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

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.

FEBS J. 2019 Jun 8. doi: 10.1111/febs.14953. [Epub ahead of print]


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

Groborz K, Kołt S, Kasperkiewicz P, Drag M.

Biochimie. 2019 May 16. pii: S0300-9084(19)30152-X. doi: 10.1016/j.biochi.2019.05.013. [Epub ahead of print]


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

Poreba M, Rut W, Groborz K, Snipas SJ, Salvesen GS, Drag M.

Cell Death Differ. 2019 Apr 11. doi: 10.1038/s41418-019-0329-2. [Epub ahead of print]


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

Cogo F, Poreba M, Rut W, Groborz K, Smyth P, Johnston MC, Williams R, Longley DB, Burden RE, Salvesen GS, Drag M, Scott CJ.

Nanoscale. 2019 Jan 3;11(2):742-751. doi: 10.1039/c8nr07859a.


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

Kasperkiewicz P, Kołt S, Janiszewski T, Groborz K, Poręba M, Snipas SJ, Salvesen GS, Drąg M.

Sci Rep. 2018 Oct 30;8(1):15998. doi: 10.1038/s41598-018-34476-7.


Protease Specificity: Towards In Vivo Imaging Applications and Biomarker Discovery.

Vizovišek M, Vidmar R, Drag M, Fonović M, Salvesen GS, Turk B.

Trends Biochem Sci. 2018 Oct;43(10):829-844. doi: 10.1016/j.tibs.2018.07.003. Epub 2018 Aug 7. Review.


SUMO-mediated regulation of NLRP3 modulates inflammasome activity.

Barry R, John SW, Liccardi G, Tenev T, Jaco I, Chen CH, Choi J, Kasperkiewicz P, Fernandes-Alnemri T, Alnemri E, Drag M, Chen Y, Meier P.

Nat Commun. 2018 Aug 1;9(1):3001. doi: 10.1038/s41467-018-05321-2.


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

Rut W, Poręba M, Kasperkiewicz P, Snipas SJ, Drąg M.

J Med Chem. 2018 Jun 28;61(12):5222-5234. doi: 10.1021/acs.jmedchem.8b00026. Epub 2018 Jun 9.


Caspase selective reagents for diagnosing apoptotic mechanisms.

Poreba M, Groborz K, Navarro M, Snipas SJ, Drag M, Salvesen GS.

Cell Death Differ. 2019 Feb;26(2):229-244. doi: 10.1038/s41418-018-0110-y. Epub 2018 May 10.


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.

Chem Sci. 2018 Jan 16;9(8):2113-2129. doi: 10.1039/c7sc04303a. eCollection 2018 Feb 28.


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 Apr 3;26(4):572-579.e4. doi: 10.1016/j.str.2018.02.008. Epub 2018 Mar 8.


Systems genomics study reveals expression quantitative trait loci, regulator genes and pathways associated with boar taint in pigs.

Drag M, Hansen MB, Kadarmideen HN.

PLoS One. 2018 Feb 13;13(2):e0192673. doi: 10.1371/journal.pone.0192673. eCollection 2018.


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

Ramirez MLG, Poreba M, Snipas SJ, Groborz K, Drag M, Salvesen GS.

J Biol Chem. 2018 May 4;293(18):7058-7067. doi: 10.1074/jbc.RA117.001329. Epub 2018 Feb 6.


Differential expression and co-expression gene networks reveal candidate biomarkers of boar taint in non-castrated pigs.

Drag M, Skinkyté-Juskiené R, Do DN, Kogelman LJA, Kadarmideen HN.

Sci Rep. 2017 Sep 22;7(1):12205. doi: 10.1038/s41598-017-11928-0.


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

Poreba M, Salvesen GS, Drag M.

Nat Protoc. 2017 Oct;12(10):2189-2214. doi: 10.1038/nprot.2017.091. Epub 2017 Sep 21.


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

Kasperkiewicz P, Altman Y, D'Angelo M, Salvesen GS, Drag M.

J Am Chem Soc. 2017 Jul 26;139(29):10115-10125. doi: 10.1021/jacs.7b04394. Epub 2017 Jul 18.


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

Lunde NN, Haugen MH, Bodin Larsen KB, Damgaard I, Pettersen SJ, Kasem R, Rut W, Drag M, Poreba M, Johansen HT, Solberg R.

Biochimie. 2017 Aug;139:27-37. doi: 10.1016/j.biochi.2017.05.009. Epub 2017 May 17.


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

Balogh D, Dahmen M, Stahl M, Poreba M, Gersch M, Drag M, Sieber SA.

Chem Sci. 2017 Feb 1;8(2):1592-1600. doi: 10.1039/c6sc03438a. Epub 2016 Oct 28.


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

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.

Sci Rep. 2017 Feb 23;7:43135. doi: 10.1038/srep43135.


