Antimitotic Agents: Agents that arrest cells in MITOSIS, most notably TUBULIN MODULATORS.Colchicine: A major alkaloid from Colchicum autumnale L. and found also in other Colchicum species. Its primary therapeutic use is in the treatment of gout, but it has been used also in the therapy of familial Mediterranean fever (PERIODIC DISEASE).Tubulin Modulators: Agents that interact with TUBULIN to inhibit or promote polymerization of MICROTUBULES.Tubulin: A microtubule subunit protein found in large quantities in mammalian brain. It has also been isolated from SPERM FLAGELLUM; CILIA; and other sources. Structurally, the protein is a dimer with a molecular weight of approximately 120,000 and a sedimentation coefficient of 5.8S. It binds to COLCHICINE; VINCRISTINE; and VINBLASTINE.Griseofulvin: An antifungal agent used in the treatment of TINEA infections.Vinca Alkaloids: A group of indole-indoline dimers which are ALKALOIDS obtained from the VINCA genus of plants. They inhibit polymerization of TUBULIN into MICROTUBULES thus blocking spindle formation and arresting cells in METAPHASE. They are some of the most useful ANTINEOPLASTIC AGENTS.Mitosis: A type of CELL NUCLEUS division by means of which the two daughter nuclei normally receive identical complements of the number of CHROMOSOMES of the somatic cells of the species.Vinblastine: Antitumor alkaloid isolated from Vinca rosea. (Merck, 11th ed.)Microtubules: Slender, cylindrical filaments found in the cytoskeleton of plant and animal cells. They are composed of the protein TUBULIN and are influenced by TUBULIN MODULATORS.Paclitaxel: A cyclodecane isolated from the bark of the Pacific yew tree, TAXUS BREVIFOLIA. It stabilizes MICROTUBULES in their polymerized form leading to cell death.Antineoplastic Agents: Substances that inhibit or prevent the proliferation of NEOPLASMS.Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Cell Line, Tumor: A cell line derived from cultured tumor cells.Maytansine: An ansa macrolide isolated from the MAYTENUS genus of East African shrubs.Depsipeptides: Compounds consisting of chains of AMINO ACIDS alternating with CARBOXYLIC ACIDS via ester and amide linkages. They are commonly cyclized.

Emi1 class of proteins regulate entry into meiosis and the meiosis I to meiosis II transition in Xenopus oocytes. (1/74)

Xenopus oocytes are arrested at the G2/prophase boundary of meiosis I and enter meiosis in response to progesterone. A hallmark of meiosis is the absence of DNA replication between the successive cell division phases meiosis I (MI) and meiosis II (MII). After the MI-MII transition, Xenopus eggs are locked in metaphase II by the cytostatic factor (CSF) arrest to prevent parthenogenesis. Early Mitotic Inhibitor 1 (Emi1) maintains CSF arrest by inhibiting the ability of the Anaphase Promoting Complex (APC) to direct the destruction of cyclin B. To investigate whether Emi1 has an earlier role in meiosis, we injected Xenopus oocytes with neutralizing antibodies against Emi1 at G2/prophase and during the MI-MII transition. Progesterone-treated G2/prophase oocytes injected with anti-Emi1 antibody fail to activate Maturation Promoting Factor (MPF), a complex of cdc2/cyclin B, and the MAPK pathway, and do not undergo germinal vesicle breakdown (GVBD). Injection of purified Delta90 cyclin B protein or blocking anti-Emi1 antibody with purified Emi1 protein rescues these meiotic processes in Emi1-neutralized oocytes. Acute inhibition of Emi1 in progesterone treated oocytes immediately after GVBD causes rapid loss of cdc2 activity with simultaneous loss of cyclin B levels and inactivation of the MAPK pathway. These oocytes decondense their chromosomes and enter a DNA replication phase instead of progressing to MII. Prior ablation of Cdc20, addition of methyl-ubiquitin, or addition of nondestructible Delta90 cyclin B rescues the MI-MII transition in Emi1-inhibited oocytes.  (+info)

Rapamycin inhibits human in stent restenosis vascular smooth muscle cells independently of pRB phosphorylation and p53. (2/74)

OBJECTIVE: Drug-eluting stents containing the immunosuppressant rapamycin markedly inhibit in stent restenosis (ISR). However, the molecular mechanisms that underlie its effect on ISR-derived vascular smooth muscle cells (VSMCs), as opposed to normal VSMCs, are unknown. Specifically, as ISR-VSMCs have altered cell cycle regulation, rapamycin may arrest these cells via novel molecular pathways. METHODS: We isolated human VSMCs from sites of ISR, and examined the effect of rapamycin on cell proliferation using MTT assay, time lapse videomicroscopy and flow cytometry. Regulation of G(1)-S transition was examined using Western blotting, and cell size and protein synthesis examined using flow cytometry and collagen assay, respectively. The requirement for pRB and p53 was examined using ISR VSMCs expressing E1A and a dominant negative p53, respectively. RESULTS: ISR-VSMC proliferation was potently inhibited by rapamycin. Arrest was confined to G(1), as cell proliferation (but not cell size) of S/G(2)-arrested cells was unaffected by rapamycin. Moreover, ISR-VSMC lines generated with disrupted p53 or pRB function still arrested in the presence of rapamycin, suggesting that these genes are dispensable for rapamycin-induced arrest. Significantly, rapamycin completely inhibited the phosphorylation of p70(S6K), an mTOR-regulated kinase implicated in the control of proliferation, but had no effect on collagen or total protein synthesis. CONCLUSIONS: We demonstrate that rapamycin is a potent inhibitor of ISR VSMC proliferation during G(1). Rapamycin's action does not require p53 or pRB. We show that p70(S6K) is markedly inhibited in rapamycin-arrested ISR cells, suggesting that regulation of its upstream kinase, mTOR, is important for the control of proliferation in ISR cells.  (+info)

The primary antimitotic mechanism of action of the synthetic halichondrin E7389 is suppression of microtubule growth. (3/74)

E7389, which is in phase I and II clinical trials, is a synthetic macrocyclic ketone analogue of the marine sponge natural product halichondrin B. Whereas its mechanism of action has not been fully elucidated, its main target seems to be tubulin and/or the microtubules responsible for the construction and proper function of the mitotic spindle. Like most microtubule-targeted antitumor drugs, it inhibits tumor cell proliferation in association with G(2)-M arrest. It binds to tubulin and inhibits microtubule polymerization. We examined the mechanism of action of E7389 with purified microtubules and in living cells and found that, unlike antimitotic drugs including vinblastine and paclitaxel that suppress both the shortening and growth phases of microtubule dynamic instability, E7389 seems to work by an end-poisoning mechanism that results predominantly in inhibition of microtubule growth, but not shortening, in association with sequestration of tubulin into aggregates. In living MCF7 cells at the concentration that half-maximally blocked cell proliferation and mitosis (1 nmol/L), E7389 did not affect the shortening events of microtubule dynamic instability nor the catastrophe or rescue frequencies, but it significantly suppressed the rate and extent of microtubule growth. Vinblastine, but not E7389, inhibited the dilution-induced microtubule disassembly rate. The results suggest that, at its lowest effective concentrations, E7389 may suppress mitosis by directly binding to microtubule ends as unliganded E7389 or by competition of E7389-induced tubulin aggregates with unliganded soluble tubulin for addition to growing microtubule ends. The result is formation of abnormal mitotic spindles that cannot pass the metaphase/anaphase checkpoint.  (+info)

