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  3. Amit Nathubhai

  • Amit is an Organic and Medicinal Chemist involved in using reagents to dissect the pharmacological pathways that can contribute to a variety of diseases and conditions. Amit performed his undergraduate and master’s degree in Biological Chemistry (University of Leicester, 2004 and 2005 respectively) and a PhD in Organic and Medicinal Chemistry (University of Dundee and later, University of Bath). Amit graduated with a PhD from the University of Bath in 2010. Amit stayed on at the University of Bath as a Postdoctoral Research Officer and secured three research grants. Whilst at Bath, Amit progressed to becoming a Research Fellow and performed a company secondment fellowship at AstraZeneca (Mӧlndal) and University of New York, which was supported by the MRC. Amit’s research involves the design, synthesis and evaluation of compounds that target the enzymes called tankyrases, which is applicable to dissect the fundamental mechanisms pertinent to colorectal cancer, prostate cancer, IPF, diabetes, obesity and new areas of regenerative medicine.

    Amit then went on to join the University of Sunderland as a Senior Lecturer in Medicinal Chemistry in 2018, which involved teaching Pharmacy and Biopharmaceutical Sciences students, whilst continuing his research on creating tankyrase inhibitors that can be used as molecular tools and new leads. Amit moved to the University of Northampton in 2022 as a Senior Lecturer in Pharmacology, which utilises his expertise at the interface of Chemistry and Biology.

    Amit’s office hours are on Tuesday afternoons and Thursday mornings in term time.

  • Amit is the am the programme leader for the Pharmacology course and module leader for SLS2015 (Pharmacology). Amit also teaches SLS1051 (Foundations of Chemistry) and contributes to teaching on other modules within Life Sciences.

     

  • Amit’s research involves the design and evaluation of compounds that can be used as molecular tools or new leads to combat particular type of cancers, diabetes and fibrotic diseases. Current projects involve the use of potent and isoform-selective inhibitors of the enzymes called Tankayrases to target Wnt/β-catenin driven processes that contribute to the progression of diseases. Tankyrases inhibitors could be used as pharmacological tools and potential drugs to target colorectal cancer, prostate cancer, idiopathic pulmonary fibrosis (IPF) and type-2 diabetes.

  • 2021:

    • *Lloyd, M. D.; Yevglevskis. M.; Nathubhai, A.; James, T. D.; Threadgill M. D.; Woodman, T. J. Racemases and epimerases operating through a 1,1-proton transfer mechanism: reactivity, mechanism and inhibition. Chemical Society Reviews, 2021, 50, 10, 5952-5984.

    2019:

    • Petrova, Y. D.; Wadda, K.; Nathubhai, A.; Yevglevskis. M.; Mitchell, P. J.; Lee, L. G.; James, T. D.; Threadgill M. D.; Woodman, T. J.; *Lloyd, M. D. Identification of novel small-molecule inhibitors of α-methylacyl-CoA racemase (AMACR; P504S) and structure-activity relationships. Bioorganic Chemistry, 2019, 92, 103263, 1-6.
    • Yevglevskis. M.; Nathubhai, A.; Wadda, K.; Lee, L. G.; Al-Rawi, S.; Jiao, T.; Mitchell, P. J.; James, T. D.; Threadgill M. D.; Woodman, T. J.; *Lloyd, M. D. Novel 2 arylthiopropanoyl-CoA inhibitors of α-methylacyl-CoA racemase 1A (AMACR; P504S) as potential anti-prostate cancer agents. Bioorganic Chemistry, 2019, 92, 103263, 1-8.

    2018:

    • Yevglevskis. M.; Lee, L. G.; Nathubhai, A.; Petrova, Y. D. James, T. D. Threadgill M. D. Woodman, T. J.; *Lloyd, M. D. Structure-activity relationships of rationally designed AMACR 1A inhibitors. Bioorganic Chemistry, 2018, 79, 145-154.
    • Gravells, P.; Neale, J.; Grant, E.; Nathubhai, A.; Smith, K. M.; James, D. I.; Bryant, H.E. Radiosensitization with an inhibitor of poly(ADP-ribose) glycohydrolase; a comparison with the PARP1/2/3 inhibitor olaparib. DNA Repair, 2018, 61, 25-36.

