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Volumn 6, Issue 8, 2011, Pages 845-856

Selective inhibition of the K ir2 family of inward rectifier potassium channels by a small molecule probe: The discovery, SAR, and pharmacological characterization of ML133

Author keywords

[No Author keywords available]

Indexed keywords

CELASTROL; CHLOROQUINE; GAMBOGIC ACID; INWARDLY RECTIFYING POTASSIUM CHANNEL SUBUNIT KIR2.1; MEPYRAMINE; ML 133; ML133; POTASSIUM CHANNEL BLOCKING AGENT; TAMOXIFEN; THIOPENTAL; UNCLASSIFIED DRUG;

EID: 80052015441     PISSN: 15548929     EISSN: 15548937     Source Type: Journal    
DOI: 10.1021/cb200146a     Document Type: Article
Times cited : (85)

References (41)
  • 1
    • 0033694834 scopus 로고    scopus 로고
    • Ion channels and synaptic organization: Analysis of the Drosophila genome
    • Littleton, J. T. and Ganetzky, B. (2000) Ion channels and synaptic organization: analysis of The Drosophila genome Neuron 26, 35-43
    • (2000) Neuron , vol.26 , pp. 35-43
    • Littleton, J.T.1    Ganetzky, B.2
  • 2
    • 0001108204 scopus 로고    scopus 로고
    • Potassium Channels and Chloride Channels
    • in, pp, Sinauer, Sunderland, MA.
    • Hille, B. (2001) Potassium Channels and Chloride Channels, in Ion Channels of Excitable Membranes, pp 131-168, Sinauer, Sunderland, MA.
    • (2001) Ion Channels of Excitable Membranes , pp. 131-168
    • Hille, B.1
  • 4
    • 34548363326 scopus 로고    scopus 로고
    • Biophysical, pharmacological, and functional characteristics of cloned and native mammalian two-pore domain K+ channels
    • DOI 10.1007/s12013-007-0007-8
    • Lotshaw, D. P. (2007) Biophysical, pharmacological, and functional characteristics of cloned and native mammalian two-pore domain K+ channels Cell Biochem. Biophys. 47, 209-56 (Pubitemid 47338363)
    • (2007) Cell Biochemistry and Biophysics , vol.47 , Issue.2 , pp. 209-256
    • Lotshaw, D.P.1
  • 6
    • 74949143771 scopus 로고    scopus 로고
    • Inwardly rectifying potassium channels: Their structure, function, and physiological roles
    • Hibino, H., Inanobe, A., Furutani, K., Murakami, I. F., and Kurachi, Y. (2010) Inwardly rectifying potassium channels: their structure, function, and physiological roles Physiol. Rev. 90 (1) 291-366
    • (2010) Physiol. Rev. , vol.90 , Issue.1 , pp. 291-366
    • Hibino, H.1    Inanobe, A.2    Furutani, K.3    Murakami, I.F.4    Kurachi, Y.5
  • 8
    • 0032751084 scopus 로고    scopus 로고
    • Channelopathies of inwardly rectifying potassium channels
    • Abraham, M. R., Jahangir, A., Alekseev, A. E., and Terzic, A. (1999) Channelopathies of inwardly rectifying potassium channels FASEB J. 13 (14) 1901-1910 (Pubitemid 29517620)
    • (1999) FASEB Journal , vol.13 , Issue.14 , pp. 1901-1910
    • Abraham, M.R.1    Jahangir, A.2    Alekseev, A.E.3    Terzic, A.4
  • 9
    • 56149096227 scopus 로고    scopus 로고
    • Inward rectifier potassium currents as a target for atrial fibrilation therapy
    • Ehrlich, J. R. (2008) Inward rectifier potassium currents as a target for atrial fibrilation therapy J. Cardiovasc. Pharmacol. 52, 129-135
