Michael Threadgill

Prof

Accepting Doctoral Students

20002020

Research output per year

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Personal profile

Research interests

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.

Current research

PARP inhibitors

The poly(ADP-ribose)polymerases (PARPs) are a family of enzymes which use ADP-ribose units from NAD+ to build poly(ADP-ribose) polymers on target proteins. PARP-1 regulates DNA repair and gene expression through NF-κB. We developed 5-AIQ as a leading inhibitor of PARP-1, potent in models of metastatic cancer, inflammation and ischaemia-reperfusion injury. We have designed some of the most isoform-selective inhibitors of PARP-2 reported to date. Currently, we use structure-based drug design to develop new potent inhibitors of the tankyrases (PARP-5a,5b) in a major project funded by AICR.

Tumour-selective delivery of drugs

In cancer chemotherapy, it is important that the cytotoxic drug acts selectively in the tumour and we have been actively researching selective delivery of cytotoxic drugs for several years. Funded by the Prostate Cancer Charity, we are constructing polymeric prodrugs which release their load of extreme cytotoxins selectively in prostate tumours, through retention by the EPR effect and cleavage by the protease PSA.

Tuberculosis

Building on previous experience in inhibition of dihydrofolate reductase in cancer, we are using structure-based drug design to develop selective inhibitors of this enzyme in Mycobacterium tuberculosis.

Natural products

Collaborating with Aberystwyth University, we identify and profile natural product cinnamates from cultivated grasses, for industrial applications.

Earlier projects

Inhibitors of NOS, sirtuins, Pin1; isotopic synthesis; gene delivery; sulfoximine chemistry; biochemical kinetic isotope effects.

Education/Academic qualification

Doctor of Science, University of Bath

Award Date: 1 Jan 1998

Doctor of Philosophy, University of Cambridge

Award Date: 1 Jan 1981

Master of Arts, University of Cambridge

Award Date: 1 Jan 1978

Education, Durham University

Award Date: 30 Jun 1975

Bachelor of Arts, University of Cambridge

Award Date: 1 Jan 1974

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Projects

Research Output

Derivatives of a PARP inhibitor TIQ-A through synthesis of 8-alkoxythieno[2,3-c]isoquinolin-5(4H)-ones

Maksimainen, M., Nurmesjärvi, A., Terho, R., Threadgill, M., Lehtiö, L. & Heiskanen, J., 2020, In : ACS OMEGA.

Research output: Contribution to journalArticle

PARP10 influences the proliferation of colorectal carcinoma cells, a preliminary study

Wu, C., Xiao, M., Wang, Y., Threadgill, M., Li, M., Tang, Y., Lin, X., Yang, L., Li, Q. & Li, X., 31 Mar 2020, In : Molecular Biology. 54, 2, p. 220-228 9 p.

Research output: Contribution to journalArticle

Open Access
File
2 Downloads (Pure)

Stimulation of insulin secretion by 5-methylcoumarins and its sulfur analogues isolated from Clutia lanceolata Forssk

Ahmed, S., Nur-e-Alam, M., Parveen, I., Coles, S. J., Hafizur, R. M., Hameed, A., Orton, J. B., Threadgill, M. D., Yousaf, M., Alqahtani, A. M. & Al-Rehaily, A. J., 1 Feb 2020, In : Phytochemistry. 170, 112213.

Research output: Contribution to journalArticle

1 Citation (Scopus)

Identification of novel small-molecule inhibitors of α-methylacyl-CoA racemase (AMACR; P504S) and structure-activity relationships

Petrova, Y., Wadda, K., Nathubhai, A., Jevglevskis, M., Mitchell, P., James, T., Threadgill, M., Woodman, T. & Lloyd, M., 1 Nov 2019, In : Bioorganic Chemistry. 92, 103264.

Research output: Contribution to journalArticle

2 Citations (Scopus)

New flavonoids from the Saudi Arabian plant: Retama raetam which stimulates secretion of insulin and inhibits α-glucosidase

Nur-e-Alam, M., Yousaf, M., Parveen, I., Hafizur, R., Ghani, U., Ahmed, S., Hameed, A., Threadgill, M. & Al-Rehaily, A. N., 7 Feb 2019, In : Organic & Biomolecular Chemistry. 17, 5, p. 1266-1276 11 p.

Research output: Contribution to journalArticle

Open Access
File
3 Citations (Scopus)
23 Downloads (Pure)

Thesis

Collected publications, 1982-1997

Author: Threadgill, M. D., 1998

Student thesis: Doctoral ThesisDoctor of Science (DSc)

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