Home Screen Our Work Who we are Publications Fun stuff


Structural requirements for the collagenase and elastase activity of cathepsin K and its selective inhibition by an exosite inhibitor. Sharma V, Panwar P, O'Donoghue AJ, Cui H, Guido RV, Craik CS, Bromme D. Biochem J. 2014 Oct 3. [Epub ahead of print] PMID: 25279554

Current and Potential Treatments for Ubiquitous but Neglected Herpesvirus Infections. Gable JE, Acker TM, Craik CS. Chem Rev. 2014 Oct 2. [Epub ahead of print] PMID: 25275644

Sensitive and selective plasmon ruler nanosensors for monitoring the apoptotic drug response in leukemia. Tajon CA, Seo D, Asmussen J, Shah N, Jun YW, Craik CS. ACS Nano. 2014 Sep 23;8(9): 9199-208. PMID: 25166742

Broad-spectrum allosteric inhibition of herpesvirus proteases. Gable JE, Lee GM, Jaishankar P, Hearn BR, Waddling CA, Renslo AR, Craik CS. Biochemistry. 2014 Jul 22;53(28): 4648-60. PMID: 24977643

Single-Molecule Sensing of Caspase Activation in Live Cells via Plasmon Coupling Nanotechnology. Tajon C, Jun YW, Craik CS. Methods Enzymol. 2014;544:271-97. PMID: 24974294

Urokinase-type plasminogen activator receptor (uPAR) ligation induces a raft-localized integrin signaling switch that mediates the hypermotile phenotype of fibrotic fibroblasts. Grove LM, Southern BD, Jin TH, White KE, Paruchuri S, Harel E, Wei Y, Rahaman SO, Gladson CL, Ding Q, Craik CS, Chapman HA, Olman MA. J Biol Chem. 2014 May 2;289(18):12791-804. PMID: 24644284

Imaging the urokinase plasminogen activator receptor in preclinical breast cancer models of acquired drug resistance. LeBeau AM, Sevillano N, King ML, Duriseti S, Murphy ST, Craik CS, Murphy LL, VanBrocklin HF. Theranostics. 2014 Jan 18;4(3):267-79. PMID: 24505235

MEK-dependent negative feedback underlies BCR-ABL-mediated oncogene addiction. Asmussen J, Lasater EA, Tajon C, Oses-Prieto J, Jun YW, Taylor BS, Burlingame A, Craik CS, Shah NP. Cancer Discov. 2014 Feb;4(2): 200-15. PMID: 24362263



Global substrate profiling of proteases in human neutrophil extracellular traps reveals consensus motif predominantly contributed by elastase. O'Donoghue AJ, Jin Y, Knudsen GM, Perera NC, Jenne DE, Murphy JE, Craik CS, Hermiston TW. PLoS One. 2013 Sept 20;8(9):e75141. PMID: 24073241

Dissecting the active site of the collagenolytic cathepsin L3 protease of the invasive stage of Fasciola hepatica. Corvo I, O'Donoghue AJ, Pastro L, Pi-Denis N, Eroy-Reveles A, Roche L, McKerrow JH, Dalton JP, Craik CS, Caffrey CR, Tort JF. PLoS Negl Trop Dis. 2013 Jul 11;7(7):e2269. PMID: 23875031

Substrate specificity of MarP, a periplasmic protease required for resistance to acid and oxidative stress in Mycobacterium tuberculosis. Small JL, O'Donoghue AJ, Boritsch EC, Tsodikov OV, Knudsen GM, Vandal O, Craik CS, Ehrt S. J Biol Chem. 2013 May 3;288(18):12489-99. PMID: 23504313

Mutational tail loss is an evolutionary mechanism for liberating marapsins and other type I serine proteases from transmembrane anchors. Raman K, Trivedi NN, Raymond WW, Ganesan R, Kirchhofer D, Verghese GM, Craik CS, Schneider EL, Nimishakavi S, Caughey GH. J Biol Chem. 2013 Apr 12;288(15):10588-98. PMID: 23447538

Targeting uPAR with Antagonistic Recombinant Human Antibodies in Aggressive Breast Cancer. LeBeau AM, Duriseti S, Murphy ST, Pepin F, Hann B, Gray JW, VanBrocklin HF, Craik CS. Cancer Res. 2013 Apr 1;73(7):2070-81. PMID: 23400595

Imaging a functional tumorigenic biomarker in the transformed epithelium. LeBeau AM, Lee M, Murphy ST, Hann BC, Warren RS, Delos Santos R, Kurhanewicz J, Hanash SM, VanBrocklin HF, Craik CS. Proc Natl Acad Sci U S A. 2013 Jan 2;110(1):93-8. PMID: 23248318



Mapping inhibitor binding modes on an active cysteine protease via nuclear magnetic resonance spectroscopy. Lee GM, Balouch E, Goetz DH, Lazic A, McKerrow JH, Craik CS. Biochemistry. 2012 Dec 18;51(50):10087-98.PMID: 23181936

Global identification of peptidase specificity by multiplex substrate profiling. O'Donoghue AJ, Eroy-Reveles AA, Knudsen GM, Ingram J, Zhou M, Statnekov JB, Greninger AL, Hostetter DR, Qu G, Maltby DA, Anderson MO, Derisi JL, McKerrow JH, Burlingame AL, Craik CS. Nat Methods. 2012 Nov;9(11):1095-100. PMID: 23023596. Software (EZ Extractor) from this manuscript can be downloaded here.

