Chemical Strategies and Solutions for Bacteria and Cancer cell Resistance

The key moment, which set the path of my research vision, came after my PhD in 2004. I realised at that point that academic medicinal chemistry is focused mostly on the optimisation of potency of new compounds and not on integrated optimisation of potency, physicochemical properties and safety. After my PhD, in addition to medicinal chemistry I proceed with interdisciplinary training and research in toxicology. It was essential for me to leave the academic environment and perform the postdoctoral training in large pharmaceutical company (AstraZeneca, Safety Assessment Department, Sweden). The industrial experience and interdisciplinary in medicinal chemistry and toxicology gave me essential competitive advantage for the applied part of my research work in the field of antibacterial and anticancer hit and hit-to-lead drug discovery.

CURRENT POSITION
2017- Full Professor of Medicinal Chemistry, University of Ljubljana
2021- in parallel associate professor of Toxicological Chemistry, University of Ljubljana

MAIN RESEARCH INTERESTS
(interdisciplinary expertise in medicinal chemistry and toxicology):
– Medicinal chemistry: new antibacterial compounds with limited resistance,  dual inhibitors of DNA gyrase B and topoisomerase IV, design of new modulators of voltage-gated potassium ion channels (K_V1.3, K_V10.1, SK channels) and their role in cancer and immune diseases; specific targeting of mitochondrial ion channels in cancer;
– Toxicology: toxicology in the early drug discovery, in vitro drug metabolism; endocrine disrupting chemicals; mechanistic toxicology.

Tomašič is an expert in computer-aided drug design and synthesis of bioactive compounds, particularly with anticancer and antibacterial activities. His research focus at present is on the development of Hsp90 and voltage-gated ion channel inhibitors with anticancer activities, and DNA gyrase inhibitors as antibacterial agents. His expertise in molecular modelling covers library design, library preparation, molecular docking, molecular dynamics simulations, homology modelling, virtual screening, pharmacophore modelling and physicochemical and ADMET property prediction and optimisation. He has also expertise in organic synthesis and analysis and characterisation of small molecules. He acts as an Editor in Pharmaceutics and Frontiers in Chemistry. He participated in several national and international research projects acting as project leader or collaborator.

CURRENT POSITION
2023- Full Professor of Medicinal Chemistry, University of Ljubljana

MAIN RESEARCH INTERESTS
– new antibacterial compounds with limited resistance acting as dual inhibitors of DNA gyrase B and topoisomerase IV
– development of new Hsp90 inhibitors acting by novel mechanisms of action as anticancer drugs
– design of new modulators of voltage-gated potassium channels (K_V1.3, K_V10.1, SK channels) and their role in cancer
– specific targeting of mitochondrial ion channels in cancer

Nace Zidar is an associate professor of medicinal chemistry at the Faculty of Pharmacy, University of Ljubljana. He graduated from Pharmacy in 2006 and received his PhD in 2011. In 2017, he completed postdoctoral training at the University of Milan (Italy). He led two research projects funded by the Slovenian Research Agency, was a member of the management committee of several European COST projects, led a bilateral project between Slovenia and the USA, and collaborated in several EU-funded drug discovery projects. He has extensive experience in medicinal chemistry. He is co-author of more than 60 SCI original scientific papers and 2 patent applications. He was awarded the UL Faculty of Pharmacy Award in 2006, the UL Faculty of Pharmacy Dean’s Award in 2010, and the Krka Award in 2011. He is a university lecturer of undergraduate courses in medicinal chemistry, biomedical analysis and drug analysis and has extensive experience in mentoring undergraduate and graduate students.

CURRENT POSITION
2017- Associate Professor of Medicinal Chemistry, University of Ljubljana

MAIN RESEARCH INTERESTS
Design, synthesis, and evaluation of new bioactive compounds, particularly those with effects on voltage-gated ion channels (Na_v1.3, Na_v1.7, H_v1), bacterial and human topoisomerases (DNA gyrase, topoisomerase IV, human DNA topoisomerase II), and with anticancer activity.

Andrej carried out his undergraduate research with Prof. D. Kikelj at the Faculty of Pharmacy, Ljubljana, in the field of antibacterials. He obtained his PhD in organic chemistry with B. Mohar at the National institute of Chemistry, Ljubljana, involving asymmetric reduction of ketones catalyzed by chiral organometallic complexes. He then joined the Košmrlj group at the Faculty of Chemistry and Chemical Technology, Ljubljana, and explored the field of palladium-catalyzed C–N coupling reactions. In 2019 Andrej returned to the Faculty of Pharmacy as a postdoctoral researcher on an Innovative Medicines Initiative funded antibacterial project ENABLE, and was appointed to the title assistant professor of medicinal chemistry in 2021. He led a basic research project funded by ARIS, a French-Slovenian bilateral project Proteus, and two teaching projects funded by the Development fund of the University of Ljubljana. His research was published in the leading journals in the fields of organic and medicinal chemistry, such as Angewandte Chemie, Journal of the American Chemical Society, Journal of Medicinal Chemistry, ACS Catalysis and Organic Letters.

CURRENT POSITION
2021- Assistant Professor of Medicinal Chemistry, University of Ljubljana

MAIN RESEARCH INTERESTS
Asymmetric synthesis, Organometallic chemistry, Escaping from flatland

Janez Ilaš is a professor of medicinal chemistry at the Faculty of Pharmacy, University of Ljubljana. He completed his undergraduate studies at the same institution in 2003 and earned his PhD in 2008. His work primarily centers on medicinal chemistry, particularly in the design, synthesis, and evaluation of antitumor and antibacterial agents. His research includes the study of topoisomerase II and HDAC inhibitors for cancer treatment and gyrase and topoisomerase IV inhibitors for antibacterial therapies. Professor Ilaš has held various positions at the Faculty of Pharmacy, beginning as an assistant professor in 2009 and becoming a full professor in 2020. He has participated in national and international research projects, including those funded by the ARRS and the European Union, such as H2020 and IMI ENABLE, contributing to the development of bioactive compounds. He is also a leader of several projects with pharmaceutical industry (Krka, Slovenia; Novartis, Switzerland). His teaching responsibilities include undergraduate and postgraduate courses in medicinal chemistry, drug analysis and biophysical methods.

CURRENT POSITION
2020 – Full Professor of Medicinal Chemistry, University of Ljubljana

MAIN RESEARCH INTERESTS
Design, synthesis, and evaluation of bioactive compounds, with a focus on topoisomerase II and HDAC inhibitors for anticancer therapies, as well as bacterial gyrase and topoisomerase IV inhibitors for antibacterial agents. His research also involves biophysical methods for evaluating enzyme inhibitory activities, including the use of isothermal titration calorimetry and biolayer interferometry to study intermolecular interactions. Additionally, he uses HPLC-MS for evaluating the inhibitory activities of compounds. In the area of pharmaceutical chemistry, he applies analytical methods such as mass spectrometry (MS) and high-resolution mass spectrometry (HRMS) to assess synthesized compounds and their potential as bioactive agents.