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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; ...
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 ...
Bromodomain and extra-terminal inhibitors-A consensus prioritisation after the Paediatric Strategy Forum for medicinal product development of epigenetic modifiers in children-ACCELERATE.
(ELSEVIER SCI LTD, 2021-02-16)
Based on biology and pre-clinical data, bromodomain and extra-terminal (BET) inhibitors have at least three potential roles in paediatric malignancies: NUT (nuclear protein in testis) carcinomas, MYC/MYCN-driven cancers and ...
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 ...
Biological Role of MYCN in Medulloblastoma: Novel Therapeutic Opportunities and Challenges Ahead.
(FRONTIERS MEDIA SA, 2021-06-14)
The constitutive and dysregulated expression of the transcription factor MYCN has a central role in the pathogenesis of the paediatric brain tumour medulloblastoma, with an increased expression of this oncogene correlating ...
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 ...
Impairment of a distinct cancer-associated fibroblast population limits tumour growth and metastasis.
(NATURE PORTFOLIO, 2021-06-10)
Profiling studies have revealed considerable phenotypic heterogeneity in cancer-associated fibroblasts (CAFs) present within the tumour microenvironment, however, functional characterisation of different CAF subsets is ...
Epigenetically defined therapeutic targeting in H3.3G34R/V high-grade gliomas.
(AMER ASSOC ADVANCEMENT SCIENCE, 2021-10-13)
High-grade gliomas with arginine or valine substitutions of the histone H3.3 glycine-34 residue (H3.3G34R/V) carry a dismal prognosis, and current treatments, including radiotherapy and chemotherapy, are not curative. ...
The Long Non-Coding RNA H19 Drives the Proliferation of Diffuse Intrinsic Pontine Glioma with H3K27 Mutation.
(MDPI, 2021-08-25)
Diffuse intrinsic pontine glioma (DIPG) is an incurable paediatric malignancy. Identifying the molecular drivers of DIPG progression is of the utmost importance. Long non-coding RNAs (lncRNAs) represent a large family of ...
Pan RAS-binding compounds selected from a chemical library by inhibiting interaction between RAS and a reduced affinity intracellular antibody.
(NATURE PORTFOLIO, 2021-01-18)
Intracellular antibodies are valuable tools for target validation studies for clinical situations such as cancer. Recently we have shown that antibodies can be used for drug discovery in screening for chemical compounds ...