10th Status Seminar Chemical Biology

Tutorial Workshop

Tuesday, 20 January 2015, 09:00-12:00 h

Drug discovery - today's success and tomorrow's hope

Dr. Kurt Ritter, Sanofi-Aventis Deutschland GmbH, R&D LGCR / Chemistry FF, Frankfurt/D

The tutorial workshop "Drug discovery - today's success and tomorrow's hope" will give insights into two exciting areas of drug discovery in academia and the pharmaceutical industry.

The first part "The HCV Revolution" deals with the "race" to provide an all oral treatment for Hepatitis C. Chronic infection with the Hepatitis C virus (HCV) is often unrecognised or undiagnosed (silent epidemic). This leads over a period of 10 to 20 years to liver diseases such as cirrhosis and cancer and is the major reason for liver transplantation. The combination of several orally available agents acting directly on different viral proteins will prevent the replication of the virus with high efficiency and low risk for emergence of resistance. This lecture will address three major targets and the development of such direct-acting antivirals (DAAs):

  • Inhibition of the viral protease by macrocyclic compounds such as Simeprevir
  • Shut-down of the viral polymerase by nucleotide inhibitor such as the prodrug Sofosbuvir
  • Identification of the drug Daclatasvir and its corresponding target via a well-designed phenotypic screening approach At the end a short outlook into the rapidly changing market and players in this field will be given.

The 2nd part will cover the rapidly expanding field of epigenetics. The term "epigenetics" refers to the changes in gene expression or in a phenotype by modifications of the DNA or the DNA-storing chromatin without changing the primary DNA sequence. The genetic code contains the unique universal plan for all proteins of an organism, but on top of it (= epi), the epigenetic machinery defines the timing of protein expression, responses to environmental changes, the characteristics of a certain cell type etc. Thus, epigenetics may play an important role in the origin of human diseases such as cancer, neurodegenerative conditions, neuropsychiatric disorders and inflammation.

The lecture gives a short, non-comprehensive introduction of the major players of this machinery:

  • The writers = enzymes which add groups to DNA or the DNA-associated histones
  • The readers = proteins which recognize and bind to these modifications
  • The erasers = enzymes which remove these groups.

Due to the inherent complexity of the field, academia and companies work together to understand the machinery by solving the structures of the involved proteins and by providing tool compounds to study functions. The first wave of small molecule epigenetic modulators has arrived in the clinic or on the market, especially in oncology. A second wave of (tool) compounds being more selective or hitting different targets is on the horizon.


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