The mitotic checkpoint in cancer therapy. (4/74)

The mitotic checkpoint is a key cell cycle control mechanism that ensures an accurate segregation of chromosomes during mitosis by delaying the onset of anaphase until all chromosomes are properly attached to a bipolar mitotic spindle. While complete loss of this checkpoint is lethal in vertebrates, a weakened mitotic checkpoint is frequently seen in cancer cells and it may contribute to tumorigenesis. Many anti-tumor drugs, including spindle assembly inhibitors and DNA damaging agents, can activate the mitotic checkpoint. However, since these drugs influence interphase events besides activating the mitotic checkpoint, the role of the mitotic checkpoint in drug-induced cell death remained unclear. Using a KSP antagonist that specifically acts on mitotic cells, we have recently shown that activation of the mitotic checkpoint followed by mitotic slippage or adaptation, activates Bax and initiates apoptosis. Notably, cells with a weakened mitotic checkpoint incur much less apoptotic death than their checkpoint-proficient counterparts, indicating the requirement of a competent mitotic checkpoint in the induction of apoptosis. In light of these findings and other recent reports, the potential influence of the mitotic checkpoint in response to chemotherapies, and the strategy to target the mitotic checkpoint for cancer therapeutics are discussed.  (+info)

Sichuan pepper extracts block the PAK1/cyclin D1 pathway and the growth of NF1-deficient cancer xenograft in mice. (5/74)

There is increasing evidence that more than 70% of cancers including pancreatic, breast and prostate cancers as well as neurofibromatosis (NF) are highly addicted to abnormal activation of the Ser/Thr kinase PAK1 for their growth. So far FK228 is the most potent among the HDAC (histone deacetylase) inhibitors that block the activation of both PAK1 and another kinase AKT, downstream of PI-3 kinase. However, FK228 is still in clinical trials (phase 2) for a variety of cancers (but not for NF as yet), and not available for most cancer/NF patients. Thus, we have been exploring an alternative which is already in the market, and therefore immediately useful for the treatment of those desperate cancer/NF patients. Here we provide the first evidence that extracts of Chinese/ Japanese peppercorns (Zanthoxyli Fructus) from the plant Zanthoxylum piperitum called "Hua Jiao"/"Sansho", block selectively the key kinase PAK1, leading to the downregulation of cyclin D1. Unlike FK228, these extracts do not inhibit AKT activation at the concentrations that block either cancer growth or PAK1 activation. The Chinese pepper extract selectively inhibits the growth of NF1-deficient malignant peripheral nerve sheath tumor (MPNST) cells, without affecting the growth of normal fibroblasts, and suppresses the growth of NF1-deficient human breast cancer (MDA-MB-231) xenograft in mice. Our data suggest that these peppercorn extracts would be potentially useful for the treatment of PAK1-dependent NF such as MPNST, in addition to a variety of PAK1-dependent cancers including breast cancers.  (+info)

Increased therapeutic potential of an experimental anti-mitotic inhibitor SB715992 by genistein in PC-3 human prostate cancer cell line. (6/74)

BACKGROUND: Kinesin spindle proteins (KSP) are motor proteins that play an essential role in mitotic spindle formation. HsEg5, a KSP, is responsible for the formation of the bipolar spindle, which is critical for proper cell division during mitosis. The function of HsEg5 provides a novel target for the manipulation of the cell cycle and the induction of apoptosis. SB715992, an experimental KSP inhibitor, has been shown to perturb bipolar spindle formation, thus making it an excellent candidate for anti-cancer agent. Our major objective was a) to investigate the cell growth inhibitory effects of SB715992 on PC-3 human prostate cancer cell line, b) to investigate whether the growth inhibitory effects of SB715992 could be enhanced when combined with genistein, a naturally occurring isoflavone and, c) to determine gene expression profile to establish molecular mechanism of action of SB715992. METHODS: PC-3 cells were treated with varying concentration of SB715992, 30 microM of genistein, and SB715992 plus 30 microM of genistein. After treatments, PC-3 cells were assayed for cell proliferation, induction of apoptosis, and alteration in gene and protein expression using cell inhibition assay, apoptosis assay, microarray analysis, real-time RT-PCR, and Western Blot analysis. RESULTS: SB715992 inhibited cell proliferation and induced apoptosis in PC-3 cells. SB715992 was found to regulate the expression of genes related to the control of cell proliferation, cell cycle, cell signaling pathways, and apoptosis. In addition, our results showed that combination treatment with SB715992 and genistein caused significantly greater cell growth inhibition and induction of apoptosis compared to the effects of either agent alone. CONCLUSION: Our results clearly show that SB715992 is a potent anti-tumor agent whose therapeutic effects could be enhanced by genistein. Hence, we believe that SB715992 could be a novel agent for the treatment of prostate cancer with greater success when combined with a non-toxic natural agent like genistein.  (+info)

Preplaced cell division: a critical mechanism of autoprotection against S-1,2-dichlorovinyl-L-cysteine-induced acute renal failure and death in mice. (7/74)

Previous studies have shown that renal injury initiated by a lethal dose of S-1,2-dichlorovinyl-l-cysteine (DCVC) progresses due to inhibition of cell division and hence renal repair, leading to acute renal failure (ARF) and death in mice. Renal injury initiated by low to moderate doses of DCVC is repaired by timely and adequate stimulation of renal cell division, tubular repair, restoration of renal structure and function leading to survival of mice. Recent studies have established that mice primed with a low dose of DCVC (15 mg/kg i.p.) 72 h before administration of a normally lethal dose (75 mg/kg i.p.) are protected from ARF and death (nephro-autoprotection). We showed that renal cell division and tissue repair stimulated by the low dose are sustained even after the lethal dose administration resulting in survival from ARF and death. If renal cell division induced by the low dose is indeed the critical mechanism of this autoprotection, then its ablation by the antimitotic agent colchicine (1.5 mg CLC/kg i.p.) should abolish autoprotection. The present interventional experiments were designed to test the hypothesis that DCVC autoprotection is due to stimulated cell division and tissue repair by the priming low dose. CLC intervention at 42 and 66 h after the priming dose resulted in marked progressive elevation of plasma blood urea nitrogen and creatinine resulting in ARF and death of mice. Light microscopic examination of hematoxylin and eosin-stained kidney sections revealed progression of renal necrosis concordant with progressively failing renal function. With CLC intervention, S-phase stimulation (as assessed by BrdU pulse labeling), G(1)-to-S phase clearance, and cell division were diminished essentially abolishing the promitogenic effect of the priming low dose of DCVC. Phospho-retinoblastoma protein (P-pRB), a crucial protein for S-phase stimulation, and other cellular signaling mechanisms regulating P-pRB were investigated. We report that decreased P-pRB via activation of protein phosphatase-1 by CLC is the critical mechanism of this inhibited S-phase stimulation and ablation of autoprotection with CLC intervention. These findings lend additional support to the notion that stimulated cell division and renal tissue repair by the priming dose of DCVC are the critical mechanisms that allow sustained compensatory tissue repair and survival of mice in nephro-autoprotection.  (+info)

A thalidomide analogue with in vitro antiproliferative, antimitotic, and microtubule-stabilizing activities. (8/74)

We discovered a thalidomide analogue [5-hydroxy-(2,6-diisopropylphenyl)-1H-isoindole-1,3-dione (5HPP-33)] with antiproliferative activity against nine cancer cell lines in vitro. Flow cytometric analyses showed that the compound caused G2-M arrest, which occurred mainly at the mitotic phase. In addition, immunofluorescence microscopy and in vitro tubulin polymerization studies showed that 5HPP-33 has antimicrotubule activity with a paclitaxel-like mode of action. It is effective against four different paclitaxel-resistant cell lines. Thus, 5HPP-33 represents a potential antitumor agent.  (+info)

*Amikhelline

Characterization of chromosomal aberrations induced in man by various antimitotic agents. (French). Comptes Rendus des Seances ... Amikhelline is an antimitotic drug. It acts as a DNA intercalator and inhibits DNA polymerase. Turchini MF, Geneix A, Perissel ...

