professor Marcin Drąg

Marcin Drąg

Born: Świdnica, Poland, July 30, 1975.

Hobby: spin fishing for predatory fish, fly fishing, diving.

Address: Department of Bioorganic Chemistry, Faculty of Chemistry, Wroclaw University of Technology, Wybrzeze Wyspianskiego 27, 50-370 Wroclaw, Poland

Phone: +48-74-320-4526 Fax: +48 71 328 40 64

Education

Master of Science, 1999, University of Wroclaw, Poland, Coordination Chemistry - Master thesis: "The synthesis, properties and structural investigation of Rh (I) complexes with chelating ligands",

PhD in Chemistry, 2003, Wroclaw University of Technology, Poland, Bioorganic Chemistry - Prof. Pawel Kafarski, PhD thesis: “Synthesis, structural investigations and biological activity of phosphonic inhibitors of leucine aminopeptidase and cathepsin C”.

Habilitation in Chemistry, 2011, Wroclaw University of Technology, Poland, Title of thesis: “Libraries of substrates and inhibitors as tools in the investigation of metalloproteases and cysteine proteases”.

Professor of Chemical Sciences, 2016, Wrocław University of Science and Technology, Poland, nomination by the President of the Republic of Poland

Current Positions

2016 Professor of Chemical Sciences, Wrocław University of Science and Technology, Poland

2018 Adjunct Professor, Sanford Burnham Prebys Medical Discovery Institute, La Jolla, CA, USA (http://www.sbpdiscovery.org)

Prof. Drag Lab at SBP Medical Discovery Institute

Tumor Microenvironment and Cancer Immunology Program

Former Positions

2000/03 – PhD student, Wroclaw University of Technology, Poland

2003/04 – Research Scientist, Wroclaw University of Technology, Poland

2004 – 2011 (brake for post-doctoral training) Junior Assistant Professor (Adjunct), Wroclaw University of Technology, Poland

2005/08 – Post-doctoral Associate, The Burnham Institute for Medical Research, La Jolla, CA, USA

2008-2011 Visiting Scientist, Sanford-Burnham Medical Research Institute, La Jolla, CA, USA

2011-2013 Assistant Professor (Adjunct) with habilitation, Wroclaw University of Technology, Poland

2013-2016 Associate Professor at Wroclaw University of Technology, Poland

Education abroad

1997 - Rome - Cassaccia - Italy, ENEA Center, dr Claudio Fabiani lab

1998 - Wien - Austria, Technical University of Wien, prof. Karl Kirchner lab

2000 - Montpellier - France, Ecole de Chimie, prof. H. J. Cristau lab

2005 - 2008, La Jolla, CA, USA, The Burnham Institute for Medical Research, prof. Guy S. Salvesen laboratory (http://www.salvesenlab.org)

2007 – Emory University, Atlanta, USA, short-term training, prof. Keith Wilkinson laboratory

2009 - La Jolla, CA, USA, The Burnham Institute for Medical Research, short-term training, prof. Stefan Riedl laboratory

Our Technology

In our group we have developed a novel chemical approach, called HyCoSuL (Hybrid Combinatorial Substrate Library), to dissect a broad substrate specificity of proteolytic enzymes. The use of natural and a wide range of unnatural amino acids in HyCoSuL structure allows for discovery of highly active and selective substrates, inhibitors, and activtiy based probes for multiple proteases. The detailed protocol for the synthesis and use of HyCoSuL has been recently published in Nature Protocols:

Synthesis of a HyCoSuL peptide substrate library to dissect protease substrate specificity

Research interests

Research interests include the design and synthesis of substrates, inhibitors and activity-based probes to decipher the mechanism of action and the function of proteases in health and disease.

Awards and honours

2003 - Rector's Award at Wroclaw University of Technology for doctoral thesis.

2004 – Award of Polish Chemical Society and “Sigma-Aldrich” for the best doctoral thesis in Poland in the field of organic chemistry

2004 - Award for best patent applications in medicinal chemistry at Wroclaw University of Technology.

2005 – Awarded by The Foundation for Polish Science with the Scholarship for the Promising Young Scientist (Program START).

2006 - Best poster award at Gordon Conference on Proteolytic Enzymes and their Inhibitors, New Hampshire, USA.

2009 - Beneficiary of FOCUS program by The Foundation for Polish Science.

2009 - Awarded with scholarship for Outstanding Young Investigators by Minister of Science and Higher Education.

2010 - Nominated to Young Scientists and Artists Academy in Wrocław.

2010 - Rector's Award at Wroclaw University of Technology for outstanding scientific achievements.

2011 - Nominated to Club of Young Intellectualists in Poland.

2011 - Award of Minister of Science and Higher Education in Poland for outstanding scientific achievements.

2012 - Rector's Award at Wroclaw University of Technology for outstanding scientific achievements.

2016 - Rector's Award at Wroclaw University of Science and Technology for outstanding scientific achievements.

2018 - awarded in WROCŁAW’S 30 CREATIVES in category Science by Wrocław City Council Wrocław`s 30 Creatives 2018 website

2019 - Foundation for Polish Science Prize in the field of chemical and material sciences for developing a new technological platform for obtaining biologically active compounds, in particular proteolytic enzymes inhibitors. FNP Prize 2019 website

