Recent submissions
Now showing items 141-160 of 658
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Droplet digital PCR-based detection of circulating tumor DNA from pediatric high grade and diffuse midline glioma patients.
(OXFORD UNIV PRESS, 2021-01-01)BACKGROUND: The use of liquid biopsy is of potential high importance for children with high grade (HGG) and diffuse midline gliomas (DMG), particularly where surgical procedures are limited, and invasive biopsy sampling ... -
Pathogenic ACVR1R206H activation by Activin A-induced receptor clustering and autophosphorylation.
(WILEY, 2021-07-15)Fibrodysplasia ossificans progressiva (FOP) and diffuse intrinsic pontine glioma (DIPG) are debilitating diseases that share causal mutations in ACVR1, a TGF-β family type I receptor. ACVR1R206H is a frequent mutation in ... -
An antibody-drug conjugate with intracellular drug release properties showing specific cytotoxicity against CD7-positive cells.
(PERGAMON-ELSEVIER SCIENCE LTD, 2021-09-01)Refractory T cell acute leukaemias that no longer respond to treatment would benefit from new modalities that target T cell-specific surface proteins. T cell associated surface proteins (the surfaceome) offer possible ... -
Biomarkers Associating with PARP Inhibitor Benefit in Prostate Cancer in the TOPARP-B Trial.
(AMER ASSOC CANCER RESEARCH, 2021-11-01)PARP inhibitors are approved for treating advanced prostate cancers (APC) with various defective DNA repair genes; however, further studies to clinically qualify predictive biomarkers are warranted. Herein we analyzed ... -
Near-InfraRed PhotoImmunoTherapy (NIR-PIT) for the local control of solid cancers: Challenges and potentials for human applications.
(ELSEVIER SCIENCE INC, 2021-05-01)Near-InfraRed PhotoImmunoTherapy (NIR-PIT) is a novel cancer-targeted treatment effected by a chemical conjugation between a photosensitiser (e.g. the NIR phthalocyanine dye IRDye700DX) and a cancer-targeting moiety (e.g. ... -
Armored CAR T-Cells: The Next Chapter in T-Cell Cancer Immunotherapy.
(DOVE MEDICAL PRESS LTD, 2021-01-01)Chimeric antigen receptor (CAR) T-cell therapy engineers T-cells to express a synthetic receptor which redirects effector function to the tumor, to improve efficacy and reduce toxicities associated with conventional ... -
Preclinical trial of a MAP4K4 inhibitor to reduce infarct size in the pig: does cardioprotection in human stem cell-derived myocytes predict success in large mammals?
(SPRINGER HEIDELBERG, 2021-05-20)Reducing infarct size (IS) by interfering with mechanisms for cardiomyocyte death remains an elusive goal. DMX-5804, a selective inhibitor of the stress-activated kinase MAP4K4, suppresses cell death in mouse myocardial ... -
Role for the Histone Demethylase KDM4B in Rhabdomyosarcoma via CDK6 and CCNA2: Compensation by KDM4A and Apoptotic Response of Targeting Both KDM4B and KDM4A.
(MDPI, 2021-04-06)Histone demethylases are epigenetic modulators that play key roles in regulating gene expression related to many critical cellular functions and are emerging as promising therapeutic targets in a number of tumor types. We ... -
HER-3 Expression and MEK Activation in Non-small Cell Lung Cancer
(Research Square, 2020-08-26)<h4>Background: </h4> HER-3 has a role in pathogenesis and development of resistance to targeted therapies in non-small cell lung cancer (NSCLC). MethodsWe analysed tumour samples from 45 patients with adenocarcinoma of ... -
A cell-based screening method using an intracellular antibody for discovering small molecules targeting the translocation protein LMO2.
(AMER ASSOC ADVANCEMENT SCIENCE, 2021-04-01)Intracellular antibodies are tools that can be used directly for target validation by interfering with properties like protein-protein interactions. An alternative use of intracellular antibodies in drug discovery is ... -
Competitive SPR using an intracellular anti-LMO2 antibody identifies novel LMO2-interacting compounds.
(ELSEVIER, 2021-03-29)The use of intracellular antibodies as templates to derive surrogate compounds is an important objective because intracellular antibodies can be employed initially for target validation in pre-clinical assays and subsequently ... -
Peritumoral Delivery of Docetaxel-TIPS Microparticles for Prostate Cancer Adjuvant Therapy.
(WILEY, 2020-10-19)Recurrence of prostate cancer after radical prostatectomy is a consequence of incomplete tumor resection. Systemic chemotherapy after surgery is associated with significant toxicity. Improved delivery methods for toxic ... -
SLFN11 informs on standard of care and novel treatments in a wide range of cancer models.
(SPRINGERNATURE, 2021-03-02)BACKGROUND: Schlafen 11 (SLFN11) has been linked with response to DNA-damaging agents (DDA) and PARP inhibitors. An in-depth understanding of several aspects of its role as a biomarker in cancer is missing, as is a ... -
JMJD6 Is a Druggable Oxygenase That Regulates AR-V7 Expression in Prostate Cancer.
(AMER ASSOC CANCER RESEARCH, 2021-02-15)Endocrine resistance (EnR) in advanced prostate cancer is fatal. EnR can be mediated by androgen receptor (AR) splice variants, with AR splice variant 7 (AR-V7) arguably the most clinically important variant. In this study, ... -
Preparation of tyrosine amide derivatives as Rho-kinase inhibitors
(2018-08-02)The invention relates to compds. of formula I and pharmaceutically acceptable salts and solvates thereof (wherein X1 and X2 are independently CH and N; p = 1 - 3; each R when present is halo; R0 and R1 are independently ... -
Targeting the PD-1/PD-L1 axis in non-small cell lung cancer.
The last decade has witnessed rapid advances in the discovery and development of immune checkpoint inhibitors in cancer medicine, particularly drugs targeting programmed cell death 1 (PD-1) and programmed cell death ligand ... -
Tuning Local Hydration Enables a Deeper Understanding of Protein-Ligand Binding: The PP1-Src Kinase Case.
(AMER CHEMICAL SOC, 2021-01-14)Water plays a key role in biomolecular recognition and binding. Despite the development of several computational and experimental approaches, it is still challenging to comprehensively characterize water-mediated effects ... -
Clinical and co-clinical genomics of paediatric solid tumours with a special focus in DIPG
(Institute of Cancer Research (University Of London), 2020-07-31)Cure rates for paediatric solid cancers have not improved in the last decade. Delivering precision medicine to stratify patients based on their molecular profiling is a key goal to support existing and upcoming adaptive ... -
Olaparib and temozolomide in desmoplastic small round cell tumors: a promising combination in vitro and in vivo.
(SPRINGER, 2020-07-01)PURPOSE: Desmoplastic small round cell tumors (DSRCTs) are highly malignant and very rare soft tissue sarcomas with a high unmet need for new therapeutic options. Therefore, we examined poly(ADP-ribose) polymerase 1 (PARP1) ... -
Immunomodulatory activity of IR700-labelled affibody targeting HER2.
(SPRINGERNATURE, 2020-10-20)There is an urgent need to develop therapeutic approaches that can increase the response rate to immuno-oncology agents. Photoimmunotherapy has recently been shown to generate anti-tumour immunological responses by releasing ...