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CDS022173
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Laura Mazzera et al.
Haematologica, 104(12), 2465-2481 (2019-04-06)
Considering that Aurora kinase inhibitors are currently under clinical investigation in hematologic cancers, the identification of molecular events that limit the response to such agents is essential for enhancing clinical outcomes. Here, we discover a NF-κB-inducing kinase (NIK)-c-Abl-STAT3 signaling-centered feedback
José Alejandro Sánchez-Gutiérrez et al.
Molecules (Basel, Switzerland), 25(1) (2019-12-28)
Asclepias linaria Cav. (Apocynaceae) is a shrubby plant endemic of Mexico which has been used in traditional medicine. However, the bioactive potential of this plant remains unexplored. In this study, the phenolic composition, antioxidant, and cytotoxic activities of A. linaria
Jean-Philippe Coppé et al.
Nature cell biology, 21(6), 778-790 (2019-06-05)
Phosphorylation networks intimately regulate mechanisms of response to therapies. Mapping the phospho-catalytic profile of kinases in cells or tissues remains a challenge. Here, we introduce a practical high-throughput system to measure the enzymatic activity of kinases using biological peptide targets
Seiichi Okabe et al.
Cancer chemotherapy and pharmacology, 85(2), 401-412 (2020-01-07)
ABL tyrosine kinase inhibitors (TKIs) have demonstrated potency in the treatment of chronic myeloid leukemia (CML) patients. However, resistance to ABL TKIs can develop in CML patients due to BCR-ABL point mutations. Furthermore, CUDC-907 is an oral inhibitor of class
Jeremy Soon Kiat Chan et al.
Cell death & disease, 8(1), e2562-e2562 (2017-01-20)
Histological inspection of visually normal tissue adjacent to neoplastic lesions often reveals multiple foci of cellular abnormalities. This suggests the presence of a regional carcinogenic signal that spreads oncogenic transformation and field cancerization. We observed an abundance of mutagenic reactive
Manon Lernoux et al.
Clinical epigenetics, 12(1), 69-69 (2020-05-21)
Chronic myeloid leukemia (CML) pathogenesis is mainly driven by the oncogenic breakpoint cluster region-Abelson murine leukemia viral oncogene homolog 1 (BCR-ABL) fusion protein. Since BCR-ABL displays abnormal constitutive tyrosine kinase activity, therapies using tyrosine kinase inhibitors (TKis) such as imatinib
Kiran Nadella et al.
Endocrine-related cancer, 27(10), 591-599 (2020-08-02)
Protein kinase A (PKA) regulatory subunit type 1A (PRKAR1A) defects lead to primary pigmented nodular adrenocortical disease (PPNAD). The KIT protooncogene (c-KIT) is not known to be expressed in the normal adrenal cortex (AC). In this study, we investigated the
J Kyle Bruner et al.
Cancer research, 77(20), 5554-5563 (2017-09-20)
FMS-like tyrosine kinase-3 (FLT3) tyrosine kinase inhibitors (TKI) have been tested extensively to limited benefit in acute myeloid leukemia (AML). We hypothesized that FLT3/internal tandem duplication (ITD) leukemia cells exhibit mechanisms of intrinsic signaling adaptation to TKI treatment that are
Leyla Hasandoost et al.
Artificial cells, nanomedicine, and biotechnology, 45(3), 665-669 (2016-05-03)
The study aimed to prepare imatinib mesylate-loaded polybutylcyanoacrylate (PBCA) nanoparticles and evaluate their efficacy on leukemia cell line K562. The formulation was prepared by miniemulsion polymerization technique. Nanoparticles were characterized by dynamic light scattering (DLS), spectrophotometry, Fourier transform infrared spectroscopy
Jiabin Lu et al.
European journal of pharmacology, 874, 173022-173022 (2020-02-23)
Glioma is a kind of lethal malignant tumor, and lacks efficient therapies. Combination therapy has been claimed to be a promising approach to combat cancer, due to its increased anti-cancer effects and reduced side effects. This study aimed to investigate
Ewelina Synowiec et al.
International journal of molecular sciences, 16(8), 18111-18128 (2015-08-08)
Chronic myeloid leukemia (CML) cells express the active BCR-ABL1 protein, which has been targeted by imatinib in CML therapy, but resistance to this drug is an emerging problem. BCR-ABL1 induces endogenous oxidative stress promoting genomic instability and imatinib resistance. In
Carolin M Morawietz et al.
Frontiers in veterinary science, 7, 611270-611270 (2021-01-08)
Protein kinases have been discussed as promising druggable targets in various parasitic helminths. New drugs are also needed for control of fascioliasis, a food-borne trematode infection and worldwide spread zoonosis, caused by the liver fluke Fasciola hepatica and related species.
Frances V Hundley et al.
Molecular cell, 81(6), 1319-1336 (2021-02-05)
The human ubiquitin proteasome system, composed of over 700 ubiquitin ligases (E3s) and deubiquitinases (DUBs), has been difficult to characterize systematically and phenotypically. We performed chemical-genetic CRISPR-Cas9 screens to identify E3s/DUBs whose loss renders cells sensitive or resistant to 41
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Fengling Wang et al.
Anti-cancer drugs, 30(2), 159-166 (2018-11-14)
The Bcr/Abl kinase is an oncogenic fusion protein that plays a central role in the pathogenesis of chronic myeloid leukemia (CML). Some small-molecule kinase inhibitors such as imatinib were developed in the treatment of CML; however, resistant to imatinib is
Bryan J Hostetler et al.