Assistant Professors

Paulina Kasperkiewicz FNP TEAM-NET young leader

Postdoc

Natalia Małek

Anna Wieczorek

PhD Students

Radosław Gładysz

Katarzyna Groborz

Sonia Kołt

Tomasz Janiszewski

TEAM PROJECT, Foundation for Polish Science

Postdocs

Izabela Małuch

Karolina Świderska

Wioletta Rut

PhD students

Justyna Czarna

Sylwia Modrzycka

Mikołaj Żmudziński

Publications

Rut W, Groborz K, Zhang L, Modrzycka S, Poreba M, Hilgenfeld R, Drag M, Profiling of flaviviral NS2B-NS3 protease specificity provides a structural basis for the development of selective chemical tools that differentiate dengue from Zika and West Nile viruses Antiviral Research 2020, 1. View at Publisher
Rut W, Groborz K, Zhang L, Sun X, Zmudzinski M, Hilgenfeld R, Drag M, Substrate specificity profiling of SARS-CoV-2 Mpro protease provides basis for anti-COVID-19 drug design bioRxiv 2020, 1. View at Publisher
Rut W, Żmudziński M, Snipas SJ, Bekes M, Huang TT, Drag M, Engineered unnatural ubiquitin for optimal detection of deubiquitinating enzymes bioRxiv 2020, 1. View at Publisher
Aaltonen N, Singha PK, Jakupović H, Wirth T, Samaranayake H, Pasonen-Seppänen S, Rilla K, Varjosalo M, Edgington-Mitchell LE, Kasperkiewicz P, Drag M, Kälvälä S, Moisio E, Savinainen JR, Laitinen JT, High-Resolution Confocal Fluorescence Imaging of Serine Hydrolase Activity in Cryosections - Application to Glioma Brain Unveils Activity Hotspots Originating from Tumor-Associated Neutrophils. Biological Procedures Online 2020, 22, 1. View at Publisher
Kołt S, Janiszewski T, Kaiserman D, Modrzycka S, Snipas SJ, Salvesen G, Dra G M, Bird PI, Kasperkiewicz P, Detection of Active Granzyme A in NK92 Cells with Fluorescent Activity-Based Probe. Journal of Medicinal Chemistry 2020, 1. View at Publisher
Poreba M, Groborz K, Navarro M, Snipas SJ, Drag M, Salvesen GS, Caspase selective reagents for diagnosing apoptotic mechanisms Cell Death and Differentiation 2019, 26, 229. View at Publisher
Cogo F, Poreba M, Rut W, Groborz K, Smyth P, Johnston MC, Williams R, Longley DB, Burden RE, Salvesen GS, Drag M, Scott Ch., Development of an advanced nanoformulation for the intracellular delivery of a caspase-3 selective activity-based probe Nanoscale 2019, 11, 742. View at Publisher
Poreba M, Rut W, Groborz K, Snipas SJ, Salvesen GS, Drag M, Potent and selective caspase-2 inhibitor prevents MDM-2 cleavage in reversine-treated colon cancer cells Cell Death and Differentiation 2019, 26, 2695. View at Publisher
Groborz K, Kolt S, Kasperkiewicz P, Drag M, Internally Quenched Fluorogenic substrates with unnatural amino acids for cathepsin G investigation Biochimie 2019, 166, 103. View at Publisher
de Vries LE, Sanchez MI, Groborz K, Kuppens L, Poreba M, Lehmann C, Nevins N, Withers-Martinez C, Hirst DJ, Yuan F, Arastu-Kapur S, Horn M, Mares M, Bogyo M, Drag M, Deu E, Characterization of P. falciparum dipeptidyl aminopeptidase 3 specificity identifies differences in amino acid preferences between peptide-based substrates and covalent inhibitors FEBS Journal 2019, 286, 3998. View at Publisher
Groborz K, Gonzalez-Ramirez ML, Snipas SJ, Salvesen GS, Drag M, Poreba M, Exploring the prime site in caspases as a novel chemical strategy for understanding the mechanisms of cell death: a proof of concept study on necroptosis in cancer cells Cell Death and Differentiation 2019, 1. View at Publisher
Drąg-Zalesińska M, Rembiałkowska N, Borska S, Saczko J, Drąg M, Poręba M, Kulbacka J, A New Betulin Derivative Stimulates the Synthesis of Collagen in Human Fibroblasts Stronger than its Precursor In vivo 2019, 33, 1087. View at Publisher
Poreba M, Groborz K, Vizovisek M, Maruggi M, Turk D, Turk B, Powis G, Drag M, Salvesen GS, Fluorescent probes towards selective cathepsin B detection and visualization in cancer cells and patient samples Chemical Science 2019, 10, 8461. View at Publisher
Rut W, Nielsen NV, Czarna J, Poreba M, Kanse SM, Drag M, Fluorescent activity-based probe for the selective detection of Factor VII activating protease (FSAP) in human plasma Thrombosis Research 2019, 182, 124. View at Publisher
Babin BM, Kasperkiewicz P, Janiszewski T, Yoo E, Drag M, Bogyo M, Leveraging peptide substrate libraries to design inhibitors of bacterial Lon protease ACS Chemical Biology 2019, 1. View at Publisher
Anderson BM, Poole DP, Aurelio L, Ng GZ, Fleischmann M, Kasperkiewicz P, Morissette C, Drag M, van Driel IR, Schmidt BL, Vanner SJ, Bunnett NW, Edgington-Mitchell LE, Application of a chemical probe to detect neutrophil elastase activation during inflammatory bowel disease Scientific Reports 2019, 9, 13295. View at Publisher
