Epigenetic Drug Discovery

ISBN-13: 9783527343140 / Angielski / Twarda / 2019 / 504 str.

Wolfgang Sippl; Manfred Jung; Raimund Mannhold

Opis

This broad view of epigenetic approaches in drug discovery combines methods and strategies with individual targets, including new and largely unexplored ones such as sirtuins and methyl–lysine reader proteins.

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Spis treści

Introduction to Epigenetics

GENERAL ASPECTS AND METHODOLOGY
Epigenetic inhibitors in cancer
Structural Biology of Epigenetic Targets
Computer–based approaches
Mass Spectrometry approaches
Peptide Microarrays for epigenetic targets
Target fishing and chemoproteomics
Chemical probe development

EPIGENETIC TARGET CLASSES
HDAC inhibitors
Sirtuins
Methyltransferases
Demethylases LSD1
JMJD
Histone Acetyltransferases
BRD Bromodomains
Methyl–Lysine Reader Proteins
DNA modifying enzymes
Parasitic Epigenetic Targets

O autorze

Wolfgang Sippl holds the chair in Medicinal Chemistry at the Institute of Pharmacy at the Martin Luther University Halle–Wittenberg. After studying pharmacy at Free University Berlin, he obtained his Ph.D. degree with Hans–Dieter Höltje at Düsseldorf University in 1997. After post–doctoral work with Camille Wermuth (Strasbourg University) he obtained his habilitation from Düsseldorf University in 2002. In 2003, he accepted the professorship at Halle, where he is mainly working in the areas of computer–based drug design, in particular for epigenetic targets. In 2001 he was awarded the innovation prize for medicinal/pharmaceutical chemistry by the German Chemical Society, GDCh.

Manfred Jung holds a Ph.D. in Pharmaceutical Chemistry from the University of Marburg. After post–doctoral work with Tony Durst at the University of Ottawa, he became group leader at Münster University in 1994, completing his habilitation in 2000. Three years later, he moved to Freiburg University, where he is now a full professor for Pharmaceutical Chemistry. The focus of his research is chemical epigenetics, including inhibitor development and screening methods for new bioactive compounds. He is currently the co–chairman of the SFB research project "Medical Epigenetics".