A screening strategy for trapping the inactive conformer of a dimeric enzyme with a small molecule inhibitor. Craik CS, Shahian T. Methods Mol Biol. 2012;928:119-31.PMID: 22956137

Activity and Inhibition of Prostasin and Matriptase on Apical and Basolateral Surfaces of Human Airway Epithelial Cells. Nimishakavi S, Besprozvannaya M, Raymond WW, Craik CS, Gruenert DC, Caughey GH. Am J Physiol Lung Cell Mol Physiol. 2012. 303(2):L97-106 PMID: 22582115

Characterization of the gut-associated cathepsin D hemoglobinase from the tick Ixodes ricinus (IrCD1). Sojka D, Franta Z, Frantová H, Bartosová P, Horn M, Váchová J, O'Donoghue AJ, Eroy-Reveles AA, Craik CS, Knudsen GM, Caffrey CR, McKerrow JH, Mares M, Kopácek P. J Biol Chem. 2012 Apr 26. [Epub ahead of print] PMID: 22539347

Investigation of the proteolytic functions of an expanded cercarial elastase gene family in Schistosoma mansoni. Ingram JR, Rafi SB, Eroy-Reveles AA, Ray M, Lambeth L, Hsieh I, Ruelas D, Lim KC, Sakanari J, Craik CS, Jacobson MP, McKerrow JH. PLoS Negl Trop Dis. 2012 Apr;6(4):e1589. PMID: 22509414

Fabs Enable Single Particle cryoEM Studies of Small Proteins. Wu S, Avila-Sakar A, Kim J, Booth DS, Greenberg CH, Rossi A, Liao M, Li X, Alian A, Griner SL, Juge N, Yu Y, Mergel CM, Chaparro-Riggers J, Strop P, Tampé R, Edwards RH, Stroud RM, Craik CS, Cheng Y. Structure. 2012 Apr 4;20(4):582-92. Epub 2012 Apr 3. PMID: 22483106

Analysis of Fasciola cathepsin L5 by S(2) subsite substitutions and determination of the P(1)-P(4) specificity reveals an unusual preference. Norbury LJ, Hung A, Beckham S, Pike RN, Spithill TW, Craik CS, Choe Y, Fecondo JV, Smooker PM. Biochimie. 2012 May;94(5):1119-27. Epub 2012 Jan 20. PMID: 22285967


Vif hijacks CBF-β to degrade APOBEC3G and promote HIV-1 infection. Jäger S, Kim DY, Hultquist JF, Shindo K, Larue RS, Kwon E, Li M, Anderson BD, Yen L, Stanley D, Mahon C, Kane J, Franks-Skiba K, Cimermancic P, Burlingame A, Sali A, Craik CS, Harris RS, Gross JD, Krogan NJ. Nature. 2011 Dec 21. [Epub ahead of print] PMID: 22190037

Global landscape of HIV-human protein complexes. Jäger S, Cimermancic P, Gulbahce N, Johnson JR, McGovern KE, Clarke SC, Shales M, Mercenne G, Pache L, Li K, Hernandez H, Jang GM, Roth SL, Akiva E, Marlett J, Stephens M, D'Orso I, Fernandes J, Fahey M, Mahon C, O'Donoghue AJ, Todorovic A, Morris JH, Maltby DA, Alber T, Cagney G, Bushman FD, Young JA, Chanda SK, Sundquist WI, Kortemme T, Hernandez RD, Craik CS, Burlingame A, Sali A, Frankel AD, Krogan NJ. Nature. 2011 Dec 21. [Epub ahead of print] PMID: 22190034

A Reverse Binding Motif That Contributes to Specific Protease Inhibition by Antibodies. Schneider EL, Lee MS, Baharuddin A, Goetz DH, Farady CJ, Ward M, Wang CI, Craik CS. J Mol Biol. 2011 Nov 27. [Epub ahead of print] PMID: 22154938

Rapid identification of recombinant Fabs that bind to membrane proteins. Kim J, Stroud RM, Craik CS. Methods. 2011. Sep 20 [Epub ahead of print] PMID: 21958987

Inhibition of Granzyme B by PI-9 protects prostate cancer cells from apoptosis. Ray M, Hostetter DR, Loeb CR, Simko J, Craik CS. Prostate. 2011 Sep 14. [Epub ahead of print] PMID: 21919028

Inhibitors of SARS-CoV entry - Identification using an internally-controlled dual envelope pseudovirion assay. Zhou Y, Agudelo J, Lu K, Goetz DH, Hansell E, Chen YT, Roush WR, McKerrow J, Craik CS, Amberg SM, Simmons G. Antiviral Res. 2011 Jul 26. [Epub ahead of print] PMID: 21820471

IrCL1 - The haemoglobinolytic cathepsin L of the hard tick, Ixodes ricinus. Franta Z, Sojka D, Frantova H, Dvorak J, Horn M, Srba J, Talacko P, Mares M, Schneider E, Craik CS, McKerrow JH, Caffrey CR, Kopacek P. Int J Parasitol. 2011 Jul 23. [Epub ahead of print] PMID: 21819989

GPS-Prot: a web-based visualization platform for integrating host-pathogen interaction data. Fahey ME, Bennett MJ, Mahon C, Jaeger S, Pache L, Kumar D, Shapiro A, Rao K, Chanda SK, Craik CS, Frankel AD, Krogan NJ. BMC Bioinformatics. 2011. 12(1):298. PMID: 21777475

Enzyme Inhibition by Allosteric Capture of an Inactive Conformation. 2011. Lee GM, Shahian T, Baharuddin A, Gable JE, Craik CS. J Mol Biol. 411(5):999-1016. PMID:21723875

