Browsing Cancer Therapeutics by title
Now showing items 165-184 of 658
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Defining variant-resistant epitopes targeted by SARS-CoV-2 antibodies: A global consortium study.
(AMER ASSOC ADVANCEMENT SCIENCE, 2021-10-22)Antibody-based therapeutics and vaccines are essential to combat COVID-19 morbidity and mortality after severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection. Multiple mutations in SARS-CoV-2 that could ... -
Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).
(AMER CHEMICAL SOC, 2018-02-08)Demonstrating intracellular protein target engagement is an essential step in the development and progression of new chemical probes and potential small molecule therapeutics. However, this can be particularly challenging ... -
Deregulated expression of HDAC9 in B cells promotes development of lymphoproliferative disease and lymphoma in mice.
(COMPANY BIOLOGISTS LTD, 2016-12-01)Histone deacetylase 9 (HDAC9) is expressed in B cells, and its overexpression has been observed in B-lymphoproliferative disorders, including B-cell non-Hodgkin lymphoma (B-NHL). We examined HDAC9 protein expression and ... -
Design and synthesis of bifunctional molecules for directing phosphorylation
(Institute of Cancer Research (University Of London), 2023-05-04)The field of bifunctional molecules such as PROTAC, DUBTAC and PhoRC has demonstrated that inducing proximity between two protein complexes is sufficient to redirect post-translational modifications (PTMs), and effect ... -
Design and synthesis of dual kinase-bromodomain inhibitors targeting ALK and BRD4
(Institute of Cancer Research (University Of London), 2019-12-31)Neuroblastoma is a paediatric cancer of neural crest origin and is the most common extracranial tumour in childhood. In high-risk patients with poor clinical outcome, mutations within the kinase domain of anaplastic lymphoma ... -
Design, Synthesis and Characterization of Covalent KDM5 Inhibitors.
(WILEY-V C H VERLAG GMBH, 2019-01-08)Histone lysine demethylases (KDMs) are involved in the dynamic regulation of gene expression and they play a critical role in several biological processes. Achieving selectivity over the different KDMs has been a major ... -
Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity.
(AMER CHEMICAL SOC, 2019-03)Concomitant inhibition of anaplastic lymphoma kinase (ALK) and bromodomain-4 (BRD4) is a potential therapeutic strategy for targeting two key oncogenic drivers that co-segregate in a significant fraction of high-risk ... -
Desmoplastic small round cell tumor (DSRCT): emerging therapeutic targets and future directions for potential therapies.
(TAYLOR & FRANCIS LTD, 2020-04-02) -
Detecting repeated cancer evolution from multi-region tumor sequencing data.
(NATURE PUBLISHING GROUP, 2018-08-31)Recurrent successions of genomic changes, both within and between patients, reflect repeated evolutionary processes that are valuable for the anticipation of cancer progression. Multi-region sequencing allows the temporal ... -
Detection of avascular necrosis on routine diffusion-weighted whole body MRI in patients with multiple myeloma.
(BRITISH INST RADIOLOGY, 2019-01-01)OBJECTIVE: Current therapies for multiple myeloma, which include corticosteroids, increase risk of avascular necrosis. The aim of this study was to assess incidental detection of femoral head avascular necrosis on routine ... -
Detection of circulating tumour cell clusters in human glioblastoma.
(NATURE PUBLISHING GROUP, 2018-08-14)Human glioblastoma (GBM) is a highly aggressive, invasive and hypervascularised malignant brain cancer. Individual circulating tumour cells (CTCs) are sporadically found in GBM patients, yet it is unclear whether multicellular ... -
Detection of the prodrug-activating enzyme carboxypeptidase G2 activity with chemical exchange saturation transfer magnetic resonance.
(SPRINGER, 2014-04-01)PURPOSE: The purpose of this study is to evaluate if the differential exchange rates with bulk water between amine and amide protons can be exploited using chemical exchange saturation transfer magnetic resonance (CEST-MR) ... -
Determination of Ligand-Binding Affinity (Kd) Using Transverse Relaxation Rate (R2) in the Ligand-Observed 1H NMR Experiment and Applications to Fragment-Based Drug Discovery.
(AMER CHEMICAL SOC, 2023-08-10)High hit rates from initial ligand-observed NMR screening can make it challenging to prioritize which hits to follow up, especially in cases where there are no available crystal structures of these hits bound to the target ... -
Developing RAS-binding antibody-derived hit compounds
(Institute of Cancer Research (University Of London), 2023-09-27) -
Development and validation of a LC-MS/MS method for the quantification of the checkpoint kinase 1 inhibitor SRA737 in human plasma.
(FUTURE SCI LTD, 2017-07-01)AIM: SRA737 is an orally active small-molecule inhibitor of checkpoint kinase 1 being investigated in an oncology setting. A HPLC-MS/MS method for quantifying plasma concentrations of SRA737 was validated. METHODS & RESULTS: ... -
Development and Validation of a New BAG-1L-Specific Antibody to Quantify BAG-1L Protein Expression in Advanced Prostate Cancer.
(ELSEVIER SCIENCE INC, 2023-08-29)BCL-2-associated athanogene-1L (BAG-1L) is a critical co-regulator that binds to and enhances the transactivation function of the androgen receptor, leading to prostate cancer development and progression. Studies investigating ... -
Development of a cell-free split-luciferase biochemical assay as a tool for screening for inhibitors of challenging protein-protein interaction targets.
(F1000 Research Ltd, 2020-01-01)Targeting the interaction of proteins with weak binding affinities or low solubility represents a particular challenge for drug screening. The NanoLuc â ® Binary Technology (NanoBiT â ®) was originally developed to detect ... -
Development of a Structured Query Language and Natural Language Processing Algorithm to Identify Lung Nodules in a Cancer Centre.
(FRONTIERS MEDIA SA, 2021-11-04)Importance: The stratification of indeterminate lung nodules is a growing problem, but the burden of lung nodules on healthcare services is not well-described. Manual service evaluation and research cohort curation can be ... -
Development of Bag-1L as a therapeutic target in androgen receptor-dependent prostate cancer.
(ELIFE SCIENCES PUBLICATIONS LTD, 2017-08-10)Targeting the activation function-1 (AF-1) domain located in the N-terminus of the androgen receptor (AR) is an attractive therapeutic alternative to the current approaches to inhibit AR action in prostate cancer (PCa). ... -
Development of Molecularly Targeted Agents and Immunotherapies in Glioblastoma: A Personalized Approach.
(SAGE PUBLICATIONS LTD, 2018-02-26)Over the past decade, precision cancer medicine has driven major advances in the management of advanced solid tumours with the identification and targeting of putative driver aberrations transforming the clinical outcomes ...