List of works - Marcin Drąg

A New Betulin Derivative Stimulates the Synthesis of Collagen in Human Fibroblasts Stronger than its Precursor

scientific article published on 01 July 2019

A constitutively active and uninhibitable caspase-3 zymogen efficiently induces apoptosis

scientific article

A molecular sensor determines the ubiquitin substrate specificity of SARS-CoV-2 papain-like protease

scientific article

A multi-step peptidolytic cascade for amino acid recovery in chloroplasts.

scientific article published on 31 October 2016

A remarkable activity of human leukotriene A4 hydrolase (LTA4H) toward unnatural amino acids

scientific article

Activation and specificity of human caspase-10.

scientific article published on September 2010

Activity profiling and crystal structures of inhibitor-bound SARS-CoV-2 papain-like protease: A framework for anti-COVID-19 drug design

scientific article published on 16 October 2020

Activity profiling and structures of inhibitor-bound SARS-CoV-2-PLpro protease provides a framework for anti-COVID-19 drug design

scientific article published on 30 April 2020

Activity profiling of aminopeptidases in cell lysates using a fluorogenic substrate library.

scientific article published on 5 October 2015

Activity profiling of human deSUMOylating enzymes (SENPs) with synthetic substrates suggests an unexpected specificity of two newly characterized members of the family

scientific article

Activity, specificity, and probe design for the smallpox virus protease K7L

scientific article

Aminopeptidase N1 (EtAPN1), an M1 metalloprotease of the apicomplexan parasite Eimeria tenella, participates in parasite development ⬇️

scientific article

Aminopeptidase fingerprints, an integrated approach for identification of good substrates and optimal inhibitors

scientific article

An alternative for proteinase K-heat-sensitive protease from fungus Onygena corvina for biotechnology: cloning, engineering, expression, characterization and special application for protein sequencing

scientific article published on 24 June 2020

An integrated approach to the ligand binding specificity of Neisseria meningitidis M1 alanine aminopeptidase by fluorogenic substrate profiling, inhibitory studies and molecular modeling.

scientific article

Anticancer properties of ester derivatives of betulin in human metastatic melanoma cells (Me-45).

scientific article published on 03 January 2017

Application of a chemical probe to detect neutrophil elastase activation during inflammatory bowel disease

scientific article published on 16 September 2019

Applications of Unnatural Amino Acids in Protease Probes

scientific article published on 30 October 2019

Barrel-shaped ClpP Proteases Display Attenuated Cleavage Specificities

scientific article published on 25 November 2015

Betulinic acid exhibits stronger cytotoxic activity on the normal melanocyte NHEM-neo cell line than on drug-resistant and drug-sensitive MeWo melanoma cell lines.

scientific article

Biochemical Characterization and Substrate Specificity of Autophagin-2 from the Parasite Trypanosoma cruzi

scientific article

Caspase Substrates and Inhibitors ⬇️

scientific article published on August 1, 2013

Caspase selective reagents for diagnosing apoptotic mechanisms

scientific article published on 10 May 2018

Characterization of P. falciparum dipeptidyl aminopeptidase 3 specificity identifies differences in amino acid preferences between peptide-based substrates and covalent inhibitors

scientific article published on 24 June 2019

Chemical target validation studies of aminopeptidase in malaria parasites using alpha-aminoalkylphosphonate and phosphonopeptide inhibitors

scientific article published on 5 May 2008

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.

scientific article published on 24 April 2009

Coordination abilities of substituted β-aminophosphonates towards Cu2+ and Zn2+ ions

Counter Selection Substrate Library Strategy for Developing Specific Protease Substrates and Probes

scientific article

Current and prospective applications of non-proteinogenic amino acids in profiling of proteases substrate specificity ⬇️

scientific article published on September 1, 2012

DeSUMOylating enzymes--SENPs

scientific article

Design and Synthesis of Activity-Based Probes and Inhibitors for Bleomycin Hydrolase.