Poreba M, Groborz K, Rut W, Pore M, Snipas SJ, Vizovisek M, Turk B, Drag M, Salvesen GS, The Activome: multiplexed probing of activity of proteolytic enzymes using mass cytometry-compatible activity-based probes (TOF-probes) bioRxiv 2019, 1. View at Publisher
Aaltonen N, Singha P, Jakupovic H, Wirth T, Samaranayake H, Pasonen-Seppanen S, Rilla K, Varjosalo M, Edgington-Mitchell L, Kasperkiewicz P, Drag M, Kalvala S, Moisio E, Savinainen JR, Laitinen JT, Tissue-ABPP enables high-resolution confocal fluorescence imaging of serine hydrolase activity in cryosections – Application to glioma brain unveils activity hotspots originating from tumor-associated neutrophils bioRxiv 2019, 1. View at Publisher
Maluch I, Czarna J, Drag M, Applications of unnatural amino acids in protease probes Chemistry - An Asian Journal 2019, 14, 4103. View at Publisher
Lunde NN, Gregersen I, Ueland T, Shetelig C, Holm S, Kong XY, Michelsen AE, Otterdal K, Yndestad A, Broch K, Gullestad L, Nyman TA, Bendz B, Eritsland J, Hoffmann P, Skagen K, Gonçalves I, Nilsson J, Grenegard M, Poreba M, Drag M, Seljeflot I, Sporsheim B, Espevik T, Skjelland M, Johansen HT, Solberg R, Aukrust P, Björkbacka H, Andersen GO, Halvorsen B, Legumain is upregulated in acute cardiovascular events and associated with improved outcome - potentially related to anti-inflammatory effects on macrophages. Atherosclerosis 2019, 1. View at Publisher
Poreba M, Rut W, Vizovisek M, Groborz K, Kasperkiewicz P, Finlay D, Vuori K, Turk D, Turk B, Salvesen GS, Drag M, Selective imaging of cathepsin L in breast cancer by fluorescent activity-based probes Chemical Science 2018, 9, 2113. View at Publisher
Gonzalez-Ramirez ML*, Poreba M*, Snipas SJ, Groborz K, Drag M, Salvesen GS (* equal contribution), Extensive peptide and natural protein substrate screens reveal that mouse caspase-11 has much narrower substrate specificity than caspase-1 Journal of Biological Chemistry 2018, 293, 7058. View at Publisher
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, Unique Substrate Specificity of SplE Serine Protease from Staphylococcus aureus Structure 2018, 26, 572. View at Publisher
Poreba M, Kasperkiewicz P, Rut W, Drag M, Screening Combinatorial Peptide Libraries in Protease Inhibitor Drug Discovery Extracellular Targeting of Cell Signaling in Cancer: Strategies Directed at MET and RON Receptor Tyrosine Kinase Pathways, 1 2018, 1. View at Publisher
Rut W, Poreba M, Kasperkiewicz P, Snipas SJ, Drag M, Selective substrates and activity-based probes for imaging of the human constitutive 20S proteasome in cells and blood samples Journal of Medicinal Chemistry 2018, 61, 5222. View at Publisher
Barry R, John SW, Liccardi G, Tenev T, Jaco J, Chen Ch, Choi J, Kasperkiewicz P, Fernandes-Alnemri T, Alnemri E, Drag M, Chen Y, Meier P, SUMO-mediated regulation of NLRP3 modulates inflammasome activity Nature Communications 2018, 9, 3001. View at Publisher
Vizovisek M, Vidmar R, Drag M, Fonovic M, Salvesen GS, Turk B, Protease Specificity: Towards In Vivo Imaging Applications and Biomarker Discovery Trends in Biochemical Sciences 2018, 1, 1. View at Publisher
Kasperkiewicz P, Kołt S, Janiszewski T, Groborz K, Poręba M, Snipas SJ, Salvesen GS, Drąg M, Determination of extended substrate specificity of the MALT1 as a strategy for the design of potent substrates and activity-based probes Scientific Reports 2018, 8, 15998. View at Publisher
Teixeira PF, Kmiec B, Branca RM, Murcha MW, Byzia A, Ivanova A, Whelan J, Drag M, Lehtiö J, Glaser E., A multi-step peptidolytic cascade for amino acid recovery in chloroplasts. Nature Chemical Biology 2017, 13, 15. View at Publisher
Balogh B, Dahmen M, Stahl M, Poreba M, Gersch M, Drag M, Sieber SA , Insights into ClpXP proteolysis: heterooligomerization and partial deactivation enhance chaperone affinity and substrate turnover in Listeria monocytogenes Chemical Science 2017, 8, 1592. View at Publisher
Rut W, Zhang L, Kasperkiewicz P, Poreba M, Hilgenfeld R, Drag M, Extended substrate specificity and first potent irreversible inhibitor/activity-based probe design for Zika virus NS2B-NS3 protease Antiviral Research 2017, 139, 88. View at Publisher
Kasperkiewicz P, Poreba M, Groborz K, Drag M, Emerging challenges in the design of selective protease substrates, inhibitors and activity-based probes for indistinguishable proteases FEBS Journal 2017, 284, 1518. View at Publisher
Drag-Zalesinska M, Drag M, Poreba M, Borska S, Kulbacka J, Saczko J, Anticancer properties of ester derivatives of betulin in human metastatic melanoma cells (Me-45) Cancer Cell International 2017, 17, 7. View at Publisher
