Research Repository

See what's under the surface


Development of novel apoferritin formulations for antitumour benzothiazoles (2019)
Journal Article
Breen, A. F., Wells, G., Turyanska, L., & Bradshaw, T. D. (2019). Development of novel apoferritin formulations for antitumour benzothiazoles. Cancer Reports, 1-7. doi:10.1002/cnr2.1155

Background The benzothiazole structure is important in medicinal chemistry, and 5‐fluoro‐2‐(3,4‐dimethoxyphenyl) benzothiazole (GW 610) is of particular interest as it shows outstanding anticancer activity in sensitive breast and colorectal carcinom... Read More

Autophagy modulation: a prudent approach in cancer treatment? (2018)
Journal Article
Bishop, E., & Bradshaw, T. D. (2018). Autophagy modulation: a prudent approach in cancer treatment?. Cancer Chemotherapy and Pharmacology, doi:10.1007/s00280-018-3669-6. ISSN 0344-5704

Autophagy is a tightly controlled process comprising lysosomal degradation and recycling of cellular proteins and organelles. In cancer, its paradoxical dual role of cytoprotection and cytotoxicity is context-dependent and controversial. Autophagy pr... Read More

Cytotoxic potential of ethanol extract of Parquetina nigrescens on MCF-7, C4-2WT, HT 29 and HTC 116 cell lines (2018)
Journal Article
M. Onyegeme-Okerenta, B., Agyare, C., D. Bradshaw, T., & A. Spriggs, K. (2018). Cytotoxic potential of ethanol extract of Parquetina nigrescens on MCF-7, C4-2WT, HT 29 and HTC 116 cell lines. African journal of pharmacy and pharmacology, 12(23), 310-318. doi:10.5897/ajpp2018.4947

The cytotoxic activity of ethanol extract of Parquetina nigrescen was investigated using a (3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, methylene blue and Trypan Blue exclusion assay on four human cancer cell lines, MCF... Read More

Lipophilic activated ester prodrug approach for drug delivery to the intestinal lymphatic system (2018)
Journal Article
Lee, J. B., Zgair, A., Malec, J., Kim, T. H., Kim, M. G., Ali, J., …Gershkovich, P. (2018). Lipophilic activated ester prodrug approach for drug delivery to the intestinal lymphatic system. Journal of Controlled Release, 286, (10-19). doi:10.1016/j.jconrel.2018.07.022. ISSN 0168-3659

The intestinal lymphatic system plays an important role in the pathophysiology of multiple diseases including lymphomas, cancer metastasis, autoimmune diseases, and human immunodeficiency virus (HIV) infection. It is thus an important compartment for... Read More

Nucleoside based self-assembling drugs for localized drug delivery (2018)
Journal Article
Skilling, K. J., Stocks, M. J., Kellam, B., Ashford, M., Bradshaw, T., Burroughs, L., & Marlow, M. (in press). Nucleoside based self-assembling drugs for localized drug delivery. ChemMedChem, doi:10.1002/cmdc.201800063. ISSN 1860-7179

We have synthesized a range of gelators based on nucleoside analogues gemcitabine and lamivudine, characterizing representative gels from the series using rheology and TEM. Growth inhibition studies of gemcitabine derivatives confirmed the feasibilit... Read More

Synthesis of highly substituted 1,2-diazetidin-3-ones, small ring scaffolds for drug discovery (2018)
Journal Article
Santos, M. S., Nortcliffe, A., Lewis, W., Bradshaw, T. D., & Moody, C. J. (in press). Synthesis of highly substituted 1,2-diazetidin-3-ones, small ring scaffolds for drug discovery. Chemistry - A European Journal, doi:10.1002/chem.201801309. ISSN 0947-6539

1,2-Diazetidin-3-ones are readily accessible, small ring scaffolds that upon functionalization have the potential to produce diverse 3-dimensional structures for drug discovery. Thus treatment of diazo hydrazides, obtained from simple hydrazides and... Read More

Self-assembling benzothiazole-based gelators: a mechanistic understanding of in vitro bioactivation and gelation (2018)
Journal Article
Citossi, F., Smith, T., Lee, J. B., Segal, J., Gershkovich, P., Stocks, M. J., …Marlow, M. (in press). Self-assembling benzothiazole-based gelators: a mechanistic understanding of in vitro bioactivation and gelation. Molecular Pharmaceutics, 15(4), doi:10.1021/acs.molpharmaceut.7b01106

