Threadgill, Michael - University of Bath - Department of Pharmacy and Pharmacology

个人简介

The research focus of the Threadgill group is drug design and delivery. We work on the application of medicinal chemistry (structure-based drug design, chemical synthesis, biochemical and cell biological evaluation) to developing new cancer treatments. Where the biochemistry of other diseases is similar (haemorrhagic shock, stroke, myocardial infarction, etc.), our work has branched out into these areas. We also research new synthetic methods in organic heterocyclic chemistry. Collaborations in Bath, Aberystwyth, Finland, India and Poland are important to our work

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Nathubhai, A., Haikarainen, T., Hayward, P. C., Munoz-Descalzo, S., Thompson, A. S., Lloyd, M. D., Lehtio, L. and Threadgill, M., 2016. Structure-activity relationships of 2-arylquinazolin-4-ones as highly selective and potent inhibitors of the tankyrases. European Journal of Medicinal Chemistry, 118, pp. 316-327. Jevglevskis, M., Lee, G. L., Nathubhai, A., James, T., Threadgill, M., Woodman, T. and Lloyd, M., 2016. A convenient colorimetric assay for alpha-methylacyl-CoA racemase (AMACR; P504S) and testing for inhibitors. Yang, X., Li, M., Wang, Y.-L., Threadgill, M., Han, J.-Y., Han, X., Chen, L., Chen, H., Hu, W.-P. and Lin, X., 2016. ART1 induces aberrant methylation of uPA promoter: a preliminary study. International Journal of Clinical and Experimental Pathology, 9 (4), pp. 4269-4282. Jevglevskis, M., Lee, G. L., Nathubhai, A., James, T., Threadgill, M., Woodman, T. and Lloyd, M., 2016. A Convenient Colorimetric Assay for α-Methylacyl-CoA Racemase (AMACR; P504S) and Testing Of Inhibitors. In: Cancer Research @ Bath 13th symposium, 2016-04-27 - 2016-04-27, University of Bath. Jevglevskis, M., Lee, G. L., Nathubhai, A., James, T., Threadgill, M., Woodman, T. and Lloyd, M., 2015. A Convenient Colorimetric Assay for α-Methylacyl-CoA Racemase (AMACR; P504S) and Testing Of Inhibitors. In: Cancer Research @ Bath symposium, 2015-11-11 - 2015-11-11, University of Bath, Claverton Down cmpus, builidng 5W. Threadgill, M. D., 2015. 5-Aminoisoquinolin-1-one (5-AIQ), a water-soluble inhibitor of the poly(ADP-ribose)polymerases (PARPs). Current Medicinal Chemistry, 22 (33), pp. 3807-3829. Paine, H. A., Nathubhai, A., Woon, E. C. Y., Sunderland, P. T., Wood, P. J., Mahon, M. F., Lloyd, M. D., Thompson, A. S., Haikarainen, T., Narwal, M., Lehtio, L. and Threadgill, M. D., 2015. Exploration of the nicotinamide-binding site of the tankyrases, identifying 3-arylisoquinolin-1-ones as potent and selective inhibitors in vitro. Bioorganic and Medicinal Chemistry, 23 (17), pp. 5891-5908. Lloyd, Matthew, 2015. methods (AMACR):None. C122Q 1/533- WO 2015 /114383 A1, 06 August 2015. Twum, E. A., Nathubhai, A., Wood, P. J., Lloyd, M. D., Thompson, A. S. and Threadgill, M. D., 2015. Initial development of a cytotoxic amino-seco-CBI warhead for delivery by prodrug systems. Bioorganic and Medicinal Chemistry, 23 (13), pp. 3481-3489. Kumpan, K., Nathubhai, A., Zhang, C., Wood, P. J., Lloyd, M. D., Thompson, A. S., Haikarainen, T., Lehtio, L. and Threadgill, M. D., 2015. Structure-based design, synthesis and evaluation in vitro of arylnaphthyridinones, arylpyridopyrimidinones and their tetrahydro derivatives as inhibitors of the tankyrases. Bioorganic and Medicinal Chemistry, 23, pp. 3013-3032. Tang, Y., Li, M., Threadgill, M., Xiao, M., Mou, C.