Human and mouse granzyme M display divergent and species-specific substrate specificities. de Poot SA, Westgeest M, Hostetter DR, Van Damme P, Plasman K, Demeyer K, Broekhuizen R, Gevaert K, Craik CS, Bovenschen N. Biochem J. 2011. 437(3):431-42. PMID: 21564021

Proteases as therapeutics. Craik CS, Page MJ, Madison EL. Biochem J. 2011. 435(1):1-1. PMID:21406063 

Peptide length and leaving-group sterics influence potency of Peptide phosphonate protease inhibitors. Brown CM, Ray M, Eroy-Reveles AA, Egea P, Tajon C, Craik CS. Chem Biol. 2011. 18(1):48-57. PMID: 21276938



Mechanisms of Macromolecular Protease Inhibitors. Farady CJ, Craik CS. Chembiochem. 2010. 11(17):2341-2346. PMID: 21053238

The Oligopeptidase B of Leishmania regulates parasite enolase and immune evasion. Swenerton RK, Zhang S, Sajid M, Medzihradszky KF, Craik CS, Kelly BL, McKerrow JH. J Biol Chem. 2010. 185(9):5360-8. PMID: 20961853

Biochemical Properties of a Novel Cysteine Protease of Plasmodium vivax, Vivapain-4. Na BK, Bae YA, Zo YG, Choe Y, Kim SH, Desai PV, Avery MA, Craik CS, Kim TS, Rosenthal PJ, Kong Y. PLoS Negl Trop Dis. 2010. 4(10). pii: e849. PMID: 20967286

How Immune Peptidases Change Specificity: Cathepsin G Gained Tryptic Function but Lost Efficiency during Primate Evolution. Raymond WW, Trivedi NN, Makarova A, Ray M, Craik CS, Caughey GH. J Immunol. 2010 185(9):5360-8. PMID: 20889553

Characterization of proteinases from the midgut of Rhipicephalus (Boophilus) microplus involved in the generation of antimicrobial peptides. Cruz CE, Fogaca AC, Nakayasu ES, Angeli CB, Belmonte R, Almeida IC, Miranda A, Miranda MT, Tanaka AS, Braz GR, Craik CS, Schneider E, Caffrey CR, Daffre S. Parasit Vectors. 2010. 3(1):63. PMID: 20663211

Prediction of Protease Substrates Using Sequence and Structure Features. Barkan DT, Hostetter DR, Mahrus S, Pieper U, Wells JA, Craik CS, Sali A. Bioinformatics. 2010. 26(14):1714-22. PMID: 20501655

Antagonstic anti-upar antibodies significantly inhibit uPAR-mediated cellular signaling and migration. Duriseti KS, Goetz DH, Hostetter DR, Wei Y, Craik CS. J Biol Chem. 2010. 285(35):26878-88. PMID: 20501655

A Novel Entamoeba histolytica Cysteine Proteinase, EhCP4, is Key for Invasive Amebiasis and a Therapeutic Target. He C, Nora GP, Schneider EL, Kerr ID, Hansell E, Hirata K, Gonzalez D, Sajid M, Boyd SE, Hruz P, Cobo ER, Le C, Liu WT, Eckmann L, Dorrestein PC, Houpt ER, Brinen LS, Craik CS, Roush WR, McKerrow JH, Reed SL. J Biol Chem. 2010. 285(24):18516-27. PMID: 20378535

Mycobacterium tuberculosis MycP1 protease plays a dual role in regulation of ESX-1 secretion and virulence. Ohol YM, Goetz DH, Chan K, Shiloh MU, Craik CS, Cox JS. Cell Host Microbe. 2010. 7(3):210-20. PMID: 20227664

Time-Resolved Single-Step Protease Activity Quantification Using Nanoplasmonic Resonator Sensors. Sun C, Su KH, Valentine J, Rosa-Bauza Ellman JA, Elboudwarej O, Mukherjee B, Craik CS, Shuman MA, Chen FF, Zhang X. ACS Nano. 2010. 4(2):978-84. PMID: 20121209

Tumor detection by imaging proteolytic activity. Darragh MR, Schneider EL, Lou J, Phojanakong PJ, Farady CJ, Marks JD, Hann BC, Craik CS. ancer Res. 2010. 70(4):1505-12. PMID: 20145119

Local Protease Signaling Contributes to Neural Tube Closure in the Mouse Embryo. Camerer E, Barker A, Duong DN, Ganesan R, Kataoka H, Cornelissen I, Darragh MR, Hussain A, Zheng YW, Srinivasan, Brown C, Xu SM, Regard JB, Lin CY, Craik CS, Kirchhofer D, Coughlin SR. Dev Cell. 2010. 18(1):25-38.PMID: 01521757

Prostate-specific antigen: an overlooked candidate for the targeted treatment and selective imaging of prostate cancer. Lebeau AM, ova M, Craik CS, Denmeade SR. Biol Chem. 2010. 391(4):333-43. PMID: 20180648

Analysis of an engineered plasma kallikrein inhibitor and its effect on contact activation. Stoop AA, Joshi RV, Eggers CT, Craik CS. Biol Chem. 2010. 391(4):425-33. PMID: 20180651


Substrate specificity of transthyretin: Identification of natural substrates in the nervous system. Liz MA, Fleming CE, Nunes AF, Almeida MR, Mar FM, Choe Y, Craik CS, Powers JC, Bogyo M, Sousa MM. Biochem J. 2009 419(2):467-74 PMID: 19138167

Active plasma kallikrein localizes to mast cells and regulates epithelial cell apoptosis, adipocyte differentiation and stromal remodeling during mammary gland involution. Lilla JN, Joshi RV, Craik CS, Werb Z. J Biol Chem. 2009 May 15;284(20):13792-803. Epub 2009 Mar 18.PMID: 19297327

Inhibition of a Viral Enzyme by a Small Molecule Dimer Disruptor Shahian, T., Lee, G., Lazic, A., Arnold, L., Velusamy P., Roels C, Guy R., Craik, C.S. Nat Chem Biol., 2009 Sep;5(9):640-6. Jul 26. PMC2752665

Trapping Moving Targets With Small Molecules, Lee, G. and Craik, C.S., Science (2009) 10;324(5924):213-5.

