NEWS
LBB-WUT crew with publication in Communications Chemistry
Our lab team together with colleagues from Austria (an „Elk Crew” headed by Prof. Wolfgang Kroutil form University of Graz) have characterized a novel biocatalyst for the asymmetric transhydrogenation of carbonyl compounds. The title biocatalyst (named Lk-ADH Prince) is a variant of alcohol dehydrogenase from Lactobacillus kefir and was prepared using a site saturation mutagenesis strategy.
In the published work, we proved that Lk-ADH Prince exhibits excellent catalytic properties, including high activity and stereoselectivity towards a wide range of ketones, which asymmetric biotransformation products are the key chiral building blocks useful in the synthesis of pharmaceuticals. Studies of the catalytic properties were also rationalized using molecular docking simulations and detailed analysis of the morphology of the tunnels leading to the enzyme’s active site.
The results were published in Communications Chemistry (ISSN: 2399-3669, IF: 5.9) and are entitled „Biocatalytic characterization of an alcohol dehydrogenase variant deduced from Lactobacillus kefir in asymmetric hydrogen transfer„.
The research published in this paper was funded by the National Science Center (NCN) under the grant „OPUS 24” (No. 2022/47/B/ST4/00139).
More information can be found on the journal’s website: https://www.nature.com/articles/s42004-023-01013-1?utm_source=rct_congratemailt&utm_medium=email&utm_campaign=oa_20231012&utm_content=10.1038/s42004-023-01013-1#Sec22
(date: 12.10.2023)
Dr. Paweł Borowiecki became a member of the European Society of Applied Biocatalysis (ESAB)
We want to inform you that Dr. Borowiecki has been invited to join the elite group of members of the ESAB – European Society of Applied Biocatalysis.
ESAB is an organization of professional biotechnologists from all over Europe, dedicated to developing and promoting Industrial Biotechnology (so-called White Biotechnology) among employees of academia, research institutes, and the industrial sector.
ESAB is involved in organizing scientific conferences, webinars, and educational workshops.
ESAB cooperates with the European Technology Platform for Sustainable Chemistry (SusChem), a public-private partnership organization established by the European Commission to increase investment in research and innovation and enhance European competitiveness in various biotechnology sectors, including but not limited to pharmaceuticals, agrochemicals, cosmetics, food, fuel, energy, textiles, etc.
(date: 21.07.2023)
LBB-WUT crew published a new paper in The Journal of Organic Chemistry
We are delighted to announce that the publication entitled: „Chemoenzymatic synthesis of tenofovir” has been published in The Journal of Organic Chemistry (ISSN: 0022-3263, IF: 3,6).
This article reports on novel chemoenzymatic routes toward tenofovir (an anti-HIV active pharmaceutical ingredient) using low-cost starting materials and commercial or homemade enzyme preparations as biocatalysts. The biocatalytic key step was accomplished either via stereoselective reduction of the respective ketones using alcohol dehydrogenases or via kinetic resolution of the corresponding racemic alcohols using lipases.
This work is another excellent example of the fruitful collaboration of Dr. Borowiecki’s research group with Prof. Wolfgang Kroutil from the University of Graz (Austria).
These studies were funded by the National Science Center (NCN) of Poland in the framework of the „SONATA 15” grant (No. 2019/35/D/ST4/01556).
For more information, see the journal’s official website:
https://pubs.acs.org/doi/10.1021/acs.joc.3c01005
(date: 20.07.2023)
LBB-WUT crew published a new paper in Pharmaceutics
We are pleased to announce that the manuscript of scientists from our Chair, entitled: „Synthesis and Anticancer Activity of Novel Dual Inhibitors of Human Protein Kinases CK2 and PIM-1” has been published in Pharmaceutics (ISSN: 1999-4923, IF: 5.4).
The published paper reports on the development and synthesis of novel polybrominated benzoazoles and their inhibitory activity toward CK2 and PIM-1 protein kinases. Concomitantly with the inhibition studies toward recombinant enzymes, the influence of the obtained compounds on the viability of three human carcinoma cell lines, i.e., acute lymphoblastic leukemia (CCRF-CEM), human chronic myelogenous leukemia (K-562), and breast cancer (MCF-7), as well as non-cancerous cells (Vero), was evaluated.
Noteworthy, among the newly developed dual inhibitors, 1,1,1-trifluoro-3-[(4,5,6,7-tetrabromo-1H-benzimidazol-2-yl)amino]propan-2-ol demonstrates the highest selectivity and the most prominent proapoptotic properties towards the studied cancer cells, especially towards acute lymphoblastic leukemia, in addition to inducing autophagy in K-562 cells.
