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Showing 1-30 of 54 results for "V1377" within Papers
Mariann MolnƔr et al.
Scientific reports, 9(1), 14284-14284 (2019-10-05)
In the last decade, avian gene preservation research has focused on the use of the early precursors of the reproductive cells, the primordial germ cells (PGCs). This is because avian PGCs have a unique migration route through the vascular system
Sean Ekins et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(12), 2302-2308 (2010-09-17)
Drug-induced liver injury (DILI) is one of the most important reasons for drug development failure at both preapproval and postapproval stages. There has been increased interest in developing predictive in vivo, in vitro, and in silico models to identify compounds
Helge Prinz et al.
Bioorganic & medicinal chemistry, 19(14), 4183-4191 (2011-06-28)
A novel series of phenylimino-10H-anthracen-9-ones and 9-(phenylhydrazone)-9,10-anthracenediones were synthesized and evaluated for interaction with tubulin and for cytotoxicity against a panel of human tumor cell lines. The 10-(3-hydroxy-4-methoxy-phenylimino)-10H-anthracen-9-one 15h and its dichloro analog 16b were identified as potent inhibitors of
Phosphorylation of mixed lineage leukemia 5 by CDC2 affects its cellular distribution and is required for mitotic entry
Liu J, et al.
The Journal of Biological Chemistry, 285(27), 20904-20914 (2010)
Nigel Greene et al.
Chemical research in toxicology, 23(7), 1215-1222 (2010-06-18)
Drug-induced liver injury is a major issue of concern and has led to the withdrawal of a significant number of marketed drugs. An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential
S Lobert et al.
Biochemistry, 35(21), 6806-6814 (1996-05-28)
Vinca alkaloids are antimitotic drugs that inhibit microtubule assembly and induce tubulin self-association into coiled spiral aggregates. Previous sedimentation velocity results with vinblastine have been interpreted by a mechanism involving isodesmic ligand-mediated or ligand-mediated plus ligand-facilitated self-association [Lobert et al.
Courtney E Coombes et al.
Current biology : CB, 30(4), 610-623 (2020-01-14)
Neuronal axons terminate as synaptic boutons that form stable yet plastic connections with their targets. Synaptic bouton development relies on an underlying network of both long-lived and dynamic microtubules that provide structural stability for the boutons while also allowing for
Claudia S Barros et al.
Cell reports, 36(1), 109325-109325 (2021-07-08)
Repair after traumatic injury often starts with mitotic activation around the lesion edges. Early midline cells in the Drosophila embryonic CNS can enter into division following the traumatic disruption of microtubules. We demonstrate that microtubule disruption activates non-canonical TNF signaling
Vural Tagal et al.
Cancer research, 81(2), 400-413 (2020-11-12)
Polyploid giant cancer cells (PGCC) are common in tumors and have been associated with resistance to cancer therapy, tumor relapse, malignancy, immunosuppression, metastasis, cancer stem cell production, and modulation of the tumor microenvironment. However, the molecular mechanisms that cause these
Macarena S ArrƔzola et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 39(20), 3832-3844 (2019-03-10)
Axonal degeneration, which contributes to functional impairment in several disorders of the nervous system, is an important target for neuroprotection. Several individual factors and subcellular events have been implicated in axonal degeneration, but researchers have so far been unable to
Noelle S Williams et al.
Proceedings of the National Academy of Sciences of the United States of America, 104(7), 2074-2079 (2007-02-09)
Blocking cell division through the inhibition of mitosis is one of the most successful clinical strategies for the treatment of cancer. Taxanes and vinca alkaloids are in widespread use and have demonstrated substantive therapeutic efficacy. Both classes of compounds bind
Shaoming Chi et al.
Journal of biomolecular structure & dynamics, 33(10), 2234-2254 (2015-01-15)
Vinblastine (VLB) is one of vinca alkaloids with high cytotoxicity toward cancer cells approved for clinical use. However, because of drug resistance, toxicity, and other side effects caused from the use of VLB, new vinca alkaloids with higher cytotoxicity toward
Juliette Humeau et al.
Cell death & disease, 11(6), 433-433 (2020-06-10)
The integrated stress response is characterized by the phosphorylation of eukaryotic initiation factor-2Ī± (eIF2Ī±) on serine 51 by one out of four specific kinases (EIF2AK1 to 4). Here we provide three series of evidence suggesting that macroautophagy (to which we
Takahisa Maki et al.
Journal of molecular biology, 427(14), 2379-2395 (2015-05-25)
CLIP-associated proteins CLASPs are mammalian microtubule (MT) plus-end tracking proteins (+TIPs) that promote MT rescue in vivo. Their plus-end localization is dependent on other +TIPs, EB1 and CLIP-170, but in the leading edge of the cell, CLASPs display lattice-binding activity.
MarĆa L GonzĆ”lez et al.
Frontiers in pharmacology, 8, 205-205 (2017-05-11)
P-glycoprotein (P-gp) is a membrane protein associated with multidrug resistance (MDR) due to its key role in mediating the traffic of chemotherapeutic drugs outside cancer cells, leading to a cellular response that hinders efforts toward successful therapy. With the aim
G K Chen et al.