    • (2008) J. Cardiovasc. Pharmacol. , vol.52 , pp. 129-135
    • Ehrlich, J.R.1
  • 10
    • 77953405501 scopus 로고    scopus 로고
    • Small-molecule modulaotrs of inward rectifier K+ channels: Recent advances and future possibilities
    • Bhave, G., Lonergan, D., Chauder, B. A., and Denton, J. S. (2010) Small-molecule modulaotrs of inward rectifier K+ channels: recent advances and future possibilities Future Med. Chem. 2 (5) 757-774
    • (2010) Future Med. Chem. , vol.2 , Issue.5 , pp. 757-774
    • Bhave, G.1    Lonergan, D.2    Chauder, B.A.3    Denton, J.S.4
  • 11
    • 0034792673 scopus 로고    scopus 로고
    • Potassium channels of glial cells: Distribution and function
    • Horio, Y. (2001) Potassium channels of glial cells: distribution and function Jpn. J. Pharmacol. 87 (1) 1-6
    • (2001) Jpn. J. Pharmacol. , vol.87 , Issue.1 , pp. 1-6
    • Horio, Y.1
  • 12
    • 33644519960 scopus 로고    scopus 로고
    • Astrocyte dysfunction in neurological disorders: A molecular perspective
    • DOI 10.1038/nrn1870, PII N1870
    • Seifert, G., Schilling, K., and Steinhauser, C. (2006) Astrocyte dysfunction in neurological disorders: a molecular perspective Nat. Rev. Neurosci. 7 (3) 194-206 (Pubitemid 43292465)
    • (2006) Nature Reviews Neuroscience , vol.7 , Issue.3 , pp. 194-206
    • Seifert, G.1    Schilling, K.2    Steinhauser, C.3
  • 15
  • 17
    • 33646851612 scopus 로고    scopus 로고
    • Chronic inhibition of cardiac Kir2.1 and hERG potassium channels by celastrol with dual effects on both ion conductivity and protein trafficking
    • DOI 10.1074/jbc.M600072200
    • Sun, H., Liu, X., Xiong, Q., Shikano, S., and Li, M. (2006) Chronic inhibition of cardiac Kir2.1 and HERG potassium channels by celastrol with dual effects on both ion conductivity and protein trafficking J. Biol. Chem. 281 (9) 5877-5884 (Pubitemid 43847688)
    • (2006) Journal of Biological Chemistry , vol.281 , Issue.9 , pp. 5877-5884
    • Sun, H.1    Liu, X.2    Xiong, Q.3    Shikano, S.4    Li, M.5
  • 18
    • 67650115847 scopus 로고    scopus 로고
    • Specific and slow inhibition of the kir2.1 K+ channel by gambogic acid
    • Zaks-Makhina, E., Li, H., Grishin, A., Salvador-Recatala, V., and Levitan, E. S. (2009) Specific and slow inhibition of the kir2.1 K+ channel by gambogic acid J. Biol. Chem. 284 (23) 15432-15438
    • (2009) J. Biol. Chem. , vol.284 , Issue.23 , pp. 15432-15438
    • Zaks-Makhina, E.1    Li, H.2    Grishin, A.3    Salvador-Recatala, V.4    Levitan, E.S.5
  • 19
    • 1642576972 scopus 로고    scopus 로고
    • + Channel Inhibitor Identified by High-Throughput Screening in Yeast
    • DOI 10.1124/mol.65.1.214
    • Zaks-Makhina, E., Kim, Y., Aizenman, E., and Levitan, E. S. (2004) Novel neuroprotective K+ channel inhibitor identified by high-throughput screening in yeast Mol. Pharmacol. 65 (1) 214-219 (Pubitemid 38113902)
    • (2004) Molecular Pharmacology , vol.65 , Issue.1 , pp. 214-219
    • Zaks-Makhina, E.1    Kim, Y.2    Aizenman, E.3    Levitan, E.S.4
  • 21
    • 17044362649 scopus 로고    scopus 로고