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

Drąg-Zalesińska M, Drąg M, Poręba M, Borska S, Kulbacka J, Saczko J.

Cancer Cell Int. 2017 Jan 3;17:4. doi: 10.1186/s12935-016-0369-3. eCollection 2017.


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

Kasperkiewicz P, Poreba M, Groborz K, Drag M.

FEBS J. 2017 May;284(10):1518-1539. doi: 10.1111/febs.14001. Epub 2017 Jan 29. Review.


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

Rut W, Zhang L, Kasperkiewicz P, Poreba M, Hilgenfeld R, Drąg M.

Antiviral Res. 2017 Mar;139:88-94. doi: 10.1016/j.antiviral.2016.12.018. Epub 2016 Dec 26.


Safety evaluation of orally administered afoxolaner and milbemycin oxime in eight-week-old dogs.

Drag M, Saik J, Harriman J, Letendre L, Yoon S, Larsen D.

J Vet Pharmacol Ther. 2017 Oct;40(5):447-453. doi: 10.1111/jvp.12375. Epub 2016 Nov 27.


Ability of an oral formulation of afoxolaner to protect dogs from Borrelia burgdorferi infection transmitted by wild Ixodes scapularis ticks.

Baker CF, McCall JW, McCall SD, Drag MD, Mitchell EB, Chester ST, Larsen D.

Comp Immunol Microbiol Infect Dis. 2016 Dec;49:65-69. doi: 10.1016/j.cimid.2016.09.004. Epub 2016 Sep 29.


Efficacy of ivermectin against gastrointestinal nematodes of cattle in Denmark evaluated by different methods for analysis of faecal egg count reduction.

Peña-Espinoza M, Thamsborg SM, Denwood MJ, Drag M, Hansen TV, Jensen VF, Enemark HL.

Int J Parasitol Drugs Drug Resist. 2016 Dec;6(3):241-250. doi: 10.1016/j.ijpddr.2016.10.004. Epub 2016 Oct 13.


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

Teixeira PF, Kmiec B, Branca RM, Murcha MW, Byzia A, Ivanova A, Whelan J, Drag M, Lehtiö J, Glaser E.

Nat Chem Biol. 2017 Jan;13(1):15-17. doi: 10.1038/nchembio.2227. Epub 2016 Oct 31.


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

Lentz CS, Ordonez AA, Kasperkiewicz P, La Greca F, O'Donoghue AJ, Schulze CJ, Powers JC, Craik CS, Drag M, Jain SK, Bogyo M.

ACS Infect Dis. 2016 Nov 11;2(11):807-815. Epub 2016 Jul 15.


The intravenous and oral pharmacokinetics of afoxolaner and milbemycin oxime when used as a combination chewable parasiticide for dogs.

Letendre L, Harriman J, Drag M, Mullins A, Malinski T, Rehbein S.

J Vet Pharmacol Ther. 2017 Jan;40(1):35-43. doi: 10.1111/jvp.12332. Epub 2016 Sep 7.


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

Poreba M, Solberg R, Rut W, Lunde NN, Kasperkiewicz P, Snipas SJ, Mihelic M, Turk D, Turk B, Salvesen GS, Drag M.

Cell Chem Biol. 2016 Aug 18;23(8):1023-35. doi: 10.1016/j.chembiol.2016.05.020. Epub 2016 Jul 28.


Structure and substrate fingerprint of aminopeptidase P from Plasmodium falciparum.

Drinkwater N, Sivaraman KK, Bamert RS, Rut W, Mohamed K, Vinh NB, Scammells PJ, Drag M, McGowan S.

Biochem J. 2016 Oct 1;473(19):3189-204. doi: 10.1042/BCJ20160550. Epub 2016 Jul 26.


The level of embryonation influences detection of Ostertagia ostertagi eggs by semi-quantitative PCR.

Drag M, Höglund J, Nejsum P, Thamsborg SM, Enemark HL.

Parasit Vectors. 2016 Jun 29;9(1):368. doi: 10.1186/s13071-016-1657-4.


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

Rut W, Drag M.

Biol Chem. 2016 Sep 1;397(9):921-6. doi: 10.1515/hsz-2016-0176.


Structural basis for substrate specificity of Helicobacter pylori M17 aminopeptidase.

Modak JK, Rut W, Wijeyewickrema LC, Pike RN, Drag M, Roujeinikova A.

Biochimie. 2016 Feb;121:60-71. doi: 10.1016/j.biochi.2015.11.021. Epub 2015 Dec 1.


Barrel-shaped ClpP Proteases Display Attenuated Cleavage Specificities.

Gersch M, Stahl M, Poreba M, Dahmen M, Dziedzic A, Drag M, Sieber SA.

ACS Chem Biol. 2016 Feb 19;11(2):389-99. doi: 10.1021/acschembio.5b00757. Epub 2015 Dec 9.