*Rhizoxin

... is an antimitotic agent with anti-tumor activity. It is isolated from a pathogenic plant fungus (Rhizopus microsporus ... Anti-mitotic and anti-tubulin activity of new antitumor antibiotics, rhizoxin and its homologues". J. Antibiot. 40 (1): 66-72. ... 1986). "Rhizoxin, a macrocyclic lactone antibiotic, as a new antitumor agent against human and murine tumor cells and their ... Ikubo, S., et al., (1999). "In vitro evaluation of antimicrotubule agents in human small-cell lung cancer cell lines". ...

*DPP7

Roberts VJ, Gorenstein C (1990). "The effect of antimitotic agents on the intraneuronal distribution of lysosomes". Brain Res. ...

*Plant tissue culture

This is usually achieved by application of antimitotic agents such as colchicine or oryzalin. As a tissue for transformation, ... Solid media are prepared from liquid media with the addition of a gelling agent, usually purified agar. The composition of the ... The hard surface of the seed is less permeable to penetration of harsh surface sterilizing agents, such as hypochlorite, so the ...

*Monomethyl auristatin F

... is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin. It is ... Monomethyl auristatin F (MMAF) is a synthetic antineoplastic agent. It is part of some experimental anti-cancer antibody-drug ...

*Monomethyl auristatin E

... is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin. The ... These drugs show potency of up to 200 times that of vinblastine, another antimitotic drug used for Hodgkin lymphoma as well as ... Monomethyl auristatin E (MMAE) is a synthetic antineoplastic agent. Because of its toxicity, it cannot be used as a drug itself ... It is a potent antimitotic drug derived from peptides occurring in marine shell-less mollusc Dolabella auricularia called ...

*Spindle poison

Two specific families of antimitotic agents, vinca alkaloids and taxanes, interrupt the cell's division by the agitation of ... Agents that affect the motor proteinkinesin are beginning to enter clinical trials. Another type, Paclitaxel, acts by attaching ... Even though numerous other spindle proteins exist that could be the target of novel chemotherapeutics, tubulin-binding agents ...

*Neoxaline

It is an antimitotic agent and shows weak inhibitory activity of blood platelet aggregation induced by simulation of the ... Neoxaline an antimiotic agent Hirano, A; Iwai, Y; Masuma, R; Tei, K; Omura, S (1979). "Neoxaline, a new alkaloid produced by ...

*Discovery and development of tubulin inhibitors

E7010 is the most active of sulfonamide antimitotic agent, which has been shown to inhibit microtubule formation by binding at ... Currently have been suggested few approaches in development of novel therapeutic agents with better properties Discovery agents ... Play media Agents which act as inhibitors of tubulin, also act as inhibitors of cell division. Microtubule exists in a ... Antivascular agents are similar to colchicine and bind to the colchicine binding site on β-tubulin so development of novel ...

*Volasertib

Common side effects as seen with other antimitotic agents such as vinca alkaloids and taxanes which include neuropathy, have ... investigating the effects of Volasertib both as a single agent and in combination with other agents in solid tumors and ... Volasertib can also cause cell death in cancer cells that have are no longer sensitive to existing anti-mitotic drugs such as ... protein being developed by Boehringer Ingelheim for use as an anti-cancer agent. Volasertib is the second in a novel class of ...

*Curacin A

... the Potent Colchicine Site Antimitotic Agent, with Tubulin and Effects of Analogs on the Growth of MCF-7 Breast Cancer Cells". ...

*List of MeSH codes (D16)

... antimitotic agents MeSH D27.505.954.248.150 --- antineoplastic agents, alkylating MeSH D27.505.954.248.169 --- antineoplastic ... anti-allergic agents MeSH D27.505.954.122 --- anti-infective agents MeSH D27.505.954.122.085 --- anti-bacterial agents MeSH ... antiviral agents MeSH D27.505.954.122.388.077 --- anti-retroviral agents MeSH D27.505.954.122.388.077.088 --- anti-hiv agents ... renal agents MeSH D27.505.954.613.056 --- anti-infective agents, urinary MeSH D27.505.954.613.860 --- uricosuric agents MeSH ...

*Index of oncology articles

... antimicrotubule agent - antimitotic agent - antineoplastic - antineoplastic antibiotic - antioxidant - antiparasitic - ... alkylating agent - ALL - all-trans retinoic acid - allogeneic - allogeneic bone marrow transplantation - allogeneic stem cell ... adjunct agent - adjunctive therapy - adjuvant therapy - adrenocortical - Adriamycin - adult T-cell leukemia/lymphoma - AE-941 ... chemotherapeutic agent - chemotherapy - chemotherapy-induced peripheral neuropathy - chest x-ray - chiasma - child-life worker ...

*Brentuximab vedotin

... and para-aminobenzylcarbamate spacers to three to five units of the antimitotic agent monomethyl auristatin E (MMAE, reflected ... These results demonstrated that single-agent brentuximab vedotin induced a 42% objective response rate and manageable safety ...

*Moroidin

... has no anti-mitotic activity. Interestingly, other anti-tubulin agents used as chemotherapy agents have painful side effects ... Of this family, celogentin C is the most potent (IC50 0.8×10−6 M), and it is more potent than the anti-mitotic agent ... It also has demonstrated anti-mitotic properties, specifically by inhibition of tubulin polymerization. Anti-mitotic activity ... Agents that disrupt microtubules therefore inhibit mitosis through activation of this checkpoint. Moroidin and its related ...

*2,5-Diketopiperazine

... verruculogen and the spiro-annulated spirotryprostatin B which represent a promising class of antimitotic arrest agents, to the ... Derivatives of cyclo(L-His-L-Pro) have been studied extensively to develop therapeutic agents for neurodegeneration. The 2,5- ... The unsaturated derivatives are illustrated by phenylahistin the anti-cancer microtubule binding agent, and the mycotoxin ... an antibacterial agent used as food additives to prevent diarrhea in animals while the thio derivatives such as the cytotoxic ...

*Endogenous regeneration

... migrating neuroblasts and immature precursors are silenced with the anti-mitotic agent and astrocytes are infected with a ...

*Vinca alkaloid

... s are a set of anti-mitotic and anti-microtubule alkaloid agents originally derived from the periwinkle plant ... The newer semi-synthetic chemotherapeutic agent vinorelbine is used in the treatment of non-small-cell lung cancer and is not ... leurosine and the chemotherapy agents vinblastine and vincristine, all of which can be obtained from the plant. ...

