Buch, Englisch, 308 Seiten, Format (B × H): 162 mm x 240 mm, Gewicht: 679 g
Buch, Englisch, 308 Seiten, Format (B × H): 162 mm x 240 mm, Gewicht: 679 g
Reihe: Novartis Foundation Symposium
ISBN: 978-0-470-02140-8
Verlag: WILEY
Drawing together contributions from the biological, pharmaceutical, and clinical sciences, this book offers a widre-ranging discussion of the structure and function of hERG and the molecular basis for compound binding. Topics include hERG channel gating, regulation of functional expression, the pharmacological properties of hERG/IKr channels, drug-induced long QT syndrome, and preclinical evaluation and regulatory recommendations for assessing QT prolongation risks. Better understanding of the role of the hERG channel in drug-induced cardiac arrhythmias should lead to the development of new, safer medicines.
Autoren/Hrsg.
Fachgebiete
Weitere Infos & Material
Chair's introduction (Michael Sanguinetti).
Gating and assembly of heteromeric hERG1a/1b channels underlying I_Kr in the heart (Gail A. Robertson, Eugenia M. C. Jones and Jinling Wang).
Structure-function studies of outer mouth and voltage sensor domain of hERG (Gea-Ny Tseng and H. Robert Guy).
Voltage sensor movement in the hERG K+ channel (David R. Piper,Michael C. Sanguinetti and Martin Tristani-Firouzi).
hERG channel trafficking (Eckhard Ficker, Adrienne Dennis,Yuri Kuryshev, Barbara A.Wible and Arthur M. Brown).
Dynamic control of hERG/_IKr_r by PKA-mediated interactions with 14-3-3 (Anna Kagan and Thomas V. McDonald).
Does hERG coassemble with a ß subunit? Evidence for roles of MinK and MiRP1 (Arun Anantharam and Geoffrey W. Abbott).
hERG block, QT liability and sudden cardiac death (Arthur M. Brown).
Structural determinants for high affinity block of hERG potassium channels ( John Mitcheson, Matthew Perry, Phillip Stansfeld,Mike Sanguinetti,Harry Witchel and Jules Hancox).
Physicochemical basis for binding and voltage-dependent block of hERG channels by structurally diverse drugs (Michael C. Sanguinetti, Jun Chen, David Fernandez, Kaichiro Kamiya,John Mitcheson and José A. Sanchez-Chapula).
In silico - modelling pharmacophores and hERG channel models (Maurizio Recanatini, Andrea Cavalli and MatteoMasetti).
The long QT syndrome: a clinical counterpart of HERG mutations (Peter J. Schwartz).
Cellular mechanisms of Torsade de Pointes (Steven Poelzing and David S. Rosenbaum).
Expression and role of HERG channels in cancer cells (Annarosa Arcangeli).
TRIad: foundation for proarrhythmia (triangulation, reverse use dependence and instability) (Luc M. Hondeghem).
Drug-induced QT interval prolongation: regulatory guidance and perspectives on hERG channel studies (Rashmi R. Shah).
Closing remarks (Michael Sanguinetti).
Index of contributors.
Subject index.
