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Announcement:

1) The seminar will be at the Praktikums-HS and starts @4:00 pm c.t.

2) Please have a carefull look at the program. We have several special appointments this semester!


Thursday 12.10.2017, 16:00 Uhr c.t., Praktikums-HS !!! GÖCH Vortrag !!!

Prof. Sven Schneider, University of Göttingen

The Fixation with Fixation: Chemical Transformations of N2

Abstract

Tuesday 07.11.2017, 16:00 Uhr c.t., Praktikums-HS !!! SONDERTERMIN !!!

Prof. Adrian Minaard, Universtiy of Groningen, NL

Site-selective catalysis in carbohydrate chemistry

Thursday 23.11.2017, 16:00 Uhr c.t., Praktikums-HS

Dr. Peter Nussbaumer, Lead Discovery Center GmbH, Dortmund, Germany

The Discovery of Potent, Selective Inhibitors of Rab Geranylgeranyltransferase (RabGGTase)

 Abstract:

Protein prenylation is important for their membrane targeting and function and is catalyzed by three enzymes (farnesyltransferase = FTase, geranylgeranyltransferase I = GGTase I, and rab geranyl­geranyltransferase = RabGGTase) with different protein substrate specificity. While substantial drug discovery efforts have yielded specific inhibitors of FTase and GGTase I, so far no selective and cellularly potent RabGGTase inhibitor is available for chemical target validation and in vivo proof-of-concept studies. Starting from a known non-specific inhibitor, we used a rational design approach to address this open topic. An initial minimization strategy yielded 3 different scaffolds. While hit exploration of two scaffolds did not result in inhibitors with cellular activity, clear structure-activity relationships could be established for the third series. Structure-guided design based on several co-crystal structures anf further medicinal chemistry optimization yielded highly potent and selective RabGGTase inhibitors with overall drug-like properties qualifying them for cellular experiments and animal studies.

Thursday 30.11.2017, 16:00 Uhr c.t., Praktikums-HS

Partick Steinbauer, FB MC

RAFT Polymers for Tissue Regeneration

Dorian Bader, FG HF

Novel annulated heterocycles based on the indolo[3,2,1-jk]carbazole scaffold

Thursday 07.12.2017, 16:00 Uhr c.t., Praktikums-HS

Prof. Emmanuel Mikros, University of Athens

TBA

Thursday 14.12.2017, 16:00 Uhr c.t., Praktikums-HS

Emanuel Sporer, FG HF

Intracellular bioorthogonal substitution

Clemens Cziegler, FG MDM

Synthesis of perillylic acid derivaties - putative novel bioactive compounds

Thursday 11.01.2018, 16:00 Uhr c.t., Praktikums-HS

Martin Anschuber, FG MDM

Alkyl halides as olefine surrogates in direct alkylation reactions via C-H activation

MSc David Siebert, FG MDM

Selective Ligands for the GABAA Receptor alpha+/beta- interface

Thursday 18.01.2018, 16:00 Uhr c.t., Praktikums-HS

Dr. Hannes Mikula, FG HF

Bioorthogonal Reactions: More than Click Chemistry?

Abstract:

The field of bioorthogonal chemistry has been growing steadily for more than 15 years with the challenge of engineering chemical transformations that can proceed within the molecularly complex and uncontrolled environment of living systems (in vivo chemistry). The fastest bioorthogonal ligation reported so far is the inverse electron demand Diels-Alder (IEDDA)-initiated conjugation between 1,2,4,5-tetrazines (Tz) and strained cycloalkenes (e.g. trans-cyclooctenes, TCO). The outstanding reaction kinetics of tetrazine ligations led to numerous applications in biomedical research, such as rapid radiolabeling (in vitro click) and pretargeted molecular imaging (in vivo click). In spite of tremendous progress in recent years, when compared to classic reaction methodology, bioorthogonal chemistry remains in its infancy. Considering the vast range of organic reactions available to synthetic chemists (additions, eliminations, substitution, oxidations, reductions, etc.), bioorthogonal chemistry has until recently been restricted to just one reaction type—bioorthogonal addition—limiting its full potential. Recently, bioorthogonal bond cleavage (or elimination) reactions have emerged as a thriving area of chemical research, such as the elimination of a carbamate-functionalized 3-OH-TCO (release-TCO) upon reaction with a Tz (click-to-release chemistry).

In recent years, we have designed and prepared numerous modified Tz as highly versatile bioorthogonal tools for in vivo chemistry. In this talk, an overview will be given of these studies and our recent activities in the field of click-to-release chemistry.

Thursday 25.01.2018, 16:00 Uhr c.t., Praktikums-HS

Prof. Bernd Niedetzky, ACIB (Austrian Center of Industrial Biotechnology)

Enzymes and sugars: challenges and opportunites for biocatalytic process development