The article was dedicated to Prof. Zygmunt Kazimierczuk (1945-2021) – one of the most recognized Polish bioorganic chemists, who dedicated the last two decades of his life to the development and synthesis of inhibitors of protein kinases! It is worth mentioning that, thanks to his knowledge and commitment, Professor Kazimierczuk contributed to the production and registration in Poland of an anticancer and immunosuppressive drug available for clinical treatment called biocladribine.
This article belongs to the Special Issue „Kinase Inhibitor for Cancer Therapy„.
For more information, see the journal’s official website: https://www.mdpi.com/1999-4923/15/7/1991
(date: 20.07.2023)
Dr. Borowiecki together with Dr. Zajda and Dr. Matczuk published a new paper in Talanta
We are pleased to announce that the publication entitled: „Effective monitoring of Platinum-DNA adducts formation under simulated physiological conditions by CE-ICP-MS/MS” has been published in Talanta (ISSN: 1873-3573, IF: 6.556).
The article presents the novel approach based on the hyphenation of capillary electrophoresis with inductively coupled plasma tandem mass spectrometry (CE-ICP-MS/MS) for studying Pt-DNA adduct formation. This work is excellent example of cooperation between Dr. Borowiecki and Dr. Joanna Zajda and Dr. Magdalena Matczuk from the Chair of Analytical Chemistry, Faculty of Chemistry, Warsaw University of Technology.
More information about the project can be found at:https://www.sciencedirect.com/science/article/abs/pii/S0039914023005003
(date: 12.06.2023)
Dr. Paweł Borowiecki received funding from NCN Opus 24 grant
The National Science Center (NCN) of Poland has announced the results of the OPUS and SONATA competitions!
The OPUS competition is aimed at all researchers regardless of the stage of their scientific career, while SONATA is aimed at projects carried out by researchers who hold a doctoral degree.
We are pleased to announce that among the winners of the Opus 24 program was Dr. Paweł Borowiecki, who received funding for his scientific project entitled:
„The Power of Hybrid – Development of Novel Multienzymatic Cascade Reactions and Photobiocatalytic Redox Systems for Asymmetric Synthesis of Optically Active Compounds with High Added Value („EnzCasc-Photo4BioCat”)”.
More information about the project can be found at: https://www.ncn.gov.pl/sites/default/files/listy-rankingowe/2022-09-15-opu8jisl/streszczenia/567774-pl.pdf
Congratulations and much success in research work!
(date: 18.05.2023)
Dr. Paweł Borowiecki as a Guest Editor for Special Issue „Chemoenzymatic Synthesis” in Commun. Chem. journal
We are proud to announce that Dr. Borowiecki, together with Dr. Jennifer Bridwell-Rabb from the Department of Chemistry at the University of Michigan, Ann Arbor, and Dr. Sandy Schmidt from the Gröningen Research Institute of Pharmacy, University of Gröningen, will coordinate the edition of a Special Issue entitled: “Chemoenzymatic synthesis” in Nature: Communications Chemistry (ISSN 2399-3669, IF: 7.211).
This Collection aims to present the latest progress in biocatalysis, with topics of interest including but not limited to:
- Enzyme engineering
- Multienzymatic cascades
- Chemoenzymatic cascades
- Metalloenzymes
- Photo-biocatalysis
- Multifunctional biocatalysts
- Enzyme promiscuity
For more details, visit: https://www.nature.com/collections/afjacdgebd/guest-editors
(date: 18.04.2023)
Dr. Paweł Borowiecki became a laureate of the Young PW grant
We are pleased to announce that Dr. Paweł Borowiecki received funding (149 983 PLN; 32 393 EUR) from YOUNG PW (IDUB) grant on his project entitled: “Biotechnological Application of a New Variant of Recombinant Alcohol Dehydrogenase from Lactobacillus kefir in the Asymmetric Synthesis of Optically Active Compounds with High Added Value“.
The YOUNG PW Project aims to support the scientific development of young scientists, i.e., Ph.D. students and employees of the Warsaw University of Technology engaged in scientific activity, who are counted as N-number members and do not have a doctoral degree or have a doctoral degree received less than seven years before the formal grant application.
The research project topics carried out within the framework of the YOUNG PW grant relate to research in the “Strategic Fields of Interaction” field as defined in the “Strategy for the Development of Warsaw University of Technology until 2030”.
(date: 27.03.2023)
Dr. Paweł Borowiecki became a laureate of the „Best of the best of PW” programme
We are pleased to announce that among the winners of the first edition of the „Best of the Best PW” programme was Dr. Paweł Borowiecki.
