Charles S. Craik, PhD

Charles S. Craik, PhD

Professor, Departments of Pharmaceutical Chemistry, Pharmacology, and Biochemistry/Biophysics, UCSF

Phone: (415) 476-8146, 476-9890 (voice)
Box 2280, UCSF
San Francisco, CA 94143-2280

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Cancer Center Membership

Program Member » Prostate Cancer» Developmental Therapeutics

Research Summary

The research interests of my lab focus on defining the roles and the mechanisms of enzymes in complex biological processes and on developing technologies to facilitate these studies. Information on my lab can be found at the following website: The primary emphasis of our work has been on enzymes, with a particular emphasis on macromolecular recognition. Our original protein engineering studies have evolved to encompass various proteases as well as their endogenous inhibitors and membrane bound receptors, including uPAR, and have recently been successful at developing functional imaging probes for breast, colon, and prostate cancer using novel technologies. Our antibody engineering studies have identified Fabs that recognize conformational states of the target enzyme or receptor and are being developed into functional probes for in vivo imaging. The methodologies we developed to identify these functional Fabs have also been applied to enzymes and membrane proteins for structural and functional studies.


Allegheny College, Meadville, PA, B.S., 1976, Chemistry
Columbia University, N.Y., NY, M.A., 1978, Chemistry
Columbia University, N.Y., NY, Ph.D., 1981, Chemistry

Professional Experience

  • 1981-85
    Postgraduate Research Biochemist, Department of Biochemistry & Biophysics, UCSF
  • 1985-91
    Assistant Professor, Departments of Pharm. Chemistry and Biochemistry & Biophysics, UCSF
  • 1991-1994
    Associate Professor, Departments of Pharm. Chemistry and Biochemistry & Biophysics, UCSF
  • 1994-present
    Professor, Departments of Pharm. Chemistry, and Biochemistry & Biophysics, UCSF
  • 1995-present
    Professor, Departments of Pharm. Chemistry, Pharmacology and Biochemistry & Biophysics, UCSF

Honors & Awards

  • 1972-75
    National Honor Society; Alden Scholar
  • 1974-75
    Doane Distinguished Scholar, Phi Beta Kappa
  • 1975
    Richard Edwin Lee Scholar
  • 1985-86
    Top 100 Innovators - Science Digest

