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Journal articleDang THT, Fagan RP, Fairweather NF, et al., 2012,
Novel inhibitors of surface layer processing in Clostridium difficile
, Bioorganic & Medicinal Chemistry, Vol: 20, Pages: 614-621, ISSN: 1464-3391Clostridium difficile, a leading cause of hospital-acquired bacterial infection, is coated in a dense surface layer (S-layer) that is thought to provide both physicochemical protection and a scaffold for host-pathogen interactions. The key structural components of the S-layer are two proteins derived from a polypeptide precursor, SlpA, via proteolytic cleavage by the protease Cwp84. Here, we report the design, synthesis and in vivo characterization of a panel of protease inhibitors and activity-based probes (ABPs) designed to target S-layer processing in live C. difficile cells. Inhibitors based on substrate-mimetic peptides bearing a C-terminal Michael acceptor warhead were found to be promising candidates for further development.
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Journal articleHeal WP, Wright MH, Thinon E, et al., 2012,
Multifunctional protein labeling via enzymatic N-terminal tagging and elaboration by click chemistry
, NATURE PROTOCOLS, Vol: 7, Pages: 105-117, ISSN: 1754-2189- Author Web Link
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- Citations: 82
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Journal articleHeal WP, Tate EW, 2012,
Application of Activity-Based Protein Profiling to the Study of Microbial Pathogenesis
, ACTIVITY-BASED PROTEIN PROFILING, Vol: 324, Pages: 115-135, ISSN: 0340-1022- Author Web Link
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- Citations: 17
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Journal articleFurse S, Brooks NJ, Seddon AM, et al., 2012,
Lipid membrane curvature induced by distearoyl phosphatidylinositol 4-phosphate
, Soft Matter -
Journal articleBradshaw RT, Aronica PGA, Tate EW, et al., 2012,
Mutational Locally Enhanced Sampling (MULES) for quantitative prediction of the effects of mutations at protein-protein interfaces
, CHEMICAL SCIENCE, Vol: 3, Pages: 1503-1511, ISSN: 2041-6520- Author Web Link
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- Citations: 2
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Journal articleTate EW, Goss RJM, 2011,
Highlights from the 46th EUCHEM Conference on stereochemistry, Bürgenstock, Switzerland, May 2011.
, Chem Commun (Camb), Vol: 47, Pages: 10869-10873 -
Journal articleDelmotte A, Tate EW, Yaliraki SN, et al., 2011,
Protein multi-scale organization through graph partitioning and robustness analysis: application to the myosin-myosin light chain interaction
, PHYSICAL BIOLOGY, Vol: 8, ISSN: 1478-3975Despite the recognized importance of the multi-scale spatio-temporal organization of proteins, most computational tools can only access a limited spectrum of time and spatial scales, thereby ignoring the effects on protein behavior of the intricate coupling between the different scales. Starting from a physico-chemical atomistic network of interactions that encodes the structure of the protein, we introduce a methodology based on multi-scale graph partitioning that can uncover partitions and levels of organization of proteins that span the whole range of scales, revealing biological features occurring at different levels of organization and tracking their effect across scales. Additionally, we introduce a measure of robustness to quantify the relevance of the partitions through the generation of biochemically-motivated surrogate random graph models. We apply the method to four distinct conformations of myosin tail interacting protein, a protein from the molecular motor of the malaria parasite, and study properties that have been experimentally addressed such as the closing mechanism, the presence of conserved clusters, and the identification through computational mutational analysis of key residues for binding.
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Journal articlede la Riva L, Willing SE, Tate EW, et al., 2011,
Roles of Cysteine Proteases Cwp84 and Cwp13 in Biogenesis of the Cell Wall of <i>Clostridium difficile</i>
, JOURNAL OF BACTERIOLOGY, Vol: 193, Pages: 3276-3285, ISSN: 0021-9193- Author Web Link
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- Citations: 42
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Journal articleSerwa R, Tate EW, 2011,
Activity-based profiling for drug discovery
, Chemistry and Biology, Vol: 18, Pages: 407-409, ISSN: 1879-1301Activity-based protein profiling (ABPP) is emerging as a game-changing tool for drug discovery, target validation, and basic biology. In this issue, Chang et al. (2011) report the ABPP-facilitated discovery of JW480, a highly selective potent and orally bioavailable inhibitor of monoalkylglycerol ether hydrolase KIAA1363 that dramatically impairs in vivo growth of human prostate cancer cell lines.
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Journal articleHeal WP, Dang TH, Tate EW, 2011,
Activity-based probes: discovering new biology and new drug targets.
, Chem Soc Rev, Vol: 40, Pages: 246-257, ISSN: 1460-4744The development and application of chemical technologies enabling direct analysis of enzyme activity in living systems has undergone explosive growth in recent years. Activity-based protein profiling (ABPP) is a key constituent of this broad field, and is among the most powerful and mature chemical proteomic technologies. This tutorial review introduces the essential features of ABPP and the design and application of activity-based probes (ABPs) from drug target elucidation and in vivo visualisation of enzyme activity to comprehensive profiling of the catalytic content of living systems, and the discovery of new biological pathways.
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Contact
Prof. Ed Tate
GSK Chair in Chemical Biology
Department of Chemistry
Molecular Sciences Research Hub, White City Campus,
82 Wood Lane, London, W12 0BZ
e.tate@imperial.ac.uk
Tel: +44 (0)20 759 + ext 43752 or 45821