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Journal articleCiepla P, Magee AI, Tate EW, 2015,
Cholesterylation: a tail of hedgehog
, BIOCHEMICAL SOCIETY TRANSACTIONS, Vol: 43, Pages: 262-267, ISSN: 0300-5127- Author Web Link
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- Citations: 12
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Journal articleWright MH, Paape D, Storck EM, et al., 2015,
Global Analysis of Protein <i>N</i>-Myristoylation and Exploration of <i>N</i>-Myristoyltransferase as a Drug Target in the Neglected Human Pathogen <i>Leishmania donovani</i>
, CHEMISTRY & BIOLOGY, Vol: 22, Pages: 342-354, ISSN: 1074-5521- Author Web Link
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- Citations: 63
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Journal articleLanyon-Hogg T, Ritzefeld M, Masumoto N, et al., 2015,
Modulation of Amide Bond Rotamers in 5-Acyl-6,7-dihydrothieno[3,2-c]pyridines
, Journal of Organic Chemistry, Vol: 80, Pages: 4370-4377, ISSN: 1520-69042-Substituted N-acyl-piperidine is a widespread and important structuralmotif, found in approximately 500 currently available structures, and present in nearly30 pharmaceutically active compounds. Restricted rotation of the acyl substituent insuch molecules can give rise to two distinct chemical environments. Here wedemonstrate, using NMR studies and density functional theory modeling of the lowestenergy structures of 5-acyl-6,7-dihydrothieno[3,2-c]pyridine derivatives, that the amideE:Z equilibrium is affected by non-covalent interactions between the amide oxygen andadjacent aromatic protons. Structural predictions were used to design molecules that promote either the E- or Z-amideconformation, enabling preparation of compounds with a tailored conformational ratio, as proven by NMR studies. Analysis ofthe available X-ray data of a variety of published N-acyl-piperidine-containing compounds further indicates that these moleculesare also clustered in the two observed conformations. This finding emphasizes that directed conformational isomerism hassignificant implications for the design of both small molecules and larger amide-containing molecular architectures.
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Journal articleKonitsiotis AD, Jovanovic B, Ciepla P, et al., 2015,
Topological Analysis of Hedgehog Acyltransferase, a Multipalmitoylated Transmembrane Protein
, JOURNAL OF BIOLOGICAL CHEMISTRY, Vol: 290, Pages: 3293-3307- Author Web Link
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- Citations: 46
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Journal articleTate EW, Kalesh KA, Lanyon-Hogg T, et al., 2015,
Global profiling of protein lipidation using chemical proteomic technologies
, CURRENT OPINION IN CHEMICAL BIOLOGY, Vol: 24, Pages: 48-57, ISSN: 1367-5931- Author Web Link
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- Citations: 80
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Journal articleDouse CH, Vrielink N, Zhang W, et al., 2015,
Targeting a Dynamic Protein-Protein Interaction: Fragment Screening against the Malaria Myosin A Motor Complex
, CHEMMEDCHEM, Vol: 10, Pages: 134-143, ISSN: 1860-7179- Author Web Link
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- Citations: 13
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Journal articleFurse S, Mak L, Tate EW, et al., 2015,
Synthesis of unsaturated phosphatidylinositol 4-phosphates and the effects of substrate unsaturation on <i>Sop</i>B phosphatase activity
, ORGANIC & BIOMOLECULAR CHEMISTRY, Vol: 13, Pages: 2001-2011, ISSN: 1477-0520- Author Web Link
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- Citations: 7
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Journal articleKalesh KA, Clulow JA, Tate EW, 2015,
Target profiling of zerumbone using a novel cell-permeable clickable probe and quantitative chemical proteomics
, CHEMICAL COMMUNICATIONS, Vol: 51, Pages: 5497-5500, ISSN: 1359-7345- Author Web Link
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- Citations: 27
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Journal articleKelly DJ, Warren SC, Alibhai D, et al., 2015,
Automated multiwell fluorescence lifetime imaging for Forster resonance energy transfer assays and high content analysis
, ANALYTICAL METHODS, Vol: 7, Pages: 4071-4089, ISSN: 1759-9660- Author Web Link
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- Citations: 10
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Journal articleYu Z, Brannigan JA, Rangachari K, et al., 2015,
Discovery of pyridyl-based inhibitors of <i>Plasmodium falciparum N</i>-myristoyltransferase
, MEDCHEMCOMM, Vol: 6, Pages: 1767-1772, ISSN: 2040-2503- Author Web Link
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- Citations: 10
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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