    2017:

    • Yevglevskis. M.; Lee, L. G.; Nathubhai, A.; Petrova, Y. D. James, T. D. Threadgill M. D. Woodman, T. J.; *Lloyd, M. D. A novel colorimetric assay for α-methylacyl-CoA racemase A1 (AMACR; P504S) utilizing the elimination of 2,4-dinitrophenolate. Chemical Communications, 2017, 53, 5087-5090.
    • *Nathubhai, A.; Haikarainen, T.; Koivunen, J.; Murthy. S.; Koumanov, F.; Lloyd, M. D.; Holman, G. D.; Pihlajaniemi, T.; Tosh. D.; Lehtiö. L.; Threadgill, M. D. Highly potent and isoform-selective dual-site-binding tankyrase/Wnt signalling inhibitors that increase cellular glucose uptake and have anti-proliferative activity. Journal of Medicinal Chemistry, 2017, 60, 814-820. 

    2016:

    • *Nathubhai, A.; Haikarainen. T.; Hayward, C. P.; Muñoz-Descalzo, S.; Thompson, A. S.; Lloyd, M. D.; Lehtiö. L.; Threadgill, M. D. Structure-activity relationship of 2-arylquinazolin-4-ones as highly selective and potent inhibitors of the tankyrases. European Journal of Medicinal Chemistry, 2016, 118, 316-327.

    2015:

    • Twum, E. A.; Nathubhai, A.; Wood, P. J.; Lloyd, M. D.; Thompson, A. S.; *Threadgill, M. D. Initial development of a cytotoxic amino-seco-CBI warhead for delivery by prodrug systems. Bioorganic and Medicinal Chemistry, 2015, 23, 3481-3489.
    • Kumpan. E.; Nathubhai, A.; Zhang. C.; Wood, P. J.; Lloyd, M. D.; Thompson A. S.; Haikarainen. T.; Narwal. M.; Lehtiö. L.; *Threadgill, M. D. Structure-based design, synthesis and evaluation in vitro of aryl­naph­th­yr­id­in­ones, arylpyridopyrimidinones and their tetrahydro derivatives as inhibitors of the tankyrases. Bioorganic and Medicinal Chemistry, 2015, 23, 3013-3032.
    • 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.; Lehtiö. L.; *Threadgill, M. D. 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, 2015, 23, 5891-5908.

    2013:

    • Nathubhai, A.; Wood, P. J.; Lloyd, M. D.; Thompson A. S.; *Threadgill, M. D. Design and discovery of 2-arylquinazolin-4-ones as potent and selective inhibitors of the tankyrases. ACS Medicinal Chemistry Letters, 2013, 4, 1173-1177.

    2011:

    • Nathubhai, A.; Patterson, R.; Woodman, T. A.; Sharp, H. C. E.; Chui, M. T. Y.; Chung, H. H. K.;  Lau, S. W. S.; Zheng, J.;  Lloyd, M.D.; Thompson A. S.; *Threadgill, M. D. N3-Alkylation during formation of quinazolin-4-ones from condensation of anthranilamides and orthoamides. Organic & Biomolecular Chemistry, 2011, 9, 6089-6099.

    2009:

    • Dixon, M. J.; Andersen, O. A.; van Aalten, D. M. F.; Nathubhai, A.; *Eggleston, I. M. Solid-Phase synthesis of cyclic peptide chitinase inhibitors: SAR of the argifin scaffold. Organic Biomolecular Chemistry, 2009, 7, 2, 259-268.
    • Dixon, M. J.; Nathubhai, A.; Andersen, O. A.; van Aalten, D. M. F.; *Eggleston, I. M. Synthesis and structure-based dissection of cyclic peptide chitinase inhibitors: New leads for antifungal and anti-inflammatory drugs. Advances in Experimental Medicine and Biology, 2009, 611, 525-526.

    2008:

    • Dixon, M. J.; Andersen, O. A.; van Aalten, D. M. F.; Nathubhai, A.; *Eggleston, I. M. Synthesis of cyclic peptide chitinase inhibitors: Natural products with chemotherapeutic potential. Journal of Peptide Science, 2008, 14, 8, 13.
    • Dixon, M. J.; Giuntini, F.; Nathubhai, A.; Andersen, O. A.; van Aalten, D. M. F.; Eggleston, I. M. Synthetic approaches to cyclic peptide natural products as chitinase inhibitors. Journal of Peptide Science, 2008, 14, 8, 55.
    • Andersen, O. A.; Nathubhai, A.; Dixon, M. J.; Eggleston, I. M.; *van Aalten, D. M. F. Structure-Based Dissection of the Natural Product Chitinase Inhibitor Argifin, Chemistry and Biology, 2008, 15, 3, 295-301.

    2007:

    • Dixon, M. J.; Andersen, O. A.; van Aalten, D. M. F.; Nathubhai, A.; *Eggleston, I. M. “Cyclic peptide chitinase inhibitors: New leads for antifungal and anti-inflammatory drugs”, Biopolymers (Peptide Science), 2007, 88, 4, 576.