Research Topics
| CHARLES SCOTT CRAIKSummaryAffiliation: University of California Country: USA Publications
Research Grants
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Detail Information
Publications
Characterization of proteinases from the midgut of Rhipicephalus (Boophilus) microplus involved in the generation of antimicrobial peptidesCarlos E Cruz
Department of Parasitology, Institute of Biomedical Sciences, University of Sao Paulo, Sao Paulo, SP 05508 900, Brazil
Parasit Vectors 3:63. 2010..abstract:..- GPS-Prot: a web-based visualization platform for integrating host-pathogen interaction dataMarie E Fahey
Department of Cellular and Molecular Pharmacology, University of California San Francisco, 1700 4th Street, San Francisco, CA 94158, USA
BMC Bioinformatics 12:298. 2011..Because these host-pathogen interactions are extensive and interactions between human proteins are found within many different databases, it is difficult to generate integrated HIV-human interaction networks... 
Proteases as therapeuticsCharles S Craik
Department of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA 94131, USA
Biochem J 435:1-16. 2011..Proteases therefore have a bright future as a distinct therapeutic class with diverse clinical applications...
Substrate specificity of schistosome versus human legumain determined by P1-P3 peptide librariesMary A Mathieu
Department of Pathology, UCSF, San Francisco, CA 94143, USA
Mol Biochem Parasitol 121:99-105. 2002..Predictions of substrate specificity from the library screen were confirmed using single peptide substrates for kinetic assays...- Prostate-specific antigen: an overlooked candidate for the targeted treatment and selective imaging of prostate cancerAaron M LeBeau
Department of Pharmacology and Molecular Science, The Johns Hopkins University School of Medicine, Baltimore, MD 2131, USA
Biol Chem 391:333-43. 2010..In addition, the unique active site characteristics of PSA and how these motifs aided our research in developing PSA targeted agents are highlighted... - Positional scanning synthetic combinatorial libraries for substrate profilingEric L Schneider
Department of Pharmaceutical Chemistry, The University of California, San Francisco, San Francisco, CA, USA
Methods Mol Biol 539:59-78. 2009..These sequences can be readily verified through kinetic measurements on single peptide substrates and utilized to further knowledge of the role of proteases in cancer... - Hemoglobin cleavage site-specificity of the Plasmodium falciparum cysteine proteases falcipain-2 and falcipain-3Shoba Subramanian
Department of Medicine, Division of Infectious Diseases, University of California San Francisco, San Francisco, California, United States of America
PLoS ONE 4:e5156. 2009..falciparum and with the possibility of developing small molecule inhibitors with optimized specificity as antimalarial agents... - Scanning the prime-site substrate specificity of proteolytic enzymes: a novel assay based on ligand-enhanced lanthanide ion fluorescenceAmy M Barrios
Department of Pharmaceutical Chemistry, University of California, San Francisco 94143, USA
Bioorg Med Chem Lett 12:3619-23. 2002..Furthermore, the continuous fluorogenic assay described may prove useful in analyzing the activity of other hydrolytic enzymes... - Identification of the major cysteine protease of Giardia and its role in encystationKelly N DuBois
Department of Pathology, the Sandler Center for Basic Research in Parasitic Diseases, University of California, San Francisco, CA 94158, USA
J Biol Chem 283:18024-31. 2008..These data suggest that Giardia cysteine protease 2 is not only the major cysteine endoprotease expressed in Giardia, but is also central to the encystation process... - Critical role of amino acid 23 in mediating activity and specificity of vinckepain-2, a papain-family cysteine protease of rodent malaria parasitesAjay Singh
Department of Medicine, San Francisco General Hospital, San Francisco, CA 94143, USA
Biochem J 368:273-81. 2002..It indicates that drug discovery studies must take into account important differences between plasmodial proteases and sheds light on the critical role of amino acid 23 in catalysis by papain-family proteases... - Substrate profiling of cysteine proteases using a combinatorial peptide library identifies functionally unique specificitiesYoungchool Choe
