Browsing Cancer Therapeutics by title
Now showing items 232-251 of 657
-
Endosialin expression in soft tissue sarcoma as a potential marker of undifferentiated mesenchymal cells.
(NATURE PUBLISHING GROUP, 2016-08-09)BACKGROUND: Soft tissue sarcomas are a group of neoplasms with differentiation towards mesenchymal tissue, many of which are aggressive and chemotherapy resistant. Histology and immunoprofiles often overlap with neoplasms ... -
Enhancer invasion shapes MYCN-dependent transcriptional amplification in neuroblastoma.
(NATURE PUBLISHING GROUP, 2018-04-01)Amplification of the locus encoding the oncogenic transcription factor MYCN is a defining feature of high-risk neuroblastoma. Here we present the first dynamic chromatin and transcriptional landscape of MYCN perturbation ... -
EpCAMhigh and EpCAMlow circulating tumor cells in metastatic prostate and breast cancer patients.
(Impact Journals, LLC, 2018-11-02)The presence of high expressing epithelial cell adhesion molecule (EpCAMhigh) circulating tumor cells (CTC) enumerated by CellSearch® in blood of cancer patients is strongly associated with poor prognosis. This raises the ... -
Epigenetically defined therapeutic targeting in H3.3G34R/V high-grade gliomas.
(AMER ASSOC ADVANCEMENT SCIENCE, 2021-10-13)High-grade gliomas with arginine or valine substitutions of the histone H3.3 glycine-34 residue (H3.3G34R/V) carry a dismal prognosis, and current treatments, including radiotherapy and chemotherapy, are not curative. ... -
Epigenome-wide association study of body mass index, and the adverse outcomes of adiposity
(Springer Science and Business Media LLC, 2017-01-01)Approximately 1.5 billion people worldwide are overweight or affected by obesity, and are at risk of developing type (2) diabetes, cardiovascular disease and related metabolic and inflammatory disturbances(1,2). Although ... -
The era of high-quality chemical probes.
(ROYAL SOC CHEMISTRY, 2022-12-14)Small-molecule chemical probes are among the most important tools to study the function of proteins in cells and organisms. Regrettably, the use of weak and non-selective small molecules has generated an abundance of ... -
Evaluating Imaging Biomarkers of Acquired Resistance to Targeted EGFR Therapy in Xenograft Models of Human Head and Neck Squamous Cell Carcinoma.
(FRONTIERS MEDIA SA, 2018-07-23)Background: Overexpression of EGFR is a negative prognostic factor in head and neck squamous cell carcinoma (HNSCC). Patients with HNSCC who respond to EGFR-targeted tyrosine kinase inhibitors (TKIs) eventually develop ... -
Evaluation of a novel antibody to define histone 3.3 G34R mutant brain tumours.
(BMC, 2017-06-06)Missense somatic mutations affecting histone H3.1 and H3.3 proteins are now accepted as the hallmark of paediatric diffuse intrinsic pontine gliomas (DIPG), non-brain stem paediatric high grade gliomas (pHGG) as well as a ... -
Evaluation of APOBEC3B Recognition Motifs by NMR Reveals Preferred Substrates.
(AMER CHEMICAL SOC, 2018-09-21)APOBEC3B (A3B) deamination activity on ssDNA is considered a contributing factor to tumor heterogeneity and drug resistance in a number of human cancers. Despite its clinical impact, little is known about A3B ssDNA substrate ... -
Evaluation of DFO-HOPO as an octadentate chelator for zirconium-89.
(ROYAL SOC CHEMISTRY, 2017-07-27)The future of 89Zr-based immuno-PET is reliant upon the development of new chelators with improved stability compared to the currently used deferoxamine (DFO). Herein, we report the evaluation of the octadentate molecule ... -
Evaluation of the combination of the dual m-TORC1/2 inhibitor vistusertib (AZD2014) and paclitaxel in ovarian cancer models.
(IMPACT JOURNALS LLC, 2017-12-26)Activation of the PI3K/mTOR pathway has been shown to be correlated with resistance to chemotherapy in ovarian cancer. We aimed to investigate the effects of combining inhibition of mTORC1 and 2 using the mTOR kinase ... -
Evaluation of the Response of Intracranial Xenografts to VEGF Signaling Inhibition Using Multiparametric MRI.
(ELSEVIER SCIENCE INC, 2017-09-01)Vascular endothelial growth factor A (VEGF-A) is considered one of the most important factors in tumor angiogenesis, and consequently, a number of therapeutics have been developed to inhibit VEGF signaling. Therapeutic ... -
Evolution of kinase polypharmacology across HSP90 drug discovery.
(CELL PRESS, 2021-10-21)Most small molecules interact with several target proteins but this polypharmacology is seldom comprehensively investigated or explicitly exploited during drug discovery. Here, we use computational and experimental methods ... -
Expanding Chemical Probe Space: Quality Criteria for Covalent and Degrader Probes.
(AMER CHEMICAL SOC, 2023-07-27)Within druggable target space, new small-molecule modalities, particularly covalent inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists. Molecules with such modes of action have a large ... -
Exploiting evolutionary steering to induce collateral drug sensitivity in cancer.
(NATURE PORTFOLIO, 2020-04-21)Drug resistance mediated by clonal evolution is arguably the biggest problem in cancer therapy today. However, evolving resistance to one drug may come at a cost of decreased fecundity or increased sensitivity to another ... -
Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70.
(AMER CHEMICAL SOC, 2016-05-26)HSP70 is a molecular chaperone and a key component of the heat-shock response. Because of its proposed importance in oncology, this protein has become a popular target for drug discovery, efforts which have as yet brought ... -
Exploiting the CRL4-CRBM E3 ubiquitin ligase complex for the development of iTAG: a versatile targeted protein degradation system to enable functional evaluation and target validation
(Institute of Cancer Research (University Of London), 2022-02-28)Modulating target protein expression to probe for its relevance and function in a disease is critical in the drug discovery process of target validation. Current genetic methods and chemico-biology tools are widely employed ... -
Exploring an oncolytic virus triggered PD-L1 response via immunoPET
(Institute of Cancer Research (University Of London), 2023-01-23)Oncolytic virotherapy (OV) exploits viruses which preferentially infect and kill cancerous cells. Moreover, oncolytic viruses stimulate the tumour-immune microenvironment towards an inflammatory phenotype. Therefore, OV ... -
Expression and clinical association of programmed cell death-1, programmed death-ligand-1 and CD8+ lymphocytes in primary sarcomas is subtype dependent.
(IMPACT JOURNALS LLC, 2017-07-07)In order to explore the potential of immune checkpoint blockade in sarcoma, we investigated expression and clinical relevance of programmed cell death-1 (PD-1), programmed death ligand-1 (PD-L1) and CD8 in tumors of 208 ...