scientific article published on 3 August 2015

Design of Selective Substrates and Activity-Based Probes for Hydrolase Important for Pathogenesis 1 (HIP1) from Mycobacterium tuberculosis.

scientific article published on 15 July 2016

Design of a Selective Substrate and Activity Based Probe for Human Neutrophil Serine Protease 4

scientific article published on 14 July 2015

Design of optical imaging probes by screening of diverse substrate libraries directly in disease tissue extracts

scientific article published on 26 June 2020

Design of ultrasensitive probes for human neutrophil elastase through hybrid combinatorial substrate library profiling

scientific article

Detection of Active Granzyme A in NK92 Cells with Fluorescent Activity-Based Probe

scientific article published on 16 March 2020

Determination of extended substrate specificity of the MALT1 as a strategy for the design of potent substrates and activity-based probes

scientific article published in Scientific Reports

Development of an advanced nanoformulation for the intracellular delivery of a caspase-3 selective activity-based probe

scientific article published on 01 January 2019

Distribution and paralogue specificity of mammalian deSUMOylating enzymes

scientific article published on September 2010

Emerging challenges in the design of selective substrates, inhibitors and activity-based probes for indistinguishable proteases

scientific article published on 4 January 2017

Emerging principles in protease-based drug discovery ⬇️

scientific article published on September 1, 2010

Engineered unnatural ubiquitin for optimal detection of deubiquitinating enzymes

scientific article

Engineered unnatural ubiquitin for optimal detection of deubiquitinating enzymes

scientific article published on 27 May 2020

Esters of betulin and betulinic acid with amino acids have improved water solubility and are selectively cytotoxic toward cancer cells.

scientific article published on 14 June 2009

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

scientific article published on 17 June 2019

Expression of aminopeptidase N/CD13 in human ovarian cancers

scientific article published on 01 September 2006

Extended substrate specificity and first potent irreversible inhibitor/activity-based probe design for Zika virus NS2B-NS3 protease

scientific article (publication date: December 2016)

Extensive peptide and natural protein substrate screens reveal that mouse caspase-11 has much narrower substrate specificity than caspase-1.

scientific article published on 6 February 2018

FLIP(L) induces caspase 8 activity in the absence of interdomain caspase 8 cleavage and alters substrate specificity

scientific article published on February 2011

Fingerprinting the substrate specificity of M1 and M17 aminopeptidases of human malaria, Plasmodium falciparum

scientific article

First example of the chemical, oxidative cleavage of the C-P bond in aminophosphonate chemistry. The oxidation of 1-amino-1-(3,4-dihydroxyphenyl)methylphosphonic acid by NaIO4.

scientific article published on 8 April 2004

Fluorescent activity-based probe for the selective detection of Factor VII activating protease (FSAP) in human plasma

scientific article published on 19 August 2019

Fluorescent probes towards selective cathepsin B detection and visualization in cancer cells and patient samples

scientific article published on 31 July 2019

Functional characterization of a SUMO deconjugating protease of Plasmodium falciparum using newly identified small molecule inhibitors

scientific article (publication date: 24 June 2011)

Gingipain aminopeptidase activities in Porphyromonas gingivalis ⬇️

scientific article published on December 1, 2012

Glycosylation is important for legumain localization and processing to active forms but not for cystatin E/M inhibitory functions

scientific article published on 17 May 2017

High-Resolution Confocal Fluorescence Imaging of Serine Hydrolase Activity in Cryosections - Application to Glioma Brain Unveils Activity Hotspots Originating from Tumor-Associated Neutrophils

scientific article published on 15 March 2020

Highly sensitive and adaptable fluorescence-quenched pair discloses the substrate specificity profiles in diverse protease families

scientific article published on 23 February 2017

Human 20S proteasome activity towards fluorogenic peptides of various chain lengths

scientific article

Identification of the molecular basis of inhibitor selectivity between the human and streptococcal type I methionine aminopeptidases