*Small molecule drug conjugate

The most advanced SMDC is vintafolide, a derivative of the anti-mitotic chemotherapy drug vinblastine which is chemically ... as well as a companion imaging agent that is created by replacing the potent drug with an imaging agent. http://www. ...

*Fisetin

It can be found in many plants, where it serves as a colouring agent. It is also found in many fruits and vegetables, such as ... In vitro screening has identified fisetin as an antimitotic compound. Sahu, Bidya Dhar; Kalvala, Anil Kumar; Koneru, Meghana; ... In lab studies it also has been shown to be an anti-proliferative agent, interfering with the cell cycle in several ways. ... Fisetin also has direct activity as a reducing agent, chemically reacting with reactive oxygen species to neutralize them. ...

*Kinesin family member 11

Zhang Y, Xu W (August 2008). "Progress on kinesin spindle protein inhibitors as anti-cancer agents". Anticancer Agents Med Chem ... Compton DA (October 1999). "New tools for the antimitotic toolbox". Science. 286 (5441): 913-4. doi:10.1126/science.286.5441. ... El-Nassan HB (2012). "Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents". Eur J Med ... Inhibitors of KIF11 have been developed as chemotherapeutic agents in the treatment of cancer. Drugs that specifically inhibit ...

*Chemotherapy

Siddik ZH (2005). Mechanisms of Action of Cancer Chemotherapeutic Agents: DNA-Interactive Alkylating Agents and Antitumour ... of the side effects of chemotherapy can be traced to damage to normal cells that divide rapidly and are thus sensitive to anti-mitotic ... Alkylating agents will work at any point in the cell cycle and thus are known as cell cycle-independent drugs. For this reason ... Unlike alkylating agents, anti-metabolites are cell cycle dependent. This means that they only work during a specific part of ...

*Vinflunine

"Antimitotic and tubulin-interacting properties of vinflunine, a novel fluorinated Vinca alkaloid". Biochem. Pharmacol. 55 (5): ... vinflunine is the only commercially-approved agent in some countries for salvage therapy of urothelial carcinoma, (with ...

*Eribulin

Anticancer agents from natural products. Washington, DC: Taylor & Francis. ISBN 0-8493-1863-7. CS1 maint: Multiple names: ... Kawano, S; Asano, M; Adachi, Y; Matsui, J (2016). "Antimitotic and Non-mitotic Effects of Eribulin Mesilate in Soft Tissue ... In addition to its cytotoxic, antimitotic-based mechanisms, preclinical studies in human breast cancer models have shown that ... Its cytotoxic effects are related to its antimitotic activities, wherein apoptosis of cancer cells is induced following ...

*Halichondria

"The primary antimitotic mechanism of action of the synthetic halichondrin E7389 is suppression of microtubule growth". ... Anticancer agents from natural products. Washington, DC: Taylor & Francis. ISBN 978-0-8493-1863-4. OCLC 57169963. Hirata, ...

