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Volumn 19, Issue 8, 2009, Pages 2299-2304

Inhibitors of potassium channels KV1.3 and IK-1 as immunosuppressants

Author keywords

Autoimmune diseases; Homology model; IK 1; KV1.3; Potassium channel; vHTS

Indexed keywords

CLOTRIMAZOLE; IMMUNOSUPPRESSIVE AGENT; OXAZOLONE; POTASSIUM CHANNEL BLOCKING AGENT; POTASSIUM CHANNEL IK 1; POTASSIUM CHANNEL IK 1 BLOCKING AGENT; POTASSIUM CHANNEL KV1.3; POTASSIUM CHANNEL KV1.3 BLOCKING AGENT; UNCLASSIFIED DRUG;

EID: 63149154393     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.02.077     Document Type: Article
Times cited : (52)

References (36)
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    • V1.3 patch clamp assay, see: whole cell patch clamp recording was performed with n ≥ 2 individual experiments at each compound concentration using different cells. Four or more different concentrations were determined per dose-response curve
    • V1.3 patch clamp assay, see:. Grissmer S., Nguyen A.N., Aiyar J., Hanson D.C., Mather R.J., Gutman G.A., Karmilowicz M.J., Auperin D.D., and Chandy K.G. Mol. Pharmacol. 45 (1994) 1227 whole cell patch clamp recording was performed with n ≥ 2 individual experiments at each compound concentration using different cells. Four or more different concentrations were determined per dose-response curve
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    • Grissmer, S.1    Nguyen, A.N.2    Aiyar, J.3    Hanson, D.C.4    Mather, R.J.5    Gutman, G.A.6    Karmilowicz, M.J.7    Auperin, D.D.8    Chandy, K.G.9
  • 24
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    • note
    • 2+ concentration was adjusted to 1 μM. Whole cell patch clamp recording was performed with n ≥ 2 individual experiments at each compound concentration using different cells. Four or more different concentrations were determined per dose-response curve.
  • 27
    • 40849089294 scopus 로고    scopus 로고
    • A general PBMC assay setup is described in (a), the readout was performed using BrdU Cell proliferation ELISA kit (Roche) according to manufacturer's instructions
    • Cianci J., Baell J.B., Flynn B.L., Gable R.W., Mould J.A., Paul D., and Harvey A.J. Bioorg. Med. Chem. Lett. 18 (2008) 2055 A general PBMC assay setup is described in (a), the readout was performed using BrdU Cell proliferation ELISA kit (Roche) according to manufacturer's instructions
    • (2008) Bioorg. Med. Chem. Lett. , vol.18 , pp. 2055
    • Cianci, J.1    Baell, J.B.2    Flynn, B.L.3    Gable, R.W.4    Mould, J.A.5    Paul, D.6    Harvey, A.J.7
  • 28
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    • 5 cell/mL and incubated with the compounds or the corresponding amount of vehicle (DMSO) for 30 min. Intracellular calcium increase was induced with 25 μM thapsigargin (Sigma-Aldrich) and was measured using FACSCalibur (BD Bioscience). For the importance of calcium signaling in T-cell proliferation, see:
    • 5 cell/mL and incubated with the compounds or the corresponding amount of vehicle (DMSO) for 30 min. Intracellular calcium increase was induced with 25 μM thapsigargin (Sigma-Aldrich) and was measured using FACSCalibur (BD Bioscience). For the importance of calcium signaling in T-cell proliferation, see:. Vig M., and Kinet J.-P. Nat. Immunol. 10 (2009) 21
    • (2009) Nat. Immunol. , vol.10 , pp. 21
    • Vig, M.1    Kinet, J.-P.2
  • 30
    • 63149168089 scopus 로고    scopus 로고
    • note
    • HaCaT keratinocytes were seeded in KBM/10% FCS and incubated for 24 h at 37 °C. Compounds were diluted in KBM/FCS with a final concn of 1% DMSO, added to the HaCaTs in triplicate and incubated for 48 h. For a readout on cell numbers, the Cell Titer Viability Assay from Promega was used.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.