scientific article

Identification of very potent inhibitor of human aminopeptidase N (CD13)

scientific article published on 04 March 2010

Insights into ClpXP proteolysis: heterooligomerization and partial deactivation enhance chaperone affinity and substrate turnover in Listeria monocytogenes

scientific article

Internally quenched fluorogenic substrates with unnatural amino acids for cathepsin G investigation

scientific article published on 16 May 2019

Legumain is upregulated in acute cardiovascular events and associated with improved outcome - potentially related to anti-inflammatory effects on macrophages

scientific article published on 14 December 2019

Mechanism and specificity of the human paracaspase MALT1.

scientific article

Mechanistic insights into COVID-19 by global analysis of the SARS-CoV-2 3CL substrate degradome

scientific article

Metallo-aminopeptidase inhibitors

scientific article published on 10 May 2010

Molecular determinants involved in activation of caspase 7

scientific article published on August 2011

Multiplexed probing of proteolytic enzymes using mass cytometry-compatible activity-based probes

scientific article published on 01 September 2020

NETosis Occurs Independently of Neutrophil Serine Proteases

scientific article published on 15 October 2020

Noninvasive optical detection of granzyme B from natural killer cells with enzyme-activated fluorogenic probes

scientific article published on 21 May 2020

Novel hydroxamic acid-related phosphinates: inhibition of neutral aminopeptidase N (APN)

scientific article published on 19 January 2007

Plasmodium falciparum neutral aminopeptidases: new targets for anti-malarials

scientific article published on 30 September 2009

Positional scanning substrate combinatorial library (PS-SCL) approach to define caspase substrate specificity

scientific article

Positional-scanning fluorigenic substrate libraries reveal unexpected specificity determinants of DUBs (deubiquitinating enzymes).

scientific article

Positive correlation between cyclooxygenase 2 and the expression of ABC transporters in non-small cell lung cancer

scientific article published in September 2008

Positive correlation between cyclooxygenase-2 and ABC-transporter expression in non-Hodgkin's lymphomas

scientific article published in December 2009

Potent and selective caspase-2 inhibitor prevents MDM-2 cleavage in reversine-treated colon cancer cells

scientific article published on 11 April 2019

Probes to monitor activity of the paracaspase MALT1.

scientific article

Probing the S1 specificity pocket of the aminopeptidases that generate antigenic peptides.

scientific article published on April 2011

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

scientific article published on 31 January 2020

Protease Specificity: Towards In Vivo Imaging Applications and Biomarker Discovery

scientific article published on 07 August 2018

Recent advances and concepts in substrate specificity determination of proteases using tailored libraries of fluorogenic substrates with unnatural amino acids

scientific article published on April 2015

Redox reaction between amino-(3,4-dihydroxyphenyl)methyl phosphonic acid and dopaquinone is responsible for the apparent inhibitory effect on tyrosinase

scientific article published in August 2002

Regio- and stereoselective synthesis of 2-amino-1-hydroxy-2-aryl ethylphosphonic esters

S1 pocket fingerprints of human and bacterial methionine aminopeptidases determined using fluorogenic libraries of substrates and phosphorus based inhibitors

scientific article

SARS hCoV papain-like protease is a unique Lys48 linkage-specific di-distributive deubiquitinating enzyme

scientific article published on June 2015

SARS-CoV-2 Mpro inhibitors and activity-based probes for patient-sample imaging

scientific article published on 22 October 2020

SUMO-mediated regulation of NLRP3 modulates inflammasome activity

scientific article published in Nature Communications

Selective Substrates and Activity-Based Probes for Imaging of the Human Constitutive 20S Proteasome in Cells and Blood Samples

scientific article published on 09 June 2018

Selective imaging of cathepsin L in breast cancer by fluorescent activity-based probes.

