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Volumn 13, Issue 11, 2003, Pages 1891-1895

N-Isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists

Author keywords

[No Author keywords available]

Indexed keywords

BETA1 INTEGRIN; N ISONICOTINOYL 4 AMINOPHENYLALANINE; PHENYLALANINE DERIVATIVE; UNCLASSIFIED DRUG;

EID: 12444302271     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00308-1     Document Type: Article
Times cited : (14)

References (19)
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    • (a) Abraham W.M., Sielczak M.W., Ahmed A., Cortes A., Lauredo I.T., Kim J., Pepinsky B., Benjamin C.D., Leone D.R., Lobb R.R., Weller P.F. J. Clin. Invest. 93:1994;776 (b) Milne A.A.Y., Piper P.J. Eur. J. Pharmacol. 282:1995;243.
    • (1995) Eur. J. Pharmacol. , vol.282 , pp. 243
    • Milne, A.A.Y.1    Piper, P.J.2
  • 3
    • 0026506799 scopus 로고
    • (a) Yednock T.A., Cannon D., Fritz L.C. Nature. 356:1992;63 (b) Keszthelyi E., Karlik S., Hyduk S., Rice A., Gordon G., Yednock T., Horner H. Neurology. 47:1996;1053.
    • (1992) Nature , vol.356 , pp. 63
    • Yednock, T.A.1    Cannon, D.2    Fritz, L.C.3
  • 12
    • 85031175948 scopus 로고    scopus 로고
    • 35S-2, binding buffer and test compound. The plates were incubated at room temperature for 30 min. The assay suspension was filtered using a vacuum apparatus, and the plates were washed once with 100 μL of binding buffer. The plates were then transferred to Packard Multiscreen adapter plates (Cat# 6005178) and 100 μL of MicroScint-20 was added to the wells. Radioactive counts were quantified in a Packard Topcount. Data Analysis was performed using the MRLCalc algorithm.
  • 13
    • 85031175213 scopus 로고    scopus 로고
    • 125I-17 and were further incubated at 37 °C for 2, 15, 30, 45, 60 and up to 180 min. Cells were collected by filtering at each time point and washed two times with 200 μL of cold binding buffer containing the appropriate cations. The plates were then transferred to Packard Multiscreen adapter plates (Cat# 6005178) and 100 μL of MicroScint-20 was added to the wells. The radioactivity associated with the cells was measured in a Packard Topcount. Cells incubated with 1% dimethyl sulfoxide were used as positive control and cells incubated with 10 μM unlabeled 17 were served as the negative control (non-specific background). The amount of non-specific radioactivity associated with the negative control cells was subtracted from all observations. The amount of radioactivity associated with the positive control cell was equated to 0% bound receptor sites. Receptor occupancy (% bound) of test compound was determined from the positive cell control. The data is the mean of duplicates.
  • 18
    • 85031176593 scopus 로고    scopus 로고
    • 2 in the presence or absence of TS2/16. The plates were then transferred to Packard Multiscreen adapter plates (Cat# 6005178) and 100 μL of MicroScint-20 was added to the wells. Radioactive counts were quantified in a Packard Topcount. Data analysis was performed using the MRLCalc algorithm.


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