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Design and synthesis of dual kinase-bromodomain inhibitors targeting ALK and BRD4
(Institute of Cancer Research (University Of London), 2019-12-31)
Neuroblastoma is a paediatric cancer of neural crest origin and is the most common extracranial tumour in childhood. In high-risk patients with poor clinical outcome, mutations within the kinase domain of anaplastic lymphoma ...
Phase 1 dose-finding and pharmacokinetic study of eribulin-liposomal formulation in patients with solid tumours.
(2019-02)
BACKGROUND:This phase 1 study examined the safety, tolerability, pharmacokinetics and preliminary efficacy of eribulin-liposomal formulation (eribulin-LF) in patients with advanced solid tumours. METHODS:Eligible patients ...
Small-molecule targeting of brachyury transcription factor addiction in chordoma.
(2019-02)
Chordoma is a primary bone cancer with no approved therapy 1 . The identification of therapeutic targets in this disease has been challenging due to the infrequent occurrence of clinically actionable somatic mutations in ...
To Cycle or Fight-CDK4/6 Inhibitors at the Crossroads of Anticancer Immunity.
(2019-01)
Dysregulation of cell division resulting in aberrant cell proliferation is a key hallmark of cancer, making it a rational and important target for innovative anticancer drug development. Three selective cyclin-dependent ...
Radium-223 in combination with paclitaxel in cancer patients with bone metastases: safety results from an open-label, multicenter phase Ib study.
(2019-05)
PURPOSE:Concomitant treatment with radium-223 and paclitaxel is a potential option for cancer patients with bone metastases; however, myelosuppression risk during coadministration is unknown. This phase Ib study in cancer ...
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 ...
miR-224 Is Significantly Upregulated and Targets Caspase-3 and Caspase-7 During Colorectal Carcinogenesis.
(ELSEVIER SCIENCE INC, 2019-02-01)
miR-224 has recently emerged as a driver oncomiR in sporadic colorectal carcinogenesis, but its pathogenetic role is still controversial. A large phenotypical and molecularly characterized series of preinvasive and invasive ...
Design, Synthesis and Characterization of Covalent KDM5 Inhibitors.
(WILEY-V C H VERLAG GMBH, 2019-01-08)
Histone lysine demethylases (KDMs) are involved in the dynamic regulation of gene expression and they play a critical role in several biological processes. Achieving selectivity over the different KDMs has been a major ...
Noncoding RNA in Cholangiocarcinoma.
(THIEME MEDICAL PUBL INC, 2019-02-01)
Cholangiocarcinomas (CCAs) are tumors with a dismal prognosis. Early diagnosis is a key challenge because of the lack of specific symptoms, and the curability rate is low due to the difficulty in achieving a radical resection ...