*Recombinant AAV mediated genome engineering

2010 The use of 'X-MAN' mutant PI3CA increases the expression of individual tubulin isoforms and promoted resistance to anti-mitotic ... Carroll D (November 2008). "Progress and prospects: zinc-finger nucleases as gene therapy agents". Gene Ther. 15 (22): 1463-8. ...
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Cell cycle arrest of malignant cells is an important option for cancer treatment. In this study, we modified the structure of antimitotic 2-phenylindole-3-carbaldehydes by condensation with hydrazides of various benzoic and pyridine carboxylic acids. The resulting hydrazones inhibited the growth of MDA-MB 231 and MCF-7 breast cancer cells with IC(50) values of 20-30 nM for the most potent derivatives. These 2-phenylindole derivatives also exerted an inhibitory effect on the growth of both proliferating and resting U-373 MG glioblastoma cells. Though the hydrazones exhibited similar structure-activity relationships as the aldehydes, they did not inhibit tubulin polymerization as the aldehydes but were capable of blocking the cell cycle in G(2)/M phase. The cell cycle arrest was accompanied by apoptosis as demonstrated by the activation of caspase-3. Since these 2-phenylindole-based hydrazones display no structural similarity with other antitumor drugs they are interesting candidates for further ...
Intervention of cancer cell mitosis by antitubulin drugs is among the most effective cancer chemotherapies. However, antitubulin drugs have dose-limiting side effects due to important functions of microtubules in resting normal cells and are often rendered to be ineffective by rapid emergence of resistance. Antimitotic agents with different mechanisms of action and improved safety profiles are needed as new treatment options. Mitosis-specific kinesin Eg5 represents an attractive anticancer target for discovering such new antimitotic agents, because Eg5 is essential only in mitotic progression and has no roles in resting, non-dividing cells. Here we show that a novel selective Eg5 inhibitor LY2523355 has broad target-mediated anticancer activity in vitro and in vivo. LY2523355 arrests cancer cells at mitosis and causes rapid cell death that requires sustained spindle-assembly checkpoint (SAC) activation with a required threshold concentration. In vivo efficacy of LY2523355 is highly ...
Patients with ovarian high-grade serous carcinoma (HGSC) initially respond to treatment with the chemotherapeutic agents carboplatin and paclitaxel, but frequently experience tumor relapse. However, the mechanisms underlying the development of resistance to these drugs remain poorly understood. Yu and colleagues found that the levels of spleen tyrosine kinase (SYK) and phosphorylated SYK were increased in recurrent ovarian tumors isolated from patients previously treated with carboplatin and paclitaxel compared with matched primary untreated tumors. In addition, SYK expression and activation were upregulated in paclitaxel-resistant ovarian cancer cell lines and positively correlated with paclitaxel response in vitro, suggesting that SYK overexpression may confer chemoresistance. SYK inactivation via knockdown or pharmacologic inhibition with the active metabolite of fostamatinib, R406, impaired the growth of ovarian cancer cells and synergistically enhanced the sensitivity of ...
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Biological activities of the 1,4-benzoquinone derivatives 5-O-ethylembelin (1) and 5-O-methylembelin (2) were investigated. Both of them showed anti proliferative activity against a panel of human tumor cell lines upon comparison to normal marsupial kidney cells (PtK2). They arrested HL-60 cells in the G(0)/G(1) phase of the cell cycle in a dose- and time-dependent manner. In HeLa cells, exposure to 100 mu M of 1 or 2 for 6 h induced a complete disassembly of the microtubule network and an increased number of cells blocked in mitotic stages. Treatment with 10 mu M of 1 and 2 for 24 h induced apoptosis in HL-60 cells. This evidence suggests that both 1 and 2 are promising novel antimitotic and anticancer molecules targeting microtubular proteins. ...
Abstract Background Kinesin spindle proteins (KSP) are motor proteins that play an essential role in mitotic spindle formation. HsEg5, a KSP, is responsible for the formation of the bipolar spindle, which is critical for proper cell division during mitosis. The function of HsEg5 provides a novel target for the manipulation of the cell cycle and the induction of apoptosis. SB715992, an experimental KSP inhibitor, has been shown to perturb bipolar spindle formation, thus making it an excellent candidate for anti-cancer agent. Our major objective was a) to investigate the cell growth inhibitory effects of SB715992 on PC-3 human prostate cancer cell line, b) to investigate whether the growth inhibitory effects of SB715992 could be enhanced when combined with genistein, a naturally occurring isoflavone and, c) to determine gene expression profile to establish molecular mechanism of action of SB715992. Methods PC-3 cells were treated with varying concentration of SB715992, 30 μM of genistein, and SB715992
0038] Pharmacological agents suitable for inclusion in prosthesis materials and/or coatings, according to embodiments of the present invention include, but are not limited to, drugs and other biologically active materials, and may be intended to perform a variety of functions, including, but not limited to: anti-cancer treatment (e.g., Resan), anti-clotting or anti-platelet formation, the prevention of smooth muscle cell growth and migration on a vessel wall, and cell cycle inhibitors. Pharmacological agentsmay include antineoplastics, antimitotics, antiinflammatories, antiplatelets, anticoagulants, antifibrins, antithrombins, antiproliferatives, antibiotics, antioxidants, immunosuppressives, and antiallergic substances as well as combinations thereof. Examples of such antineoplastics and/or antimitotics include paclitaxel (e.g., TAXOL® by Bristol-Myers Squibb Co., Stamford, Conn.), docetaxel (e.g., TAXOTERE® from Aventis S. A., Frankfurt, Germany) methotrexate, azathioprine, vincristine, ...
Drugs that block mitosis; the term is often used of those which cause metaphase arrest such as colchicine and the vinca alkaloids. Many anti tumour drugs are antimitotic, blocking proliferation rather than being cytotoxic
Amikhelline is an antimitotic drug. It acts as a DNA intercalator and inhibits DNA polymerase. Turchini MF, Geneix A, Perissel B, Malet P, Turchini JP. Characterization of chromosomal aberrations induced in man by various antimitotic agents. (French). Comptes Rendus des Seances de la Societe de Biologie et de ses Filiales. 1985;179(3):331-9. PMID 2417673 Rucheton M, Jeanteur P. Studies on amikhellin. I. Intercalative binding to double-stranded DNA. Biochimie. 1973;55(11):1415-20. PMID 4364376 Rucheton M, Jeanteur P. Studies on amikhellin. II.-Inhibition of dna-polymerase from murine sarcoma leukemia virus. Biochimie. 1976;58(6):689-95. PMID ...
Overexpression of the anti-apoptotic factor, BCL-2, is a frequent feature of malignant disease and is commonly associated with poor prognosis and resistance to conventional chemotherapy. In breast cancer, however, high BCL-2 expression is associated with favourable prognosis, estrogen receptor (ER) positivity and low tumour grade; whilst low expression is included in several molecular signatures associated with resistance to endocrine therapy. In the present study, we correlate BCL-2 expression and DNA methylation profiles in human breast cancer and in multiple cell models of acquired endocrine-resistance to determine whether BCL-2 hypermethylation could provide a useful biomarker of response to cytotoxic therapy. In human disease, diminished expression of BCL-2 was associated with hypermethylation of the second exon, in a region that overlapped a CpG island and an ER-binding site. Hypermethylation of this region, which occurred in 10% of primary tumours, provided a stronger predictor of patient
Understanding the molecular mechanisms of action of antitumor agents is significant for advancing fundamental knowledge and for improvement in cancer treatment....
Name: Drug, bio-affecting and body treating compositions > Designated organic active ingredient containing (doai) > Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., o,s,se or te) or nitrogen as the only ring hetero atoms doai > Hetero ring is seven-membered consisting of two nitrogens and five carbon atoms > Polycyclo ring system having the seven-membered hetero ring as one of the cyclos > Bicyclo ring system having the seven-membered hetero ring as one of the ...
Name: Drug, bio-affecting and body treating compositions > Designated organic active ingredient containing (doai) > Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., o,s,se or te) or nitrogen as the only ring hetero atoms doai > Hetero ring is seven-membered consisting of two nitrogens and five carbon atoms > Polycyclo ring system having the seven-membered hetero ring as one of the cyclos > Tricyclo ring system having the seven-membered hetero ring as one of the ...
