216761
Seminar
SoSe 21: Wirkstoffentwicklung - Vom hit zum klinischen Kandidaten (Teil 2)
Roman Hillig, Holger Steuber
Hinweise für Studierende
The seminar will be presented in English.
Students can participate in the two parts of this seminar series (part I in WS and part II in SS) in any sequence.
Kommentar
Comment:
Drug discovery is a highly interdisciplinary process which involves project teams of pharmacologists, medicinal chemists, protein chemists/molecular biologists, structural biologists and computational chemists. The lecture series will provide an introduction to the drug discovery process as run in the pharmaceutical industry, from target identification and validation, via hit finding methods and the hit-to-lead process, to lead optimization, development and clinical studies. Emphasis will be on the contributions which protein crystallography and further biophysical methods (such as NMR, ITC and SPR) can make during target selection, hit prioritization and lead optimization. In addition, typical target families such as protein kinases will be discussed in the context of available crystal structures, and co-complex crystal structures with lead and drug molecules will be analyzed in detail: How do drug molecules interact with their target proteins, and what can we learn from their optimization process? The aim of the course is to develop an understanding of the molecular mechanisms of drug discovery.
Kontakt:
Dr. R. Hillig: roman.hillig@nuvisan.com
Dr. H. Steuber: holger.steuber@nuvisan.com
Content:
1. Introduction;
2. Protein-Ligand Interactions;
3. Target Class: Protein Kinases;
4. Hit-to-Lead and Lead Optimization;
5. ADMEtox;
6. Target Class: GPCRs;
7. PROTACs;
8. Chemical Biology Schließen
Drug discovery is a highly interdisciplinary process which involves project teams of pharmacologists, medicinal chemists, protein chemists/molecular biologists, structural biologists and computational chemists. The lecture series will provide an introduction to the drug discovery process as run in the pharmaceutical industry, from target identification and validation, via hit finding methods and the hit-to-lead process, to lead optimization, development and clinical studies. Emphasis will be on the contributions which protein crystallography and further biophysical methods (such as NMR, ITC and SPR) can make during target selection, hit prioritization and lead optimization. In addition, typical target families such as protein kinases will be discussed in the context of available crystal structures, and co-complex crystal structures with lead and drug molecules will be analyzed in detail: How do drug molecules interact with their target proteins, and what can we learn from their optimization process? The aim of the course is to develop an understanding of the molecular mechanisms of drug discovery.
Kontakt:
Dr. R. Hillig: roman.hillig@nuvisan.com
Dr. H. Steuber: holger.steuber@nuvisan.com
Content:
1. Introduction;
2. Protein-Ligand Interactions;
3. Target Class: Protein Kinases;
4. Hit-to-Lead and Lead Optimization;
5. ADMEtox;
6. Target Class: GPCRs;
7. PROTACs;
8. Chemical Biology Schließen