose Response confirmation of uHTS inhibitors of Mouse Intestinal Alkaline Phosphatase using Human Intestinal Alkaline Phosphataseconfirmatory
488879Dose Response confirmation of uHTS inhibitors of Mouse Intestinal Alkaline Phosphatase using Placental Alkaline Phosphataseconfirmatory
488906Dose Response confirmation of uHTS inhibitors of Mouse Intestinal Alkaline Phosphatase using Tissue Nonspecific Alkaline Phosphatase.confirmatory
588639SAR analysis of small molecule inhibitors of Mouse Intestinal Alkaline Phosphatase using Tissue Nonspecific Alkaline Phosphatase - Set 2confirmatory
588641SAR analysis of small molecule inhibitors of Mouse Intestinal Alkaline Phosphatase using Placental Alkaline Phosphatase - Set 2confirmatory
588645SAR analysis of small molecule inhibitors of Mouse Intestinal Alkaline Phosphatase using Human Intestinal Alkaline Phosphatase - Set 2confirmatory
588647SAR analysis of small molecule inhibitors of mouse intestinal alkaline phosphatase via a luminescent assay - Set 2confirmatory
Description:
Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG)
Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego, CA)
Network: NIH Molecular Probe Production Centers Network (MLPCN)
Grant Proposal Number: X01-MH077602-01
Assay Provider: Dr. Jose Luis Millan, Sanford-Burnham Medical Research Institute, San Diego, CA.

Alkaline phosphatase (EC 3.1.3.1) (APs) catalyze the hydrolysis of phosphomonoesters, releasing inorganic phosphate and alcohol. APs are dimeric enzymes found in most organisms. In human, four isozymes of APs have been identified. One isozyme is tissue-nonspecific (designated TNAP) and three other isozymes are tissue-specific and named according to the tissue of their predominant expression: intestinal (IAP), placental (PLAP) and germ cell (GCAP) alkaline phosphatases. IAP expression is largely restricted to the gut, especially to the epithelial cells (enterocytes) of the small intestinal mucosa. The exact biological function of IAP is unknown.

The goal of this project is to identify novel and specific inhibitors of mouse IAP. IAP is inhibited by a number of inhibitors (1). They include L-phenylalanine, (2, 3), L-tryptophan (4), L-leucine and phenylalanine-glycylglycine (5). While the biological implications of this inhibition are not known, these inhibitors have proven to be useful in the differential determination of AP isozymes as important diagnostic markers in many diseases. However, these known inhibitors of IAP are not entirely specific for IAP isozyme and have milllimolar affinity. In addition, they are common aminoacids that are ubiquitously present in the tissues and involved in diverse metabolic pathways, and therefore, are not appropriate tools for biological studies. Thus, the aim of this MLSCN probe project is to obtain novel chemical scaffolds that can be used as chemical probes.
Protocol
Please see pertinent AIDs: 2806, 493135, 493136, 493144, 493148


Comment
Probe molecules are defined as the positives of this assay and assigned a score of 100. Testing has not progressed to the point where a probe molecule has been identified.
Additional Information
Grant Number: X01-MH077602-01

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