British journal of cancer, 83(7), 892-898 (2000-09-06)
Single-step selection with vinblastine was performed in populations of the human sarcoma cell line MES-SA, to assess cellular mechanisms of resistance to the drug and mutation rates via fluctuation analysis. At a stringent selection with 20 nM vinblastine, resulting in
Inhibition of transcription by dactinomycin reveals a new characteristic of immunogenic cell stress.
Juliette Humeau et al.
EMBO molecular medicine, 12(5), e11622-e11622 (2020-04-24)
Chemotherapy still constitutes the standard of care for the treatment of most neoplastic diseases. Certain chemotherapeutics from the oncological armamentarium are able to trigger pre-mortem stress signals that lead to immunogenic cell death (ICD), thus inducing an antitumor immune response
Rosa Tundis et al.
Bioorganic & medicinal chemistry, 17(13), 4542-4547 (2009-05-27)
Three triterpene saponins isolated from the roots of Physospermum verticillatum and identified as saikosaponin a (1), buddlejasaponin IV (2), and songarosaponin D (3) were investigated in vitro for their cytotoxic activity against a panel of seven different cancer cell lines
Evolutionary conservation of vertebrate blood-brain barrier chemoprotective mechanisms in Drosophila
Mayer F, et al.
The Journal of Neuroscience, 29(11), 3538-3550 (2009)
M V Blagosklonny et al.
Cancer research, 57(1), 130-135 (1997-01-01)
Recent studies have shown that paclitaxel leads to activation of Raf-1 kinase and have suggested that this activation is essential for bcl-2 phosphorylation and apoptosis. In the present study, we demonstrate that, in addition to paclitaxel, other agents that interact
Georg Surkau et al.
European journal of medicinal chemistry, 45(8), 3354-3364 (2010-06-16)
A series of anthracenone-based oxime ethers and -esters were synthesized in order to evaluate their antiproliferative activity. Several investigated compounds displayed strong antiproliferative activity against K562 leukemia cells and proved to be strong inhibitors of tubulin polymerization. In this context
Mizuki Kuboki et al.
Biochemical and biophysical research communications, 456(3), 810-814 (2014-12-17)
DTCM-glutarimide (DTCM-G) is a newly found anti-inflammatory agent. In the course of experiments with lymphoma cells, we found that DTCM-G induced specific RelB cleavage. Anticancer agent vinblastine also induced the specific RelB cleavage in human fibrosarcoma HT1080 cells. The site-directed
Fahima Mayer et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 29(11), 3538-3550 (2009-03-20)
Pharmacologic remedy of many brain diseases is difficult because of the powerful drug exclusion properties of the blood-brain barrier (BBB). Chemical isolation of the vertebrate brain is achieved through the highly integrated, anatomically compact and functionally overlapping chemical isolation processes
Phedias Diamandis et al.
Nature chemical biology, 3(5), 268-273 (2007-04-10)
The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain cancer. However, the complete repertoire of signaling pathways that governs the
Zhichao Liu et al.
PLoS computational biology, 7(12), e1002310-e1002310 (2011-12-24)
Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI types (hepatotoxic side effects) seen in the clinic can be translated
Gowdahalli Krishnegowda et al.
Bioorganic & medicinal chemistry, 19(20), 6006-6014 (2011-09-17)
A novel series of 5,7-dibromoisatin analogs were synthesized and evaluated for their cytotoxicities against four human cancer cell lines including colon HT29, breast MCF-7, lung A549 and melanoma UACC903. Analogs 6, 11 and 13 displayed good in vitro anticancer activity
Peter Jan Hooikaas et al.
eLife, 9 (2020-12-22)
When a T cell and an antigen-presenting cell form an immunological synapse, rapid dynein-driven translocation of the centrosome toward the contact site leads to reorganization of microtubules and associated organelles. Currently, little is known about how the regulation of microtubule
X R Zhou-Pan et al.
Cancer research, 53(21), 5121-5126 (1993-11-01)
Vinblastine biotransformation was investigated by using a human liver microsomes library. The drug was converted into one major metabolite (M) upon incubation with the microsomes. A large interindividual variation in vinblastine metabolism was observed among the samples tested, with a
Anne Zuse et al.
Journal of medicinal chemistry, 49(26), 7816-7825 (2006-12-22)
A novel series of 9-benzylidene-naphtho[2,3-b]thiophen-4-ones and structurally related compounds were synthesized and evaluated for their ability to inhibit tubulin polymerization. The 4-hydroxy-3,5-dimethoxy-benzylidene analogue 15d was identified as a potent cytotoxic agent in an assay based on K562 leukemia cells. Antiproliferative
R B Tishler et al.
The British journal of cancer. Supplement, 27, S82-S85 (1996-07-01)
The combination of the microtubule active drug taxol with radiation has shown promise for use in combined modality therapy. Recent studies have demonstrated that radiation and a wide range of chemotherapy agents, including microtubule active drugs, induce p53. In certain
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