Poreba M, Szalek A, Rut W, Kasperkiewicz P, Rutkowska-Wlodarczyk I, Snipas SJ, Itoh Y, Turk D, Turk B, Overall CM, Kaczmarek L, Salvesen GS, Drag M, Highly sensitive and adaptable fluorescence-quenched pair discloses the substrate specificity profiles in diverse protease families Scientific Reports 2017, 7, 43135. View at Publisher
Lunde NN, Haugen MH, Bodin Larsen KB, Damgaard I, Pettersen SJ, Kasem R, Rut W, Drag M, Poreba M, Johansen HT, Solberg R, Glycosylation is important for legumain localization and processing to active forms but not for cystatin E/M inhibitory functions Biochimie 2017, 139, 27. View at Publisher
Kasperkiewicz P, Altman Y, D'Angelo M, Salvesen GS, Drag M, A toolbox of fluorescent probes for parallel imaging reveals uneven location of serine proteases in neutrophils Journal of the American Chemical Society 2017, 139, 10115. View at Publisher
Poreba M, Salvesen GS, Drag M, Synthesis of a HyCoSuL peptide substrate library to dissect protease substrate specificity Nature Protocols 2017, 12, 2189. View at Publisher
Gersch M, Stahl M, Poreba M, Dahmen M, Dziedzic A, Drag M, Sieber SA, Barrel-shaped ClpP proteases display attenuated cleavage specificity ACS Chemical Biology 2016, 11, 389. View at Publisher
Byzia, A.; Szeffler, A.; Kalinowski, L.; Drąg, M., Activity profiling of aminopeptidases in cell lysates using a fluorogenic substrate library Biochimie 2016, 122, 31. View at Publisher
Modak, J. K.; Rut, W.; Wijeyewickrema, L. C.; Pike, R. N.; Drąg, M.; Roujeinkova, A., Structural basis for substrate specificity of Helicobacter pylori M17 aminopeptidase Biochimie 2016, 121, 60. View at Publisher
Rut, W.; Drąg, M., Human 20S proteasome activity towards fluorogenic peptides of various chain lengths Biol. Chem. 2016, 396, 921. View at Publisher
Drinkwater N, Sivaraman KK, Bamert RS, Rut W, Mohamed K, Vinh NB, Scammells PJ, Drag M, McGowan S, Structure and substrate fingerprint of aminopeptidase P from Plasmodium falciparum Biochemical Journal 2016, 473, 3189. View at Publisher
Poreba M, Solberg R, Rut W, Lunde NN, Kasperkiewicz P, Snipas SJ, Mihelic M, Turk D, Turk B, Salvesen GS, Drag M., Counter Selection Substrate Library Strategy for Developing Specific Protease Substrates and Probes Cell Chemical Biology 2016, 23, 1023. View at Publisher
Lentz CS, Ordonez AA, Kasperkiewicz P, La Greca F, O'Donoghue AJ, Schulze CJ, Powers JC, Craik CS, Drag M, Jain SK, Bogyo M, Design of Selective Substrates and Activity-Based Probes for Hydrolase Important for Pathogenesis 1 (HIP1) from Mycobacterium tuberculosis. ACS infectious diseases 2016, 2, 807. View at Publisher
Hachmann, J.; Edgington-Mitchell, L. E.; Poreba, M.; Sanman, L. E.; Drag, M.; Bogyo, M.; Salvesen, G. S., Probes to Monitor Activity of the Paracaspase MALT1 Chem. Biol. 2015, 22, 139. View at Publisher
Lechtenberg, B. C.; Kasperkiewicz, P.; Robinson, H.; Drag, M.; Riedl, S. J., The Elastase-PK101 structure: Mechanism of an ultrasensitive activity-based probe revealed ACS Chem. Biol. 2015, 10, 945. View at Publisher
Rut, W.; Kasperkiewicz, P.; Byzia, A.; Poreba, M.; Groborz, K.; Drag, M., Recent advances and concepts in substrate specificity determination of proteases using tailored libraries of fluorogenic substrates with unnatural amino acids Biol. Chem. 2015, 396, 329. View at Publisher
Arya, T.; Reddi, R.; Kishor, C.; Ganji, R.J.; Bhukya, S.; Gumpena, R.; McGowan, S.; Drag, M.; Addlagatta, A., Identification of the molecular basis of inhibitor selectivity between the human and Streptococcal Type I methionine aminopeptidases. J. Med. Chem. 2015, 58, 2350. View at Publisher
Bekes, M.; Rut, W.; Kasperkiewicz, P. Mulder, M. P.; Ovaa, H.; Drag, M.; Lima, C. D.; Huang, T. T., SARS hCoV papain-like protease is a unique Lys48 linkage-specific di-distributive deubiquitinating enzyme. Biochem. J. 2015, 468, 215. View at Publisher
Drag-Zalesinska M, Wysocka T, Borska S, Drag M, Poreba M, Choromanska A, Kulbacka J, Saczko J., The new esters derivatives of betulin and betulinic acid in epidermoid squamous carcinoma treatment - In vitro studies. Biomedicine & Pharmacotherapy 2015, 72, 91. View at Publisher
Kasperkiewicz P, Poreba M, Snipas SJ, Lin SJ, Kirchhofer D, Salvesen GS, Drag M., Design of a Selective Substrate and Activity Based Probe for Human Neutrophil Serine Protease 4. PLoS One 2015, 10, 1. View at Publisher
Rajkovic, J.; Poreba, M.; Caglic, D.; Vidmar, R.; Wilk, A.; Borowik, A.; Salvesen, G. S.; Turk, V.; Drag, M.; Turk, B., Biochemical Characterization and Substrate Specificity of Autophagin-2 from the Parasite Trypanosoma cruzi J. Biol. Chem. 2015, 290, 28231. View at Publisher
Galiullina RA, Kasperkiewicz P, Chichkova NV, Szalek A, Serebryakova MV, Poreba M, Drag M, Vartapetian AB, Substrate Specificity and Possible Heterologous Targets of Phytaspase, a Plant Cell Death Protease. Journal of Biological Chemistry 2015, 290, 24806. View at Publisher
