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Department of Bioorganic Chemistry is one of 15 departments of Faculty of Chemistry, Wrocław University of Technology. It was founded in 1971 by Professor Przemysław Mastalerz in response to introduction of biochemistry and biotechnology curricula at Faculty of Chemistry. Now it is headed by Professor Paweł Kafarski and formed by 6 professors, 10 assistant professors and over 25 PhD students doing research on a border of chemistry and biology.


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Research

Publications


Open positions for PhD studies


Symposium on Biotransformations for Pharmaceutical and Cosmetic Industry



Recent papers

Aminobisphosphonates based on cyclohexane backbone as coordinating agents for metal ions. Thermodynamic, spectroscopic and biological studies
Gałęzowska, J.; Czapor-Irzabek, H.; Chmielewska, E.; Kafarski, P.; Janek, T.
New J. Chem. 2018, 42, 7723
DOI: 10.1039/c8nj01158c

Abstract
Single and double amino-bisphosphonates were synthesized and tested for coordination capabilities towards Ca2+, Mg2+, Cu2+ and Ni2+ metal ions by means of potentiometry, UV-vis spectroscopy, mass spectrometry (ESI-MS) and isothermal titration calorimetry (ITC), as well as for cytotoxic activity by MTT [(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide)] assay. Half minimal inhibitory concentrations (IC50) were determined with respect to two cell lines (human melanoma A375 and human colorectal adenocarcinoma HT29). Basing the structure of compounds on a cyclohexane ring allowed for a slight reduction of high hydrophilic character of the studied bisphosphonates (BPs). The ligands efficiently bind the examined metal ions forming complex equilibria with diversified stoichiometry of equimolar, polynuclear species and biscomplexes. Both ligands as well as their Ca2+ and Mg2+ complexes show selective antiproliferative activity toward the studied cancer cell lines. Given the thermodynamic and biological data, it can be assumed that ligands are good candidates for linking compounds that may be used in the design of new drug delivery systems. In this approach, one bisphosphonate moiety acts as a bone-targeting molecule, while another molecule can be readily attached to the second donor function (primary amine or bisphosphonate).

Recent papers

Recent advances in design of new urease inhibitors: A review
Aminobisphosphonates based on cyclohexane backbone as coordinating agents for metal ions. Thermodynamic, spectroscopic and biological studies
New J. Chem. 2018, 42, 7723
DOI: 10.1039/c8nj01158c

Abstract
Single and double amino-bisphosphonates were synthesized and tested for coordination capabilities towards Ca2+, Mg2+, Cu2+ and Ni2+ metal ions by means of potentiometry, UV-vis spectroscopy, mass spectrometry (ESI-MS) and isothermal titration calorimetry (ITC), as well as for cytotoxic activity by MTT [(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide)] assay. Half minimal inhibitory concentrations (IC50) were determined with respect to two cell lines (human melanoma A375 and human colorectal adenocarcinoma HT29). Basing the structure of compounds on a cyclohexane ring allowed for a slight reduction of high hydrophilic character of the studied bisphosphonates (BPs). The ligands efficiently bind the examined metal ions forming complex equilibria with diversified stoichiometry of equimolar, polynuclear species and biscomplexes. Both ligands as well as their Ca2+ and Mg2+ complexes show selective antiproliferative activity toward the studied cancer cell lines. Given the thermodynamic and biological data, it can be assumed that ligands are good candidates for linking compounds that may be used in the design of new drug delivery systems. In this approach, one bisphosphonate moiety acts as a bone-targeting molecule, while another molecule can be readily attached to the second donor function (primary amine or bisphosphonate).

Recent papers

Non-symmetrical bis(aminoalkyl)phosphinates: new ligands with enhanced binding of Cu(II) ions.
Piasta, K.; Dziełak, A.; Mucha, A.; Gumienna-Kontecka, E.
New J. Chem. 2018, 42, 7737
DOI: DOI: 10.1039/c8nj01094c
Abstract
Three novel, non-symmetrical bis(aminoalkyl)phosphinic acids, L1–L3, have been synthesized and characterized. Solution studies on the coordination abilities of the ligands have shown that these compounds form various protonated mono- and bis-complexes, where copper(II) coordination is realized through the nitrogen atom(s) of the amino group(s), supported by oxygen(s) from the phosphinate unit(s). Potentiometric titrations and a full spectroscopic analysis clarified the species distribution profiles and detailed coordination modes. The results show that L1–L3 ligands are efficient chelating agents for Cu(II) ions; their metal binding abilities were compared to structurally related compounds described earlier in the literature.

Recent papers

Screening Combinatorial Peptide Libraries in Protease Inhibitor Drug Discovery
Poreba M, Kasperkiewicz P, Rut W, Drag M
Extracellular Targeting of Cell Signaling in Cancer: Strategies Directed at MET and RON Receptor Tyrosine Kinase Pathways, 1 2018, 1
DOI: 10.1002/9781119300229.ch11

Recent papers

Caspase selective reagents for diagnosing apoptotic mechanisms
Poreba M, Groborz K, Navarro M, Snipas SJ, Drag M, Salvesen GS
Cell Death and Differentiation 2018, 1
DOI: 10.1038/s41418-018-0110-y

Recent papers

Nanosilica synthesis mediated by Aspergillus parasiticus strain.
Pieła A, Żymańczyk-Duda E, Brzezińska-Rodak M, Duda M, Grzesiak J, Klimek-Ochab M
Fungal Biology 2018, 1
DOI: 10.1016/j.funbio.2018.02.004

Recent papers

Unique Substrate Specificity of SplE Serine Protease from Staphylococcus aureus
Stach N, Kalinska M, Zdzalik M, Kitel R, Karim A, Serwin K, Rut W, Larsen K, Jabaiah A, Firlej M, Wladyka B, Daugherty P, Stennicke H, Drag M, Potempa J, Dubin G
Structure 2018, 1
DOI: 10.1016/j.str.2018.02.008

Recent papers

Fungal synthesis of chiral phosphonic synthetic platform – Scope and limitations of the method
Serafin-Lewańczuk M, Klimek-Ochab M,Brzezińska-Rodak M, Żymańczyk-Duda E
Bioorganic Chemistry 2018, 77, 402
DOI: 10.1016/j.bioorg.2018.01.027

Recent papers

Extensive peptide and natural protein substrate screens reveal that mouse caspase-11 has much narrower substrate specificity than caspase-1
Gonzalez-Ramirez ML*, Poreba M*, Snipas SJ, Groborz K, Drag M, Salvesen GS (* equal contribution)
Journal of Biological Chemistry 2018, 1
DOI: 10.1074/jbc.RA117.001329

Recent papers

Selective imaging of cathepsin L in breast cancer by fluorescent activity-based probes
Poreba M, Rut W, Vizovisek M, Groborz K, Kasperkiewicz P, Finlay D, Vuori K, Turk D, Turk B, Salvesen GS, Drag M
Chemical Science 2018, 1
DOI: 10.1039/c7sc04303a