Termine WintERSEMESTER 2022/2023
Aufgrund der Corona-Pandemie finden die Vorträge zur Zeit sowohl als Zoom-Meetings als auch wahlweise in Präsenz (Hybridveranstaltungen) statt. Sie finden die Daten zur Einwahl in das Zoom-Meeting bei dem jeweiligen Vortrag.
Dienstag, 25.10.2022, 18 Uhr c. t.
Referent: Prof. Dr. Andreas Brunschweiger, TU Dortmund University, Dortmund
Thema: A chemically stabilized DNA barcode for DNA-encoded libraries
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Meeting ID: 662 2161 3926
DNA-encoded libraries are investigated by many pharmaceutical companies and academic research groups as small molecule screening technology. The design of these libraries is a generative chemistry problem. Validated DEL designs rely on the narrow canon of heavily utilized parallel synthesis reaction methods. These use carbonyl chemistry, cross-coupling reactions, and only a very few heterocycle-forming reactions. Thus, validated library design is focused on a small area of the vast chemical reaction space. This area of reaction space furnishes primarily unsaturated, flat-shaped products. We developed a barcoding strategy based on chemically stabilized DNA barcodes that allows, in principle, to use a much larger reaction spectrum. The reasons for this are a greater chemical stability to protic acids, and an optional solid phase-initiated DEL synthesis strategy that prevents barcode nucleobase deamination and allows for dry conditions in encoded compound synthesis. Arguably, the transition from barcoding methods development to parallelization and scaling for library synthesis is challenging. Non-standard reactions for DEL design and their scope will be discussed. They include a suite of heterocyclic scaffold-forming reactions, including isocyanide multi-component reaction chemistries. Pooling strategies for encoded substrates are developed to provide high-quality pools for further DEL built. Beyond current DEL synthesis, a computational workflow for the identification of suitable DEL reactions from large chemistry databases will be shown, the assessment of reactions fit for purpose and our approach to reaction translation.
Dienstag, 08.11.2022, 18 Uhr c. t.
Referent: Prof. Dr. Paul M. Selzer, Boehringer Ingelheim Vetmedica GmbH
Thema: Anitiparasitic Research: An Animal Health Perspective.
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Meeting ID: 645 2696 7278
Antiparasitics acting on endo- or ectoparasites represent the second largest segment of the global animal health market, accounting for 23% of market share. However, relatively few novel antiparasitic agents have been introduced into the market during recent decades. One exception, and a groundbreaking 21st century success story, are the isoxazolines, whose full potential has not yet been entirely explored. Unfortunately, resistance issues are present across most parasitic diseases, which generates a clear market need for novel resistance-breaking antiparasitics with new modes/mechanisms of action. Recent advances in science and technologies strongly suggest that the time is right to invest in new modalities such as parasitic vaccines or in environmentally friendly interventions.
Dienstag, 24.01.2023, 18 Uhr c. t.
Referent: Prof. Dr. Stefanie Kaiser, Institution of Pharmaceutical Chemistry, Goethe University Frankfurt
Thema: Chemical modification of RNA beyound RNA drugs.
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Meeting ID: 679 1003 4607
RNA plays a central role in the cell because, on the one hand, RNA is significantly involved in the production of proteins and, on the other hand, RNA is a regulator of gene expression. Despite its cellular importance, attempts to use RNA as a therapeutic agent have long been ridiculed because RNA is chemically unstable. In this talk, I will describe how chemical modification of RNA allows access to the RNA drug class. For this purpose, we will look at some representatives of the already approved RNA substance classes outside the currently prominent messenger RNA vaccines. The focus will be on splicing inhibitors, aptamers and small-interfering RNAs.
The detection and quantification of RNA modifications in RNA drugs but also native RNA is possible by modern mass spectrometry. Yet, the temporal dynamics is not accessible with regular mass spectrometry.
Here, we present nucleic acid isotope labeling coupled mass spectrometry (NAIL-MS) for efficient, monoisotopic stable isotope labeling in both RNA and DNA in standard cell culture. With NAIL-MS, we design pulse chase experiments and study the temporal placement of modified nucleosides in human tRNAPhe, 18S rRNA and mRNA. This technology allows studies on RNA modification kinetics and stress response in a previously unachieved depths and is used to study the impact of drugs on the human RNA modification landscape.
48149 Münster statt. ! Aktuell auch als Zoom-Meetings!