The PhD Award 2024 was presented on 19 March 2024 to Dr Silvia Arifi, Dr Carsten Peukert and Dr Raphael Steimbach on the occasion of the Division's annual conference "Frontiers in Medicinal Chemistry 2024" in Munich.

Dr Silvia Arifi: in recognition of her dissertation entitled Development of chemical tools for nuclear receptors. "Dr. Arifi developed innovative ligands for the peroxisome proliferator-activated receptor gamma (PPARγ) and the orphan receptors Nur77 and NOR-1. In her work, she used a fragment-based approach to identify new ligands for the little-studied nuclear receptors Nur77 and NOR-1. The discovery of allosteric modulators for PPARγ was successfully used to demonstrate new pharmacological effects in comparison to established PPARγ ligands."

Dr. Carsten Peukert: in recognition of his dissertation entitled Using iron to catch a ride - synthetic siderophores as molecular 'Trojan Horses' to visualise and treat MDR bacterial pathogens. "Dr Peukert made significant contributions to the diagnosis and control of bacterial infections As part of his doctorate, he dealt with the insufficient transport of active substances in Gram-negative pathogens, which is considered a key problem of intrinsic antibiotic resistance. He designed highly sensitive probes to detect these pathogens and translated the principle into a PET probe, which is now being further developed for use in humans."

Dr Raphael Steimbach: in recognition of his dissertation entitled Selective Inhibitors and Targeted Degraders of Histone Deacetylase 10. "Dr Steimbach's thesis demonstrates the design, synthesis and characterisation of the first class of highly selective inhibitors of histone deacetylase 10. Dr Steimbach identified a selective chemical probe that could validate for the first time the presumed cellular function of HDAC10 as a polyamine deacetylase, and he discovered the first compounds that led to targeted degradation of HDAC in cells. His findings devalidated the role of HDAC10 in the treatment of neuroblastoma and opened the way for potential new therapeutic applications of HDAC10 inhibitors."

The PhD Award 2023 was presented on 3 April 2023 at the FiMC 2023 in Vienna to Dr Alaa Alhayek and Dr Li Gao

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Mrs Dr Alhayek: in recognition of her dissertation entitled Exploring bacterial metalloproteases as promising drug targets. "Dr Dr Alhayek "Dr Alhayek characterised biological metalloproteases as promising drug targets. Alhayek characterised the biological effect of new, selective and chemically stable inhibitors of bacterial metalloprotease virulence factors in cellular in vitro assays, in ex vivo and in vivo infection models. Her work has also led to the discovery of new inhibitors of bacterial virulence factors. In her work, Dr Alhayek was able to successfully shed light on the role of such inhibitors in the infection process and thus demonstrate the potential of inhibiting bacterial virulence factors for the future treatment of bacterial infections."

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Mr Dr Gao: in recognition of his dissertation entitled Use of styrylbenzothiazole photoswitches in drugs for spatiotemporal control over microtubule-dependent biology. "Dr Gao developed and synthesised in vivo active and light-switchable substances based on so-called "styryl[benzo]thiazole photoswitches" (S[B]Ts), which allow the precise control of biological effects on the cytoskeleton. Mr Dr. Gao demonstrated the improvement of the molecular properties through photochemical and metabolic resilience tests up to complex biological applications in living organisms. The biomolecules described in this work are the first light-switchable substances that are compatible with fluorescence protein imaging and can therefore be used for high-precision studies on biological systems."

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

Dr. Kunig: in recognition of her dissertation entitled DNA-encoded compound libraries: Chemical stabilisation of DNA, development of new synthesis methods and identification of TEAD-YAP inhibitors. "In her work, Dr Kunig has succeeded in significantly expanding the methodological arsenal for DNA-encoded molecular libraries. The developed synthesis methods based on multicomponentreactions significantly expand the possibilities of library design. In addition, the contributions to the development of chemically stabilised coding strategies enable application for a wide range of synthesis methods. The discovery of new TEAD-YAP inhibitors also underlines the potential of DNA-encoded molecular libraries in drug discovery.

The dissertation was carried out in the working group of Prof. Dr Andreas Brunschweiger at the Technical University of Dortmund."

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Dr Morstein: in recognition of his dissertation entitled "Optical Control of Lipid Signaling. "Dr Morstein successfully introduces light-switchable functional groups into lipids involved in various signalling processes, thus opening up completely new possibilities for the control of certain signalling pathways by light. The potential of these new tools was used directly to study signalling processes in this outstanding work. The work thus contributes significantly to expanding the possibilities for targeted control of biological functions using chemical tools. The dissertation was completed in the working group of Prof. Dr Dirk Trauner at New York University."

Dr Zanon: in recognition 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 characterise their reactivity towards electrophiles in the bacterial proteome. This work thus illustrates the potential of new chemical methods in drug research 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."

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The PhD Awards were presented at the "Online-FiMC 2021" to Dr Edith Bartole, Dr Benedikt Heinrich and Dr Dasha Nelidova.

Dr. Bartole: in recognition of her dissertation entitled Design, Synthesis and Characterisation of Molecular Tools for the Histamine H3 and H4 Receptors - In Particular Radio- and Fluorescent Ligands. "Dr Bartole succeeded in developing and applying two complementary tools for the study of histamine H4 receptors. Her fluorescent ligand and her high-affinity radioligand enable the localisation of the hH4 receptor in living cells and, for the first time, comparative binding studies on h/m/rH4 receptors and on NanoLuc-labelled 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 started in the working group of Prof. Dr Armin Buschauer at the University of Regensburg and continued to be supervised by Prof. Dr Günther Bernhardt after his death."

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Dr Heinrich: in honour of his dissertation entitled Chemical Biology Applications of Photoresponsive DNA-Binding Agents. "In this outstanding work, chemical alternatives to the well-known Green Fluorescent Protein (GFP) are described which, with the new 6 TramTO 3 molecule, make it possible 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 medicinal 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 Junior Professor Dr Olalla Vázquez at the Philipps University of Marburg.

Dr Nelidova: in recognition 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 TRP channel-binding antibodies, light from the NIR range can be converted into signals from the TRP channel. These signals enable mice to perceive corresponding light signals. The work thus opens up a possible path to new therapeutic approaches for 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 the Institute of Molecular and Clinical Ophthalmology in Basel."

The PhD Awards 2020 went to Dr. Charlotte Steiniger and Dr Bent Alexander Praefke for their outstanding dissertations.

Dr Charlotte Steiniger in recognition of her dissertation entitled Studies on the Mechanism and the Reprogramming of Fungal Iterative Cyclodepsipeptide Synthetases. "In her work, Dr Steiniger modified fungal, nonribosomal peptide synthetases. This enabled her to make novel bioactive cyclodepsipeptide derivatives accessible, for which, among other things, a high antiparasitic effect was demonstrated. This enabled her to enter the field of bioengineering and the design of new peptides with pharmacological potential for the research area of fungal systems. Her results provided concrete indications for an 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). "Using vemurafenib as a starting point, Dr Praefke succeeded in obtaining highly potent inhibitors of MKK4 in a multi-parameter optimisation. In addition to their potency, the innovative compounds are characterised by outstanding selectivity towards key anti-targets. Another focus of his work is the optimisation of the synthetic access to the target structures, which allowed him to make target compounds available for in vivo experiments in high purity and 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.