    • Mechanism of the voltage sensitivity of IRK1 inward-rectifier K+ channel block by the polyamine spermine
    • Shin, H. G. and Lu, Z. (2005) Mechanism of the voltage sensitivity of IRK1 inward-rectifier K+ channel block by the polyamine spermine J Gen Physiol 125 (4) 413-426
    • (2005) J Gen Physiol , vol.125 , Issue.4 , pp. 413-426
    • Shin, H.G.1    Lu, Z.2
  • 23
    • 84855688302 scopus 로고    scopus 로고
    • For details on the MLPCN, see
    • For details on the MLPCN, see: http://mli.nih.gov/mli/mlpcn/
  • 25
    • 17644399838 scopus 로고    scopus 로고
    • Short QT syndrome or Andersen syndrome: Yin and Yang of Kir2.1 channel dysfunction
    • DOI 10.1161/01.RES.0000164186.86838.09
    • Schulze-Bahr, E. (2005) Short QT Syndrome or Andersen Syndrome: yin and yang of Kir2.1 channel dysfunction Circ. Res. 96 (7) 703-704 (Pubitemid 40559505)
    • (2005) Circulation Research , vol.96 , Issue.7 , pp. 703-704
    • Schulze-Bahr, E.1
  • 27
    • 73549109843 scopus 로고    scopus 로고
    • Genetically increased cell-intrinsic excitability enhances neuronal integration into adult brain circuits
    • Lin, C. W., Sim, S., Ainsworth, A., Okada, M., Kelsh, W., and Lois, C. (2010) Genetically increased cell-intrinsic excitability enhances neuronal integration into adult brain circuits Neuron 65 (1) 32-39
    • (2010) Neuron , vol.65 , Issue.1 , pp. 32-39
    • Lin, C.W.1    Sim, S.2    Ainsworth, A.3    Okada, M.4    Kelsh, W.5    Lois, C.6
  • 28
    • 60449086065 scopus 로고    scopus 로고
    • Control of the postmating behavioral switch in Drosophila females by internal sensory neurons
    • Yang, C. H., Rumpf, S., Xiang, Y., Gordon, M. D., Song, W., Jan, L. Y., and Jan, Y.-N. (2009) Control of the postmating behavioral switch in Drosophila females by internal sensory neurons Neuron 61 (4) 519-526
    • (2009) Neuron , vol.61 , Issue.4 , pp. 519-526
    • Yang, C.H.1    Rumpf, S.2    Xiang, Y.3    Gordon, M.D.4    Song, W.5    Jan, L.Y.6    Jan, Y.-N.7
  • 29
    • 84855663983 scopus 로고    scopus 로고
    • For information on PubChem, please see
    • For information on PubChem, please see: http://pubchem.ncbi.nlm.nih.gov/
  • 31
    • 84855663984 scopus 로고    scopus 로고
    • For information of the Ricera Lead Profiling Screen, see
    • For information of the Ricera Lead Profiling Screen, see: http://www.ricerca.com/
  • 32
    • 1842776149 scopus 로고    scopus 로고
    • Potassium-Dependent Slow Inactivation of Kir1.1 (ROMK) Channels
    • Sackin, H., Palmer, L. G., and Krambis, M. (2004) Potassium-dependent slow inactivation of Kir1.1 (ROMK) channels Biophys. J. 86 (4) 2145-2155 (Pubitemid 38524405)
    • (2004) Biophysical Journal , vol.86 , Issue.4 , pp. 2145-2155
    • Sackin, H.1    Palmer, L.G.2    Krambis, M.3
  • 33
    • 72949091450 scopus 로고    scopus 로고
    • Crystal structure of the eukaryotic strong inward-rectifier K+ channel Kir2.2 at 3.1 A resolution
    • Tao, X., Avalos, J. L., Chen, J., and MacKinnon, R. (2009) Crystal structure of the eukaryotic strong inward-rectifier K+ channel Kir2.2 at 3.1 A resolution Science 326 (5960) 1668-1674
    • (2009) Science , vol.326 , Issue.5960 , pp. 1668-1674
