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New Treatments in Renal Cancer: The AhR Ligands (2020)
Journal Article
Turyanska, L., Itkin, B., Breen, A., Loaiza-Perez, A. I., Sandes, E. O., & Bradshaw, T. D. (2020). New Treatments in Renal Cancer: The AhR Ligands. International Journal of Molecular Sciences, 21(10), https://doi.org/10.3390/ijms21103551

Kidney cancer rapidly acquires resistance to antiangiogenic agents, such as sunitinib, developing an aggressive migratory phenotype (facilitated by c-Metsignal transduction). The Aryl hydrocarbon receptor (AhR) has recently been postulated as a molec... Read More about New Treatments in Renal Cancer: The AhR Ligands.

Delivery of temozolomide and N3-propargyl analog to brain tumors using an apoferritin nanocage (2020)
Journal Article
Bouzinab, K., Summers, H., Stevens, M. F., Moody, C. J., Thomas, N. R., Gershkovich, P., …Turyanska, L. (2020). Delivery of temozolomide and N3-propargyl analog to brain tumors using an apoferritin nanocage. ACS Applied Materials and Interfaces, 12(11), 12609-12617. https://doi.org/10.1021/acsami.0c01514

Glioblastoma multiforme (GBM) is a grade IV astrocytoma, which is the most aggressive form of brain tumor. The standard of care for this disease includes surgery, radiotherapy and temozolomide (TMZ) chemotherapy. Poor accumulation of TMZ at the tumor... Read More about Delivery of temozolomide and N3-propargyl analog to brain tumors using an apoferritin nanocage.

Protein Encapsulation of Experimental Anticancer Agents 5F 203 and Phortress: Towards Precision Drug Delivery (2019)
Journal Article
Breen, A. F., Scurr, D., Cassioli, M. L., Wells, G., Thomas, N. R., Zhang, J., …Bradshaw, T. D. (2019). Protein Encapsulation of Experimental Anticancer Agents 5F 203 and Phortress: Towards Precision Drug Delivery. International Journal of Nanomedicine, 14, 9525-9534. https://doi.org/10.2147/IJN.S226293

Introduction: Advancment of novel anticancer drugs into clinic is frequently halted by their lack of solubility, reduced stability under physiological conditions, and non-specific uptake by normal tissues, causing systemic toxicity. Their progress to... Read More about Protein Encapsulation of Experimental Anticancer Agents 5F 203 and Phortress: Towards Precision Drug Delivery.

Apoferritin encapsulation of cysteine protease inhibitors for cathepsin L inhibition in cancer cells (2019)
Journal Article
Quilles Junior, J. C., Bradshaw, T. D., Turyanska, L., Carlos, F. D. R. R., Montanari, A., Leitão, A., …Bradshaw, T. D. (2019). Apoferritin encapsulation of cysteine protease inhibitors for cathepsin L inhibition in cancer cells. RSC Advances, 9(63), 36699-36706. https://doi.org/10.1039/c9ra07161j

Cysteine proteases play a key role in tumorigenesis causing protein degradation and promoting invasive tumour growth. Cathepsin L is overexpressed in cancer cells and could provide a specific target for delivery of anticancer agents. We encapsulated... Read More about Apoferritin encapsulation of cysteine protease inhibitors for cathepsin L inhibition in cancer cells.

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, 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), 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.

Tripodal O-N-O bis-Phenolato Amine Titanium(IV) Complexes Show High In Vitro Anti-Cancer Activity (2019)
Journal Article
Abid, M., Nouch, R., Bradshaw, T. D., Lewis, W., & Woodward, S. (2019). Tripodal O-N-O bis-Phenolato Amine Titanium(IV) Complexes Show High In Vitro Anti-Cancer Activity. European Journal of Inorganic Chemistry, doi:10.1002/ejic.201900510

The octahedral titanium(IV) complexes trans,mer‐[Ti{R3N(CH2C6H2‐2‐O‐4‐R2‐6‐R1)2}2] (R1 = Me, OMe, Cl; R2 = Me, OMe, F, Cl; R3 = Me, Et; not all combinations) are synthesised in two steps from simple phenols in 36‐53% overall yield. The highly crystal... Read More about Tripodal O-N-O bis-Phenolato Amine Titanium(IV) Complexes Show High In Vitro Anti-Cancer Activity.

Listeria innocua Dps as a nanoplatform for bioluminescence based photodynamic therapy utilizing Gaussia princeps luciferase and zinc protoporphyrin IX (2019)
Journal Article
Al-Ani, A. W., Zhang, L., Ferreira, L., Turyanska, L., Bradshaw, T. D., & Thomas, N. R. (2019). Listeria innocua Dps as a nanoplatform for bioluminescence based photodynamic therapy utilizing Gaussia princeps luciferase and zinc protoporphyrin IX. Nanomedicine: Nanotechnology, Biology and Medicine, 20, https://doi.org/10.1016/j.nano.2019.04.008

Listeria innocua DNA binding protein from starved cells (LiDps) belongs to the ferritin family and provides a promising self-assembling spherical 12-mer protein scaffold for the generation of functional nanomaterials. We report the creation of a Gaus... Read More about Listeria innocua Dps as a nanoplatform for bioluminescence based photodynamic therapy utilizing Gaussia princeps luciferase and zinc protoporphyrin IX.

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. doi: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.

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, https://doi.org/10.1007/s00280-018-3669-6

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 about Autophagy modulation: a prudent approach in cancer treatment?.

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 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. 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.

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

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 about Nucleoside based self-assembling drugs for localized drug delivery.

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

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 about Synthesis of highly substituted 1,2-diazetidin-3-ones, small ring scaffolds for drug discovery.

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 about Self-assembling benzothiazole-based gelators: a mechanistic understanding of in vitro bioactivation and gelation.


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