Recent submissions
Now showing items 101-120 of 658
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Individualized Prediction of Drug Response and Rational Combination Therapy in NSCLC Using Artificial Intelligence-Enabled Studies of Acute Phosphoproteomic Changes.
(AMER ASSOC CANCER RESEARCH, 2022-06-01)We hypothesize that the study of acute protein perturbation in signal transduction by targeted anticancer drugs can predict drug sensitivity of these agents used as single agents and rational combination therapy. We assayed ... -
Presence of human breast cancer xenograft changes the diurnal profile of amino acids in mice.
(NATURE PORTFOLIO, 2022-01-19)Human xenografts are extremely useful models to study the biology of human cancers and the effects of novel potential therapies. Deregulation of metabolism, including changes in amino acids (AAs), is a common characteristic ... -
New Fully Automated Preparation of High Apparent Molar Activity 68Ga-FAPI-46 on a Trasis AiO Platform.
(MDPI, 2022-01-20)A large number of applications for fibroblast activation protein inhibitors (FAPI)-based PET agents have been evaluated in conditions ranging from cancer to non-malignant diseases such as myocardial infarction. In particular, ... -
Dual blockade of the PI3K/AKT/mTOR (AZD8055) and RAS/MEK/ERK (AZD6244) pathways synergistically inhibits rhabdomyosarcoma cell growth in vitro and in vivo.
(AMER ASSOC CANCER RESEARCH, 2013-08-05)PURPOSE: To provide rationale for using phosphoinositide 3-kinase (PI3K) and/or mitogen-activated protein kinase (MAPK) pathway inhibitors to treat rhabdomyosarcomas, a major cause of pediatric and adolescent cancer deaths. ... -
Prostate specific membrane antigen and DNA damage repair in advanced prostate cancer
(Institute of Cancer Research (University Of London), 2022-03-31)Identification and implementation of novel therapeutic strategies for advanced prostate cancer (PCa) remains an urgent, unmet clinical need. Prostate Specific Membrane Antigen (PSMA), a PCa biomarker, is currently being ... -
Dual IGF1R/IR inhibitors in combination with GD2-CAR T-cells display a potent anti-tumor activity in diffuse midline glioma H3K27M-mutant.
(OXFORD UNIV PRESS INC, 2022-07-01)BACKGROUND: Diffuse midline gliomas (DMG) H3K27M-mutant, including diffuse intrinsic pontine glioma (DIPG), are pediatric brain tumors associated with grim prognosis. Although GD2-CAR T-cells demonstrated significant ... -
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 ... -
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; ... -
Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket.
(AMER CHEMICAL SOC, 2021-12-09)We describe the optimization of modestly active starting points to potent inhibitors of BCL6 by growing into a subpocket, which was occupied by a network of five stably bound water molecules. Identifying potent inhibitors ... -
Discovery and Characterization of a Cryptic Secondary Binding Site in the Molecular Chaperone HSP70.
(MDPI, 2022-01-26)Heat Shock Protein 70s (HSP70s) are key molecular chaperones that are overexpressed in many cancers and often associated with metastasis and poor prognosis. It has proven difficult to develop ATP-competitive, drug-like ... -
HER3 Is an Actionable Target in Advanced Prostate Cancer.
(AMER ASSOC CANCER RESEARCH, 2021-12-15)It has been recognized for decades that ERBB signaling is important in prostate cancer, but targeting ERBB receptors as a therapeutic strategy for prostate cancer has been ineffective clinically. However, we show here that ... -
Targeted therapy for LIMD1-deficient non-small cell lung cancer subtypes.
(SPRINGERNATURE, 2021-11-11)An early event in lung oncogenesis is loss of the tumour suppressor gene LIMD1 (LIM domains containing 1); this encodes a scaffold protein, which suppresses tumorigenesis via a number of different mechanisms. Approximately ... -
Triggering anti-GBM immune response with EGFR-mediated photoimmunotherapy.
(BMC, 2022-01-21)BACKGROUND: Surgical resection followed by chemo-radiation postpones glioblastoma (GBM) progression and extends patient survival, but these tumours eventually recur. Multimodal treatment plans combining intraoperative ... -
Target 2035 - update on the quest for a probe for every protein.
(ROYAL SOC CHEMISTRY, 2022-01-27)Twenty years after the publication of the first draft of the human genome, our knowledge of the human proteome is still fragmented. The challenge of translating the wealth of new knowledge from genomics into new medicines ... -
Targeted PET/MRI Imaging Super Probes: A Critical Review of Opportunities and Challenges.
(DOVE MEDICAL PRESS LTD, 2021-01-01)Recently, the demand for hybrid PET/MRI imaging techniques has increased significantly, which has sparked the investigation into new ways to simultaneously track multiple molecular targets and improve the localization and ... -
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 ... -
Circulating tumour DNA sequencing to determine therapeutic response and identify tumour heterogeneity in patients with paediatric solid tumours.
(ELSEVIER SCI LTD, 2021-12-18)OBJECTIVE: Clinical diagnostic sequencing of circulating tumour DNA (ctDNA) is well advanced for adult patients, but application to paediatric cancer patients lags behind. METHODS: To address this, we have developed a ... -
Semi-Quantitative Mass Spectrometry in AML Cells Identifies New Non-Genomic Targets of the EZH2 Methyltransferase.
(MDPI, 2017-07-05)Alterations to the gene encoding the EZH2 (KMT6A) methyltransferase, including both gain-of-function and loss-of-function, have been linked to a variety of haematological malignancies and solid tumours, suggesting a complex, ... -
The biguanide polyamine analog verlindamycin promotes differentiation in neuroblastoma via induction of antizyme.
(SPRINGERNATURE, 2021-09-14)Deregulated polyamine biosynthesis is emerging as a common feature of neuroblastoma and drugs targeting this metabolic pathway such as DFMO are in clinical and preclinical development. The polyamine analog verlindamycin ...