Poreba M, Szalek A, Kasperkiewicz P, Rut W, Salvesen GS, Drag M, Small Molecule Active Site Directed Tools for Studying Human Caspases Chemical Reviews 2015, 115, 12546. View at Publisher
van der Linden, W. A.; Segal, E.; Child, M. A.; Byzia, A. Drąg, M.; Bogyo, M., Design and Synthesis of Activity-Based Probes and Inhibitors for Bleomycin Hydrolase Chem. Biol. 2015, 22, 995.
Poręba, M.; Mihelic, M.; Krai, P.; Rajkovic, J.; Krężel, A.; Pawełczak, M.; Klemba, M.; Turk, D.; Turk, B.; Latajka, R.; Drąg, M., Unnatural amino acids increase activity and specificity of synthetic substrates for human and malarial cathepsin C. Amino Acids 2014, 46, 931. View at Publisher
Kasperkiewicz, P.; Poreba, M.; Snipas, S. J.; Parker, H.; Winterbourn, C. C.; Salvesen, G. S.; Drag, M., Design of ultrasensitive probes for human neutrophil elastase through hybrid combinatorial substrate library profiling. Proc. Natl. Acad. Sci. U. S. A. 2014, 111, 2518. View at Publisher
Byzia, A; Haeggström, J.Z.; Salvesen, G.S.; Drąg, M., A remarkable activity of human leukotriene A4 hydrolase (LTA4H) toward unnatural amino acids. Amino Acids 2014, 46, 1313. View at Publisher
Poręba, M.; Szalek, A.; Kasperkiewicz, P.; Drąg, M., Positional Scanning Substrate Combinatorial Library (PS-SCL) Approach to Define Caspase Substrate Specificity. Methods Mol. Biol. 2014, 1133, 41. View at Publisher
Pustelny, K.; Zdzalik, M.; Stach, N.; Stec-Niemczyk, J.; Cichon, P.; Czarna, A.; Popowicz, G.; Mak, P.; Drag, M.; Salvesen, G. S.; Wladyka, B.; Potempa, J.; Dubin, A.; Dubin, G., Staphylococcal SplB serine protease utilizes a novel molecular mechanism of activation. J. Biol. Chem. 2014, 298, 15544. View at Publisher
Gras, S.; Byzia, A.; Gilbert, F.B.; McGowan, S.; Drąg, M.; Silvestre, A.; Niepceron, A.; Lecaille, F.; Lalmanach, G.; Fabien Brossier, F., Aminopeptidase N1 (Et-ApN1), a M1 metalloprotease of the apicomplexan parasite Eimeria tenella participates in parasite development Eukaryotic Cell 2014, 13, 884. View at Publisher
Poreba, M.; Kasperkiewicz, P.; Snipas, S. J.; Fasci, D.; Salvesen, G. S.; Drąg, M., Unnatural amino acids increase sensitivity and provide for the design of highly selective caspase substrates Cell Death & Differentiation 2014, 21, 1482. View at Publisher
Mistry, S.N.; Drinkwater, N.; Ruggeri, C.; Kannan Sivaraman, K.; Loganathan, S.; Fletcher, S.; Drag, M.; Paiardini, A.; Avery, V.M.; Scammells, P.J.; McGowan, S., A Two-pronged Attack: Dual Inhibition of Plasmodium falciparum M1 and M17 Metalloaminopeptidases by a Novel Series of Hydroxamic acid-based Inhibitors. J. Med. Chem. 2014, 57, 9168. View at Publisher
Węglarz-Tomczak, E.; Poręba, M.; Byzia, A.; Berlicki, Ł.; Nocek, B.; Mulligan, R.; Joachimiak, A.; Drąg, M.; Mucha, A., An integrated approach to the ligand binding specificity of Neisseria meningitidis M1 alanine aminopeptidase by fluorogenic substrate profiling, inhibitory studies and molecular modeling. Biochimie 2013, 95, 419. View at Publisher
Carroll, R.K.; Veillard, F.; Gagne, D.T.; Lindenmuth, J.M.; Poreba, M.; Drag, M.; Potempa, J.; Shaw, L.N., The Staphylococcus aureus leucine aminopeptidase LAP is localized to the bacterial cytosol and demonstrates a broad substrate range that extends beyond leucine. Biol. Chem. 2013, 394, 791. View at Publisher
Drąg, M. , Chapter 478 – OTU1 Peptidase Handbook of Proteolytic Enzymes 2013, 2, 2121. View at Publisher
Drąg, M. , Chapter 532 – SENP8 Peptidase Handbook of Proteolytic Enzymes 2013, 2, 2379. View at Publisher
Drąg, M.; Wieczerzak, E.; Pawełczak, M.; Berlicki, Ł.; Grzonka, Z.; Kafarski, P., Toward very potent, non-covalent organophosphonate inhibitors of cathepsin C and related enzymes by 2-amino-1-hydroxy-alkanephosphonates dipeptides. Biochemie 2013, 95, 1640. View at Publisher
Zeiler, E.; List, A.; Alte, F.; Gersch, M.; Wachtel, R.; Poręba, M.; Drąg, M.; Groll, M.; Sieber, S.A., Structural and functional insights into caseinolytic proteases reveal an unprecedented regulation principle of their catalytic triad. Proc. Natl. Acad. Sci. U. S. A. 2013, 110, 11302. View at Publisher
Kannan Sivaraman,K.; Paiardini, A.; Sieńczyk, M.; Ruggeri, C.; Oellig, C. A.; Dalton, J. P.; Scammells, P. J.; Drag, M.; McGowan , S., Synthesis and Structure-Activity Relationships of Phosphonic Arginine Mimetics as Inhibitors of the M1 and M17 Aminopeptidases from Plasmodium falciparum. J. Med. Chem. 2013, 56, 5213. View at Publisher
Poręba, M.; Stróżyk, A.; Salvesen, G.S.; Drag, M. , Caspase Substrates and Inhibitors. Cold Spring Harb. Perspect. Biol. 2013, 5, 1. View at Publisher