Small Molecule Active Site Directed Tools for Studying Human Caspases.

Poreba M, Szalek A, Kasperkiewicz P, Rut W, Salvesen GS, Drag M.

Chem Rev. 2015 Nov 25;115(22):12546-629. doi: 10.1021/acs.chemrev.5b00434. Epub 2015 Nov 9. Review.


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

Byzia A, Szeffler A, Kalinowski L, Drag M.

Biochimie. 2016 Mar;122:31-7. doi: 10.1016/j.biochi.2015.09.035. Epub 2015 Oct 9.


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

Rajković J, Poreba M, Caglič D, Vidmar R, Wilk A, Borowik A, Salvesen G, Turk V, Drag M, Turk B.

J Biol Chem. 2015 Nov 20;290(47):28231-44. doi: 10.1074/jbc.M115.687764. Epub 2015 Oct 7.


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

Galiullina RA, Kasperkiewicz P, Chichkova NV, Szalek A, Serebryakova MV, Poreba M, Drag M, Vartapetian AB.

J Biol Chem. 2015 Oct 9;290(41):24806-15. doi: 10.1074/jbc.M115.675819. Epub 2015 Aug 17.


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

van der Linden WA, Segal E, Child MA, Byzia A, Drąg M, Bogyo M.

Chem Biol. 2015 Aug 20;22(8):995-1001. doi: 10.1016/j.chembiol.2015.07.010. Epub 2015 Aug 6.


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

Kasperkiewicz P, Poreba M, Snipas SJ, Lin SJ, Kirchhofer D, Salvesen GS, Drag M.

PLoS One. 2015 Jul 14;10(7):e0132818. doi: 10.1371/journal.pone.0132818. eCollection 2015.


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

Drąg-Zalesińska M, Wysocka T, Borska S, Drąg M, Poręba M, Choromańska A, Kulbacka J, Saczko J.

Biomed Pharmacother. 2015 May;72:91-7. doi: 10.1016/j.biopha.2015.04.003. Epub 2015 Apr 13.


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

Békés M, Rut W, Kasperkiewicz P, Mulder MP, Ovaa H, Drag M, Lima CD, Huang TT.

Biochem J. 2015 Jun 1;468(2):215-26. doi: 10.1042/BJ20141170.


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

Rut W, Kasperkiewicz P, Byzia A, Poreba M, Groborz K, Drag M.

Biol Chem. 2015 Apr;396(4):329-37. doi: 10.1515/hsz-2014-0315. Review.


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

Arya T, Reddi R, Kishor C, Ganji RJ, Bhukya S, Gumpena R, McGowan S, Drag M, Addlagatta A.

J Med Chem. 2015 Mar 12;58(5):2350-7. doi: 10.1021/jm501790e. Epub 2015 Feb 27.


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

Lechtenberg BC, Kasperkiewicz P, Robinson H, Drag M, Riedl SJ.

ACS Chem Biol. 2015 Apr 17;10(4):945-51. doi: 10.1021/cb500909n. Epub 2015 Jan 22.


Probes to monitor activity of the paracaspase MALT1.

Hachmann J, Edgington-Mitchell LE, Poreba M, Sanman LE, Drag M, Bogyo M, Salvesen GS.

Chem Biol. 2015 Jan 22;22(1):139-47. doi: 10.1016/j.chembiol.2014.11.011. Epub 2014 Dec 31.


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

Mistry SN, Drinkwater N, Ruggeri C, Sivaraman KK, Loganathan S, Fletcher S, Drag M, Paiardini A, Avery VM, Scammells PJ, McGowan S.

J Med Chem. 2014 Nov 13;57(21):9168-83. doi: 10.1021/jm501323a. Epub 2014 Oct 24.


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

Gras S, Byzia A, Gilbert FB, McGowan S, Drag M, Silvestre A, Niepceron A, Lecaille F, Lalmanach G, Brossier F.

Eukaryot Cell. 2014 Jul;13(7):884-95. doi: 10.1128/EC.00062-14. Epub 2014 May 16.


Unnatural amino acids increase sensitivity and provide for the design of highly selective caspase substrates.

Poreba M, Kasperkiewicz P, Snipas SJ, Fasci D, Salvesen GS, Drag M.

Cell Death Differ. 2014 Sep;21(9):1482-92. doi: 10.1038/cdd.2014.64. Epub 2014 May 16.


Staphylococcal SplB serine protease utilizes a novel molecular mechanism of activation.

Pustelny K, Zdzalik M, Stach N, Stec-Niemczyk J, Cichon P, Czarna A, Popowicz G, Mak P, Drag M, Salvesen GS, Wladyka B, Potempa J, Dubin A, Dubin G.

J Biol Chem. 2014 May 30;289(22):15544-53. doi: 10.1074/jbc.M113.507616. Epub 2014 Apr 8.

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