scientific article

Small Molecule Active Site Directed Tools for Studying Human Caspases

scientific article published on 9 November 2015

Small molecules not direct activators of caspases

scientific article published on 01 September 2007

Small ubiquitin-related modifier (SUMO)-specific proteases: profiling the specificities and activities of human SENPs

scientific article

Solution conformations of 2-amino-1-hydroxy-2-aryl ethylphosphonic acids and their diethyl esters

Staphylococcal SplB Serine Protease Utilizes a Novel Molecular Mechanism of Activation

scientific article

Stereoselective synthesis of 1-aminoalkanephosphonic acids with two chiral centers and their activity towards leucine aminopeptidase.

scientific article published in January 2003

Stereoselective synthesis, solution structure and metal complexes of (1S,2S)-2-amino-1-hydroxyalkylphosphonic acids

Structural and functional insights into caseinolytic proteases reveal an unprecedented regulation principle of their catalytic triad ⬇️

scientific article published on June 24, 2013

Structural basis for substrate specificity of Helicobacter pylori M17 aminopeptidase

scientific article

Structure and substrate fingerprint of aminopeptidase P from Plasmodium falciparum

scientific article

Substrate Specificity and Possible Heterologous Targets of Phytaspase, a Plant Cell Death Protease

scientific article published on 17 August 2015

Substrate specificity profiling of SARS-CoV-2 Mpro protease provides basis for anti-COVID-19 drug design

scientific article (preprint)

Substrate specificity screening of oat (Avena sativa) seeds aminopeptidase demonstrate unusually broad tolerance in S1 pocket ⬇️

scientific article published on February 8, 2012

Synthesis and structure-activity relationships of phosphonic arginine mimetics as inhibitors of the M1 and M17 aminopeptidases from Plasmodium falciparum

scientific article

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

scientific article published on 21 September 2017

Synthetic substrates for measuring activity of autophagy proteases-autophagins (Atg4) ⬇️

scientific article published on October 19, 2010

The Computer-Aided Design, Synthesis, and Activity Prediction of New Leucine Aminopeptidase Inhibitors

The Staphylococcus aureus leucine aminopeptidase is localized to the bacterial cytosol and demonstrates a broad substrate range that extends beyond leucine

scientific article published on June 2013

The Strategies to Support the COVID-19 Vaccination with Evidence-Based Communication and Tackling Misinformation

scientific article

The elastase-PK101 structure: mechanism of an ultrasensitive activity-based probe revealed

scientific article

The new esters derivatives of betulin and betulinic acid in epidermoid squamous carcinoma treatment - In vitro studies.

scientific article published on 13 April 2015

Toolbox of Fluorescent Probes for Parallel Imaging Reveals Uneven Location of Serine Proteases in Neutrophils.

scientific article published on 3 July 2017

Toward very potent, non-covalent organophosphonate inhibitors of cathepsin C and related enzymes by 2-amino-1-hydroxy-alkanephosphonates dipeptides

scientific article published on 24 May 2013

Trojan Horse Strategies Used by Pathogens to Influence the Small Ubiquitin-Like Modifier (SUMO) System of Host Eukaryotic Cells ⬇️

scientific article published on 03 January 2012

Two-pronged attack: dual inhibition of Plasmodium falciparum M1 and M17 metalloaminopeptidases by a novel series of hydroxamic acid-based inhibitors

scientific article

Unique Substrate Specificity of SplE Serine Protease from Staphylococcus aureus

scientific article published in March 2018

Unnatural amino acids increase activity and specificity of synthetic substrates for human and malarial cathepsin C.

scientific article

X-ray crystal structure and specificity of the Plasmodium falciparum malaria aminopeptidase PfM18AAP

scientific article

X-ray crystal structure and specificity of the Toxoplasma gondii ME49 TgAPN2

scientific article published on 14 September 2020

alpha-Aminoalkylphosphonates as a tool in experimental optimisation of P1 side chain shape of potential inhibitors in S1 pocket of leucine- and neutral aminopeptidases

scientific article published on 20 April 2005

List of works by Marcin Drąg

A New Betulin Derivative Stimulates the Synthesis of Collagen in Human Fibroblasts Stronger than its Precursor

A constitutively active and uninhibitable caspase-3 zymogen efficiently induces apoptosis

A molecular sensor determines the ubiquitin substrate specificity of SARS-CoV-2 papain-like protease

A multi-step peptidolytic cascade for amino acid recovery in chloroplasts.