Poreba, M.; McGowan, S.; Skinner-Adams, T. S.; Trenholme, K. R.; Gardiner, D. L.; Whisstock, J. C.; To, J.; Salvesen, G. S.; Dalton, J. P.; Drąg, M., Fingerprinting the Substrate Specificity of M1 and M17 Aminopeptidases of Human Malaria, Plasmodium Falciparum. PLoS One 2012, 7, 31938. View at Publisher
Gajda, A. D.; Pawleczak, M.; Drąg, M., Substrate specificity screening of oat (Avena sativa) seeds aminopeptidase demonstrate unusually broad tolerance in S1 pocket. Plant Physiol. Biochem. 2012, 54, 6. View at Publisher
Poręba, M.; Gajda, A.; Picha, J.; Jiracek, J.; Marschner, A.; Klein, C.; Salvesen, G. S.; Drąg, M., S1 pocket fingerprints of human and bacterial methionine aminopeptidases determined using fluorogenic libraries of substrates and phosphorus based inhibitors. Biochimie 2012, 94, 704. View at Publisher
Bekes, M.; Drąg, M., Trojan horse strategies used by pathogens to influence the SUMO system of host eukaryotic cells. J. Innate Immun. 2012, 4, 159. View at Publisher
Sivaraman, K.K.; Oellig, C.A.; Huynh, K.; Atkinson, S.C.; Poreba, M.; Perugini, M.A.; Trenholme, K.R.; Gardiner, D.L.; Salvesen, G.; Drag, M.; Dalton, J.P.; Whisstock, J.C.; McGowan, S., X-ray crystal structure and specificity of the Plasmodium falciparum malaria aminopeptidase PfM18AAP. J. Mol. Biol. 2012, 422, 495. View at Publisher
Veillard, F.; Potempa, B.; Poreba, M.; Drag, M.; Potempa, J., Gingipain aminopeptidase activities in Porphyromonas gingivalis. Biol. Chem. 2012, 393, 1471. View at Publisher
Aleshin, A.E.; Marcin Drag, M.; Gombosuren, N.; Wei, G.; Mikolajczyk, J.; Arnold C. Satterthwait, A.C.; Strongin, A. Y.; Liddington, R.C.; Salvesen, G.S., Activity, Specificity and Probe Design for the Smallpox Virus Protease K7L. J. Biol. Chem. 2012, 287, 47. View at Publisher
Kasperkiewicz, P.; Gajda, A. D.; Drąg, M., Current and prospective applications of non-proteinogenic amino acids in profiling of proteases substrate specificity Biol. Chem. 2012, 393, 843. View at Publisher
Hachmann, J.; Snipas, S. J.; van Raam, B. J.; Cancino, E. M.; Houlihan, E. J.; Poreba, M.; Kasperkiewicz, P.; Drag, M.; Salvesen, G. S., Mechanism and specificity of the human paracaspase MALT1 Biochem. J. 2012, 443, 287. View at Publisher
Ponder, E. L.; Albrow, V. E.; Leader, B. A.; Bekes, M.; Mikolajczyk, J.; Pecar Fonovic, U.; Shen, A.; Drąg, M.; Xiao, J.; Deu, E.; Campbell, A. J.; Powers, J. C.; Salvesen, G. S.; Bogyo, M. , Functional Characterization of a SUMO Deconjugating Protease of Plasmodium falciparum Using Newly Identified Small Molecule Inhibitors. Chemistry & Biology 2011, 18, 711. View at Publisher
Volle, J.-N.; Filippini, D.; Midrier, C.; Sobecki, M.; Drąg, M.; Virieux, D.; Pirat, J.-L., Revisited Synthesis of Aryl-H-phosphinates. Synthesis 2011, 2011, 2490. View at Publisher
Zervoudi, E.; Papakyriakou, A.; Georgiadou, D.; Evnouchidou, I.; Gajda, A.; Poręba, M.; Salvesen, G. S.; Drąg, M.; Hattori, A.; Swevers, L.; Vourloumis, D.; Stratikos, E., Probing the S1 specificity pocket of the aminopeptidases that generate antigenic peptides. Biochem J. 2011, 435, 411. View at Publisher
Boucher, D.; Blais, V.; Drąg, M.; Denault, J.-B., Molecular determinants involved in activation of caspase 7. Biosci Rep. 2011, 31, 283. View at Publisher
Pop, C.; Oberst, A.; Drąg, M.; Van Raam, B. J.; Riedl, S. J.; Green, D. R.; Salvesen, G. S. , FLIP(L) induces caspase 8 activity in the absence of interdomain caspase 8 cleavage and alters substrate specificity. Biochem J. 2011, 433, 447. View at Publisher
Skinner-Adams, T. S.; Stack, C. M.; Trenholme, K. R.; Brown, C. L.; Grembecka, J.; Lowther, J.; Mucha, A.; Drag, M.; Kafarski, P.; McGowan, S.; Whisstock, J. C.; Gardiner, D. L.; Dalton, J. P., Plasmodium falciparum neutral aminopeptidases: new targets for anti-malarials. Trends Biochem. Sci. 2010, 35, 53. View at Publisher
Mucha, A.; Drąg, M.; Dalton, J. P.; Kafarski, P., Metallo-aminopeptidase inhibitors. Biochimie 2010, 92, 1509. View at Publisher
Drąg, M.; Bogyo, M.; Ellman, J. A.; Salvesen, G. S. , Aminopeptidase fingerprints. An integrated approach for identification of good substrates and optimal inhibitors. J. Biol. Chem. 2010, 285, 3310. View at Publisher
Grzywa, R.; Oleksyszyn, J.; Salvesen, G. S.; Drąg, M. , Identification of very potent inhibitor of human aminopeptidase N (CD13). Bioorg. Med. Chem. Lett. 2010, 20, 2497. View at Publisher
Shu, C.-W.; Drąg, M.; Bekes, M.; Zhai, D.; Salvesen, G. S.; Reed, J. C., Synthetic substrates for measuring activity of autophagy proteases: autophagins (Atg4). Autophagy 2010, 6, 936. View at Publisher