Anticancer research, 37(3), 997-1004 (2017-03-21)
The current study examined the effectiveness of glycyrrhizic acid (GA) in reducing cell viability and inducing apoptosis in human chronic myeloid leukemia (CML) in vitro and a mouse lymphoma in vivo. Additionally, we assessed GA as a candidate for combinational
Nicolas R Chevalier et al.
American journal of physiology. Gastrointestinal and liver physiology, 319(4), G519-G528 (2020-09-03)
The first contractile waves in the developing embryonic gut are purely myogenic; they only involve smooth muscle. Here, we provide evidence for a transition from smooth muscle to interstitial cell of Cajal (ICC)-driven contractile waves in the developing chicken gut.
Adrian M Seifert et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 23(2), 454-465 (2016-07-30)
Tyrosine kinase inhibitors are effective in gastrointestinal stromal tumors (GISTs) but often are of transient benefit as resistance commonly develops. Immunotherapy, particularly blockade of the inhibitory receptor programmed death 1 (PD-1) or the ligand programmed death ligand 1 (PD-L1), has
Lobna Alkebsi et al.
International journal of hematology, 113(3), 441-455 (2021-01-05)
Adverse vascular events have become a serious clinical problem in chronic myeloid leukemia (CML) patients who receive certain BCR/ABL1 tyrosine kinase inhibitors (TKIs). Studies have shown that endothelial-to-mesenchymal transition (EndMT) can contribute to various vascular diseases. We investigated the effects
Mohammad Reza Molaahmadi et al.
Iranian journal of pharmaceutical research : IJPR, 18(4), 1676-1693 (2020-03-19)
Lipid nanocapsules (LNCs) represent a stable, biocompatible and worthwhile drug delivery system, demonstrating significant potential as gene/drug delivery platforms for cancer therapy. Imatinib, a potent tyrosine kinase inhibitor, has revolutionized the therapy of malignancies resulting from abnormal tyrosine kinase activity.
Astrid Weiss et al.
Nature communications, 10(1), 2204-2204 (2019-05-19)
Pulmonary arterial hypertension (PAH) is a devastating disease with poor prognosis and limited therapeutic options. We screened for pathways that may be responsible for the abnormal phenotype of pulmonary arterial smooth muscle cells (PASMCs), a major contributor of PAH pathobiology
Yutaro Hoshi et al.
Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, 40(2), 420-436 (2019-01-10)
Exposure of the brain to high levels of glucocorticoids during ischemia-reperfusion induces neuronal cell death. Oxidative stress alters blood-brain barrier (BBB) function during ischemia-reperfusion, and so we hypothesized that it might impair P-glycoprotein (P-gp)-mediated efflux transport of glucocorticoids at the
Liu Jiaxin et al.
Aging, 12(12), 11416-11430 (2020-06-21)
Rectal gastrointestinal stromal tumors (RGISTs) are biologically characterized tumors that are relatively rare. Thus, few studies have reported a specific prognostic system for this subset of tumors but integrated it into parallel systems, such as small intestine. Our aim is
Marit D Moen et al.
Drugs, 67(2), 299-320 (2007-02-08)
Imatinib (Gleevec, Glivec) is a synthetic tyrosine kinase inhibitor used in the treatment of chronic myeloid leukaemia (CML). It is specifically designed to inhibit the breakpoint cluster region (BCR)-Abelson (ABL) fusion protein that results from the chromosomal abnormality known as
Yijin Kuang et al.
Blood cells, molecules & diseases, 85, 102477-102477 (2020-07-28)
Chronic myeloid leukemia (CML) is a kind of myeloproliferative disorder caused by a constitutively active BCR-ABL tyrosine kinase. Tyrosine kinase inhibitors (TKIs), imatinib and its derivatives, have achieved great progress in the treatment of CML. However, many CML patients do
Corina Anastasaki et al.
Oncotarget, 8(29), 47574-47585 (2017-05-27)
Dermal neurofibromas (DNFs) are benign peripheral nerve sheath tumors thought to originate from Schwann cell progenitors. These tumors represent one of the hallmarks of the neurofibromatosis type 1 (NF1) tumor predisposition syndrome, where they can number in the thousands. While
Daisuke Watanabe et al.
Cancers, 11(12) (2019-11-24)
FLT3-ITD is the most frequent tyrosine kinase mutation in acute myeloid leukemia (AML) associated with poor prognosis. We previously found that FLT3-ITD activates the mTORC1/S6K/4EBP1 pathway cooperatively through the STAT5/PIM and PI3K/AKT pathways to promote proliferation and survival by enhancing
Zilai Wang et al.
Cancer cell, 38(3), 366-379 (2020-07-11)
Glioblastoma, the predominant adult malignant brain tumor, has been computationally classified into molecular subtypes whose functional relevance remains to be comprehensively established. Tumors from genetically engineered glioblastoma mouse models initiated by identical driver mutations in distinct cells of origin portray
Islem Ben Hassine et al.
Cancer chemotherapy and pharmacology, 80(4), 829-839 (2017-08-25)
The introduction and success of imatinib mesylate have become a paradigm shift in chronic myeloid leukemia (CML) treatment. However, despite its high efficiency, resistance to imatinib has emerged as a significant problem, which may in part be caused by pharmacogenetic
Prahalathan Pichavaram et al.
European journal of pharmacology, 890, 173666-173666 (2020-11-03)
Imatinib, a PDGF receptor tyrosine kinase inhibitor, has been shown to suppress intimal hyperplasia in different animal models under normal metabolic milieu, diabetic, and/or hypercholesterolemic conditions. However, the impact of imatinib treatment on injury-induced neointimal hyperplasia has not yet been
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