Advanced Assays in Epigenetics

Nowadays, science is proving that our body possesses incredible self-healing and self-repairing ability. These mechanisms are markedly influenced by our lifestyle, environmental factors and also our beliefs, thoughts, emotions and intentions. A change in the aforementioned factors can affect or even alter completely the tendency for expression. During this process, our enormous code base, the DNA, will be read and the manifestation which will be expressed is heavily influenced by epigenetic marks. These marks are either written, read or modified. So we are based not only on plain code, but we are the modifiers of the code through readers, writers and erasers. So we have a profound vibrational effect on our continually evolving genetic code. We are the programmers of the code. DNA activation is our “software upgrade”. The specific scientific term “epigenetics” for these code reading, writing and erasing has been first defined in 1942 by C.H. Waddington. This term has been used in various contexts. Etymologically speaking, epigenetics deals with a precise branch of genetics as the Greek prefix epi means “after”, “post” or “additionally”. Today, in the molecular realm, all three meanings of epi are somewhat proven in the rapidly growing body of literature especially in the last decade dealing with fundamental processes in a living cell which are outside of the classical genetic processes and sources of genetic information like the DNA base pair sequence. Today researches try to link an observed phenomenon or a disease down to the molecular level. Besides the longer known epigenetic targets such as histone deacetylases or DNA methyltransferases, a whole bunch of new enzymes and enzyme complexes have been discovered in the last 15 years. This book mainly discusses the recent advances in the drug development of epigenetic modulators from a medicinal chemist’s viewpoint. Modern techniques in biology, biochemistry and chemical biology allow researchers faster than ever to describe and discover new epigenetic players as well as novel functions of old and known ones. Medicinal chemistry plays a fundamental role in the discovery process as it provides not only tools to better understand the function of an epigenetic player but also novel therapy options where aberrant epigenetic mechanisms are involved. The book comprises 16 chapters. Each chapter includes a short introduction for a single epigenetic target or a target family ranging from structural biology aspects to cell biology and biochemistry. Most of the space is devoted to target modulation, either inhibition or activation. The authors give an insight into the discovery and development of mainly small organic molecules and also peptides influencing epigenetic pathways. Modern aspects of drug design such as new methodologies, ranging from computational approaches, crystallography to structural biology are presented with hands-on examples.