|
Abstract: . . . sy can all result from malfunctions in ion channels. By Professor Andreas Busch Drug Discovery World Winter 2004/5 17 Lead Generation Leveraging the ion channel platform for lead generation in atrial fibrillation Competition in the pharmaceutical industry requires a reduction in research . . . . . . 300 400 500 Control 1m AVEO118 10m AVEO118 TIME (ms) 1.5 1.0 0.5 0.0 References 1 Drews, J, Ryser, S.The role of innovation in drug development. Nat Biotechnol 1997; 15(13):1318-1319. 2 Xu, J,Wang, X, Ensign, B, Li, M,Wu, L, Guia,A et al. Ion- . . . . . . J,Wang, X, Ensign, B, Li, M,Wu, L, Guia,A et al. Ion- channel assay technologies: quo vadis? Drug Discov Today 2001; 6(24):1278-1287. 3 Bajorath, J. Rational drug discovery revisited: interfacing experimental programs with bio- and chemo-informatics. Drug Discov Today 2001; 6(19):989-995. 4 Ggelein, . . . . . . role of innovation in drug development. Nat Biotechnol 1997; 15(13):1318-1319. 2 Xu, J,Wang, X, Ensign, B, Li, M,Wu, L, Guia,A et al. Ion- channel assay technologies: quo vadis? Drug Discov Today 2001; 6(24):1278-1287. 3 Bajorath, J. Rational drug discovery revisited: interfacing experimental . . . . . . channels Kv1.5 and Kv4.3 are regarded as promising targets, which should not be associated with ventricular side-effects unlike classical anti- arrhythmics. Our ion channel platform has aided the development of the drug candidates AVE0118 and AVE1231, two Kv1.5 and Kv4.3 blockers demon- strating efficacy in several atrial fibrillation animal . . . . . . vadis? Drug Discov Today 2001; 6(24):1278-1287. 3 Bajorath, J. Rational drug discovery revisited: interfacing experimental programs with bio- and chemo-informatics. Drug Discov Today 2001; 6(19):989-995. 4 Ggelein, H, Brendel, J, Steinmeyer, K, Strbing, C, Picard, N et al. Naunyn- Schmiedeberg's Arch . . . . . . Figure 4 Whole-cell patch-clamp recording of pig atrial myocyte treated with control or AVE0118 20 Drug Discovery World Winter 2004/5 Lead Generation 0 100 200 300 400 500 Control 1m AVEO118 10m AVEO118 TIME (ms) 1.5 1.0 0.5 0.0 . . . --2619,7,187,3108,13097
|