Department of Pharmaceutical Chemistry, University of California at San Francisco, California 94143, USA
J Biol Chem 281:12824-32. 2006..This approach provides useful information for developing selective chemical probes to study protease-related pathologies and physiologies... - Using specificity to strategically target proteasesMark D Lim
Department of Pharmaceutical Chemistry, University of California, School of Pharmacy, 513 Parnassus Avenue Room S 926, San Francisco, CA 94158, USA
Bioorg Med Chem 17:1094-100. 2009..The use of these approaches to better understand a protease's natural substrate will be discussed as well as the technologies that emerged... - Characterization of structural determinants of granzyme B reveals potent mediators of extended substrate specificitySandra Waugh Ruggles
Graduate Group in Biophysics, University of California, San Francisco, California 94143 2280, USA
J Biol Chem 279:30751-9. 2004..This study confirms four determinants of granzyme B extended substrate specificity that constitute a canon applicable to the study of the remaining family members... - Granzyme M is a regulatory protease that inactivates proteinase inhibitor 9, an endogenous inhibitor of granzyme BSami Mahrus
Chemistry and Chemical Biology Graduate Program, University of California, San Francisco, California 94143 2280, USA
J Biol Chem 279:54275-82. 2004..Proteinase inhibitor 9 was effectively hydrolyzed and inactivated by human granzyme M, raising the possibility that this orphan granzyme bypasses proteinase inhibitor 9 inhibition of granzyme B... - Herpesvirus protease inhibition by dimer disruptionNobuhisa Shimba
Department of Pharmaceutical Chemistry, University of California-San Francisco, 600 16th St, Box 2280, San Francisco, CA 94143-2280, USA
J Virol 78:6657-65. 2004..These results indicate that the dimer interface, as well as the active sites, of herpesvirus proteases is a viable target for inhibiting enzyme activity... - SmCL3, a gastrodermal cysteine protease of the human blood fluke Schistosoma mansoniJan Dvorak
Sandler Center for Basic Research in Parasitic Diseases, California Institute for Quantitative Biosciences, University of California San Francisco, San Francisco, California, United States of America
PLoS Negl Trop Dis 3:e449. 2009..Digestion of nutrients from the host bloodstream is essential for parasite development and reproduction. A network of proteolytic enzymes (proteases) facilitates hydrolysis of host hemoglobin and serum proteins... - Vinyl sulfones as antiparasitic agents and a structural basis for drug designIain D Kerr
Department of Cellular and Molecular Pharmacology, University of California, San Francisco, California 94158 2550, USA
J Biol Chem 284:25697-703. 2009.... - Development of alpha-keto-based inhibitors of cruzain, a cysteine protease implicated in Chagas diseaseYoungchool Choe
Department of Pharmaceutical Chemistry, 600 16th Street, University of California at San Francisco, San Francisco, CA 94143-2280, USA
Bioorg Med Chem 13:2141-56. 2005..This study also demonstrates the validity of structure-guided approaches to focused library design and lead compound optimization... - Albumin is a substrate of human chymase. Prediction by combinatorial peptide screening and development of a selective inhibitor based on the albumin cleavage siteWilfred W Raymond
Cardiovascular Research Institute and Department of Medicine, University of California at San Francisco, San Francisco, California 94143 0911, USA
J Biol Chem 278:34517-24. 2003..8 nM) and 2,700- and 1,300-fold selective for chymase over cathepsin G and chymotrypsin, respectively. In summary, these findings reveal albumin to be a substrate for chymase and identify a potentially useful new chymase inhibitor... - Potent and selective inhibition of membrane-type serine protease 1 by human single-chain antibodiesJeonghoon Sun
Department of Pharmaceutical Chemistry, University of California, San Francisco, 513 Parnassus, San Francisco, California 94143, USA
Biochemistry 42:892-900. 2003..These antibodies constitute a new class of highly selective protease inhibitors that can be used to dissect the biological roles of proteolytic enzymes as well as to develop diagnostic and therapeutic reagents... - Cercarial elastase is encoded by a functionally conserved gene family across multiple species of schistosomesJason P Salter