Low molecular weight gelators (LMWGs) of chemotherapeutic drugs represent a valid alternative to the existing poly-mer-based formulations used for targeted delivery of anticancer drugs. Herein we report the design and development of novel self-assemb... Read More

Temozolomide analog PMX 465 downregulates MGMT expression in HCT116 colorectal carcinoma cells (2018)
Journal Article
Yang, Z., Wei, D., Liu, F., Liu, J., Wu, X., Stevens, M. F. G., …Zhang, J. (in press). Temozolomide analog PMX 465 downregulates MGMT expression in HCT116 colorectal carcinoma cells. Journal of Cellular Biochemistry, doi:10.1002/jcb.26674. ISSN 0730-2312

The efficacy of temozolomide (TMZ) treatment for cancers is currently limited by inherent or the development of resistance, particularly, but not exclusively, due to the expression of the DNA repair enzyme O6-methylguanine-DNA methyltransferase (MGMT... Read More

Cellular pharmacology studies of anticancer agents: recommendations from the EORTC-PAMM group (2017)
Journal Article
Perego, P., Hempel, G., Linder, S., Bradshaw, T. D., Larsen, A. K., Peters, G. J., & Phillips, R. M. (in press). Cellular pharmacology studies of anticancer agents: recommendations from the EORTC-PAMM group. Cancer Chemotherapy and Pharmacology, doi:10.1007/s00280-017-3502-7. ISSN 0344-5704

An increasing number of manuscripts focus on the in vitro evaluation of established and novel anti-tumour agents in experimental models. Whilst the design of such in vitro assays is inherently flexible, some of these studies lack the minimum informat... Read More

Development of a series of bis-triazoles as G-quadruplex ligands (2017)
Journal Article
Saleh, M., Laughton, C. A., Bradshaw, T. D., & Moody, C. J. (in press). Development of a series of bis-triazoles as G-quadruplex ligands. RSC Advances, 7, doi:10.1039/c7ra07257k

Maintenance of telomeres – specialized complexes that protect the ends of chromosomes – is provided by the enzyme complex telomerase, which is a key factor that is activated in more than 80% of cancer cells, but absent in most normal cells. Targeting... Read More

Jerantinine A induces tumor-specific cell death through modulation of splicing factor 3b subunit 1 (SF3B1) (2017)
Journal Article
Chung, F. F., Tan, P. F. T. M., Raja, V. J., Tan, B., Lim, K., Kam, T., …Leong, C. (2017). Jerantinine A induces tumor-specific cell death through modulation of splicing factor 3b subunit 1 (SF3B1). Scientific Reports, 7(42504), doi:10.1038/srep42504. ISSN 2045-2322

Precursor mRNA (pre-mRNA) splicing is catalyzed by a large ribonucleoprotein complex known as the spliceosome. Numerous studies have indicated that aberrant splicing patterns or mutations in spliceosome components, including the splicing factor 3b su... Read More

Using titanium complexes to defeat cancer: the view from the shoulders of titans (2017)
Journal Article
Cini, M., Bradshaw, T. D., & Woodward, S. (in press). Using titanium complexes to defeat cancer: the view from the shoulders of titans. Chemical Society Reviews, doi:10.1039/C6CS00860G. ISSN 0306-0012

When the first titanium complex with anticancer activity was identified in the 1970s, it was attractive, based on the presence of the dichloride unit in TiCl2Cp2 (Cp = η-C5H5)2, to assume its mode of biological action was closely aligned with cisplat... Read More

Developing a self-healing supramolecular nucleoside hydrogel (2016)
Journal Article
Skilling, K. J., Kellam, B., Ashford, M., Bradshaw, T. D., & Marlow, M. (in press). Developing a self-healing supramolecular nucleoside hydrogel. Soft Matter, doi:10.1039/C6SM01779G. ISSN 1744-683X

Low molecular weight gelator hydrogels provide a viable alternative to traditional polymer based drug delivery platforms, owing to their tunable stability and in most cases inherent biocompatibility. Here we report the first self-healing nucleoside h... Read More