The aim of this programme is to provide individualized support for outstanding young PW employees in the development of their academic career, both scientific and teaching at WUT.
The program of individualized support for young scientists is funded by the „Excellence Initiative: Research University (IDUB)’.
The list of all winners of the first edition of the „Best of the Best PW” is available at: https://badawcza.pw.edu.pl/Konkursy/Wyniki-konkursow/2023/Wyniki-konkursu-Najlepsi-z-najlepszych-PW
(date: 27.03.2023)
LBB-WUT crew published a new paper in Catalysts
We are pleased to announce that the publication entitled: „Chemoenzymatic Synthesis of Optically Active Alcohols Possessing 1,2,3,4-Tetrahydroquinoline Moiety Employing Lipases or Variants of the Acyltransferase from Mycobacterium smegmatis” has been published in Catalysts (ISSN: 2073-4344, IF: 4.501) and is part of the Special Issue „Applications of Hydrolases in Medicinal Chemistry” hosted by Dr. Borowiecki and Dr. Dominik Koszelewski from the IChO PAS.
The article presents the kinetic resolution of racemic alcohols bearing 1,2,3,4-tetraquinoline substituents using commercially available lipases and the engineered variants of acyltransferase from Mycobacterium smegmatis (MsAcT). Interestingly, the employment of MsAcT variants enabled the separation of the titled enantiomers in an aqueous media, which contradicts the fundamentals of the convenient synthesis of esters due to the unfavorable equilibrium of such reactions in water. This work is another excellent example of fruitful cooperation between Dr. Borowiecki’s team and Prof. Wolfgang Kroutil from the University of Graz.
(date: 12.12.2022)
LBB-WUT crew published a new paper in CrystEngComm
We are pleased to announce that the publication entitled: ‘Supramolecular synthon hierarchy in cyclopropyl-containing peptide-derived compounds’ has been published in CrystEngComm (ISSN: 1466-8033, IF: 3.756).
It is worth noting that this work was carried out in international cooperation with researchers Slovakia and Poland and reports on important aspects of the molecular basis of biological activity of set of novel cyclopropyl-containing peptide-derived compounds, which might be promising candidates for prostate cancer prevention or management.
(date: 24.11.2022)
LBB-WUT crew published a new paper in the International Journal of Molecular Sciences
We are pleased to announce that the publication entitled: „Chemoenzymatic Synthesis of Optically Active Ethereal Analog of iso-Moramide—A Novel Potentially Powerful Analgesic” has been published International Journal of Molecular Sciences (ISSN: 1422-0067, IF: 6.208).
This article reports on design and synthesize a novel potent analog of iso-moramide utilizing molecular docking calculations and a chemoenzymatic methodology. We also want to inform you that this article has been dedicated in memory of Dr Paul Janssen (1926-2003) who revolutionized medicinal chemistry and human therapies!
These studies were funded by the National Science Center (NCN) of Poland grant „SONATA 15” (Grant No. 2019/35/D/ST4/01556).
(date: 15.10.2022)
Warsaw University of Technology Rector’s Awards for Academic Teachers
We are pleased to announce that on September 30, 2022, Dr. Paweł Borowiecki was awarded the 'Rector of Warsaw University of Technology Awards’ in the science category. The official presentation of commemorative diplomas received from the Dean of the Faculty of Chemistry of the Warsaw University of Technology, Prof. Władysław Wieczorek, Ph.D., took place during the official inauguration of the new academic year 2022/23 in the Middle Hall of the Main Building of the Warsaw University of Technology.
Dr. Paweł Borowiecki received the „Individual Award of Degree I” of the Rector of the Warsaw University of Technology for scientific achievements in 2020-2021.
This award is given for prestigious scientific publications that significantly impact the state of the art and development of further research directions.
(date: 30.09.2022)
Dr. Paweł Borowiecki became an Affiliate member of the Royal Society of Chemistry
We want to inform you that Dr. Borowiecki has been invited to join the elite group of Affiliate Members of the Royal Society of Chemistry. It is worth mentioning that the favorable decision was determined by the high scientific level of articles published this year in prestigious journals of the Royal Society of Chemistry. We invite all interested persons to read those publications at Catalysis Science & Technology and RSC Advances
(date: 11.08.2022)
LBB-WUT crew published a new paper in RSC Advances
We are delighted to announce that the publication entitled: „Development of a novel chemoenzymatic route to enantiomerically enriched β-adrenolytic agents. A case study toward propranolol, alprenolol, pindolol, carazolol, moprolol, and metoprolol” has been published in RSC Advances (ISSN: 2046-2069, IF: 4.036).
