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Volumn 17, Issue 2, 2007, Pages 507-510

Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor

Author keywords

Dipeptidyl peptidase

Indexed keywords

AX 8819; AZABICYCLO[3.3.0]OCTANE; DIPEPTIDYL PEPTIDASE II INHIBITOR; ENZYME INHIBITOR; OCTANE; UNCLASSIFIED DRUG;

EID: 33846101646     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.10.012     Document Type: Article
Times cited : (17)

References (27)
  • 22
    • 33846070032 scopus 로고    scopus 로고
    • note
    • 2, 2 mM EDTA, 10 mM KCl, 0.1% Nonidet P-40, 5 μg/ml antipain, and 5 μg/ml leupeptin) for 30 min at 4 °C. DPP activity was measured using the fluorogenic substrate AP-AFC (2 mM in 50 mM Hepes buffer, pH 7.5) on an Fmax fluorescence plate reader (Molecular Devices, Menlo Park, CA) excitation, 410 nm; emission, 510 nm. The specificity of compounds was investigated by treating untransfected HEK cells with the same concentration of compound that inhibited approximately half of the overexpressed DPP II activity (293T HEK column).
  • 23
    • 33846078344 scopus 로고    scopus 로고
    • note
    • 6 PBMCs in 0.5 ml of culturing media were plated in 24-well flat-bottomed plates in triplicate and treated with VbP at final concentration 10 μM DMSO (vehicle control), and AX8819 at 4.4, 8.8, 22, and 44 μM final concentrations. Cells were washed twice with PBS and were stained with 2 μl AnV-Allophycocyanin (APC) in 50 μl of Annexin V binding buffer for 15 min on ice, after that 350 μl FACS buffer (phosphate-buffered saline (PBS) supplemented with 1% FBS and 0.01% sodium azide) and PI (propidium iodide 10 μg/ml) were added. Experiments were repeated at least twice. PBMCs from different individuals were used to confirm the reproducibility of results.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.