Contents
Function, Structure and Topology of Protein Kinases . . . . . . . . . . . . . . .
1
Sandra Röhm, Andreas Krämer, and Stefan Knapp
Molecular Modeling of Protein Kinases: Current Status
and Challenges . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 25
Antti Poso
Covalent Kinase Inhibitors: An Overview . . . . . . . . . . . . . . . . . . . . . . . 43
Matthias Gehringer
Achieving High Levels of Selectivity for Kinase Inhibitors . . . . . . . . . . . 95
Laurent Schio and Herve Minoux
Exploiting Kinase Inhibitors for Cancer Treatment: An Overview
of Clinical Results and Outlook . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 125
Athina Moschopoulou, Stefan Zwirner, Lars Zender, and Daniel Dauch
Case Study on Receptor Tyrosine Kinases EGFR, VEGFR,
and PDGFR . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 155
Lídia Moreira Lima, Maria Letícia de Castro Barbosa,
Daniel Nascimento do Amaral, and Eliezer J. Barreiro
Inhibitors of c-Jun N-Terminal Kinase 3 . . . . . . . . . . . . . . . . . . . . . . . . 203
Pierre Koch
Covalent Janus Kinase 3 Inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . 225
Matthias Gehringer and Michael Forster
vii
Function, Structure and Topology of Protein Kinases . . . . . . . . . . . . . . .
1
Sandra Röhm, Andreas Krämer, and Stefan Knapp
Molecular Modeling of Protein Kinases: Current Status
and Challenges . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 25
Antti Poso
Covalent Kinase Inhibitors: An Overview . . . . . . . . . . . . . . . . . . . . . . . 43
Matthias Gehringer
Achieving High Levels of Selectivity for Kinase Inhibitors . . . . . . . . . . . 95
Laurent Schio and Herve Minoux
Exploiting Kinase Inhibitors for Cancer Treatment: An Overview
of Clinical Results and Outlook . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 125
Athina Moschopoulou, Stefan Zwirner, Lars Zender, and Daniel Dauch
Case Study on Receptor Tyrosine Kinases EGFR, VEGFR,
and PDGFR . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 155
Lídia Moreira Lima, Maria Letícia de Castro Barbosa,
Daniel Nascimento do Amaral, and Eliezer J. Barreiro
Inhibitors of c-Jun N-Terminal Kinase 3 . . . . . . . . . . . . . . . . . . . . . . . . 203
Pierre Koch
Covalent Janus Kinase 3 Inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . 225
Matthias Gehringer and Michael Forster
vii