Selected Publications

  1. Page MJ, Lourenço AL, David T, LeBeau AM, Cattaruzza F, Castro HC, VanBrocklin HF, Coughlin SR, Craik CS. Non-invasive imaging and cellular tracking of pulmonary emboli by near-infrared fluorescence and positron-emission tomography. Nat Commun. 2015; 6:8448.
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  2. O'Donoghue AJ, Knudsen GM, Beekman C, Perry JA, Johnson AD, DeRisi JL, Craik CS, Bennett RJ. Destructin-1 is a collagen-degrading endopeptidase secreted by Pseudogymnoascus destructans, the causative agent of white-nose syndrome. Proc Natl Acad Sci U S A. 2015 Jun 16; 112(24):7478-83.
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  3. Wermelinger LS, Frattani FS, Carneiro-Lobo TC, Craik CS, Castro HC, Zingali RB. Ecotin: Exploring a feasible antithrombotic profile. Int J Biol Macromol. 2015 Jul; 78:296-303.
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  4. LeBeau AM, Sevillano N, Markham K, Winter MB, Murphy ST, Hostetter DR, West J, Lowman H, Craik CS, VanBrocklin HF. Imaging active urokinase plasminogen activator in prostate cancer. Cancer Res. 2015 Apr 1; 75(7):1225-35.
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  5. Sharma V, Panwar P, O'Donoghue AJ, Cui H, Guido RV, Craik CS, Brömme D. Structural requirements for the collagenase and elastase activity of cathepsin K and its selective inhibition by an exosite inhibitor. Biochem J. 2015 Jan 1; 465(1):163-73.
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  6. Kim J, Wu S, Tomasiak TM, Mergel C, Winter MB, Stiller SB, Robles-Colmanares Y, Stroud RM, Tampé R, Craik CS, Cheng Y. Subnanometre-resolution electron cryomicroscopy structure of a heterodimeric ABC exporter. Nature. 2015 Jan 15; 517(7534):396-400.
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  7. Skala W, Utzschneider DT, Magdolen V, Debela M, Guo S, Craik CS, Brandstetter H, Goettig P. Structure-Function Analyses of Human Kallikrein-related Peptidase 2 Establish the 99-Loop as Master Regulator of Activity. J Biol Chem. 2014 Dec 5; 289(49):34267-83.
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  8. Mahon C, Krogan NJ, Craik CS, Pick E. Cullin E3 ligases and their rewiring by viral factors. Biomolecules. 2014; 4(4):897-930.
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  9. Gable JE, Acker TM, Craik CS. Current and Potential Treatments for Ubiquitous but Neglected Herpesvirus Infections. Chem Rev. 2014 Nov 26; 114(22):11382-412.
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  10. Tajon CA, Seo D, Asmussen J, Shah N, Jun YW, Craik CS. Sensitive and selective plasmon ruler nanosensors for monitoring the apoptotic drug response in leukemia. ACS Nano. 2014 Sep 23; 8(9):9199-208.
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  11. Lucas JM, Heinlein C, Kim T, Hernandez SA, Malik MS, True LD, Morrissey C, Corey E, Montgomery B, Mostaghel E, Clegg N, Coleman I, Brown CM, Schneider EL, Craik C, Simon JA, Bedalov A, Nelson PS. The Androgen-Regulated Protease TMPRSS2 Activates a Proteolytic Cascade Involving Components of the Tumor Microenvironment and Promotes Prostate Cancer Metastasis. Cancer Discov. 2014 Nov; 4(11):1310-25.
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  12. Gable JE, Lee GM, Jaishankar P, Hearn BR, Waddling CA, Renslo AR, Craik CS. Broad-spectrum allosteric inhibition of herpesvirus proteases. Biochemistry. 2014 Jul 22; 53(28):4648-60.
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  13. 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. Urokinase-type plasminogen activator receptor (uPAR) ligation induces a raft-localized integrin signaling switch that mediates the hypermotile phenotype of fibrotic fibroblasts. J Biol Chem. 2014 May 2; 289(18):12791-804.
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  14. LeBeau AM, Sevillano N, King ML, Duriseti S, Murphy ST, Craik CS, Murphy LL, VanBrocklin HF. Imaging the urokinase plasminongen activator receptor in preclinical breast cancer models of acquired drug resistance. Theranostics. 2014; 4(3):267-79.
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  15. Tajon C, Jun YW, Craik CS. Single-molecule sensing of caspase activation in live cells via plasmon coupling nanotechnology. Methods Enzymol. 2014; 544:271-97.
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  16. Asmussen J, Lasater EA, Tajon C, Oses-Prieto J, Jun YW, Taylor BS, Burlingame A, Craik CS, Shah NP. MEK-dependent negative feedback underlies BCR-ABL-mediated oncogene addiction. Cancer Discov. 2014 Feb; 4(2):200-15.
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  17. Du X, Chen NL, Wong A, Craik CS, Brömme D. Elastin degradation by cathepsin V requires two exosites. J Biol Chem. 2013 Nov 29; 288(48):34871-81.
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  18. O'Donoghue AJ, Jin Y, Knudsen GM, Perera NC, Jenne DE, Murphy JE, Craik CS, Hermiston TW. Global substrate profiling of proteases in human neutrophil extracellular traps reveals consensus motif predominantly contributed by elastase. PLoS One. 2013; 8(9):e75141.
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  19. 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. Dissecting the active site of the collagenolytic cathepsin L3 protease of the invasive stage of Fasciola hepatica. PLoS Negl Trop Dis. 2013; 7(7):e2269.
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  20. Small JL, O'Donoghue AJ, Boritsch EC, Tsodikov OV, Knudsen GM, Vandal O, Craik CS, Ehrt S. Substrate specificity of MarP, a periplasmic protease required for resistance to acid and oxidative stress in Mycobacterium tuberculosis. J Biol Chem. 2013 May 3; 288(18):12489-99.
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