Hemoglobin cleavage site-specificity of the Plasmodium falciparum cysteine proteases falcipain-2 and falcipain-3.Subramanian S, Hardt M, Choe Y, Niles RK, Johansen EB, Legac J, Gut J, Kerr ID, Craik CS, Rosenthal PJ. PLoS ONE. 2009;4(4):e5156. PMC2663817.

Positional scanning synthetic combinatorial libraries for substrate profiling. Schneider EL, Craik CS. Methods Mol Biol. 2009;539:1-20. PMID: 19377970.

Improving the species cross-reactivity of an antibody using computational design. Farady CJ, Sellers BD, Jacobson MP, Craik CS, Bioorg Med Chem Lett. 2009. 19(14):3744-7. PMC2724971.

SmCL3, a Gastrodermal Cysteine Protease of the Human Blood Fluke Schistosoma mansoni. Dvorák J, Mashiyama ST, Sajid M, Braschi S, Delcroixx M, Schneider EL, McKerrow WH, Bahgat M, Hansell E, Babbitt PC, Craik CS, McKerrow JH, Caffrey CR. PLoS Negl Trop Dis. 2009. 3(6). PMCID: PMC2685030.

Characterization of a multimeric, eukaryotic prolyl aminopeptidase: an inducible and highly specific intracellular peptidase from the non-pathgenic fungus Talaromyces emersonii. Mahon CS, O'Donoghue AJ, Goetz DH, Murray PG, Craik CS, Tuohy MG. Microbiology 2009. 155(Pt 11):3673-82.PMID: 19556294.

Vinyl sulfones as antiparasitic agents and a structural basis for drug design. Kerr ID, Lee JH, Farady CJ, Marion R, Rickert M, Sajid M, ndey KC, Caffrey CR, Legac J, Hansell E, McKerrow JH, Craik CS, Rosenthal PJ, Brinen LS. J Biol Chem. 2009. 284(38):25697-703. PMC2757971.

Inhibition of a viral enzyme by a small-molecule dimer disruptor. Shahian T, Lee GM, Lazic A, Arnold LA, Velusamy P, Roels CM, Guy RK, k CS. Nat Chem Biol. 2009. 5(9):640-6. PMID: 1963365

Engineering Ecotin for Identifying Proteins with a Trypsin Fold. Sathler PC, Craik CS, Takeuchi T, Zingali RB, Castro HC. Appl Biochem echnol. 2009. PMID: 19728173

Two approaches to discovering and developing new drugs for Chagas disease. McKerrow JH, Doyle PS, Engel JC, Podust LM, Robertson SA, ra R, Saxton T, Arkin M, Kerr ID, Brinen LS, Craik CS. Mem Inst Oswaldo Cruz. 2009. 104 Suppl 1:263-9. PMID: 19753483

Continuous imaging of plasmon rulers in live cells reveals early stage caspase-3 activation at the single molecule level. Jin YW, Sassan S, on C, Craik CS, Alvisatos AP. Proc Natl Acad Sci USA. 2009.106(42):17735-40. PMC2764940


Using Specificity to Strategically Target Proteases. Lim, M.D. Craik, .C.S., Bioorg Med 17(3):1094-100 (2008) PMID: 18434168

Identification of the Major Cysteine Protease of Giardia and its Role in Encystation. Dubios, K.N., Abodeely, M., Sakanari, J., Craik, C.S., Lee, M., McKerrow, J.H., Sajid, M. J Biol Chem 283(26):18024-31 (2008) PMID:18445589

Structure of an Fab-Protease Complex Reveals a Highly Specific Non-canonical Mechanism of Inhibition. Farady, C.T., Egea, P.F., Schneider, E.L., Darragh, M.R., Craik, C.S. J Mol Biol 380(2), 351-60 (2008) PMID: 18514224

Characterization of a Cysteine Protease from Tritrichomonas Foetus that Induces Host Cell Apoptosis. Lucas, J.J., Hayes, G.R., Kalsi, H.K., Gilbert, R.O., Choe, Y., Craik, C.S., Singh, B.N. Arch Biochem Biophys 77(2):239-43 (2008) PMID: 18554499

Structures and Specificity of the human kallikrein-related peptidases KLKs 4, 5, 6, and 7. Debela, M., Beaufort, N., Magdolen, V., Schecter, N.M., Craik, C.S., Schmitt, M., Bode, W., Goettig, P. Biol. Chem, 389(6) 623-32. (2008) PMID: 18627297

A Parasite Cysteine Protease is Key to Host Protein Degradation and Iron Acquisition. O'Brien, T.C., Mackey, Z.B., Fetter, R.D., Choe, Y., O'Donoghue, A.J., Zhou, M., Craik, C.S., Caffrey, C.R., McKerrow, J.H. J. Biol Chem 283(43):28934-43 (2008).PMID: 18701454

Inhibition of a Secreted Glutamic Peptidase Prevents Growth of the Fungus Talaromyces emersonii. O'Donoghue, A.J., Mahon, C.S., Goetz, D.H., O'Malley, J.M., Gallagher, D.M., Zhou, M., Murray, P.G., Craik, C.S. Tuohy, M.G. J. Biol. Chem 283(43):29186-95.PMID: 18687686