The central role of cyclin-dependent kinases (CDKs) in cell cycle regulation makes them a promising target for studying inhibitory molecules that can modify the degree of cell proliferation. The discovery of specific inhibitors of CDKs such as polyhydroxylated flavones has opened the way to investigation and design of antimitotic compounds. A novel flavone, (-)-cis-5,7-dihydroxyphenyl-8-[4-(3-hydroxy-1-methyl)piperidinyl] -4H-1-benzopyran-4-one hydrochloride hemihydrate (L868276), is a potent inhibitor of CDKs. A chlorinated form, flavopiridol, is currently in phase I clinical trials as a drug against breast tumors. We determined the crystal structure of a complex between CDK2 and L868276 at 2.33 angstroms resolution and refined to an Rfactor 20.3%. The aromatic portion of the inhibitor binds to the adenine-binding pocket of CDK2, and the position of the phenyl group of the inhibitor enables the inhibitor to make contacts with the enzyme not observed in the ATP complex structure. The analysis of ...
Free Online Library: Onconova Therapeutics Announces Presentation of Nonclinical Data on Lead Compound ON 01910.Na and New Jak 2/Bcr-abl Inhibitors at AACR.(Clinical report) by Business Wire; Business, international Antimitotic agents Antineoplastic agents Cancer Care and treatment Cancer treatment
Activation of Phenyl 4-(2-Oxo-3-alkylimidazolidin-1-yl)benzenesulfonates Prodrugs by CYP1A1 as New Antimitotics Targeting Breast Cancer Cells J. Med. Chem. 2017 [CYP1A1 ...
Activation of Phenyl 4-(2-Oxo-3-alkylimidazolidin-1-yl)benzenesulfonates Prodrugs by CYP1A1 as New Antimitotics Targeting Breast Cancer Cells J. Med. Chem. 2017 [CYP1A1 ...
Mouse Monoclonal Anti-Mitotic Cells Antibody (8B3G) [DyLight 488]. Validated: Flow, ICC/IF. Tested Reactivity: Human. 100% Guaranteed.
The application discloses novel 2-alkoxyestradiol analogs which exhibit anti-proliferative properties, and methods of making and using such compounds to inhibit undesired cell proliferation and tumor growth. Additionally, methods are disclosed of treating diseases associated with undesired angiogenesis and undesired proliferation, and methods of treating infectious disease wherein the infectious agent is particularly susceptible to inhibition by agents that disrupt microtubule organization and function.
Synonyms for hetero chromosomes at Thesaurus.com with free online thesaurus, antonyms, and definitions. Dictionary and Word of the Day.
BACKGROUND : Autophagy can either be protective and confer survival to stressed cells, or it can contribute to cell death. The antimitotic drug 2-ethyl-3-O-sulpamoyl-estra-1,3,5(10),15-tetraen-17-ol (ESE-15-ol) is an in ...
Buy Dinitramine (CAS 29091-05-2), a water soluble plant and parasite-selective antimitotic, microtubule disrupting agent. Join researchers using high quality…
ABT-751 (CAS: 857447-92-8) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 μM in neuroblastoma and non-neuroblastoma cell lines, respectively. ABT-751 binds to the colchicine-binding site on beta-tu
Fisetin is a natural flavonol present in edible vegetables, fruits and wine at 2-160 microg/g concentrations and an ingredient in nutritional supplements with much higher concentrations. The compound has been reported to exert anticarcinogenic effects as well as antioxidant and anti-inflammatory activity via its ability to act as an inhibitor of cell proliferation and free radical scavenger, respectively. Our cell-based high-throughput screen for small molecules that override chemically induced mitotic arrest identified fisetin as an antimitotic compound. Fisetin rapidly compromised microtubule drug-induced mitotic block in a proteasome-dependent manner in several human cell lines. Moreover, in unperturbed human cancer cells fisetin caused premature initiation of chromosome segregation and exit from mitosis without normal cytokinesis. To understand the molecular mechanism behind these mitotic errors, we analyzed the consequences of fisetin treatment on the localization and phoshorylation of ...
Vincristine is the active ingredient in a drug used to treat acute leukemia. It is used in combination with other drugs to treat Hodgkin disease, non-Hodgkin lymphoma, rhabdomyosarcoma, neuroblastoma, and Wilms tumor. Vincristine is also being studied in the treatment of other types of cancer. It blocks cell growth by stopping cell division. It is a type of vinca alkaloid and a type of antimitotic agent ...
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Polyamine analogues have been shown to have antitumor activity as single agents in multiple experimental model systems (7, 8, 9, 10, 11, 12, 13, 14) . Their ability to modulate response to chemotherapeutic agents is worthy of study. This study addressed the activity of two polyamine analogues, CPENSpm and CHENSpm, in combination with multiple chemotherapeutic agents in breast cancer cell lines. The chemotherapeutic agents used were selected because they: (a) have antitumor activity in breast cancer; (b) are currently in use in the treatment of breast cancer; and (c) represent a broad spectrum of mechanisms of action. They include alkylating agents (4HC), topoisomerase II inhibitors (doxorubicin), antimetabolites (5-FU and FdURd), antimitotic agents (vinorelbine, paclitaxel, and docetaxel), and the DNA-reactive agent, c-DDP, which causes both intra- and interstrand DNA adducts.. Synergistic combinations were identified using one or both of the polyamine analogues in all of the cell lines ...
Free Online Library: Research and Markets: This Essential Report on Cancer Drug Resistance is Available Now. by Business Wire; Business, international Antimitotic agents Market research Reports Antineoplastic agents Care and treatment Drug therapy Cancer research Cancer treatment Drug resistance in microorganisms Microbial drug resistance Oncology, Experimental Pharmaceutical industry
The antimitotic agent docetaxel is the standard therapy for patients with hormone-refractory prostate cancer (HRPC), but fatal resistance ultimately develops despite an initial response. Domingo-Domenech and colleagues generated docetaxel-resistant HRPC cell lines to gain insight into the underlying resistance mechanisms and identify potential targets to prevent the development of docetaxel resistance in HRPC. Docetaxel-resistant cells showed downregulation of epithelial differentiation markers such as cytokeratins (CK) and a marked upregulation of developmental genes in the Notch and Hedgehog signaling pathways. To determine whether these observations had clinical relevance, the authors evaluated a panel of primary and metastatic prostate cancer samples and identified a small subpopulation of preexisting CK-negative cells with upregulated Notch and Hedgehog signaling in each tumor. Of note, these cells were more abundant in samples from patients with advanced disease and a higher percentage of ...
Article Title : Targeting Urokinase and the Transferrin Receptor with Novel, Anti-Mitotic N-Alkylisatin Cytotoxin Conjugates Causes Selective Cancer Cell Death and Reduces Tumor ...
Computational models have been playing a significant role for the computer-based analysis of biological and biomedical data. Given the recent availability of genomic sequences and microarray gene expression data, there is an increasing demand for developing and applying advanced computational techniques for exploring these types of data such as functional interpretation of gene expression data, deciphering of how genes and proteins work together in pathways and networks, extracting and analysing phenotypic features of mitotic cells for high throughput screening of novel anti-mitotic drugs. Successful applications of advanced computational algorithms to solving modern life-science problems will make significant impacts on several important and promising issues related to genomic medicine, molecular imaging, and the scientific knowledge of the genetic basis of diseases ...
Jim Wells (UCSF) gave a magisterial keynote address that emphasized how useful fragments can be for tackling difficult targets such as protein-protein interactions (PPIs). In fact, many of the talks in the protein-protein interaction track relied on fragments. Thats not to say its easy. Rod Hubbard (University of York and Vernalis) emphasized that advancing fragments to leads against such targets can take a long time and often requires patience that strains the management of many organizations. Fragment hits against PPIs usually have lower ligand efficiencies (0.23-0.25 kcal/mol/HA if youre lucky), and improving potency can be a bear. Rhian Holvey (University of Cambridge) presented a nice example of how she was able to find millimolar fragments that bind to the anti-mitotic target TPX2, potentially blocking its interaction with importin-alpha, but even structural information was not enough to get to potent inhibitors ...
