Retaining the proven didactic concept of the successful ‘Chemical Biology – Learning through Case Studies’, this sequel features 27 new case studies, reflecting the rapid growth in this interdisciplinary topic over the past few years.
Edited by two of the world’s leading researchers in the field, this textbook introduces students and researchers to the modern approaches in chemical biology, as well as important results, and the techniques and methods applied. Each chapter presents a different biological problem taken from everyday lab work, elucidated by an international team of renowned scientists.
With its broad coverage, this is a valuable source of information for students, graduate students, and researchers working on the borderline between chemistry, biology, and biochemistry.
Cuprins
Introduction and Preface
Abbreviations
REAL-TIME AND CONTINUOUS SENSORS OF PROTEIN KINASE ACTIVITY UTILIZING CHELATION-ENHANCED FLUORESCENCE
Introduction
The Biological Problem
The Chemical Approach
Chemical Biological Research/Evaluation
Conclusions
FLi K AND FLi P: DIRECT BINDING ASSAYS FOR THE IDENTIFICATION OF STABILIZERS OF INACTIVE KINASE AND PHOSPHATASE CONFORMATIONS
Introduction – The Biological Problem
The Chemical Approach
Chemical Biological Research/Evaluation
Conclusions
STRATEGIES FOR DESIGNING SPECIFIC PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND THEIR INTRACELLULAR ACTIVATION
Introduction – The Biological Problem
The Chemical Approach
Chemical Biological Research/Evaluation
Conclusions
DESIGN AND APPLICATION OF CHEMICAL PROBES FOR PROTEIN SERINE/THREONINE PHOSPHATASE ACTIVATION
Introduction
The Biological Problem
The Chemical Approach
Chemical Biological Research/Evaluation
Conclusion
AUTOPHAGY: ASSAYS AND SMALL-MOLECULE MODULATORS
Introduction
The Biological Problem
The Chemical Approach
Chemical Biological Evaluation
Conclusion
ELUCIDATION OF PROTEIN FUNCTION BY CHEMICAL MODIFICATION
Introduction
The Biological Problem
The Chemical Approach
Biological Research/Evaluation
Conclusion
INHIBITION OF ONCOGENIC K-Ras SIGNALING BY TARGETING K-Ras-PDEDelta
Introduction
The Biological Problem
The Chemical Approach
Chemical Biological Evaluation
Conclusions
DEVELOPMENT OF ACYL PROTEIN THIOESTERASE 1 (APT1) INHIBITOR PALMOSTATIN B THAT REVERT UNREGULATED H/N-Ras-SIGNALING
Introduction
The Biological Problem – The Role of APT1 in Ras Signaling
The Chemical Approach
Chemical Biological Research/Evaluation
Conclusions
FUNCTIONAL ANALYSIS OF HOST-PATHOGEN POSTTRANSLATIONAL MODIFICATION CROSSTALK OF RAB PROTEINS
Introduction
The Biological Problem
The Chemical Approach
Chemical Biological Research/Evaluation
Conclusions
CHEMICAL BIOLOGY APPROACH TO SUPPRESSION OF STATIN-INDUCED MUSCLE TOXICITY
Introduction
The Biological Problem
The Chemical Approach
Chemical Biological Research/Evaluation
Conclusion
A TARGET IDENTIFICATION SYSTEM BASED ON MORPHOBASE, CHEMPROTEOBASE, AND PHOTO-CROSS-LINKING BEADS
Introduction
The Biological Problem
The Chemical Approach
Chemical Biological Research/Evaluation
Conclusion
ACTIVITY-BASED PROTEASOME PROFILING IN MEDICINAL CHEMISTRY AND CHEMICAL BIOLOGY
Introduction
The Biological Problem
The Chemical Approach
Biological Research/Evaluation
Conclusions
RATIONAL DESIGN OF ACTIVITY-BASED RETAINING BETA-EXOGLUCOSIDASE PROBES
Introduction
The Biological Problem
The Chemical Approach
Biological Research/Evaluation
Conclusions
MODULATION OF Clp P PROTEASE ACTIVITY: FROM ANTIBIOTICS TO ANTIVIRULENCE
Introduction
The Biological Problem
The Chemical Approach
The Discovery of a Novel Antibiotic Mechanism
The Antivirulence Approach
Conclusions
AFFINITY-BASED ISOLATION OF MOLECULAR TARGETS OF CLINICALLY USED DRUGS
Introduction – The Biological/Medicinal Problem
The Chemical Approach
Chemical Biological Research
Conclusion
IDENTIFICATION OF THE TARGETS OF NATURAL-PRODUCT-INSPIRED MITOTIC INHIBITORS
Introduction
The Biological Problem
The Chemical Approach
Chemical Biological Evaluation
Conclusion
FINDING A NEEDLE IN A HAYSTAY. IDENTIFICATION OF TANKYRASE, A NOVEL THERAPEUTIC TARGET OF THE WNT PATHWAY USING CHEMICAL GENETICS
Introduction
The Biological Problem
The Chemical Approach
Chemical Biological Research/Evaluation
Conclusion
THE IDENTIFICATION OF THE MOLECULAR RECEPTOR OF THE PLANT HORMONE ABSCISIC ACID
Introduction
The Biological Problem
The Chemical Genetics Approach
The Chemical Biology Approach
Conclusion
CHEMICAL BIOLOGY IN PLANTS: FINDING NEW CONNECTIONS BETWEEN PATHWAYS USING THE SMALL MOLECULE SORTIN 1
Introduction
The Biological Problem
The Chemical Approach
Biological Research/Evaluation
Conclusion
SELECTIVE TARGETING OF PROTEIN INTERACTIONS MEDIATED BY BET BROMODOMAINS
Introduction
The Biological Problem
The Chemical Approach
Chemical Biological Investigations
Conclusion
THE
Despre autor
Herbert Waldmann obtained his Ph D in organic chemistry from the University of Mainz, Germany, in 1985 working with Professor H. Kunz, after which he completed a postdoctoral appointment with Professor G. Whitesides at Harvard University (USA). He was appointed as Professor of Organic Chemistry at the University of Bonn (1991), full Professor of Organic Chemistry at the University of Karlsruhe (1993), and Director at the Max-Planck-Institute of Molecular Physiology Dortmund and Professor of Organic Chemistry at the University of Dortmund, Germany, in 1999. He has received numerous awards, e.g. the Otto-Bayer-Award (2001), the Max Bergmann Medal (2003), and recently the Emil-Fischer-Prize (2012). His research interests lie in bioactive compound development, target identification, and the chemical biology of Ras proteins.
Petra Janning studied chemistry at the University of Münster, Germany, and did her Ph D thesis at the Institute for Analytical Sciences in Dortmund, Germany in 1995. After different positions where she worked in the area of analytical chemistry and on the borderline between chemistry and biology she joined the Max-Planck-Institute of Molecular Physiology, Dortmund, in the department of Professor H. Waldmann, where she is currently working. She is responsible for the Bioorganic Practical Course and the analytics in the department. She focused her work on mass spectrometry based methods in proteome research in particular in target protein identification of small molecules.