The Functional Expression and Characterisation of a Cysteine Peptidase from the invasive Stage of the Neuropathogenic Schistosome Trichobilharzia regenti. Doleckovák, Kasný M, Mikes L, Cartwright J, Jedelský P, Schneider EL, Dvorák J, Mountford AP, Craik CS, Horák P. Int J Parasitol. 2008. 39(2):201-11. PMID: 18708063

Quantitative and Label-Free Technique for Measuring Protease Activity and Inhibition using a Microfluidic Cantilever Array. Raorane DA, Lim MD, Chen FF, Craik CS, Majumdar A. Nano Lett. 2008 10;8(9):2968-2974. PMID: 18720973

MT-SP1 Proteolysis and Regulation of Cell-Microenvironment Interactions. Darragh, M.R., Bhatt, A.S., and Craik, C.S. Front in Biosci. 2008. 13:528-39. PMID: 17981566


Craik, C. (2007), "Fundamentals and Principles for Engineering Proteolytic Activity", in Dunn, B. (ed.), Protein Epidemiology: Understanding Human Diseases at the Level of Protein Structure and Function, The Biomedical & Life Sciences Collection, Henry Stewart Talks Ltd, London (online at

Coordinate Expression and Functional Profiling Identify an Extracellular Proteolytic Signaling Pathway. Bhatt, A.S., Welm, A., Farady, C.J., Vasquez, Wilson, K., and Craik, C.S. Proc Natl Acad Sci U S A. 2007. 104(14):5771-6. PMID: 17389401

The Mechanism of Inhibition of Antibody-Based Inhibitors of Membrane-Type Serine Protease 1 (MT-SP1). Farady, C.J., Sun, J., Darragh, M.R., Miller, S.M., and Craik, C.S. J Mol Biol. 2007. 369(4):1041-51. PMID: 17475279

IrAE – An Asparaginyl Endopeptidase (Legumain) in the Gut of the Hard Tick Ixodes Ricinus. Sojka, D. Hajdusek, O., Dvorak, J., Sajid, M., Franta, Z., Schneider, E.L., Craik, C.S., Vancova, M., Buresova, V., Bogyo, M., Sexton, K.B., McKerrow, J.H., Caffrey, C.R., Kopacek, P. Int J Parasitol. 2007. 37(7):713-24. PMID: 17336985

Substrate Specificity Profiling and Identification of a New Class of Inhibitor for the Major Protease of the SARS Caronavirus. Goetz, D.H., Choe, Y., Hansell, E., Chen, Y.T., McDowell, M., Jonsson, C.B., Roush, W.R., McKerrow, J., and Craik, C.S. Biochemistry. 2007. 46(30):8744-52. PMID: 17605471

Hip is a Pro-survival Substrate of Granzyme B. Hostetter, D.R., Loeb, C.R.K., Chu, F. and Craik, C.S.J Biol Chem. 2007. 282(38):27865-74. PMID: 17620340

Substrate Modulation of Enzyme Activity in the Herpesvirus Protease Family. Lazic, A., Goetz, D.H., Nomura, A.M., Marnett, A.B. and Craik, C.S.J Mol Biol. 2007. 373(4):913-23. PMID: 17870089  


One Functional Switch Mediates Reversible and Irreversible Inactivation of a Herpesvirus Protease. Normura, A.M., Marnett, A.B., Shimba, N., Dötch, and Craik, C.S. Biochemistry 45(11), 3572-9 (2006)

Substrate Profiling of Cysteine Proteases Using a Combinatorial Peptide Library Identifies Functionally Unique Specificities. Choe, Y., Leonetti, F., Greenbaum, D.C., Lecaille, F., Bogyo, M., Brömme, D., Ellman, J.A., and Craik, C.S. J. Biol Chem. 281(18), 12824-32 (2006)

Conversion of Trypsin to a Functional Threonine Protease. Baird, T.T., Wright, W.D. and Craik, C.S. Protein Sci. 15(6), 1229-38 (2006)

Specificity Profiling of Seven Human Tissue Kallikreins Reveals Individual Subsite Preferences. Debela, M., Magdolen, V., Schechter, N., Valachova, M., Lottspeich, F., Craik, C.S., Choe, Y., Bode, W., and Goettig, P. J. Biol. Chem. 281(35), 25678-88 (2006)

Plasminogen Activation Independent of uPA and tPA Maintains Wound Healing in Gene-Deficient Mice. Lund, L.R., Green, K.A., Stoop, A.A., Ploug, M., Almholt, K., Lilla, J., Nielsen, B.S., Christensen, I.J., Craik, C.S., Werb, Z., Dano, K. and Romer, J. EMBO25(12), 2686-97 (2006)

Granzyme B Proteolyzes Receptors Important to Proliferation and Survival, Tipping the Balance Towards Apoptosis. Loeb, C.R.K., Harris, J. and Craik, C.S. J. Biol. Chem. 281(38), 28326-35 (2006)

Isotope-coded and Affinity-tagged Cross-linking (ICATXL): An Efficient Strategy to Probe Protein Interaction Surfaces. Chu, F., Mahrus, S., Craik, C.S., and Burlingame, A. J. Amer. Chem Soc. 123(32), 10362-3. (2006)

Expression and Characterization of Constitutively Active Human Caspase-14. Park, K., Keuchle, M.K., Choe, Y., Craik, C.S. Lawrence, O.T., and Presland, R.B. Biochem Biophys Res Commun. 347(4), 941-8 (2006).


