A5084095542- Cancer therapeutics and mechanisms
- Pharmacogenetics and Drug Metabolism
- Cancer, Hypoxia, and Metabolism
- Chemical Reactions and Isotopes
- Chemical Synthesis and Analysis
- Colorectal Cancer Treatments and Studies
- Lung Cancer Treatments and Mutations
- Synthesis and Biological Evaluation
- Epigenetics and DNA Methylation
- Prostate Cancer Treatment and Research
- Bioactive Compounds and Antitumor Agents
- Cancer Treatment and Pharmacology
- Cancer, Lipids, and Metabolism
- DNA Repair Mechanisms
- Drug Transport and Resistance Mechanisms
- Aldose Reductase and Taurine
- Cancer Cells and Metastasis
- Metabolomics and Mass Spectrometry Studies
- Synthesis and Catalytic Reactions
- Computational Drug Discovery Methods
- Synthesis and biological activity
- Click Chemistry and Applications
- Microbial Natural Products and Biosynthesis
- Nanoparticle-Based Drug Delivery
- Phytochemistry and biological activity of medicinal plants
University of Bradford
2015-2024
University of Michigan
2021
West Yorkshire Police
2019
Karolinska Institutet
2013
University of East Anglia
2012
Durham University
2012
Stockholm University
2007
Cardiff University
2005-2006
University of London
2003-2006
University College London
2004-2006
Abstract There are hundreds of ligands which can interact with G-quadruplex DNA, yet very few target i-motif. To appreciate an understanding between the dynamics these structures and how they be affected by intervention small molecule ligands, more i-motif binding compounds required. Herein we describe drug mitoxantrone bind, induce folding stabilise forming DNA sequences, even at physiological pH. Additionally, was found to bind sequences preferentially over double helical DNA. We also...
Abstract Polysialic acid (polySia) is a unique carbohydrate polymer expressed on the surface of NCAM (neuronal cell adhesion molecule) in number cancers where it modulates cell-cell and cell-matrix adhesion, migration, invasion metastasis strongly associated with poor clinical prognosis. We have carried out first investigation into effect polySia expression behaviour cancer cells hypoxia, key source chemoresistance tumours. The role polysialylation tumour migration were studied along effects...
AKR1C3 is an enzyme that overexpressed in several types of radiotherapy- and chemotherapy-resistant cancers. Despite a validated target for drug development, no inhibitor has been approved clinical use. In this manuscript, we describe our study new series potent AKR1C3-targeting 3-hydroxybenzoisoxazole based inhibitors display high selectivity over the AKR1C2 isoform low micromolar activity inhibiting 22Rv1 prostate cancer cell proliferation. silico studies suggested proper substituents to...
Cytochrome P450 2W1 (CYP2W1) is a monooxygenase detected in 30% of colon cancers, whereas its expression nontransformed adult tissues absent, rendering it tumor-specific drug target for development novel cancer chemotherapy. Previously, we have identified duocarmycin synthetic derivatives as CYP2W1 substrates. In this study, investigated whether two these compounds, ICT2705 and ICT2706, could be activated by into potent antitumor agents.The cytotoxic activity ICT2706 vitro was tested cell...
Chemerin is an adipokine involved in inflammation, adipogenesis, angiogenesis and energy metabolism, has been hypothesized as a link between obesity type II diabetes. In humans affected by obesity, chemerin gene expression peripheral tissues circulating levels are elevated. mice, plasma of upregulated high-fat feeding gain loss function studies show association with body weight, food intake glucose homeostasis. Therefore, important blood-borne mediator that, amongst its other functions,...
Mitoxantrone (MTX) is a drug employed in breast cancer treatment, but its application largely limited due to side effects. A controlled delivery approach can potentially reduce the In this study, two zirconium (Zr)-based MOFs, UiO-66 and UiO-66-NH2, were studied for more of MTX with 40% 21% loading capacity, respectively. Characterisation via powder X-ray diffraction, thermogravimetric analysis, Fourier transform infrared spectrometry, scanning electron microscopy, dynamic light scattering...
The identification of an agent that is selectively activated by a cytochrome P450 (CYP) has the potential for tissue specific dose intensification as means significantly improving its therapeutic value. Towards this goal, we disclose evidence pathway activation duocarmycin analogue, ICT2700, which targets CYP1A1 biological activity.
We identify cytochrome P450 1A1 (CYP1A1) as a target for tumor-selective drug development in bladder cancer and describe the characterization of ICT2700, designed to be metabolized from prodrug potent cytotoxin selectively by CYP1A1. Elevated CYP1A1 expression was shown human relative normal tissues. RT112 cells, endogenously expressing CYP1A1, were chemosensitive whereas EJ138 cells that do not express significantly less responsive. Introduction into resulted 75-fold increased...
Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer and considered a potential target for therapeutic intervention. 4-(Diethylamino)benzaldehyde (DEAB) has been extensively reported as pan-inhibitor of ALDH isoforms, here, we report on the synthesis, isoform selectivity, cellular potencies cells 40 DEAB analogues; three analogues (14, 15, 16) showed potent inhibitory activity against ALDH1A3, two (18 19) ALDH3A1. Significantly, 16 displayed...
A library of duocarmycin bioprecursors based on the CPI and CBI scaffolds was synthesized used to probe selective activation by cells expressing CYP1A1 2W1, CYPs known be expressed in high frequency some tumors. Several CPI-based compounds were pM-nM potent cells. CYP2W1 also shown sensitize proliferating several compounds, demonstrating its potential as a target for tumor bioprecursors.
Cytochrome P450 (CYP) is one of the most important drug-metabolizing enzyme families, which participates in biotransformation many endogenous and exogenous compounds. Quantitative analysis CYP expression levels when studying efficacy new drug molecules assessing drug-drug interactions development. At present, chemical probe-based assay widely used approach for evaluation activity although there are cross-reactions between isoforms with high sequence homologies. Therefore, quantification each...
A novel series of 1,4-disubstituted chloroethylaminoanthraquinones, containing alkylating chloroethylamino functionalities as part a rigid piperidinyl or pyrrolidinyl ring-system, have been prepared. The target compounds were prepared by ipso-displacement halides various anthraquinone chromophores either hydroxylated chlorinated piperidinyl- pyrrolidinyl-alkylamino side chains. chloroethylaminoanthraquinones shown to alkylate guanine residues linearized pBR322 (1−20 μM), and two...
Deacetylcolchicine was reacted with substituted benzyl halides to provide a library of compounds for biological analysis. Compound 7 (3,4-difluorobenzyl-N-aminocolchicine) shown possess cytotoxicity in cancer cell lines the low nanomolar range. Significantly, it showed no loss activity resistant A2780AD ovarian carcinoma line known overexpress ABCB1 drug transporter and also unaffected by overexpression class III β-tubulin HeLa transfected cells.
The Journal of Cancer Metastasis and Treatment is an open access journal focused on cancer metastasis treatment, including the occurrence, development, progression, metastasis, treatment oncologic disease. It covers basic, translational clinical research related to cell biology, genomics, precision medicine, oncology internal radiotherapy radiology, obstetrics gynecology, pediatrics, surgery, hematology, neurooncology, etc.
The Journal of Cancer Metastasis and Treatment is an open access journal focused on cancer metastasis treatment, including the occurrence, development, progression, metastasis, treatment oncologic disease. It covers basic, translational clinical research related to cell biology, genomics, precision medicine, oncology internal radiotherapy radiology, obstetrics gynecology, pediatrics, surgery, hematology, neurooncology, etc.