Numerous compounds are known which are useful in the prevention and treatment of various types of cancer. In order to effectively deliver these compounds by intravenous administration, it is generally preferred that the compounds be in solution to avoid or reduce the risk of blood clotting or other adverse effects that could result if the compounds were delivered in particulate form. Unfortunately, many of these compounds have poor solubility in water, the preferred solvent, and must be delivered using solvents which can cause adverse patient reactions that must in turn be prevented or controlled through the administration of other compounds. For example, paclitaxel is a known inhibitor of cell division or mitosis and is widely used in the treatment of ovarian, breast, lung, esophageal, bladder, head and neck cancers. Paclitaxel is a natural product originally purified from the bark of yew trees, but now obtained by semisynthesis from 10-desacetylbaccatin, a precursor purified from yew leaves. ...
PubMed comprises more than 30 million citations for biomedical literature from MEDLINE, life science journals, and online books. Citations may include links to full-text content from PubMed Central and publisher web sites.
Buy Ampilin 1gm Injection - vial of 1 Injection at online at 1mg.com. Know the uses, side effects, price, composition, substitutes, How it works, Precautions and Expert Advice for Ampilin 1gm Injection manufactured by Hetero Drugs Ltd
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select /*+ index(customs_tariff_heading,description_of_goods,port_of_destination,country_code,indian_Port,unit_quantity_code,file_date) */ SQL_CALC_FOUND_ROWS id,port_of_destination as port_of_destination,description_of_goods,customs_tariff_heading,quantity,unit_quantity_code,country_code,value_of_goods_in_rupees,indian_Port,unit_value,date_format(file_date,%d-%b-%y) as date_time from eximpuls_export.export_master where 1=1 and match(description_of_goods)Against(+Hetero +Ltd IN BOOLEAN MODE) order by sort_date desc limit 50 offset ...
Purplepen -. It may well be true that everything else being equal, two hetero parents are prefferable to same sex parents. The juries still out, every study that I have seen thus far has been dubious at best. It will be a few more years before sample sizes can provide any definitive data. The only reasonable study thus far is out of Sweden, which really wouldnt apply to U.S. culture.. For the sake of argument and in the face of a dearth of reliable data, Ill capitulate that there are some advantages to two hetero parents raising children in the U.S. This doesnt change anything I said. This does not change the fact that the children of same sex couples, are just as deserving of the legal security that marriage provides their hetero parented counterparts. Nor does it mean that their parents relationship is any less valid than that of heteros. The only thing that is remotely in question, is whether their family unit is somehow inferior to that of their hetero parented counterparts, everything ...
Founded in 2001, Hetero Labs Ltd. is a large organization in the pharmaceutical preparation companies industry located in Hyderabad, India. It generates $595 million in annual revenue.
Important to note that the learned Judge knowing that there is no legal provision to restrain the DCGI from approving the application for generic Dasatinib, has diligently and aptly used the word ought while referring BMS ex parte relief of restraining Hetero from pursuing application before the DCGI. In fact, the Delhi HC order finds reasonable support in Sec. 2 of the Drugs & Cosmetic Act, 1940 (DCA) which states that the provisions under DCA shall be in addition to and not in derogation of any other law for the time being in force. Further it is important to note that this is just a temporary order which is passed to stop Hetero generic dasatinib during the pendency of the trial and also the order is restrictively limited to Hetero case. Till here, both the Delhi HC and BMS acted within the periphery of the law. The order nowhere creates any patent-drug regulatory linkage or authorizes the DCGI to monitor drug patents and framing such an opinion at this moment when the Delhi HC has not ...
The report presents a summary of a study of the products and mechanisms of reactions wherein unsaturated systems containing nitrogen or sulfur are photolyzed. Included are studies of (1) the photochemical Beckmann rearrangement, (2) the general heteroatom transfer, (3) coumalin dimerization, and (4) the photolytic decomposition of beta-ketosulphones. (Author)(*PHOTOCHEMICAL REACTIONS
F. Hoffman La-Roche, Gilead Sciences Inc, Hetero Labs Ltd, Janssen Scientific Affairs, Lupin Pharmaceuticals, Merck & Co. Inc, Mylan ...
A general redox‐neutral approach into the o‐,o′‐heteroatom‐linked N‐(hetero)aryl‐imidazole family of heteroaromatics has been developed. New types of ...
0112] A drug or active agent can include, but is not limited to, any substance capable of exerting a therapeutic, prophylactic, or diagnostic effect. The drugs for use in the implantable medical device, such as a stent or non-load bearing scaffolding structure may be of any or a combination of a therapeutic, prophylactic, or diagnostic agent. Examples of active agents include antiproliferative substances such as actinomycin D, or derivatives and analogs thereof (manufactured by Sigma-Aldrich 1001 West Saint Paul Avenue, Milwaukee, Wis. 53233; or COSMEGEN available from Merck). Synonyms of actinomycin D include dactinomycin, actinomycin IV, actinomycin I1, actinomycin X1, and actinomycin C1. The bioactive agent can also fall under the genus of antineoplastic, anti-inflammatory, antiplatelet, anticoagulant, antifibrin, antithrombin, antimitotic, antibiotic, antiallergic and antioxidant substances. Examples of such antineoplastics and/or antimitotics include paclitaxel, (e.g., TAXOL® by ...
The present invention provides tricyclic compounds, pharmaceutically acceptable salts, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-gl
Cellular factors may contribute to the decreased efficacy of chemotherapy in HIV infection. Indeed, prolonged treatment with nucleoside analogues, such as azidothymidine (AZT), 2′,3′-deoxycytidine or 9-(2-phosphonylmethoxyethyl)adenine, induces cellular resistance. We have developed a human T lymphoblastoid cell line (CEM3TC) that is selectively resistant to the antiproliferative effect of 2′,3′-dideoxy-3′-thiacytidine (3TC) because the CEM3TC cells were equally sensitive to AZT, as well as the antimitotic agent, vinblastine. The anti-retroviral activity of 3TC against HIV-1 was also severely impaired in the CEM3TC cells. Despite similar deoxycytidine kinase activity and unchanged uptake of nucleosides such as AZT and 2′-deoxycytidine, CEM3TC had profoundly impaired 3TC accumulation. Further studies indicated that CEM3TC retained much less 3TC. However, despite a small overexpression of multidrug resistance protein (MRP) 4, additional studies with cells specifically engineered to ...
Podofilox, also called podophyllotoxin, is a purer and more stable form of podophyllin in which only the biologically active portion of the compound is present. Podofilox is used to remove certain types of warts on the outside skin of the genital areas ...
Podofilox, also called podophyllotoxin, is a purer and more stable form of podophyllin in which only the biologically active portion of the compound is present. Podofilox is used to remove certain types of warts on the outside skin of the genital areas ...
In this overview we describe the main plant-derived bioactive compounds used in cancer therapy which has the cell cytoskeleton as therapeutic target. Three major classes of these compounds are described: antimitotics with microtubule-destabilizing and-stabilizing effects, plant-bioactive compounds that interact with intermediate filaments/actin, and plant-bioactive compounds that interact with intermediate filaments like keratins and vimentin. We also focus on the molecular aspects of interactions with their cellular targets: microtubules, intermediate filaments, and microfilaments. Some critical aspects of cardiac side effects of cancer chemotherapy are also discussed, focusing on cardiac cytoskeleton and protective effect of plant-derived compounds. The application of plant bioactives in the treatment of cancer has resulted in increased therapeutic efficacy through targeting the cytoskeleton, respectively, prevention of the injury of cytoskeletal components elicited by chemotherapeutics.
We are leading Docetrust Tablets distributers , dealers & suppliers in Mumbai. Docetrust Tablets (trade name Taxotere) is a clinically well established anti-mitotic .Nephrology Medicines
Background: TTFields is an established antimitotic treatment modality delivered to patients by a portable, home use, medical device. Here we evaluate whether this antimitotic effect can be translated into improved survival in a clinical setting. Based on a pre-specified interim analysis on 315 patients, the IDMC recommended early trial closure; we here report the first analysis of the full dataset of 700 randomized patients. Methods: This prospective phase 3 trial randomized patients with newly diagnosed glioblastoma, after completion of concomitant chemoradiotherapy, to receive either adjuvant temozolomide (TMZ) chemotherapy alone, or TMZ with TTFields (TTF/TMZ). The primary endpoint was progression-free survival, with overall survival, safety, cognitive function and quality of life as secondary endpoints. Results: (ITT) From 2009 to 2014, 700 Grade IV astrocytoma (glioblastoma) patients (68% male) were randomized 2:1. Patient characteristics were well balanced: median age was 56 and 57 years ...