A remarkable activity of human leukotriene A4 hydrolase (LTA4H) toward unnatural amino acids

Activation and specificity of human caspase-10.

Activity profiling and crystal structures of inhibitor-bound SARS-CoV-2 papain-like protease: A framework for anti-COVID-19 drug design

Activity profiling and structures of inhibitor-bound SARS-CoV-2-PLpro protease provides a framework for anti-COVID-19 drug design

Activity profiling of aminopeptidases in cell lysates using a fluorogenic substrate library.

Activity profiling of human deSUMOylating enzymes (SENPs) with synthetic substrates suggests an unexpected specificity of two newly characterized members of the family

Activity, specificity, and probe design for the smallpox virus protease K7L

Aminopeptidase N1 (EtAPN1), an M1 metalloprotease of the apicomplexan parasite Eimeria tenella, participates in parasite development ⬇️

Aminopeptidase fingerprints, an integrated approach for identification of good substrates and optimal inhibitors

An alternative for proteinase K-heat-sensitive protease from fungus Onygena corvina for biotechnology: cloning, engineering, expression, characterization and special application for protein sequencing

An integrated approach to the ligand binding specificity of Neisseria meningitidis M1 alanine aminopeptidase by fluorogenic substrate profiling, inhibitory studies and molecular modeling.

Anticancer properties of ester derivatives of betulin in human metastatic melanoma cells (Me-45).

Application of a chemical probe to detect neutrophil elastase activation during inflammatory bowel disease

Applications of Unnatural Amino Acids in Protease Probes

Barrel-shaped ClpP Proteases Display Attenuated Cleavage Specificities

Betulinic acid exhibits stronger cytotoxic activity on the normal melanocyte NHEM-neo cell line than on drug-resistant and drug-sensitive MeWo melanoma cell lines.

Biochemical Characterization and Substrate Specificity of Autophagin-2 from the Parasite Trypanosoma cruzi

Caspase Substrates and Inhibitors ⬇️

Caspase selective reagents for diagnosing apoptotic mechanisms

Characterization of P. falciparum dipeptidyl aminopeptidase 3 specificity identifies differences in amino acid preferences between peptide-based substrates and covalent inhibitors

Chemical target validation studies of aminopeptidase in malaria parasites using alpha-aminoalkylphosphonate and phosphonopeptide inhibitors

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.

Coordination abilities of substituted β-aminophosphonates towards Cu2+ and Zn2+ ions

Counter Selection Substrate Library Strategy for Developing Specific Protease Substrates and Probes

Current and prospective applications of non-proteinogenic amino acids in profiling of proteases substrate specificity ⬇️

DeSUMOylating enzymes--SENPs

Design and Synthesis of Activity-Based Probes and Inhibitors for Bleomycin Hydrolase.

Design of Selective Substrates and Activity-Based Probes for Hydrolase Important for Pathogenesis 1 (HIP1) from Mycobacterium tuberculosis.

Design of a Selective Substrate and Activity Based Probe for Human Neutrophil Serine Protease 4

Design of optical imaging probes by screening of diverse substrate libraries directly in disease tissue extracts

Design of ultrasensitive probes for human neutrophil elastase through hybrid combinatorial substrate library profiling

Detection of Active Granzyme A in NK92 Cells with Fluorescent Activity-Based Probe

Determination of extended substrate specificity of the MALT1 as a strategy for the design of potent substrates and activity-based probes

Development of an advanced nanoformulation for the intracellular delivery of a caspase-3 selective activity-based probe

Distribution and paralogue specificity of mammalian deSUMOylating enzymes

Emerging challenges in the design of selective substrates, inhibitors and activity-based probes for indistinguishable proteases

Emerging principles in protease-based drug discovery ⬇️

Engineered unnatural ubiquitin for optimal detection of deubiquitinating enzymes

Engineered unnatural ubiquitin for optimal detection of deubiquitinating enzymes

Esters of betulin and betulinic acid with amino acids have improved water solubility and are selectively cytotoxic toward cancer cells.