This article reports on efficient chemoenzymatic routes toward both enantiomers of β-blockers, which were accomplished by identifying a central chiral building block prepared using either lipase-catalyzed kinetic resolution methodology or ADH-catalyzed biotranshydrogenation. This work is another excellent example of fruitful collaboration of our lab team with Prof. Wolfgang Kroutil from the University of Graz.
P.S. We are happy to say ufffff …. we made it! It was as hard as establishing a new route in the high mountains!
These studies were funded by the National Science Center (NCN) of Poland grant „SONATA 15” (Grant No. 2019/35/D/ST4/01556).
(date: 10.08.2022)
LBB-WUT crew published a new paper in Bioorganic Chemistry
We are pleased to announce that the publication entitled: „Biocatalytic Hydrogen-Transfer To Access Enantiomerically Pure Proxyphylline, Xanthinol, and Diprophylline” has been published in Bioorganic Chemistry (ISSN: 0045-2068, IF: 5.307).
This article reports on a novel biocatalytic synthetic route toward optically pure xanthine-based APIs, which are very useful as efficient bronchial vasodilators. It is worth noting that this work was carried out in international cooperation with Professor Wolfgang Kroutil from the University of Graz, Austria (Karl-Franzens-Universität Graz). We also want to inform you that this article has been dedicated in memory of Prof. Jacek K. Gawroński (1943–2020), who was a fabulous scientist, academic tutor, and author of the cult academic textbook entitled: „Stereochemistry in Organic Synthesis”!
These studies were funded by the National Science Center (NCN) of Poland grant „SONATA 15” (Grant No. 2019/35/D/ST4/01556).
(date: 14.06.2022)
LBB-WUT crew published a new paper in Catalysis Science & Technology
We are delighted to announce that the publication entitled: „Chemoenzymatic deracemization of lisofylline catalyzed by a (laccase/TEMPO)-alcohol dehydrogenase system” has been published in Catalysis Science & Technology (ISSN: 2044-4761, IF: 6.177).
This article reports on a novel biocatalytic method for the synthesis of both enantiomers of lisofylline based on Trametes versicolor laccase, TEMPO as a redox mediator, and stereocomplementary recombinant alcohol dehydrogenases as biocatalysts. It is also worth noting that this work was carried out in international cooperation with Professor Wolfgang Kroutil from the University of Graz, Austria (Karl-Franzens-Universität Graz). By the way, we are pleased that this paper is our first one accepted in the journal published by the Royal Chemical Society (RSC), and we hope not the last! This is also a first paper published by our first-year PhD Student – Ola Rudzka. Congrads for her!
These studies were funded by the National Science Center (NCN) of Poland grant „SONATA 15” (Grant No. 2019/35/D/ST4/01556).
(date: 16.05.2022)
LBB-WUT crew published a new paper in Catalysts
We are pleased to announce that the publication entitled: „Expanding Access to Optically Active Non-Steroidal Anti-Inflammatory Drugs via Lipase-Catalyzed KR of Racemic Acids Using Trialkyl Orthoesters as Irreversible Alkoxy Group Donors” has been published in Catalysts (ISSN: 2073-4344, IF: 4.501) and is a part of Special Issue „Applications of Hydrolases in Medicinal Chemistry” hosted by Dr. Borowiecki and Dr. Koszelewski from IChO PAS.
This article reports on a novel biocatalytic method for the synthesis of enantiomerically enriched blockbuster (S)-profens, namely naproxen, ibuprofen, flurbiprofen, and ketoprofen. It is also worth noting that this work was carried out in cooperation with Dr. Jan Kutner from the Laboratory for Structural and Biochemical Research, Biological and Chemical Research Centre, Department of Chemistry, University of Warsaw.
These studies were funded by the National Science Center (NCN) of Poland grant „SONATA 15” (Grant No. 2019/35/D/ST4/01556).
(date: 16.05.2022)
Dr. Paweł Borowiecki’s publication on the cover of ACS Sustainable Chemistry & Engineering
We are delighted to share our research published in ACS Sustainable Chemistry & Engineering (IF = 8.198) demonstrating an innovative and cost-effective lipase-catalyzed kinetic resolution of secondary alcohols based on a fully renewable and non-toxic α-angelica lactone as an irreversible acylating agent. The designed biocatalytic approach was integrated with a simple Girard’s P reagent strategy, which can be performed on a multi-gram scale, leading to enantiomerically pure pharmaceutically relevant building blocks isolated in satisfactory yields without using preparative chromatography. Furthermore, the elaborated methodology based on extractive purification strategy reduces the emission of volatile solvents, eliminates hazardous materials, such as cancerogenic silica gel and vinyl acetate, and enables more process waste to be recycled. Therefore, it might open avenues for possible broader synthetic applications in the resolution of enantiomers useful in the pharamceuticals manufacturing. We hope that over two years of research in a narrow collaboration between Dr. Borowiecki and Dr. Poterała from the Chair of Organic Chemistry WUT resulted in an impactful manuscript. The paper is entitled: „From Waste to Value – Direct Utilization of α-Angelica Lactone as a Non-conventional Irreversible Acylating Agent in a Chromatography-free Lipase-catalyzed KR Approach Towards sec-Alcohols” and was also recognized by the Journal’s Editors as 'a very important paper’ by highlighting it with the Cover art work.