University of California San Francisco Graduate Program in Biomedical Sciences and the Department of Pathology, University of California, San Francisco, California 94143, USA
J Biol Chem 277:24618-24. 2002.... - Identification and biochemical characterization of vivapains, cysteine proteases of the malaria parasite Plasmodium vivaxByoung-Kuk Na
Department of Medicine, San Francisco General Hospital, University of California, San Francisco, CA 94143-0811, USA
Biochem J 378:529-38. 2004..Considering inhibitor profiles, the vivapains were inhibited by fluoromethylketone and vinyl sulphone inhibitors that also inhibited falcipains and have demonstrated potent antimalarial activity... - A parasite cysteine protease is key to host protein degradation and iron acquisitionTheresa C O'Brien
Department of Pathology and Sandler Center for Basic Research in Parasitic Diseases, University of California, San Francisco, California 94158 2550, USA
J Biol Chem 283:28934-43. 2008..Because even a modest deficiency in tbcatB is lethal for the parasite, tbcatB is a logical target for the development of new anti-trypanosomal chemotherapy... - Inhibition of a viral enzyme by a small-molecule dimer disruptorTina Shahian
Graduate Group in Biochemistry and Molecular Biology, University of California, San Francisco, California, USA
Nat Chem Biol 5:640-6. 2009..These results validate the interface of herpesvirus proteases and other similar oligomeric interactions as suitable targets for the development of small-molecule inhibitors... - Analysis of an engineered plasma kallikrein inhibitor and its effect on contact activationA Allart Stoop
Department of Pharmaceutical Chemistry, University of California San Francisco, 94143 2280, USA
Biol Chem 391:425-33. 2010..We used ecotin-Pkal to specifically inhibit contact activation of human plasma at the level mediated by plasma kallikrein... - How immune peptidases change specificity: cathepsin G gained tryptic function but lost efficiency during primate evolutionWilfred W Raymond
Cardiovascular Research Institute, University of California at San Francisco, San Francisco, CA 94143, USA
J Immunol 185:5360-8. 2010.... - Coordinate expression and functional profiling identify an extracellular proteolytic signaling pathwayAmi S Bhatt
Department of Pharmaceutical Chemistry, University of California, 600 16th Street, San Francisco, CA 94158, USA
Proc Natl Acad Sci U S A 104:5771-6. 2007..Individually, MT-SP1 and RON overexpression have been implicated in cancer progression and metastasis. Transcriptional coexpression of these genes suggests that this signaling pathway may be involved in several human cancers... - Granzyme B proteolyzes receptors important to proliferation and survival, tipping the balance toward apoptosisCarly R K Loeb
Department of Biochemistry and Biophysics, Tetrad Graduate Program, University of California, San Francisco, 94131, USA
J Biol Chem 281:28326-35. 2006..Therefore, granzyme B not only activates pro-death functions within a target, but also has a previously unidentified role in inactivating pro-growth signals to cause cell death... - Altered substrate specificity of drug-resistant human immunodeficiency virus type 1 proteaseDeborah S Dauber
Graduate Program in Chemistry and Chemical Biology, University of California, San Francisco, San Francisco, California 94143, USA
J Virol 76:1359-68. 2002..Understanding the altered substrate specificity of drug-resistant HIV PR should be valuable in the design of future generations of protease inhibitors as well as in elucidating the molecular basis of regulation of proteolysis in HIV... - Anisotropic dynamics of the JE-2147-HIV protease complex: drug resistance and thermodynamic binding mode examined in a 1.09 A structureK Kinkead Reiling
Department of Biochemistry and Biophysics, Graduate Group in Biophysics, University of California at San Francisco, San Francisco, California 94143, USA
Biochemistry 41:4582-94. 2002.... - The oligomeric structure of human granzyme A is a determinant of its extended substrate specificityJessica K Bell
Department of Pharmaceutical Chemistry, University of California, San Francisco, California 94143, USA
Nat Struct Biol 10:527-34. 2003..The crystal structure, along with substrate library profiling and mutagenesis, has allowed us to identify and rationally manipulate key components involved in GzmA substrate specificity... - The periplasmic serine protease inhibitor ecotin protects bacteria against neutrophil elastaseChristopher T Eggers
