Course “Medicinal Chemistry & Drug Design for Bioinformaticians”

Extent: 2 SWS (in the summer term "SoSe") & written exam (graded)

Lecturers: PD Dr. Martin Empting, Dr. Walid Elgaher

Content:

The lecture series will tackle the fundamentals of modern medicinal chemistry including an overview on common pharmaceutical drug targets, pharmacodynamics, structure-activity relationships as well as considerations regarding pharmacokinetics (ADME-T; Absorption, Distribution, Metabolism, Excretion, Toxicology). The students will learn about the different types of assay systems for determining pharmacodynamics and pharmacokinetic parameters. A special focus are the core principles medicinal chemistry optimization applied in the hit-identification, lead generation and lead optimization phases. These include various kinds of hit-finding and screening methodologies, specific effects and characteristics of frequent substituents, bioisosterism, ringtransformations, binding modes, as well as ligand- and structure-based approaches. Finally, methods for quantifying drug-target interactions will be covered.

The lecture series will be held in English.

Bioorthogonal Chemistry & Bioconjugation Dr. Martin Empting, HIPS Saarbrücken

or students enrolled in Pharmacy, MSc Chemistry, MSc Biology, MSc Biotechnology or related advanced studies, and Chemistry/Pharmacy/Biology PhD students

Contents:
Azide-alkyne cycloadditions and beyond - from click chemistry to bioorthogonal reactions;
What is the status of in vivo chemistry/biocompatible reactions? Chemical modifications
of proteins and peptides; Applications of bioconjugate chemistry in biomedical research
and biopharmaceutical drugs (e.g. antibody-drug conjugates and theranostics).

Course Language: English
2 SWS, final exam (online; multiple choice; not graded), 3 ECTS-Points, Modul Naturwissenschaften
Weekly lectures will be made available digitally via Moodle in the section
"Courses > Naturwissenschaftlich-Technische Fakultät (NT) > Pharmazie > Pharmazeutische und Medizinische Chemie (Empting)"
starting Do. Nov 4th.


Interested students can contact Martin Empting in advance via email: martin.empting@helmholtz-hzi.de