Selective Chemical Functional Probes of Granzymes A and B Demonstrate Granzyme B is a Major Effector of Natural Killer Cell-Mediated Lysis of Target Cells. Mahrus, S. and Craik, C.S. Chem. Biol. 12(5), 567-77 (2005)

Adhesion Signaling By a Novel Mitotic Substrate of SRC Kinases. Bhatt, A., Erdjument-Bromage, H., Tempst, P., Craik, C.S., and Moasser, M. Oncogene, 24(34) 5333-43 (2005)

Hepatocyte Growth Factor is a Preferred In Vitro Substrate for Human Hepsin, a Membrane-anchored Serine Protease Implicated in Prostate and Ovarian Cancers. Herter, S., Piper, D.E., Aaron, W., Gabriele, T., Cutler, G., Cao, P., Bhatt, A.S., Choe, Y., Craik, C.S., Walker, N., Meininger, D., Hoey, T. and Austin, R.J. Biochem J. 390(1), 125-36 (2005)

Induced Structure: A Transitional Helix Switch that Regulates Enzyme Activity. *Nomura, A.M., *Marnett, A.B., Shimba, N., Doetch, V., and Craik, C.S. Nat. Struc. Mol. Bio. 12(11) 1019-20 (2005)

Substrates of the Prostate-specific Serine Protease Prostate/KLK4 Defined by Positional-scanning Peptide Libraries. Matsumura, M. Bhatt, A.S., Andress, D., Clegg, N., Takayama, T.K. and Craik, C.S. Prostate 62(1), 1-13 (2005)

Papa's Got a Brand New Tag: Advances in Identification of Proteases and their Substrates. Marnett, A.B. and Craik, C.S. Trends in Biotechnol. 23(2), 59-64 (2005)

Development of Alpha-Keto-based Inhibitors of Cruzain, a Cysteine Protease Implicated in Chagas Disease. Choe, Y., Brinen, L.S., Price, M.S., Engel, J.C., Lange, M. Grisostomi, C., Weston, S.G., Pallai, P.V., Cheng, H., Hardy, L.W., Hartsough, D.S., McMakin, M., Tilto, R.F. Baldino, C.M., and Craik, C.S. Bioorg. Med. Chem. 13(6), 2141-56 (2005)


A Multi-Enzyme Cascade of Hemoglobin Proteolysis in the Intestine of Blood-Feeding Hookworms. Williamson, A.L., Lecchi, P.X., Turk, B.E., Choe, Y., Hotez, P.J., McKerrow, J.H., Cantley, L.C., Sajid, M., Craik, C.S. and Loukas, A. J. Biol. Chem. 279(34), 35950-7 (2004)

Methyl Groups as Probes for Proteins and Complexes in In-Cell NMR Experiments. Serber, Z., Straub, W. Corsini, L.. Nomura, A.M., Shimba, Craik. C.S., N., Ortiz de Montellano, P. and Dotsch V. J. Amer. Chem. Soc. 126(22) 7119-25 (2004)

Optimization of (13) C direct detection NMR methods. Shimba, N. Kovack, H., Stern, A.S., Nomura, A.M., Shimada, I. Hoch, J.C., Craik, C.S., and Dotsch V. J. Biomol. NMR 30(2), 175-9. (2004)

Granzyme M is a Regulatory Protease that Inactivates Proteinase Inhibitor 9, an Endogenous Inhibitor of Granzyme B. Mahrus, S. Kisiel, W. and Craik, C.S. J. Biol. Chem. 279(52), 54275-82 (2004)

Trypsin. Halfon, S., Baird, T.T., and Craik, C.S. Handbook of Proteolytic Enzymes 3nd Ed. updated 2013. (2004)

Brachyurins. Tsu, C., and Craik, C.S. Handbook of Proteolytic Enzymes 2nd Ed. (2004)

Identification and Biochemical Characterization of Vivapains, Cysteine Proteases of the Malaria Parasite Vivax. Na, B.K., Shenai, B.R., Sijwali, P.S., Choe, Y. Pandey, K.C., Singh, A. Craik, C.S. and Rosenthal, P.J. Biochem. J. 378(2), 529-38 (2004)

The Periplasmic Serine Protease Inhibitor Ecotin Protects Bacteria Against Neutrophil Elastase. Eggers, C.T., Murray, I.A., Delmar, V.A., Day, A.G. and Craik, C.S. Biochem J. 379(1), 107-18 (2004)

Communication Between the Active Site and Dimer Interface of a Herpesvirus Protease Revealed by a Transition-State Inhibitor. Marnett, A.B., Nomura, A.M., Shimba, N., Ortiz de Montellano, P.R. and Craik, C.S. PNAS 101(18), 6870-5 (2004)

Characterization of Structural Determinants of Granzyme B Reveals Potent Mediators of Extended Substrate Specificity. Ruggles, S.W., Fletterick, R.J., and Craik, C.S. J Biol. Chem. 279(29), 30751—59 (2004)

Herpesviral Protease Inhibition by Dimer Disruption. Shimba, N. Nomura, A.M., Marnett, A.B. and Craik, C.S. J. Virol. 78(12) 6657-65 (2004)


Quantitation of Membrane Type Serine Protease 1 (MT-SP1) in Transformed and Normal Cells. A.S. Bhatt, T. Takeuchi, B. Ylstra, D. Ginzinger, D. Albertson, M.A. Shuman and C.S. Craik. Biological Chemistry 384(2), 257-66 (2003)

Design and Synthesis of Novel Inhibitors of Gelatinase B. X. Wang, Y. Choe C.S. Craik and J.A. Ellman. Bioorg & Med. Chem. Ltrs. 12(16), 2201-4 (2003)