    • Tao, X.1    Avalos, J.L.2    Chen, J.3    MacKinnon, R.4
  • 34
    • 0027160197 scopus 로고
    • Backbone-dependent rotamer library for proteins. Application to side-chain prediction
    • DOI 10.1006/jmbi.1993.1170
    • Dunbrack, R. L. and Karplus, M. (1993) Backbone-dependent rotamer library for proteins application to side-chain prediction J. Mol. Biol. 230, 543-574 (Pubitemid 23161363)
    • (1993) Journal of Molecular Biology , vol.230 , Issue.2 , pp. 543-574
    • Dunbrack Jr., R.L.1    Karplus, M.2
  • 36
    • 0345327793 scopus 로고    scopus 로고
    • The effects of spermine on the accessibility of residues in the M2 segment of Kir2.1 channels expressed in Xenopus oocytes
    • Chang, H. K., Yeh, S. H., and Shieh, R. C. (2003) The effects of spermine on the accessibility of residues in the M2 segment of Kir2.1 channels expressed in Xenopus oocytes J. Physiol. 553 (Pt 1) 101-112
    • (2003) J. Physiol. , vol.553 , Issue.PART 1 , pp. 101-112
    • Chang, H.K.1    Yeh, S.H.2    Shieh, R.C.3
  • 37
    • 0033103166 scopus 로고    scopus 로고
    • + channel inner pore revealed by stoichiometric covalent modification
    • Lu, T., Nguyen, B., Zhang, X., and Yang, J. (1999) Architecture of a K+ channel inner pore revealed by stoichiometric covalent modification Neuron 22 (3) 571-580 (Pubitemid 29159855)
    • (1999) Neuron , vol.22 , Issue.3 , pp. 571-580
    • Lu, T.1    Nguyen, B.2    Zhang, X.3    Yang, J.4
  • 38
    • 0035049090 scopus 로고    scopus 로고
    • Yeast screen for constitutively active mutant G protein-activated potassium channels
    • DOI 10.1016/S0896-6273(01)00241-0
    • Yi, B. A., Lin, Y. F., Jan, Y. N., and Jan, L. Y. (2001) Yeast screen for constitutively active mutant G protein-activated potassium channels Neuron 29 (3) 657-667 (Pubitemid 32323939)
    • (2001) Neuron , vol.29 , Issue.3 , pp. 657-667
    • Yi, B.A.1    Lin, Y.-F.2    Jan, Y.N.3    Jan, L.Y.4
  • 40
    • 3242669872 scopus 로고    scopus 로고
    • Improved statistical methods for hit selection in high-throughput screening
    • Brideau, C., Gunter, B., Pikounis, B., and Liaw, A. (2003) Improved statistical methods for hit selection in high-throughput screening J. Biomol. Screen. 8, 634-647
    • (2003) J. Biomol. Screen. , vol.8 , pp. 634-647
    • Brideau, C.1    Gunter, B.2    Pikounis, B.3    Liaw, A.4
  • 41
    • 0037032469 scopus 로고    scopus 로고
    • Identification of human Kir2.2 (KCNJ12) gene encoding functional inward rectifier potassium channel in both mammalian cells and Xenopus oocytes
    • DOI 10.1016/S0014-5793(02)03512-3, PII S0014579302035123
    • Kaibara, M, Ishihara, K, Doi, Y, Hayashi, H, Ehara, T, and Taniyama, K. (2002) Identification of human Kir2.2 (KCNJ12) gene encoding functional inward rectifier potassium channel in both mammalian cells and Xenopus oocytes FEBS Lett. 531, 250-254 (Pubitemid 35341203)
    • (2002) FEBS Letters , vol.531 , Issue.2 , pp. 250-254
    • Kaibara, M.1    Ishihara, K.2    Doi, Y.3    Hayashi, H.4    Ehara, T.5    Taniyama, K.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.