Biological Information
Background Information:
Cathepsin E (E.C.3.4.23.34) is an intracellular non-lysosomal enzyme, aspartic peptidase of the pepsin family and has a limited cell and tissue distribution such as stomach, lymphoid tissues and urinary bladder. The presence of an N-linked oligosaccharide on cathepsin E indicates that it is glycosylated in the rough ER. Cathepsins D and E play an important role in the degradation of proteins, the generation of bioactive proteins, and antigen processing. Both enzymes are efficient in cleaving Swedish mutant of amyloid precursor protein (APP) at the b site but show almost no reactivity with wide-type APP. Inhibitors of cathepsin E may be immune suppressant.
Family:
Protease
Sub Family:
Pepsin
Class:
Aspartic Peptidase
Protein Name:
Cathepsin E
Uniprot Number:
P14091
Gene Name:
CTSE
Gene ID:
1510
Accession Number:
NM_001910
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 cathepsin E expressed in a murine myeloma NS0 cells is used. Test compound and/or vehicle is preincubated with 330 ng/ml enzyme‡ in modified acetate buffer pH 3.5 for 15 minutes at 25°C. The reaction is initiated by addition of 5 μM Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH2 for another 15 minute incubation period. Determination of the amount of Mca-Pro-Leu-Gly formed is read spectrofluorimetrically at 340 nm/400 nm. Compounds are screened at 10 μM.
Substrate:
5 µM Mca-Pro-Leu-Gly-Leu-Dap-Ala-Arg-NH₂
Incubation:
15 min at 25°C
Control Inhibitor:
Pepstatin
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
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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