PhD Award of the GDCh Division of Medicinal Chemistry

The PhD Award 2025 was presented on 3 April 2025 on the occasion of the Divisions’ annual meeting "Frontiers in Medicinal Chemistry 2025" in Erlangen to Dr. Florian Brandt and Dr. Wenxin Felix Zhu .

Dr. Florian Brandt: in recognition of his dissertation entitled Modulation of the Pharmacokinetics of Peptide-Based Radiotheranostics – Characterisation of Albumin Binders and Neprilysin-Targeted Cleavage Sequences. "In his doctoral research, Dr. Brandt optimised theranostic radioligands using small-molecule albumin binders and linkers cleavable by neprilysin. The novel heterobivalent radioligands, which target both somatostatin receptor subtype 2 and albumin, show increased tumour uptake and reduced renal accumulation. His outstanding work demonstrates the potential of new radioligands for clinical translation."

Dr. Wenxin Felix Zhu: in recognition of his dissertation entitled Synthesis of Bioactive Tricycles. "In his doctoral research, Dr. Zhu established the potassium channel Slack as a new drug target for the treatment of histamine-independent itching and synthesised promising bioactive tricycles that were successfully tested in animal studies. His research shows that the pharmacological activation of Slack represents a safe and effective strategy for reducing itching. In addition, he developed new chemical reactions based on the nitrene-like reactivity of the oxadiazolone and worked on a nitrene-based cycloaddition to form relevant bicyclic compounds for drug development."

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

Dr. Silvia Arifi: in recognition of her dissertation entitled Development of Chemical Tools for Nuclear Receptors. "Dr. Arifi developed innovative ligands for peroxisome proliferator-activated receptor gamma (PPARγ) and the orphan receptors Nur77 and NOR-1. In her work, starting from a fragment-based approach, she identified new ligands for the poorly researched nuclear receptors Nur77 and NOR-1. The discovery of allosteric modulators for PPARγ was successfully used to demonstrate new pharmacological effects compared with 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 visualize and treat MDR bacterial pathogens. "Dr. Peukert made significant contributions to the diagnosis and combating of bacterial infections. As part of his doctoral research, he addressed the inadequate transport of active substances into Gram-negative pathogens, which is considered a key problem underlying intrinsic antibiotic resistance. He designed highly sensitive probes for detecting 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 dissertation 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, for the first time, enabled the presumed cellular function of HDAC10 as a polyamine deacetylase to be validated, and he discovered the first compounds that led to the targeted degradation of HDAC in cells. His findings devalidated the role of HDAC10 in the treatment of neuroblastomas and paved the way for possible new therapeutic applications of HDAC10 inhibitors."

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

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

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, light-switchable compounds based on so-called ‘styryl[benzo]thiazole photoswitches’ (S[B]Ts), which enable the precise control of biological effects on the cytoskeleton. Dr. Gao demonstrated the improvement of the molecular properties through photochemical and metabolic stability tests, extending to complex biological applications in living organisms. The biomolecules described in this work are the first light-switchable compounds compatible with fluorescent protein imaging and can therefore be used for highly precise studies of biological systems."

The PhD Award was presented on 14 March 2022 on the occasion of 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 succeeds in significantly expanding the methodological arsenal for DNA-encoded molecular libraries. The synthesis methods developed on the basis of multicomponent­ reactions substantially expand the possibilities for library design. In addition, the contributions to the development of chemically stabilised encoding strategies enable applications 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 Dortmund University of Technology."

Dr. Morstein: in recognition of his dissertation entitled "Optical Control of Lipid Signaling. "Dr Morstein successfully introduces photoswitchable functional groups into lipids that are involved in various signalling processes, thereby enabling entirely new possibilities for controlling specific signalling pathways with light. The potential of these new tools was used directly in this outstanding work to study signalling processes. The work thus makes a significant contribution to expanding the possibilities for the 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. "This outstanding work develops selective chemical probes to investigate the addressability of nine different amino acids and uses them to characterise their reactivity towards electrophiles in the bacterial proteome. This work thereby demonstrates the potential of new chemical methods in drug research and opens up new possibilities for treating antibiotic-resistant infectious diseases. The dissertation was carried out in the working group of Prof. Dr Stephan Hacker at Technical University of Munich."

The doctoral 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 Characterization 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 studying 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 NanoLuc-labelled receptors (h/mH4R and hH3R). Through her results and tools, Dr. Bartole has made a significant contribution to the field of H4 receptor research. The dissertation was begun in the working group of Prof. Dr. Armin Buschauer at the University of Regensburg and, following his death, was supervised by Prof. Dr. Günther Bernhardt."

Dr. Heinrich: in recognition of his dissertation entitled Chemical Biology Applications of Photoresponsive DNA-Binding Agents. "This 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 multidrug-resistant bacteria such as Klebsiella pneumoniae. This work demonstrates the innovative power of new chemical methods and tools at the interface of medicinal chemistry and chemical biology, as well as their direct applicability to improving our understanding of infectious diseases. The dissertation was conducted in the working group of Jun.-Prof. Dr. Olalla Vázquez at Philipps-Universität 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 TRP channel signals. These signals enable mice to perceive the corresponding light signals. The work thus opens up a possible path towards new therapeutic approaches for treating macular degeneration. The dissertation was conducted 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 2020 doctoral awards 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 non-ribosomal 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 establish a foothold in bioengineering and the design of new peptides with pharmacological potential in the field of fungal systems. Her results provided concrete evidence for the active and application-oriented reprogramming of both iterative and linear synthetases for future manipulation approaches. The dissertation was carried out in the working group of Prof. Dr. Roderich D. Süssmuth at Technische Universität 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 MKK4 inhibitors through multiparameter optimisation. In addition to their potency, the innovative compounds are distinguished by outstanding selectivity towards key anti-targets. A further focus of his work was the optimisation of synthetic access to the target structures, enabling him to make target compounds for in vivo experiments available in high purity and sufficient quantities on schedule. The dissertation was carried out in the working group of Prof. Dr. Stefan Laufer at Eberhard Karls University Tübingen."