Department of Biochemistry and Biophysics, University of California at San Francisco, San Francisco, CA 94143 92280, USA
Biochem J 379:107-18. 2004..This suggests that an important part of the antimicrobial mechanism of neutrophil elastase may be a periplasmic bacteriostatic effect of protease that has translocated across the damaged outer membrane... - Communication between the active sites and dimer interface of a herpesvirus protease revealed by a transition-state inhibitorAlan B Marnett
Program in Chemistry and Chemical Biology, Department of Pharmaceutical Chemistry, University of California, San Francisco, CA 94143, USA
Proc Natl Acad Sci U S A 101:6870-5. 2004.... - Substrate modulation of enzyme activity in the herpesvirus protease familyAna Lazic
Department of Pharmaceutical Chemistry, University of California, San Francisco, CA 94158 2517, USA
J Mol Biol 373:913-23. 2007..This suggests that the mechanism by which herpesvirus proteases achieve their high specificity is by using extended substrates to modulate both the structure and activity of the enzyme... - Papa's got a brand new tag: advances in identification of proteases and their substratesAlan B Marnett
Program in Chemistry and Chemical Biology, Department of Pharmaceutical Chemistry, The University of California, San Francisco, California 94143, USA
Trends Biotechnol 23:59-64. 2005..Here, we focus on several recently developed techniques representing crucial advances toward identification of proteases and their natural substrates... - Conversion of trypsin to a functional threonine proteaseTeaster T Baird
University of California, San Francisco, Department of Pharmaceutical Chemistry, San Francisco, California 94143-2280, USA
Protein Sci 15:1229-38. 2006..Removal of the disulfide bridge decreases the overall thermostability of the enzyme, but it is partially rescued by the presence of threonine at position 195... - Selective inhibition of the collagenolytic activity of human cathepsin K by altering its S2 subsite specificityFabien Lecaille
Department of Human Genetics, Mount Sinai School of Medicine, Box 1498, New York, New York 10029, USA
Biochemistry 41:8447-54. 2002..These results indicate that Tyr67 and Leu205 play a key role in the binding of proline residues in the S2 pocket of cathepsin K and are required for its unique collagenase activity... - Characterization of a cysteine protease from Tritrichomonas foetus that induces host-cell apoptosisJohn J Lucas
Department of Biochemistry and Molecular Biology, SUNY Upstate Medical University, 4257 Weiskotten Hall, 766 Irving Avenue, Syracuse, NY 13210, USA
Arch Biochem Biophys 477:239-43. 2008..In addition, the DNA sequence was completed by 3' and 5' rapid amplification of cDNA ends (RACE) and the full-length amino acid sequence was obtained... - Expedient solid-phase synthesis of fluorogenic protease substrates using the 7-amino-4-carbamoylmethylcoumarin (ACC) fluorophoreDustin J Maly
Department of Chemistry, University of California, Berkeley, California 94720, USA
J Org Chem 67:910-5. 2002..Finally, procedures are included for the preparative synthesis of optimized ACC substrates for HIV-1 protease and plasmin... - IrAE: an asparaginyl endopeptidase (legumain) in the gut of the hard tick Ixodes ricinusDaniel Sojka
Institute of Parasitology, Biology Centre of the Academy of Sciences of the Czech Republic and Faculty of Biological Sciences, University of South Bohemia, Ceske Budejovice, Czech Republic
Int J Parasitol 37:713-24. 2007..The possible functions of IrAE in the gut digestive processes of I. ricinus are compared with those suggested for other hematophagous parasites... - Computer-assisted mutagenesis of ecotin to engineer its secondary binding site for urokinase inhibitionMartha C A Laboissière
Departamento de Ciencias Farmaceuticas, Faculdade de Ciencias da Saude, Universidade de Brasilia, Campus Universitario Darcy Ribeiro, 70910 900 Brasilia, DF Brasil
J Biol Chem 277:26623-31. 2002..This technology can be applied to select for enhanced binding interactions at protein-protein interfaces and accelerate the process of protease inhibitor development... - Specificity profiling of seven human tissue kallikreins reveals individual subsite preferencesMekdes Debela