These studies were funded by the National Science Center (NCN) of Poland grant „SONATA 15” (Grant No. 2019/35/D/ST4/01556).
(date: 07.08.2021)
NEW paper of our Lab-Team in the International Journal of Molecular Sciences
We are pleased to announce that the publication of Dr Borowiecki, entitled: ‘Synthesis of Novel Acyl Derivatives of 3‐(4,5,6,7‐Tetrabromo‐1H‐benzimidazol‐1‐yl)propan‐1‐ols — Intracellular TBBi‐Based CK2 Inhibitors with Proapoptotic Properties’ was published in highly prestigious International Journal of Molecular Sciences (ISSN: 1422-0067, IF: 5.923).
It is worth noting that this research was carried out in cooperation with scientists from the National Institute of Medicines and the Nencki Institute of Experimental Biology of the Polish Academy of Sciences and raises important aspects concerning the synthesis of polybrominated benzoazole prodrugs and their inhibitory activity toward CK2 protein kinase as well as anti-cancer properties against breast cancer cells. The article was published in the Open Access (OA) model, which greatly increases the chances of its wider impact.
(date: 10.06.2021)
LBB-WUT crew published a new paper in Frontiers in Chemistry
We are pleased to announce that the publication entitled: ’The First Insight Into the Supramolecular System of D,L-α-Difluoromethylornithine: A New Antiviral Perspective’ has been published in Frontiers in Chemistry (ISSN: 2296-2646, IF: 5.221).
It is worth noting that this work was carried out in international cooperation with researchers from the UK, Slovakia and Poland (Dr Joanna Bojarska and Prof. Wojciech Wolf) and reports on important aspects of the molecular basis of biological activity of DFMO and its halogenated analogs.
(date: 15.05.2021)
LBB-WUT crew with a new paper in Molecular Catalysis journal
We are extremely happy that our new paper on ‘Chemoenzymatic Enantioselective and Stereo-Convergent Syntheses of Lisofylline Enantiomers via Lipase-catalyzed Kinetic Resolution and Optical Inversion Approach’ was published today in Molecular Catalysis (ISSN: 2468-8231; IF: )!
We hope that our paper will help medicinal chemists to prepare this enantiomeric API in preparative scale to complete on-going clinical trials on extremely interesting pharmacological properties of its enantiomers. Congrats to all authors!
(date: 18.03.2021)
Dr Borowiecki & Dr Koszelewski as a Guest Editors for Special Issue “Applications of Hydrolases in Medicinal Chemistry”
We are proud to announce that Doctor Borowiecki together with his colleague from IChO PAS, Dr Dominik Koszelewski, will coordinate the edition of a Special Issue of the journal Catalysts (ISSN 2073-4344; IF: 4.146), entitled: “Applications of Hydrolases in Medicinal Chemistry”. The aims of this Special Issue are as follows: the application of hydrolases for chemoenzymatic syntheses of new compounds of defined biological activities; development of novel or significantly-improved hydrolase-catalyzed routes toward key pharmaceutical intermediates and/or enantiomeric drugs; biotransformations carried out using isolated enzymes and/or whole-cell biocatalysts.
The deadline for collaboration is now open.
See: https://www.mdpi.com/journal/catalysts/special_issues/hydrolases_medicinal for details of the submission.
hydrolases_medicinal-flyer.pdf
(date: 01.03.2021)
LBB-WUT crew with a new paper in Bioorganic Chemistry journal
We are pleased to announce that a new article entitled: ‘Chemoenzymatic synthesis of enantiomerically enriched diprophylline and xanthinol nicotinate’ from the members of LBB-WUT is available in the Bioorganic Chemistry (ISSN: 0045-2068; IF: 5.275). We hope that this paper will inspire other researchers to elaborate alternative asymmetric routes toward optically active broncho- and vaso-dilators.
More info on this topic can be found: https://www.sciencedirect.com/science/article/abs/pii/S0045206820317466
(date: 01.02.2021)