Wachmann, K.; Pop, C.; van Raam, B. J.; Drąg, M.; Mace, P. D.; Snipas, S. J.; Zmasek, C.; Schwarzenbacher, R.; Salvesen, G. S.; Riedl, S. J., Activation and specificity of human caspase-10. Biochemistry 2010, 49, 8307. View at Publisher
Kolli, N.; Mikolajczyk, J.; Drąg, M.; Mukhopadhyay, D.; Moffatt, N.; Dasso, M.; Salvesen, G. S.; Wilkinson, K. D., Distribution and paralogue specificity of mammalian deSUMOylating enzymes. Biochem. J. 2010, 430, 335. View at Publisher
Drąg, M.; Salvesen, G. S., Emerging principles in protease-based drug discovery. Nature Reviews Drug Discovery 2010, 9, 690. View at Publisher
Poręba, M.; Drąg, M., Current strategies for probing substrate specificity of proteases. Curr. Med. Chem. 2010, 17, 3968. View at Publisher
Podstawka, E.; Kudelski, A.; Drąg, M.; Oleksyszyn, J.; Proniewicz, L. M., Adsorbed states of substituted ?-aminophosphinic acids on silver electrode surface. Comparison with colloidal silver substrate. J. Raman Spect. 2009, 11, 1578. View at Publisher
Podstawka, E.; Drąg, M.; Oleksyszyn, J., Raman and surface-enhanced Raman studies of ?-aminophosphinic inhibitors of metalloenzymes. J. Raman Spect. 2009, 11, 1564. View at Publisher
Surowiak, P.; Drąg, M.; Materna, V.; Dietel, M.; Lage, H., Betulinic acid reveal stronger cytotoxic activity toward normal melanocyte cell line (NHEM-neo) than drug-resistant and drug-sensitive melanoma cell lines (MeWo). Mol. Med. Rep. 2009, 2, 543. View at Publisher
Szczuraszek, K.; Materna, V.; Halon, A.; Mazur, G.; Wróbel, T.; Kuliczkowski, K.; Maciejczyk, A.; Zabel, M.; Drąg, M.; Dietel, M.; Lage, H.; Surowiak, P., Positive correlation between cyclooxygenase-2 and ABC-transporter expression in non-Hodgkin Oncol. Rep. 2009, 22, 1315. View at Publisher
Walters, J.; Pop, C.; Scott, F. L.; Drąg, M.; Swartz, P.; Mattos, C.; Salvesen, G. S.; Clark, C. A., A constitutively active and uninhibitable caspase-3 zymogen efficiently induces apoptosis. Biochem. J. 2009, 424, 335. View at Publisher
Drąg-Zalesińska, M.; Kulbacka, J.; Saczko, J.; Wysocka, T.; Zabel, M.; Surowiak, P.; Drąg, M., Esters of betulin and betulinic acid with amino acids have improved water solubility and are selectively cytotoxic toward cancer cells. Bioorg. Med. Chem. Lett. 2009, 19, 4814. View at Publisher
Drąg, M.; Surowiak, P.; Drąg-Zalesinska, M.; Dietel, M.; Lage, H.; Oleksyszyn, J., Comparision of the cytotoxic effects of birch bark extract, betulin and betulinic acid towards human gastric carcinoma and pancreatic carcinoma drug-sensitive and drug-resistant cell lines. Molecules 2009, 14, 1639. View at Publisher
Cunningham, E.; Drąg, M.; Kafarski, P.; Bell, A., Chemical Target Validation Studies of Aminopeptidase in Malaria Parasites Using alpha-Aminoalkylphosphonate and Phosphonopeptide Inhibitors Antimicrob. Agents Chemother. 2008, 52, 3221. View at Publisher
Drąg, M.; Mikołajczyk, J.; Menon, K.; Huang, Z.; Salvesen, G. S., Activity profiling of human deSUMOylating enzymes (SENPs) with synthetic substrates reveals unexpected specificity of two newly characterized members of the family. Biochem. J. 2008, 409, 461. View at Publisher
Eckelman, B. P.; Drąg, M.; Snipas, S. J.; Salvesen, G. S., The Mechanism of Peptide Binding Specificity of IAP BIR domains. Cell Death Differ. 2008, 15, 920. View at Publisher
Snipas, S. J.; Drąg, M.; Stennicke, H. R.; Salvesen, G. S., Activation mechanism and substrate specificity of the Drosophila initiator caspase DRONC. Cell Death Differ. 2008, 15, 938. View at Publisher
Surowiak, P.; Pawełczyk, K.; Maciejczyk, A.; Pudełko, M.; Kołodziej, J.; Zabel, M.; Murawa, D.; Drąg, M.; Gansukh, T.; Dietel, M.; Lage, H. , Positive Correlation between Cyclooxygenase 2 and the Expression of ABC-transporters in Non-small Cell Lung Cancer. Anticancer Res. 2008, 28, 2867.
Drąg, M.; Salvesen, G. S., DeSUMOylating enzymes-SENPs (Review). IUBMB Life 2008, 60, 734. View at Publisher
Drąg, M.; Mikolajczyk, J.; Bekes, M.; Reyes-Turcu, F.; Ellman, J. A.; Wilkinson, K. D.; Salvesen, G. S., Positional-scanning fluorogenic substrate libraries reveal unexpected specificity determinants of deubiquitinating enzymes (DUBs). Biochem. J. 2008, 415, 367. View at Publisher
Drąg, M.; Grzywa, R.; Oleksyszyn, J. , Novel hydroxamic acid related phosphinates: inhibitor of neutral aminopeptidase N (APN). Bioorg. Med. Chem. Lett. 2007, 17, 1516. View at Publisher
Mikolajczyk, J.; Drąg, M.; Bekes, M.; Cao, J. T.; Ronai, Z.; Salvesen, G. S. , SUMO-specific proteases: Profiling the specificities and activities of human SENPs. J. Biol. Chem. 2007, 282, 26217. View at Publisher
Denault, J.-B.; Drąg, M.; Salvesen, G. S.; Alves, J.; Heidt, A.; Deveraux, Q.; Harris, J. L., Small molecules not direct activators of caspases. Nature-Chemical Biology 2007, 9, 520. View at Publisher
