Browsing Cancer Therapeutics by title
Now showing items 245-264 of 658
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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 ... -
Extracranial Soft-Tissue Tumors: Repeatability of Apparent Diffusion Coefficient Estimates from Diffusion-weighted MR Imaging.
(RADIOLOGICAL SOC NORTH AMERICA, 2017-07-01)Purpose To assess the repeatability of apparent diffusion coefficient (ADC) estimates in extracranial soft-tissue diffusion-weighted magnetic resonance imaging across a wide range of imaging protocols and patient populations. ... -
Fadraciclib (CYC065), a novel CDK inhibitor, targets key pro-survival and oncogenic pathways in cancer.
(PUBLIC LIBRARY SCIENCE, 2020-07-09)Cyclin-dependent kinases (CDKs) contribute to the cancer hallmarks of uncontrolled proliferation and increased survival. As a result, over the last two decades substantial efforts have been directed towards identification ... -
FGF7-FGFR2 autocrine signaling increases growth and chemoresistance of fusion-positive rhabdomyosarcomas.
(WILEY, 2021-11-30)Rhabdomyosarcomas are aggressive pediatric soft-tissue sarcomas and include high-risk PAX3-FOXO1 fusion-gene-positive cases. Fibroblast growth factor receptor 4 (FGFR4) is known to contribute to rhabdomyosarcoma progression; ... -
FGFR1 Expression and Role in Migration in Low and High Grade Pediatric Gliomas.
(Frontiers Media SA, 2019-03-13)The heterogeneous and invasive nature of pediatric gliomas poses significant treatment challenges, highlighting the importance of identifying novel chemotherapeutic targets. Recently, recurrent Fibroblast growth factor ... -
Fibroblast Activation Protein (FAP)-Targeted CAR-T Cells: Launching an Attack on Tumor Stroma.
(DOVE MEDICAL PRESS LTD, 2021-01-01)Fibroblast activation protein (FAP) is a membrane protease that is highly expressed by cancer-associated fibroblasts (CAFs). FAP can modulate the tumor microenvironment (TME) by remodeling the extracellular matrix (ECM), ... -
First-in-Human Pharmacokinetic and Pharmacodynamic Study of the Dual m-TORC 1/2 Inhibitor AZD2014.
(AMER ASSOC CANCER RESEARCH, 2015-08-01)PURPOSE: AZD2014 is a novel, oral, m-TORC 1/2 inhibitor that has shown in vitro and in vivo efficacy across a range of preclinical human cancer models. EXPERIMENTAL DESIGN: A rolling six-dose escalation was performed to ... -
First-in-Human Phase I Study of an Oral HSP90 Inhibitor, TAS-116, in Patients with Advanced Solid Tumors.
(AMER ASSOC CANCER RESEARCH, 2019-03-01)HSP90 is involved in stability and function of cancer-related proteins. This study was conducted to define the MTD, safety, pharmacokinetics, pharmacodynamics, and preliminary antitumor efficacy of TAS-116, a novel class, ... -
First-in-Human Study of AT13148, a Dual ROCK-AKT Inhibitor in Patients with Solid Tumors.
(AMER ASSOC CANCER RESEARCH, 2020-09-15)PURPOSE: AT13148 is an oral AGC kinase inhibitor, which potently inhibits ROCK and AKT kinases. In preclinical models, AT13148 has been shown to have antimetastatic and antiproliferative activity. PATIENTS AND METHODS: The ... -
Focal Adhesion Kinase (FAK) tyrosine 397E mutation restores the vascular leakage defect in endothelium‐specific FAK‐kinase dead mice
(Wiley, 2017-07-01)<jats:title>Abstract</jats:title><jats:p>Focal adhesion kinase (<jats:styled-content style="fixed-case">FAK</jats:styled-content>) inhibitors have been developed as potential anticancer agents and are undergoing clinical ... -
Fragment growing to retain or alter the selectivity of anchored kinase hinge-binding fragments
(ROYAL SOC CHEMISTRY, 2014-01-01)<p>The selectivity patterns of kinase hinge-binding fragments can be retained during fragment growing, suggesting a new way to control poly-pharmacology.</p> -
Fragment-based discovery of HSP70 inhibitors
(Institute of Cancer Research (University Of London), 2021-01-31)Heat Shock Protein 70s (HSP70s) are key molecular chaperones that are overexpressed in many cancers and are often associated with metastasis and poor prognosis. Dual silencing of two isoforms, HSP72 and HSC70, using siRNA ... -
Fragment-based screening identifies molecules targeting the substrate-binding ankyrin repeat domains of tankyrase.
(NATURE PORTFOLIO, 2019-12-13)The PARP enzyme and scaffolding protein tankyrase (TNKS, TNKS2) uses its ankyrin repeat clusters (ARCs) to bind a wide range of proteins and thereby controls diverse cellular functions. A number of these are implicated in ...