Browsing Cancer Therapeutics by title
Now showing items 375-394 of 647
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Low expression of hexokinase-2 is associated with false-negative FDG-positron emission tomography in multiple myeloma.
(AMER SOC HEMATOLOGY, 2017-07-06)18F-Fluorodeoxyglucose (FDG)-positron emission tomography (PET) and diffusion-weighted magnetic resonance imaging with background signal suppression (DWIBS) are 2 powerful functional imaging modalities in the evaluation ... -
Lysine-targeting covalent inhibitors
(Institute of Cancer Research (University Of London), 2023-12-14)Targeted Covalent Inhibitors (TCIs) represent an increasingly important strategy in modern drug discovery. TCIs exploit high affinity, reversible ligands which are then modified with modestly-reactive electrophilic warheads ... -
Lysine-Targeting Covalent Inhibitors.
(WILEY-V C H VERLAG GMBH, 2017-11-27)Targeted covalent inhibitors have gained widespread attention in drug discovery as a validated method to circumvent acquired resistance in oncology. This strategy exploits small-molecule/protein crystal structures to design ... -
Lysyl oxidase drives tumour progression by trapping EGF receptors at the cell surface.
(NATURE PUBLISHING GROUP, 2017-04-18)Lysyl oxidase (LOX) remodels the tumour microenvironment by cross-linking the extracellular matrix. LOX overexpression is associated with poor cancer outcomes. Here, we find that LOX regulates the epidermal growth factor ... -
Macrophage-Derived IL1β and TNFα Regulate Arginine Metabolism in Neuroblastoma.
(AMER ASSOC CANCER RESEARCH, 2019-02-01)Neuroblastoma is the most common childhood solid tumor, yet the prognosis for high-risk disease remains poor. We demonstrate here that arginase 2 (ARG2) drives neuroblastoma cell proliferation via regulation of arginine ... -
MAP4K4 Inhibition Promotes Survival of Human Stem Cell-Derived Cardiomyocytes and Reduces Infarct Size In Vivo.
(CELL PRESS, 2019-04-04)Heart disease is a paramount cause of global death and disability. Although cardiomyocyte death plays a causal role and its suppression would be logical, no clinical counter-measures target the responsible intracellular ... -
MAP4K4 Inhibitors
(2020-06-11)This invention relates to compounds that may be useful as inhibitors of Mitogen-activated Protein Kinase Kinase Kinase Kinase-4 (MAP4K4). The invention also relates to the use of these compounds, for example in a method ... -
MAP4K4 Inhibitors
(2019-04-18)This invention relates to pyrrolopyrimidine comprising compounds that may be useful as inhibitors of Mitogen-activated Protein Kinase Kinase Kinase Kinase-4 (MAP4K4). The invention also relates to the use of these ... -
Mapping the 3D structures of small molecule binding sites
(BMC, 2016-12-06) -
Mathematical modeling identifies optimum lapatinib dosing schedules for the treatment of glioblastoma patients.
(PUBLIC LIBRARY SCIENCE, 2018-01-01)Human primary glioblastomas (GBM) often harbor mutations within the epidermal growth factor receptor (EGFR). Treatment of EGFR-mutant GBM cell lines with the EGFR/HER2 tyrosine kinase inhibitor lapatinib can effectively ... -
Maximising the potential of AKT inhibitors as anti-cancer treatments.
(PERGAMON-ELSEVIER SCIENCE LTD, 2017-04-01)PI3K/AKT signalling is commonly disrupted in human cancers, with AKT being a central component of the pathway, influencing multiple processes that are directly involved in tumourigenesis. Targeting AKT is therefore a highly ... -
Mechanism and non-mechanism based imaging biomarkers for assessing biological response to treatment in non-small cell lung cancer.
(ELSEVIER SCI LTD, 2016-05-01)Therapeutic options in locally advanced non-small cell lung cancer (NSCLC) have expanded in the past decade to include a palate of targeted interventions such as high dose targeted thermal ablations, radiotherapy and growing ... -
Mesothelin-targeted CAR-T cell therapy for solid tumors.
(TAYLOR & FRANCIS LTD, 2021-04-03)Introduction: Mesothelin (MSLN) is a tumor differentiation antigen normally restricted to the body's mesothelial surfaces, but significantly overexpressed in a broad range of solid tumors. For this reason, MSLN has emerged ... -
Metabolic biomarkers of response to the AKT inhibitor MK-2206 in pre-clinical models of human colorectal and prostate carcinoma.
(NATURE PUBLISHING GROUP, 2018-10-30)BACKGROUND: AKT is commonly overexpressed in tumours and plays an important role in the metabolic reprogramming of cancer. We have used magnetic resonance spectroscopy (MRS) to assess whether inhibition of AKT signalling ... -
Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species.
(ELSEVIER, 2019-11-01)CCT241736 is a dual fms-like tyrosine kinase 3 (FLT3)/Aurora kinase inhibitor in development for the treatment of acute myeloid leukaemia. The successful development of any new drug relies on adequate safety testing including ... -
Metabolomic changes of the multi (-AGC-) kinase inhibitor AT13148 in cells, mice and patients are associated with NOS regulation.
(SPRINGER, 2020-04-13)INTRODUCTION: To generate biomarkers of target engagement or predictive response for multi-target drugs is challenging. One such compound is the multi-AGC kinase inhibitor AT13148. Metabolic signatures of selective signal ... -
Methylome analysis identifies a Wilms tumor epigenetic biomarker detectable in blood
(2014-01-01)Background Wilms tumor is the most common pediatric renal malignancy and there is a clinical need for a molecular biomarker to assess treatment response and predict relapse. The known mutated genes in this tumor type show ... -
MicroRNA 193b-3p as a predictive biomarker of chronic kidney disease in patients undergoing radical nephrectomy for renal cell carcinoma.
(SPRINGERNATURE, 2016-11-01)BACKGROUND: A significant proportion of patients undergoing radical nephrectomy (RN) for clear-cell renal cell carcinoma (RCC) develop chronic kidney disease (CKD) within a few years following surgery. Chronic kidney disease ... -
MicroRNA and gene co-expression networks characterize biological and clinical behavior of rhabdomyosarcomas.
(ELSEVIER IRELAND LTD, 2017-01-28)Rhabdomyosarcomas (RMS) in children and adolescents are heterogeneous sarcomas broadly defined by skeletal muscle features and the presence/absence of PAX3/7-FOXO1 fusion genes. MicroRNAs are small non-coding RNAs that ... -
MicroRNA-135b promotes cancer progression by acting as a downstream effector of oncogenic pathways in colon cancer.
(CELL PRESS, 2014-04-14)MicroRNA deregulation is frequent in human colorectal cancers (CRCs), but little is known as to whether it represents a bystander event or actually drives tumor progression in vivo. We show that miR-135b overexpression is ...