Catalytic Properties and Inhibition of Proline-Specific Dipeptidyl Peptidases II, IV and VII. B. Leiting, K.D. Pryor, J.K. Wu, F. Marsilio, R.A. Patel, C.S. Craik, J.A. Ellman, R.T. Cummings and N. Thornberry. Biochemistry 371(2), 525-32(2003)

Potent and Selective Inhibition of Membrane Type Serine Protease 1 by Human Single-Chain Antibodies. J. Sun, J. Pons and C.S. Craik. Biochemistry 42, 892-900 (2003)

The CD8+ Cell Noncytotoxic Anti-HIV Response Can Be Blocked by Protease Inhibitors. Mackewicz, C.S. Craik and J.A. Levy. PNAS 100(6), 3433-8 (2003)

Elimination of 13Ca Splitting in Protein NMR Spectra by Deconvolution with Maximum Entropy Reconstruction. N. Shimba, A.S. Stern, C.S. Craik, J.C. Hoch and V. Döetsch. J. Amer. Chem. Soc. 125(9), 2382-3 (2003)

Albumin is a Substrate of Human Chymase: Prediction by Combinatorial Peptide Screening and Development of a Selective Inhibitor Based on the Albumin Cleavage Site. W.W. Raymond, S. Waugh Ruggles, C.S. Craik, G.H. Caughey. J. Biol. Chem. 278(36), 34517-24 (2003)

The Oligomeric Structure of Human Granzyme A is a Determinant of its Extended Substrate Specificity. J.K. Bell, D.H. Goetz, S. Mahrus, J.L. Harris, R.J. Fletterick, C.S. Craik. Nat Struct Biol. 10(7), 527-34 (2003)

Engineering of a Macromolecular Scaffold to Develop Specific Protease Inhibitors. Stoop, A.A., Craik, C.S. Nat Biotechnol. 21(9), 1036-8 (2003)

Quantitative Identification of the Protonation State of Histidines In Vitro and In Vivo. Shimba, N., Serber, Z., Ledwidge, R., Miller, S.M., Craik, C.S. and Doetsch, V. Biochem. 42(30), 9227-34 (2003)


Altered Substrate Specificity of Drug-Resistant HIV-1 Protease. D. Dauber, R. Zierman, N. Parkin, D.J. Maly, S. Mahrus, J.L. Harris, J.A. Ellman, C. Petropoulos, C.S. Craik. J. Virol. 76, 1359-1368 (2002)

Conformational Change Coupling the Dimerization and Activation of KSHV Protease. T.R. Pray, K.K. Reiling, B.G. Dermirjian, C.S. Craik. Biochemistry 41(5), 1474-82 (2002)

Expedient Solid-Phase Synthesis of Fluorogenic Protease Substrates Using the 7-Amino-4-Carbamoylmethylcoumarin (ACC) Fluorophore. D.J. Maly, F. Leonetti, B.J. Backes, D.S. Dauber, J.L. Harris, C.S. Craik and J.A. Ellman. J. Org. Chem. 67(3), 910-915 (2002)

Chemically Mediated Site-specific Proteolysis. Alteration of Protein-Protein Interaction. B. Wang, K.C. Brown, M. Lodder, C.S. Craik, S.M. Hecht. Biochemistry 41 (8), 2805-2813 (2002)

Substrate Specificity of Schistosome Versus Human Legumain Determined by P1-P3 Peptide Libraries. M.A. Mathieu, M. Boygo, C.R. Caffrey, Y. Choe, J. Lee, H. Chapman, M. Sajid, C.S. Craik & J. McKerrow. Mol. Biochem. Parisitol 121 (1), 99-105 (2002)

Anisotropic Dynamics of the JE-2147-HIV Protease Complex: Drug Resistance and Thermodynamic Binding Mode Examined in a 1.09Å structure. K.K. Reiling, N.F. Endres, D.S. Dauber, C.S. Craik, R.M. Stroud. Biochemistry 41(14), 4582-4594 (2002)

Computer-Assisted Mutagenesis of Ecotin to Engineer its Secondary Binding Site for Urokinase Inhibition. M.C. Laboissiere, M.M. Young, R.G. Pinho, S. Todd, R.J. Fletterick, I. Kuntz, C.S. Craik. J Bio. Chem. 277 (29), 26623-31 (2002)

Special Delivery (Letter to the Editor). C. Berry, B.M. Dunn, C.S. Craik and John Kay. Biochem & Mol. Bio. Education, 30(3), 151. (2002)

Selective Inhibition of the Collagenolytic Activity of Human Cathepsin K by Altering its S2 Subsite Specificity. F. LeCaille, Y. Choe, W. Brandt, Z. Li, C.S. Craik and Bromme D. Biochemistry 41(26), 8447-54 (2002)

Scanning the Prime-Site Substrate Specificity of Proteolytic Enzymes: A Novel Assay Based on Ligand-Enhanced lanthanide Ion Fluorescence. A. Barrios and C.S. Craik. Bioorg Med Chem Ltrs. 12(24), 3619-23 (2002)

Cercarial Elastase is Encoded by a Functionally Conserved Gene Family Across Multiple Species of Schistosomes. J.P. Salter, Y. Choe, H. Albrecht, C. Franklin, K.C. Lim, C.S. Craik, J.H. McKerrow. J. Bio. Chem. 277(27), 24618-24 (2002)

Critical Role of Amino Acid 23 in Mediating Activity and Specificity of Vickepain-2, a Papain-family Cysteine Protease of Rodent Malaria Parasites. A. Singh, B.R. Shenai, Y. Choe, J. Gut, P.S. Sijwali, C.S. Craik and P.J. Rosenthal. Biochem J. 368(1), 273-81 (2002)