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

Expression of aminopeptidase N/CD13 in human ovarian cancers

Extended substrate specificity and first potent irreversible inhibitor/activity-based probe design for Zika virus NS2B-NS3 protease

Extensive peptide and natural protein substrate screens reveal that mouse caspase-11 has much narrower substrate specificity than caspase-1.

FLIP(L) induces caspase 8 activity in the absence of interdomain caspase 8 cleavage and alters substrate specificity

Fingerprinting the substrate specificity of M1 and M17 aminopeptidases of human malaria, Plasmodium falciparum

First example of the chemical, oxidative cleavage of the C-P bond in aminophosphonate chemistry. The oxidation of 1-amino-1-(3,4-dihydroxyphenyl)methylphosphonic acid by NaIO4.

Fluorescent activity-based probe for the selective detection of Factor VII activating protease (FSAP) in human plasma

Fluorescent probes towards selective cathepsin B detection and visualization in cancer cells and patient samples

Functional characterization of a SUMO deconjugating protease of Plasmodium falciparum using newly identified small molecule inhibitors

Gingipain aminopeptidase activities in Porphyromonas gingivalis ⬇️

Glycosylation is important for legumain localization and processing to active forms but not for cystatin E/M inhibitory functions

High-Resolution Confocal Fluorescence Imaging of Serine Hydrolase Activity in Cryosections - Application to Glioma Brain Unveils Activity Hotspots Originating from Tumor-Associated Neutrophils

Highly sensitive and adaptable fluorescence-quenched pair discloses the substrate specificity profiles in diverse protease families

Human 20S proteasome activity towards fluorogenic peptides of various chain lengths

Identification of the molecular basis of inhibitor selectivity between the human and streptococcal type I methionine aminopeptidases

Identification of very potent inhibitor of human aminopeptidase N (CD13)

Insights into ClpXP proteolysis: heterooligomerization and partial deactivation enhance chaperone affinity and substrate turnover in Listeria monocytogenes

Internally quenched fluorogenic substrates with unnatural amino acids for cathepsin G investigation

Legumain is upregulated in acute cardiovascular events and associated with improved outcome - potentially related to anti-inflammatory effects on macrophages

Mechanism and specificity of the human paracaspase MALT1.

Mechanistic insights into COVID-19 by global analysis of the SARS-CoV-2 3CL substrate degradome

Metallo-aminopeptidase inhibitors

Molecular determinants involved in activation of caspase 7

Multiplexed probing of proteolytic enzymes using mass cytometry-compatible activity-based probes

NETosis Occurs Independently of Neutrophil Serine Proteases

Noninvasive optical detection of granzyme B from natural killer cells with enzyme-activated fluorogenic probes

Novel hydroxamic acid-related phosphinates: inhibition of neutral aminopeptidase N (APN)

Plasmodium falciparum neutral aminopeptidases: new targets for anti-malarials

Positional scanning substrate combinatorial library (PS-SCL) approach to define caspase substrate specificity

Positional-scanning fluorigenic substrate libraries reveal unexpected specificity determinants of DUBs (deubiquitinating enzymes).

Positive correlation between cyclooxygenase 2 and the expression of ABC transporters in non-small cell lung cancer

Positive correlation between cyclooxygenase-2 and ABC-transporter expression in non-Hodgkin's lymphomas

Potent and selective caspase-2 inhibitor prevents MDM-2 cleavage in reversine-treated colon cancer cells

Probes to monitor activity of the paracaspase MALT1.