Fragment-based Drug Discovery (eBook)
528 Seiten
Wiley-VCH (Verlag)
978-3-527-68361-1 (ISBN)
In this handbook, the first-hand knowledge imparted by the world's leading experts provides a comprehensive overview of current methods and applications of fragment-based discovery. The first part discusses basic considerations concerning when to use such methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel, and emerging techniques for fragment screening, including empirical as well as computational approaches, while also discussing such special cases as complex target systems and covalent inhibitors. The third and final part presents a number of successful real-world studies from recent and on-going drug discovery projects relating to a variety of target classes, from kinases and phosphatases to beta-secretase and epigenetic targets.
With its discussion of future developments and potential novel applications, this will remain a valuable reference source for years to come.
Daniel A. Erlanson is the co-founder and President of Carmot Therapeutics, Inc., which is developing fragment-based approaches to address unmet needs in drug discovery. Prior to Carmot, Dr. Erlanson worked in medicinal chemistry and technology development at Sunesis Pharmaceuticals, which he joined at the company's inception. Before Sunesis, he was an NIH postdoctoral fellow with Dr. James A. Wells at Genentech. Dr. Erlanson earned his Ph.D. in chemistry from Harvard University in the laboratory of Gregory L. Verdine and his BA in chemistry from Carleton College. He edits a blog devoted to fragment-based drug discovery, Practical Fragments. Wolfgang Jahnke is a Director and Leading Scientist at the Novartis Institutes for Biomedical Research in Basel, Switzerland. His major interests are Structural Biophysics and Fragment-based Drug Discovery. He has received several honors, among them the Industrial Investigator Award from the Swiss Chemical Society, and several Novartis-internal Awards. Dr. Jahnke received his PhD from the TU München, working with Horst Kessler on the development and application of novel NMR methods. Prior to joining Novartis, he worked with Peter Wright at the Scripps Research Institute in La Jolla.
PART I: The Concept of Fragment-based Drug Discovery
# 01 The Role of Fragment-Based Approaches in Lead Finding
# 02 Selecting the Right Targets for FBDD
# 03 Enumeration of Chemical Fragment Space
# 04 Ligand Efficiency Metrics and their Use in Fragment Optimizations
PART II: Methods and Approaches for Fragment-based Drug Discovery
# 05 Strategies for Fragment Library Design
# 06 The Synthesis of Biophysical Methods In Support of Robust Fragment-Based Lead Discovery
# 07 Differential Scanning Fluorimetry as Part of a Biophysical Screening Cascade
# 08 Emerging Technologies for Fragment Screening
# 09 Computational Methods to Support Fragment Based Drug Discovery
# 10 Making FBDD Work in Academia
# 11 Site-Directed Fragment Discovery for Allostery
# 12 Fragment Screening in Complex Systems
# 13 Protein-Templated Fragment Ligation Methods: Emerging Technologies in Fragment-Based Drug Discovery
PART III: Successes from Fragment-based Drug Discovery
# 14 BACE Inhibitors
# 15 Epigenetics and Fragment Based Drug Discovery
# 16 Discovery of Inhibitors of Protein-Protein Interactions Using Fragment-Based Methods
# 17 Fragment-Based Discovery of Inhibitors of Lactate Dehydrogenase A
# 18 FBDD Applications to Kinase Drug Hunting
# 19 An Integrated Approach for Fragment Based Lead Discovery: Virtual, NMR and High-Throughput Screening Combined with Structure Guided Design. Application to the Aspartyl Protease Renin
Erscheint lt. Verlag | 4.12.2015 |
---|---|
Reihe/Serie | Methods and Principles in Medicinal Chemistry | Methods and Principles in Medicinal Chemistry |
Mitarbeit |
Herausgeber (Serie): Raimund Mannhold, Hugo Kubinyi, Gerd Folkers |
Sprache | englisch |
Themenwelt | Naturwissenschaften ► Chemie |
Technik | |
Schlagworte | Chemie • Chemistry • Computational Chemistry & Molecular Modeling • Computational Chemistry u. Molecular Modeling • Drug Discovery & Development • Fragmentbasierte Wirkstoffforschung • Methods - Synthesis & Techniques • Organische Chemie • Organische Chemie / Methoden, Synthesen, Verfahren • Wirkstoffforschung • Wirkstoffforschung u. -entwicklung |
ISBN-10 | 3-527-68361-5 / 3527683615 |
ISBN-13 | 978-3-527-68361-1 / 9783527683611 |
Haben Sie eine Frage zum Produkt? |
![PDF](/img/icon_pdf_big.jpg)
Größe: 44,0 MB
Kopierschutz: Adobe-DRM
Adobe-DRM ist ein Kopierschutz, der das eBook vor Mißbrauch schützen soll. Dabei wird das eBook bereits beim Download auf Ihre persönliche Adobe-ID autorisiert. Lesen können Sie das eBook dann nur auf den Geräten, welche ebenfalls auf Ihre Adobe-ID registriert sind.
Details zum Adobe-DRM
Dateiformat: PDF (Portable Document Format)
Mit einem festen Seitenlayout eignet sich die PDF besonders für Fachbücher mit Spalten, Tabellen und Abbildungen. Eine PDF kann auf fast allen Geräten angezeigt werden, ist aber für kleine Displays (Smartphone, eReader) nur eingeschränkt geeignet.
Systemvoraussetzungen:
PC/Mac: Mit einem PC oder Mac können Sie dieses eBook lesen. Sie benötigen eine
eReader: Dieses eBook kann mit (fast) allen eBook-Readern gelesen werden. Mit dem amazon-Kindle ist es aber nicht kompatibel.
Smartphone/Tablet: Egal ob Apple oder Android, dieses eBook können Sie lesen. Sie benötigen eine
Geräteliste und zusätzliche Hinweise
Zusätzliches Feature: Online Lesen
Dieses eBook können Sie zusätzlich zum Download auch online im Webbrowser lesen.
Buying eBooks from abroad
For tax law reasons we can sell eBooks just within Germany and Switzerland. Regrettably we cannot fulfill eBook-orders from other countries.
aus dem Bereich