Trypsin. T.T. Baird Jr. & C.S. Craik. Encyclopedia of Genetics. Academic Press (2001)

A Plasma Kallikrein-dependent Plasminogen Cascade Required for Adipocyte Differentiation. S. Selvarajan, L.R. Lund, T. Takeuchi, C.S. Craik & Z. Werb. Nature Cell Biology, 3, 267-275 (2001)

Lytic Replication of Kaposi’s Sarcoma-Associated Herpesvirus Results in the Formation of Multiple Capsid Species: Isolation and Molecular Characterization of A, B, and C Capsids from a Gammaherpesvirus. K. Nealon, W. W. Newcomb, T.R. Pray, C.S. Craik, J.C. Brown and D.H. Kedes. J. Virol. 75, 2866-78 (2001)

Novel Inter-Protein Cross-link Identified in the GGH-ecotin D137Y Dimer. M. Person, K. Brown, S. Mahrus, C.S. Craik and A. Burlingame. Protein Science, 10, 1549-1562 (2001).

The Role of Ecotin Dimerization in Protease Inhibition. C. Eggers, S. Wang, R. J. Fletterick and C. S. Craik. J. Mol. Bio. 308, 975-991 (2001)

Definition of the Extended Substrate Specificity Determinants for Beta-Tryptases I and II. J.L. Harris, A. Niles, K. Burdick, M. Maffitt, B.J. Backus, J.A. Ellman, I. Kuntz, M. Haak-Frendscho, C.S. Craik, J. Bio. Chem., 276 (37), 34941-34947 (2001)

Structural Features of a Snake Venom Thrombin-like Enzyme: Thrombin and Trypsin on a Single Catalytic Platform. H.C. Castro, D.M. Silva, C.S. Craik, R.B. Zingali. Biochim Biophys Acta 1547, 183-95 (2001)


Cathespin G Activates Protease-Activated Receptor-4 in Human Platelets. G. Sambrano, W. Huang, T. Farugi, S. Mahrus, C.S. Craik & S.R. Coughlin. J. Bio. Chem. 275 (10), 6819-6823 (2000)

Yeast Two-Hybrid Assay for Examining HIV Protease Heterodimer Formation with Dominant Negative Inhibitors and Multidrug-Resistant Variants. S. Todd, M. Laboissiere, and C.S. Craik. Anal Biochem. 277,247-253 (2000)

Synthesis of Positional Scanning Libraries of Fluorogenic Peptide Substrates to Define the Substrate Specificity of Plasmin and Thrombin. B.J. Backes, J.L. Harris, F. Leonetti, C.S. Craik & J.A. Ellman. Nature Biotech.18(2), 187-193 (2000)

HIV Protease as a Target for Retrovirus Vector-mediated Gene Therapy. S. Todd & C.S. Craik. Biochem Et Biophys. Acta 1477 (1-2), 168-188 (2000).

Proteases: The Tip of the Iceberg. J. Harris & C.S. Craik. Cell 101, 136-137 (2000)

Macromolecular Inhibitors of HIV-1 Protease. J.E. Rozzelle, D.S. Dauber, S. Todd, R. Kelley, & C.S. Craik. J. Bio. Chem. 275 (10) 7080-7086.

Compromise and Accomodation in Ecotin, a Dimeric Macromolecular Inhibitor of Serine Proteases. S.A. Gillmore, T. Takeuchi, S.Q. Yang, C.S. Craik & R. Fletterick. J. Mol. Bio. 299, 993-1003 (2000)

Functional Consequences of the Kaposi’s Sarcoma-Associated Herpesvirus Protease Structure: Regulation of Activity and Dimerization by Conserved Structural Elements. K.K. Reiling, T.R. Pray, C.S. Craik, R.M. Stroud. Biochem. 39(42), 12796-12803 (2000)

Rapid and General Profiling of Protease Specificity by Using Combinatorial Fluorogenic Substrate Libraries. J.L. Harris, B.J. Backes, F. Leonetti, S. Mahrus, J.A. Ellman and C.S. Craik. Proc. Natl. Acad. Sci., 275, 7754-59 (2000)

Chemically Mediated Site-Specific Cleavage of Proteins. B. Wang, M. Lodder, J. Zhou, T.T. Baird, Jr., K.C. Brown, C.S. Craik, S.M. Hecht. J. Am. Chem. Soc., 122, 7402-7403 (2000)

Generation of Active Trypsin by Chemical Cleavage. T.T. Baird Jr., B. Wang, M. Lodder, S.M. Hecht and C.S. Craik. Tetrahedron Letters, 56, 9477-9485 (2000)

Cellular Localization of Membrane-type Serine Protease 1 and Identification of Protease Activated Receptor-2 and Single-chain Urokinase-type Plasminogen Activator as Substrates. T. Takeuchi, J.L. Harris, W. Huang, K.W. Yan, S.R. Coughlin and C.S. Craik. J. Bio. Chem., 275, 26333-42 (2000)

Functional Consequences of the Kaposi’s Sarcoma-Associated Herpesviral Protease Structure: Regulation of Activity and Dimerization by Conserved Structural Elements. K.K. Reiling, T.R. Pray, C.S. Craik, R.M. Stroud. Biochemistry, 24, 12796-803 (2000)

The Structure of the Pro-apoptotic Protease Granzyme B Reveals the Molecular Determinants of its Specificity. S. Waugh, J. Harris, R. Fletterick, and C.S. Craik Nature Structural Biology 7, 762-765 (2000)