General information

Name: Tihomir

Surname: Tomašič

E-mail: tihomir.tomasic@ffa.uni-lj.si

Cell phone number with international prefix: +38640847825

Country: Slovenia

Affiliation: University of Ljubljana, Faculty of Pharmacy

Gender: F □ M ×

Year of the PhD title: 2011

Personal web page: http://www.ffa.uni-lj.si/en/faculty/employees/oseba/tomasic-tihomir/

Previous COST participation: No □ Yes ×

 

List of 10 selected publications within last 5 years

1. TOMAŠIČ, Tihomir, KATSAMAKAS, Sotirios, HODNIK, Žiga, ILAŠ, Janez, BRVAR, Matjaž, ŠOLMAJER, Tomaž, MONTALVÃO, Sofia, TAMMELA, Päivi, BANJANAC, Mihailo, ERGOVIĆ, Gabrijela, ANDERLUH, Marko, PETERLIN-MAŠIČ, Lucija, KIKELJ, Danijel. Discovery of 4,5,6,7-tetrahydrobenzo[1, 2-d]thiazoles as novel DNA gyrase inhibitors targeting the ATP-binding site. Journal of medicinal chemistry, 2015, 58, 5501-521.

2. ZIDAR, Nace, MACUT, Helena, TOMAŠIČ, Tihomir, BRVAR, Matjaž, MONTALVÃO, Sofia, TAMMELA, Päivi, ŠOLMAJER, Tomaž, PETERLIN-MAŠIČ, Lucija, ILAŠ, Janez, KIKELJ, Danijel. N-phenyl-4,5-dibromopyrrolamides and N-phenylindolamides as ATP competitive DNA gyrase B inhibitors: design, synthesis, and evaluation. Journal of medicinal chemistry, 2015, 58, 6179-6194.

3. HODNIK, Žiga, TOMAŠIČ, Tihomir, SMODIŠ, Domen, D’AMORE, Claudio, PETERLIN-MAŠIČ, Lucija, FIORUCCI, Stefano, KIKELJ, Danijel. Diethylstilbestrol-scaffold-based pregnane X receptor modulators. European Journal of Medicinal Chemistry, 2015, 103, 551-562.

4. JUG, Gregor, ANDERLUH, Marko, TOMAŠIČ, Tihomir. Comparative evaluation of several docking tools for docking small molecule ligands to DC-SIGN. Journal of molecular modeling, 2015, 21, 1-12.

5. KOTAR, Anita, TOMAŠIČ, Tihomir, LENARČIČ ŽIVKOVIĆ, Martina, JUG, Gregor, PLAVEC, Janez, ANDERLUH, Marko. STD NMR and molecular modelling insights into interaction of novel mannose-based ligands with DC-SIGN. Organic and Biomolecular Chemistry, 2016, 14, 862-875.

6. TOMAŠIČ, Tihomir, NABERGOJ, Dominik, VRBEK, Sanja, ZIDAR, Nace, JAKOPIN, Žiga, ŽULA, Aleš, HODNIK, Žiga, JUKIČ, Marko, ANDERLUH, Marko, ILAŠ, Janez, SOLLNER DOLENC, Marija, PELUSO, Jean, UBEAUD-SÉQUIER, Geneviève, MULLER, Christian D., PETERLIN-MAŠIČ, Lucija, KIKELJ, Danijel. Analogues of the marine alkaloids oroidin, clathrodin, and hymenidin induce apoptosis in human HepG2 and THP-1 cancer cells. MedChemComm, 2015, 6, 105-110.

7. HODNIK, Žiga, PETERLIN-MAŠIČ, Lucija, TOMAŠIČ, Tihomir, SMODIŠ, Domen, D’AMORE, Claudio, FIORUCCI, Stefano, KIKELJ, Danijel. Bazedoxifene scaffold-based mimetics of solomonsterols A and B as novel pregnane X receptor antagonists. Journal of medicinal chemistry, 2014, 57, 4819-4833.

8. TOMAŠIČ, Tihomir, RABBANI, Said Rahnamaye, GOBEC, Martina, MLINARIČ-RAŠČAN, Irena, PODLIPNIK, Črtomir, ERNST, Beat, ANDERLUH, Marko. Branched [alpha]-D-mannopyranosides; a new class of potent FimH antagonists. MedChemComm, 2014, 5, 1247-1253.

9. TOMAŠIČ, Tihomir, HARTZOULAKIS, Basil, ZIDAR, Nace, CHAN, Fiona, KIRBY, Robert W., MADGE, David J., PEIGNEUR, Steve, TYTGAT, Jan, KIKELJ, Danijel. Ligand- and structure-based virtual screening for clathrodin-derived human voltage-gated sodium channel modulators. Journal of chemical information and modeling, 2013, 53, 3223-3232.

10. TOMAŠIČ, Tihomir, ŠINK, Roman, ZIDAR, Nace, FIC, Anja, CONTRERAS-MARTEL, Carlos, DESSEN, Andréa, PATIN, Delphine, BLANOT, Didier, MÜLLER-PREMRU, Manica, GOBEC, Stanislav, ZEGA, Anamarija, KIKELJ, Danijel, PETERLIN-MAŠIČ, Lucija. Dual inhibitor of MurD and MurE ligases from Escherichia coli and Staphylococcus aureus. ACS Medicinal Chemistry Letters, 2012, 3, 626-630.

 

Main skills and expertise (up to 5)

1. Medicinal chemistry – design, synthesis and biological evaluation of small molecules

2. Computational chemistry – molecular docking, virtual screening, homology modelling, molecular dynamics

3. Chemical analysis – NMR, MS, IR, HPLC analysis of organic compounds

4.

5.

 

Main equipment/facilities available in the participants’ lab (up to 5)

1. 400 MHz Bruker AVANCE III spectrometer

2. VGAnalytical Autospec Q mass spectrometer

3. Workstation: 4 x 16 core AMD Opteron (Interlagos) 6272, 32 GB RAM, two 1 TB hard drives

4.

5.

 

 

Short personal activity proposal for the COST Action CA15135 (max 1000 characters)

My research activities include mainly the structure- and/or ligand-based design and synthesis of small molecules possessing biological activity acting on a single target or multiple targets. My activity proposal for the COST Action CA15135 is a research focused on the design of dual-targeting inhibitors of bacterial DNA gyrase and topoisomerase IV possessing antibacterial activity. Compounds will be designed using molecular docking in the available crystal structures of enzyme-inhibitor complexes, selected compounds synthesized and biologically evaluated and their interactions with the target(s) studied by a combination of molecular docking and molecular dynamics simulations. Since broad-spectrum antibacterial activity is a desired property of dual DNA gyrase/topoisomerase IV inhibitors, differences and similarities of these enzymes from different bacterial strains will be taken into account in the design of novel dual inhibitors. This work fits well in the WG1: Development of new chemical entities.

 

Work Group preference: score from 1 (preferred) to 4 (not preferred)

Work Group of the CA15135 COST Action	Score
WG1: Development of new chemical entities	1
WG2: Selection of biological targets and assessment of biological data	4
WG3: Development of chemical databases	2
WG4: Development of Computational methods for multiple ligand design and discovery	3