Outputs (48)

In search of effective therapies to overcome resistance to Temozolomide in brain tumours (2019)
Journal Article
Grundy, R., Bouzinab, K., Summers, H., Zhang, J., Stevens, M. F. G., Moody, C. J., …Bradshaw, T. D. (2019). In search of effective therapies to overcome resistance to Temozolomide in brain tumours. Cancer Drug Resistance, 2(4), 1018-1031. https://doi.org/10.20517/cdr.2019.64

Glioblastoma multiforme is the most common and lethal brain tumour-type. The current standard of care includes Temozolomide (TMZ) chemotherapy. However, inherent and acquired resistance to TMZ thwart successful treatment. The direct repair protein me... Read More about In search of effective therapies to overcome resistance to Temozolomide in brain tumours.

Codrug Approach for the Potential Treatment of EML4-ALK Positive Lung Cancer (2019)
Journal Article
Garces, A. E., Al-Hayali, M., Lee, J. B., Li, J., Gershkovich, P., Bradshaw, T. D., & Stocks, M. J. (2020). Codrug Approach for the Potential Treatment of EML4-ALK Positive Lung Cancer. ACS Medicinal Chemistry Letters, 11(3), 316-321. https://doi.org/10.1021/acsmedchemlett.9b00378

We report on the synergistic effect of PI3K inhibition with ALK inhibition for the possible treatment of EML4-ALK positive lung cancer. We have brought together ceritinib (ALK inhibitor) and pictilisib (PI3K inhibitor) into a single bivalent molecule... Read More about Codrug Approach for the Potential Treatment of EML4-ALK Positive Lung Cancer.

Synthesis of folic acid functionalized gold nanoclusters for targeting folate receptor-positive cells (2019)
Journal Article
Liu, Z., Turyanska, L., Zamberlan, F., Pacifico, S., Bradshaw, T. D., Moro, F., …Thomas, N. R. (2019). Synthesis of folic acid functionalized gold nanoclusters for targeting folate receptor-positive cells. Nanotechnology, 30(50), Article 505102. https://doi.org/10.1088/1361-6528/ab437c

We report on the synthesis of water-soluble gold nanoclusters capped with polyethylene glycol (PEG)-based ligands and further functionalized with folic acid for specific cellular uptake. The dihydrolipoic acid-PEG-based ligands terminated with -OMe,... Read More about Synthesis of folic acid functionalized gold nanoclusters for targeting folate receptor-positive cells.

C8-substituted imidazotetrazine analogs overcome temozolomide resistance by inducing DNA adducts and DNA damage (2019)
Journal Article
Yang, Z., Wei, D., Dai, X., Stevens, M. F., Bradshaw, T. D., Luo, Y., & Zhang, J. (2019). C8-substituted imidazotetrazine analogs overcome temozolomide resistance by inducing DNA adducts and DNA damage. Frontiers in Oncology, 9, https://doi.org/10.3389/fonc.2019.00485

Copyright © 2019 Yang, Wei, Dai, Stevens, Bradshaw, Luo and Zhang. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, pro... Read More about C8-substituted imidazotetrazine analogs overcome temozolomide resistance by inducing DNA adducts and DNA damage.

A novel low molecular weight nanocomposite hydrogel formulation for intra-tumoural delivery of anti-cancer drugs (2019)
Journal Article
Štaka, I., Cadete, A., Surikutchi, B. T., Abuzaid, H., Bradshaw, T. D., Alonso, M. J., & Marlow, M. (2019). A novel low molecular weight nanocomposite hydrogel formulation for intra-tumoural delivery of anti-cancer drugs. International Journal of Pharmaceutics, 565, 151-161. https://doi.org/10.1016/j.ijpharm.2019.04.070

Herein, an injectable formulation composed of a low molecular weight gelator (LMWG) based hydrogel and drug-loaded polymeric nanocapsules (NCs) is described. The NCs, made of hyaluronic acid and polyglutamic acid and loaded with C14-Gemcitabine (GEM... Read More about A novel low molecular weight nanocomposite hydrogel formulation for intra-tumoural delivery of anti-cancer drugs.

Cardiac glycoside cerberin exerts anticancer activity through PI3K/AKT/mTOR signal transduction inhibition (2019)
Journal Article
Hossan, M. S., Chan, Z. Y., Collins, H. M., Shipton, F. N., Butler, M. S., Rahmatullah, M., …Bradshaw, T. D. (2019). Cardiac glycoside cerberin exerts anticancer activity through PI3K/AKT/mTOR signal transduction inhibition. Cancer Letters, 453, 57-73. https://doi.org/10.1016/j.canlet.2019.03.034

Natural products possess a significant role in anticancer therapy and many currently-used anticancer drugs are of natural origin. Cerberin (CR), a cardenolide isolated from the fruit kernel of Cerbera odollam, was found to potently inhibit cancer cel... Read More about Cardiac glycoside cerberin exerts anticancer activity through PI3K/AKT/mTOR signal transduction inhibition.

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, 2(4), 1-7. https://doi.org/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 about Development of novel apoferritin formulations for antitumour benzothiazoles.

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. https://doi.org/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 about Cytotoxic potential of ethanol extract of Parquetina nigrescens on MCF-7, C4-2WT, HT 29 and HTC 116 cell lines.

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. https://doi.org/10.1016/j.jconrel.2018.07.022

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 about Lipophilic activated ester prodrug approach for drug delivery to the intestinal lymphatic system.

Sustainable Syntheses of (-)-Jerantinines A & e and Structural Characterisation of the Jerantinine-Tubulin Complex at the Colchicine Binding Site (2018)
Journal Article
Smedley, C. J., Stanley, P. A., Qazzaz, M. E., Prota, A. E., Olieric, N., Collins, H., …Moses, J. E. (2018). Sustainable Syntheses of (-)-Jerantinines A & e and Structural Characterisation of the Jerantinine-Tubulin Complex at the Colchicine Binding Site. Scientific Reports, 8(1), Article 10617. https://doi.org/10.1038/s41598-018-28880-2

The jerantinine family of Aspidosperma indole alkaloids from Tabernaemontana corymbosa are potent microtubule-targeting agents with broad spectrum anticancer activity. The natural supply of these precious metabolites has been significantly disrupted... Read More about Sustainable Syntheses of (-)-Jerantinines A & e and Structural Characterisation of the Jerantinine-Tubulin Complex at the Colchicine Binding Site.