, Proteinase Research Group, Am Klopferspitz 18, D-82152 Martinsried, Germany
J Biol Chem 281:25678-88. 2006..The specificity profiles may lead to a better understanding of human tissue kallikrein functions and assist in identifying their physiological protein substrates as well as in designing more selective inhibitors... - Catalytic properties and inhibition of proline-specific dipeptidyl peptidases II, IV and VIIBarbara Leiting
Department of Metabolic Disorders, Merck Research Laboratories, Mail code RY50G 236, P O Box 2000, Rahway, NJ 07065, USA
Biochem J 371:525-32. 2003..Selective DPP-IV and DPP-VII substrates were identified and they can be used to design selective inhibitors and probe further into the biology of these enzymes... - Substrates of the prostate-specific serine protease prostase/KLK4 defined by positional-scanning peptide librariesMasazumi Matsumura
Division of Human Biology, Fred Hutchinson Cancer Research Center, 1100 Fairview Ave. N, Seattle, WA 98109, USA
Prostate 62:1-13. 2005..CONCLUSIONS: These results identify potential KLK4 substrates that may serve to define the role of this protease in normal prostate physiology, and facilitate studies of the consequences of KLK4 expression in pathological conditions... - Structural and functional relationships in the virulence-associated cathepsin L proteases of the parasitic liver fluke, Fasciola hepaticaColin M Stack
Institute for the Biotechnology of Infectious Diseases, University of Technology Sydney, Sydney, New South Wales 2007, Australia
J Biol Chem 283:9896-908. 2008..The emergence of a specialized collagenolytic function in Fasciola likely contributes to the success of this tissue-invasive parasite... - A multi-enzyme cascade of hemoglobin proteolysis in the intestine of blood-feeding hookwormsAngela L Williamson
Department of Microbiology and Tropical Medicine, The George Washington University, Washington, DC 20037, USA
J Biol Chem 279:35950-7. 2004.... - Quantitative and label-free technique for measuring protease activity and inhibition using a microfluidic cantilever arrayDigvijay A Raorane
Department of Mechanical Engineering, University of California, Berkeley, California 94720, USA
Nano Lett 8:2968-74. 2008..58 x 10 (-6) M). Inhibition of surface-immobilized trypsin by soybean trypsin inhibitor (SBTI) was also observed using this system... - Hepatocyte growth factor is a preferred in vitro substrate for human hepsin, a membrane-anchored serine protease implicated in prostate and ovarian cancersSylvia Herter
Department of Biology, Amgen San Francisco, 1120 Veterans Boulevard, South San Francisco, CA 94080, USA
Biochem J 390:125-36. 2005.... - Structures and specificity of the human kallikrein-related peptidases KLK 4, 5, 6, and 7Mekdes Debela
Max Planck Institut fur Biochemie, Proteinase Research Group, Am Klopferspitz 18, D 82152 Martinsried, Germany
Biol Chem 389:623-32. 2008..Interestingly, for KLK4, 5, and 7 extended charged surface regions were observed that most likely serve as exosites for physiological substrates... - Expression and characterization of constitutively active human caspase-14Kyewhan Park
Department of Oral Biology, University of Washington, Seattle, WA 98195, USA
Biochem Biophys Res Commun 347:941-8. 2006....
Research Grants
- RESEARCH TRAINING IN CHEMISTRY AND CHEMICAL BIOLOGYCharles Craik; Fiscal Year: 2007..Expansion into the new Mission Bay campus has greatly strengthened the program by providing state of the art chemistry and chemical biology lab space. ..
- Targeting Allosteric Studies to Modulate Protein Interactions and FunctionCharles Craik; Fiscal Year: 2007....
- A Technological Platform for the Identification of Serine Proteases in CancerCharles Craik; Fiscal Year: 2009..Support functions include the Molecular Foundry, the Microfabrication Laboratory, the Biomolecular Nanotechnology Center, facilities for manufacture of microarrays, and data management and integration. RELEVANCE ..
- Targeting Allosteric Studies to Modulate Protein Interactions and FunctionCharles Craik; Fiscal Year: 2009....
- A Technological Platform for the Identification of Serine Proteases in CancerCHARLES SCOTT CRAIK; Fiscal Year: 2010..Support functions include the Molecular Foundry, the Microfabrication Laboratory, the Biomolecular Nanotechnology Center, facilities for manufacture of microarrays, and data management and integration. RELEVANCE ..