Drąg, M.; Długosz, K.; Oleksyszyn J., A facile synthesis of bis-alpha-aminoalkyl- phosphinates. Synthetic Commun. 2006, 36, 2787. View at Publisher
Surowiak, P.; Drąg, M.; Materna, V.; Suchocki, S.; Grzywa, R.; Spaczynski, M.; Dietel, M.; Oleksyszyn, J.; Zabel, M.; Lage H., Expression of aminopeptidase N/CD13 in human ovarian cancers. Int. J. Gynecol. Cancer 2006, 16, 1783.
Lejczak, B.; Wojtasek, H.; Berlicki, Ł.; Forlani, G.; Obojska, A.; Drąg. M.; Gąsowska, B.; Grembecka, J.; Olechnowicz. D., Design, Synthesis and Evaluation of Environmentally Friendly Herbicides. Pol. J. Environ. Stud. 2005, 14, 64.
Gałezowska, J.; Sobek, S.; Drag, M.; Mucha, A.; Kafarski, P.; Kozłowski, H. , Specific interactions of divalent metal ions with phosphonic analogues of dipeptide inhibitors of proteases. Pol. J. Chem. 2005, 79, 603.
DrÄg, M.; Grembecka, J.; PaweĹczak, M.; Kafarski, P. , alpha-Aminoalkylphosphonates as a tool in experimental optimisation of P1 side chain shape of potential inhibitors in S1 pocket of leucine - and neutral aminopeptidases. Eur. J. Med. Chem. 2005, 40, 764. View at Publisher
Podstawka, E.; Borszowska, R.; Grabowska, M.; Drag, M.; Kafarski, P.; Proniewicz, L.M., Investigation of molecular structures and adsorption mechanisms of phosphonodipeptides by surface-enhanced Raman, Raman, and infrared spectroscopies. Surf. Sci. 2005, 599, 207. View at Publisher
Drąg, M.; Oleksyszyn, J. , Synthesis of a1-(Cbz-aminoalkyl)-a2-(hydroxyalkyl)phosphinic esters. Tetrahedron Lett. 2005, 46, 3359. View at Publisher
Drąg, M.; Sieńczyk, M.; Marcinkowska, A.; Drąg-Zalesińska, M.; Wysocka, T.; Oleksyszyn, J., Alpha-Aminophosphonates Induce Apoptosis in Human Tumor Cell Lines Pol. J. Chem 2005, 79, 593.
Gumienna-Kontecka, E.; Galezowska, J.; Drag, M.; Latajka, R.; Kafarski, P.; Kozlowski, H., Coordination abilities of substituted beta-aminophosphonates towards Cu2+ and Zn2+ ions. Inorganica Chimica Acta 2004, 357, 1632. View at Publisher
Drag, M.; Jezierski, A.; Kafarski, P., First example of the chemical, oxidative cleavage of the C-P bond in aminophosphonate chemistry. The oxidation of 1-amino-1-amino-1-(3,4-dihydroxyphenyl)methylphosphonic acid by NaIO4. Chem. Comm. 2004, 9, 1132. View at Publisher
Kafarski, P.; Grembecka, J.; Mucha, A.; Pawełczak, M.; Drąg, M.; Berlicki, Ł.; Olechnowicz, D., Projektowanie Potencjalnych Leków i Pestycydów z Wykorzystaniem Wiedzy o Strukturze Przestrzennej Enzymów. Przem. Chem. 2003, 82, 1087.
Drag, M.; Pawelczak, M.; Kafarski, P., Stereoselective synthesis of 1-aminoalkanephosphonic acids with two chiral centers and their activity towards leucine aminopeptidase. Chirality 2003, 15, 104. View at Publisher
Drag, M.; Latajka, R.; Gumienna-Kontecka, E.; Kozlowski, H.; Kafarski, P. , Stereoselective synthesis, solution structure and metal complexes of (1S,2S)-2-amino-1-hydroxyalkylphosphonic acids. Tetrahedron-Asymmetry 2003, 14, 1837. View at Publisher
Kafarski, P.; Drąg, M.; Berlicki, Ł.;Pawełczak, M., Synthesis and evaluation of phosphonopeptide Cathepsin C inhibitors. in Peptide Revolution: Genomics, Proteomics and Therapeutics, Eds. M. Chorev, T.K. Sawyer, Americam Peptide Society, Boston 2003, 310.
Drag, M.; Grembecka, J.; Kafarski, P., The computer-aided design, synthesis, and activity prediction of new leucine aminopeptidase inhibitors. Phosphorus, Sulfur 2002, 177, 1591. View at Publisher
Drag, M.; Latajka, R.; Gancarz, R.; Kafarski, P.; Pirat, J.L.; Cristau, H.J. , Regio- and stereoselective synthesis, solution conformations of 2-amino-1-hydroxy-2-arylethylphosphonic esters and acids. Phosphrus, Sulfur, and Silicon, and Rel. Elem. 2002, 177, 2191. View at Publisher
Latajka, R.; Drag, M.; Gancarz, R.; Kafarski, P. , Solution conformations of 2-amino-1-hydroxy-2-aryl ethylphosphonic acids and their diethyl esters. J. Mol. Struct. 2002, 605, 79. View at Publisher
Gasowska, B.; Wojtasek, H.; Hurek, J.; DrÄg, M.; Nowak, K.; Kafarski, P., Redox reaction between amino-(3,4-dihydroxyphenyl)methylphosphonic acid and dopaquinone is responsible for the apparent inhibitory effect on tyrosinase Eur. J. Biochem. 2002, 269, 4098. View at Publisher
Drąg, M.; Kafarski, P.; Pirat, J.-L.; Cristau, H.-J., Unexpected opening of diethyl (+/-) - (S,S) - 1,2 - epoxy - 2 – phenylpentyl- phosphonate by NH3(aqu.): An easy entry to ethyl 1 - formyl - 1 – phenylbuthyl- phosphonate Phosphorus, Sulfur and Silicon 2002, 177, 1153. View at Publisher
Cristau, H.-J.; Pirat, J.-L.; DrÄg, M.; Kafarski, P., Regio- and stereoselective synthesis of 2-amino-1-hydroxy-2-aryl ethylphosphonic esters Tetrahedron Lett. 2000, 41, 9781. View at Publisher

Department of Chemical Biology and Bioimaging