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This book reviews the principles of design and examples of successful implementation of proteinkinase inhibitors (PKI), and offers a comprehensive and authoritative overview of the history and latest developments in the field. Chapters written by experts from industry and academia cover the function, structure and topology of Proteinkinases, molecular modelling, disclose how to achieve high level of selectivity for kinase inhibitors, and exploit kinase inhibitors for cancer treatment. Particular attention is given to Inhibitors of c-Jun N-terminal kinase 3, and to covalent Janus Kinase 3 Inhibitors. A case study on Receptor Tyrosine Kinases EGFR, VEGFR, PDGFR is also presented in this book.
Given its breath, this book will appeal to medicinal chemists, students, researchers and professionals alike.
Sommario
ProteinKinase-Inhibitors: A Story of Success.- Function, Structure and Topology of Proteinkinases.- Molecular Modelling.- Case study on Receptor Tyrosine Kinases EGFR, VEGFR, PDGFR.- Achieving high level of selectivity for kinase inhibitors.- Inhibitors of c-Jun N-terminal kinase 3.- Exploiting kinase inhibitors for cancer treatment - An Overview of Clinical Results and Outlook.- Covalent Janus Kinase 3 Inhibitors.
Info autore
Stefan Laufer is a Professor of Pharmaceutical/Medicinal Chemistry at Tuebingen University, Germany, and he had previously worked for 10 years in the Pharmaceutical Industry. His research interests are anti-inflammatory and cancer drug discovery with various eicosanoid (COX-1,2,3, LOXs, mPGES1, cPLA2) and protein kinase targets (p38, JAKs, JNKs, CK1d, mtEGRFs). Three compounds from his lab entered clinical development phases. Dr. Laufer chairs the ICEPHA (Interfaculty Center for Pharmacogenomics and Drug Research) and TüCADD, Tuebingen Center for Academic Drug Discovery. As part of this work, a proprietary kinase inhibitor collection is established (TüKIC, 10.000 cpds). He authored more than 500 publications, 14 books/bookchapters, and is inventor in 42 patent families.