-F., Song, G.-L., Kuang, J., Yang, X., Yang, L., Gao, X.-J., Wang, Y.-P. and Meng, Y.-P., 2015. ART1 promotes starvation-induced autophagy: a possible protective role in the development of colon carcinoma. American Journal of Cancer Research, 5 (2), pp. 498-513. Kenny, M. B. C., Cheng, K. K. Y., Cheung, J. Y. C., Fung, S. K. M., Kumpan, E., Nathubhai, A. and Threadgill, M. D., 2015. Comparison of the inhibition of tankyrase-2 by 2-aryl-7,8-dihydrothiopyrano[4,3-d]pyrimidin-4-ones and 2-aryl-5,6,7,8-tetrahydroquinazolin-4-ones. In: 23rd Conference of the Groupement des Pharmacochimistes de l’Arc Atlantique (GP2A), 2015-08-26 - 2015-08-27. Lee, G. L., Jevglevskis, M., Threadgill, M., Woodman, T. and Lloyd, M., 2015. New routes to fight castrate-resistant prostate cancer: targeting α-methylacyl-CoA racemase (AMACR). In: European School of Medicinal Chemistry, 2015-06-28 - 2015-07-03. Lee, G. L., Jevglevskis, M., Threadgill, M., Woodman, T. and Lloyd, M., 2015. New routes to fight castrate-resistant prostate cancer: targeting α-methylacyl-CoA racemase (AMACR). In: 10th CR@B (Cancer Research at Bath) symposium, 2014-11-12 - 2014-11-12, University of Bath. Jevglevskis, M., Lee, G. L., Threadgill, M. D., Woodman, T. J. and Lloyd, M. D., 2014. The perils of rational design – unexpected irreversible elimination of fluoride from 3-fluoro-2-methylacyl-CoA esters catalysed by α-methylacyl-CoA racemase (AMACR; P504S). Chemical Communications, 50 (91), pp. 14164-14166. Jevglevskis, M., Bowskill, C.R., Chan, C.C.Y., Heng, J.H.-J., Threadgill, M. D., Woodman, T.J. and Lloyd, M.D., 2014. A study on the chiral inversion of mandelic acid in humans. Organic and Biomolecular Chemistry, 12 (34), pp. 6737-6744. Parveen, I., Wilson, T., Threadgill, M.D., Luyten, J., Roberts, R.E., Robson, P.R.H., Donnison, I.S., Hauck, B. and Winters, A.L., 2014. Screening for potential co-products in a Miscanthus sinensis mapping family by liquid chromatography with mass spectrometry detection. Phytochemistry, 105, pp. 186-196. Jevglevskis, M., Threadgill, M. D., Woodman, T. J. and Lloyd, M. D., 2014. A novel elimination reaction catalysed by human alpha-methylacyl-CoA racemase (AMACR; P504S) and potential applications for measuring enzyme activity. In: Early Career Researchers Day, Prostate Cancer UK, 2014, 2014-03-20. Jevglevskis, M., Threadgill, M. D., Woodman, T. J. and Lloyd, M. D., 2014. A novel elimination reaction catalysed by human alpha-methylacyl-CoA racemase (AMACR; P504S) and potential applications for measuring enzyme activity. In: RSC Chemical Biology and Bio-Organic Chemistry Postgraduate Symposium, 2014, 2014-04-01, University of Warwick. Jevglevskis, M., Threadgill, M. D., Woodman, T. J. and Lloyd, M. D., 2014. A novel elimination reaction catalysed by human alpha-methylacyl-CoA racemase (AMACR; P504S) and potential applications for measuring enzyme activity. In: Oslo Prostate Cancer Symposium, University of Oslo, Norway, 2014-05-14 - 2014-05-16, University of Oslo.