PhD Award of the GDCh Division of Medicinal Chemistry

The PhD Award was presented to Dr. on March 14, 2022 on the occasion of the Online FiMC 2022. Verena Kunig, Dr. Johannes Morstein and Dr. Patrick Zanon awarded.

Dr. Kunig: in recognition of her dissertation entitled DNA-encoded substance libraries: chemical stabilization of DNA, development of new synthesis methods and identification of TEAD-YAP inhibitors. "In her work, Dr. Kunig succeeds in significantly expanding the methodological arsenal for DNA-encoded molecular libraries. The synthetic methods developed based on multicomponent reactions significantly expand the possibilities for library design. In addition, the contributions to the development of chemically stabilized libraries are made possible Coding strategies application for a wide variety of synthesis methods. By discovering new TEAD-YAP inhibitors, the work also underlines the potential of DNA-encoded molecule libraries in drug discovery. The dissertation was carried out in the working group of Prof. Dr. Andreas Brunschweiger at the Technical University of Dortmund."

Dr. Morstein: in appreciation of his dissertation entitled "Optical Control of Lipid Signaling. " Dr. Morstein successfully introduces light-switchable functional groups into lipids that are involved in various signaling processes, thereby enabling completely new possibilities for controlling certain signaling pathways with light. The potential of these new tools was used directly to study signaling processes in the outstanding work. The work therefore contributes significantly to expanding the possibilities for the targeted control of biological functions using chemical tools. The dissertation was carried out in the working group of Prof. Dr. Dirk Trauner graduated from New York University."

Dr. Zanon: in appreciation of his dissertation entitled Development of methods and covalent ligands for the chemoproteomic exploration of the ligandability of bacterial proteomes. "In this outstanding work, selective chemical probes are developed to investigate the addressability of nine different amino acids and used to characterize their reactivity towards electrophiles in the bacterial proteome. This work thus illustrates the potential of new chemical methods in drug discovery and opens up new possibilities for the treatment of antibiotic-resistant infectious diseases. The dissertation was carried out in the working group of Prof. Dr. Stephan Hacker at the Technical University of Munich."

The doctoral awards were presented on the occasion of the Online“FiMC 2021” to Dr. Edith Bartole, Dr. Benedict Heinrich and Dr. Awarded to Dasha Nelidova.

Dr. Bartole: in appreciation of her dissertation entitled Design, Synthesis and Characterization of Molecular Tools for the Histamine H3 and H4 Receptors – In Particular Radio- and Fluorescent Ligands. "Dr. Bartole managed to develop and apply two complementary tools for the study of histamine H4 receptors. Their fluorescent ligand and their high-affinity radioligand enable the localization of the hH4 receptor in living cells and, for the first time, comparative binding studies on h/m/rH4 Receptors and NanoLuc-labeled receptors (h/mH4R and hH3R). With her results and her tools, Dr. Bartole has significantly enriched the research field of H4 receptors. The dissertation was carried out in the working group of Prof. Dr. Armin Buschauer at the university Regensburg and continued to be looked after by Prof. Dr. Günther Bernhardt after his death."

Dr. Heinrich: in recognition of his dissertation entitled Chemical Biology Applications of Photoresponsive DNA-Binding Agents. "The outstanding work describes chemical alternatives to the well-known Green-Fluorescent Protein (GFP), which, with the new 6 TramTO 3 molecule, make it possible, among other things, to observe living multi-resistant bacteria such as Klebsiella pneumoniae. This work illustrates the innovative power of new chemical methods and tools in the border area of ​​medical chemistry and chemical biology and their direct applicability for a better understanding of infectious diseases. The dissertation was carried out in the working group of Jun.-Prof. Dr. Olalla Vázquez at the Philipps University of Marburg."

Dr. Nelidova: in appreciation of her dissertation entitled Restoring light sensitivity using tunable near-infrared sensors. "The work combines nanotechnology and genetic engineering in an innovative approach. By conjugating gold nanoparticles to antibodies that bind to the TRP channel, light from the NIR range can be converted into signals from the TRP channel. These signals enable mice to to perceive corresponding light signals. The work thus opens up a possible path to new therapeutic approaches to the treatment of macular degeneration. The dissertation was carried out in the working group of Prof. Dr. Botond Roska at the Friedrich Miescher Institute for Biomedical Research and at the Institute of Molecular and Clinical Ophthalmology in Basel carried out."

The 2020 doctoral awards went to Dr. Charlotte Steiniger   and Dr. Bent Alexander Praefke for your outstanding dissertations.

Dr. Charlotte Steiniger in appreciation of her dissertation entitled Studies on the Mechanism and the Reprogramming of Fungal Iterative Cyclodepsipeptide Synthetases.   "In her work, Dr. Steiniger modified fungal, non-ribosomal peptide synthetases. This enabled her to make novel bioactive cyclodepsipeptide derivatives accessible, which, among other things, have been shown to have a high antiparasitic effect. This enabled her to enter bioengineering in the research area of ​​fungal systems and the design of new peptides with pharmacological potential. Their results provided concrete evidence for active and application-oriented reprogramming of iterative as well as linear synthetases for future manipulation approaches. The dissertation was carried out in the working group of Prof. Dr. Roderich D. Süssmuth at the Technical University of Berlin ."

Dr. Bent Alexander Praefke in recognition of his dissertation entitled Design and synthesis of novel inhibitors of mitogen-activated protein kinase kinase 4 (MKK4). "Starting with vemurafenib as a starting point, Dr. Praefke succeeded in obtaining highly potent inhibitors of MKK4 using multi-parameter optimization. In addition to their potency, the innovative compounds are characterized by outstanding selectivity towards crucial anti-targets. Another focus of his work is the optimization of the synthetic access to the target structures, which allowed him to make target compounds available for in-vivo experiments in high purity and in sufficient quantities in a timely manner. The dissertation was carried out in the working group of Prof. Dr. Stefan Laufer at the Eberhard Karls University of Tübingen ."

The doctoral awards were presented at FiMC 2019 to Dr. Elena De Vita, Dr. Natascha Stergiou and Dr. Robert Heinze for your outstanding dissertations.

Dr. Elena De Vita synthesized and characterized selective and potent KLK6 inhibitors and KLK6 activity probes in her dissertation “ Small molecule KLK6 inhibitors ”. Their “tool compounds” enable the physiological and patho-physiological validation of KLK6 as a potential drug target.

Dr. Natasha Stergiou In her dissertation " Use of tumor-associated mucin 1 (MUC1) to generate anti-tumor vaccines and monoclonal antibody derivatives as a basis for therapy and diagnosis of breast cancer " succeeded in selecting suitable synthetic glycopeptide MUC1-TTox vaccines showed greatly delayed tumor growth in the preclinical breast tumor model and led to a significant extension of lifespan in vaccinated animals. This means that crucial prerequisites for the clinical and immunotherapeutic testing of this vaccine have been achieved.

Dr. Robert Heinze In his dissertation " Scaffold Manipulations for the Synthesis of Seco- and abeo-Steroids " describes new ways to synthesize abeo-steroids and was able to synthesize a promising lead structure in Alzheimer's therapy with Stophasterol A. With a new approach to 9,11-secosteroids, efficient syntheses of the three natural substances ganoderin A, leptosterol A and pinnisterol D can also be achieved.