The process for the production of light olefins from a feedstock comprising at least an aliphatic hetero compound comprising contacting said feedstock with a silicoaluminophosphate molecular sieve of U.S. Pat. No. 4,440,871 at effective process conditions to produce light olefins.
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Eribulin is a medicine available in a number of countries worldwide. A list of US medications equivalent to Eribulin is available on the Drugs.com website.
BioAssay record AID 242686 submitted by ChEMBL: In vitro inhibitory concentration towards kinesin spindle protein activity of ATP hydrolysis in the presence of microtubules measured by ATPase assay (n=3).
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Monomethyl auristatin E (MMAE; Vedotin) is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin. Buy Microtubule inhibitor Monomethyl auristatin E (MMAE, Vedotin) from AbMole BioScience.
Detailed, critical reviews on chemotherapy of trichomoniasis, and cestode and trematode infections; lysosomes in drug and hormonal activity; polyanions as antimitotic agents. Opening chapter is a concise summary of some statistical methods applicable to chemotherapeutic research (linear regression and correlation, sequential analysis, poisson distribution, nonparametric methods).. Recommended for libraries of medical schools, pharmacological institutes and companies, and clinical pharmacologists. ...
Importance: Podophyllotoxin is an antimitotic agent primarily used in the local treatment of anogenital warts. Data that enable the assessment of the fetal safety of podophyllotoxin use during pregnancy are lacking.. Objective: To investigate the association between local podophyllotoxin exposure during pregnancy and risk of adverse fetal outcomes.. Design, Setting, and Participants: This cohort study obtained individual-level pregnancy data from various nationwide registries in Denmark from the study period of January 1, 1997, through December 31, 2016, resulting in a cohort of 1 650 649 pregnancies. Pregnancies with multiple records on overlapping dates and pregnancy records with implausible or missing information on gestational age were excluded. Local podophyllotoxin-exposed pregnancies were compared with unexposed pregnancies and matched in a 1:10 ratio according to propensity scores on a wide set of baseline characteristics. Five distinct study cohorts were constructed, one for each ...
The microtubule system of the eukaryotic cell plays indispensable role in the process of separating duplicated chromosomes before the cell division. Due to this essential function, they have been an important target for the development of cancer therapeutics. Several natural products such as Taxol, Vinca alkaloids, colchicine and their synthetic analogues that target microtubules have been used to treat several malignancies. However, cancer cells develop resistance to several of these agents by altering drug transporters and signaling pathways. Recently, combretastatins (CA) a group of diarylstilbenes isolated originally from stem wood of the South African tree Combretum caffrum have received much attention due to their potent anticancer activity against wide variety of human cancers including those that are multidrug resistant. These molecules specifically bind to the colchicine-binding site of the tubulins and prevent their polymerization required for the mitotic tubule formation thus ...
Discovered and developed by Eisai, eribulin is a synthetic analog of halichondrin B, a natural product that was isolated from the marine sponge Halichondria okadai. First in the halichondrin class, Halaven is a microtubule dynamics inhibitor. Eribulin is believed to work primarily via a tubulin-based mechanism that causes prolonged and irreversible mitotic blockage, ultimately leading to apoptotic cell death. Additionally, in preclinical studies of human breast cancer, eribulin demonstrated complex effects on the tumor biology of surviving cancer cells, including increases in vascular perfusion resulting in reduced tumor hypoxia, and changes in the expression of genes in tumor specimens associated with a change in phenotype, promoting the epithelial phenotype, opposing the mesenchymal phenotype. Eribulin has also been shown to decrease the migration and invasiveness of human breast cancer cells.. Important Safety Information for Halaven (eribulin mesylate) Injection. Warnings and ...
Usnic acid, a lichen secondary metabolite inhibits Group A Streptococcus biofilms.: Group A Streptococci (GAS) are involved in a number of life threatening dise
Paclitaxel is commercially formulated as Taxol® in a castor oil solvent (Cremophor EL) which is quite toxic and can have serious side effects. Taxol®, a unique anti-mitotic agent, has been approved by the FDA for use in ovarian and breast cancers, and is in clinical use for a number of other indications. Taxol® sales have increased from $50 million in 1992 to approximately $1 billion in 1997, compounding at a rate of 85 % per year. Taxol® is a registered trademark of the Bristol-Myers Squibb Company ...
...Woodcliff Lake N.J. May 15 2008The investigational chemotherapeutic...The anti-tumor activity of eribulin mesylate as observed in this stud...About Study 211Study 211 is a Phase II open-label single-arm study...Of 299 patients enrolled in the study 291 were treated with eribulin ...,Eribulin,mesylate,demonstrated,anti-tumor,activity,in,patients,with,advanced,breast,cancer,biological,biology news articles,biology news today,latest biology news,current biology news,biology newsletters
The cells we identify here as primary precursors for new neurons in the adult hippocampus have the characteristics of astrocytes at the light and electron microscope. They contain multiple processes with intermediate filaments rich in GFAP. Results from three independent experiments support this conclusion. First, many proliferating SGL astrocytes rapidly convert to a cell type that is GFAP negative and that possesses characteristics of D cells. Second, anti-mitotic treatment resulted in the elimination of D cells from the SGL, but neurogenesis returned. Because new neurons are born at a time when [3H]thymidine-labeled astrocytes were observed, we infer that astrocytes function as primary precursors. Finally, we show that SGL astrocytes, specifically labeled with an avian retrovirus, give rise to granule neurons. We observed granule neurons at different stages of maturation by killing animals at different survivals after retroviral infection. Some SGL astrocytes remain labeled with thymidine ...
The process for the production of light olefins from a feedstock comprising at least an aliphatic hetero compound comprising contacting said feedstock with a silicoaluminophosphate molecular sieve of U.S. Pat. No. 4,440,871 at effective process conditions to produce light olefins.
Results from a phase III clinical trial comparing a newer chemotherapy agent called eribulin mesylate with capecitabine showed that eribulin demonstrated a trend toward improved overall survival.
InChI=1/C40H34Cl2N6O6/c1-15(2)27-37-46-29-32(54-37)40-20-9-5-8-19(18-7-6-10-22-25(18)26(33(41)43-22)31-34(42)48-38(29)53-31)28(20)47-39(40)52-24-12-11-17(13-21(24)40)14-23(35(50)45-27)44-36(51)30(49)16(3)4/h5-13,15-16,23,27,30,39,43,47,49H,14H2,1-4H3,(H,44,51)(H,45,50)/t23-,27-,30-,39-,40u /m0/s1/f/h44-45HÂ ChemSpider CID: 10478902Â InChI=1/C40H34Cl2N6O6/c1-15(2)27-37-46-29-32(54-37)40-20-9-5-8-19(18-7-6-10-22-25(18)26(33(41)43-22)31-34(42)48-38(29)53-31)28(20)47-39(40)52-24-12-11-17(13-21(24)40)14-23(35(50)45-27)44-36(51)30(49)16(3)4/h5-13,15-16,23,27,30,39,43,47,49H,14H2,1-4H3,(H,44,51)(H,45,50)/t23?,27-,30-,39?,40-/m0/s1/f/h44-45H Â ChemSpider CID: 17212293Â InChI=1/C40H34Cl2N6O6/c1-15(2)27-37-46-29-32(54-37)40-20-9-5-8-19(18-7-6-10-22-25(18)26(33(41)43-22)31-34(42)48-38(29)53-31)28(20)47-39(40)52-24-12-11-17(13-21(24)40)14-23(35(50)45-27)44-36(51)30(49)1 6(3)4/h5-13,15-16,23,27,30,39,43,47,49H,14H2,1-4H3,(H,44,51)(H,45,50)/t23-,27+,30+,39-,40+/m1/s1Â Totally ...
The in vitro SI Pi agonist activity of the compound of the present invention was evaluated by the increase in the functional bonding activity into the G-Protein of a GTP[y-35S] using the membrane of a human SIPi expressing cell. A cDNA encoding a human SIPi was cloned from a human colorectal cDNA library, and introduced to an expression vector pcDNA3.1 to construct a SlPi-pcDNA3.1. Then, by Lipofectamine 2000 (GIBCO), the SIPrpcDNA3.1 was transfected into a CHO cell, and cultured in a Hams F-12 culture medium containing 10% fetal bovine serum, 100 U/mL Penicillin, 100 ug/mL Streptomycin, and 1 mg/mL G418 disulfate, to obtain a stable, G418-resistant strain. The cultured human SI Pi expressing cells were isolated in a 1 mM EDTA/2Na-containing PBS, and disrupted under ice-cooling by a homogenizer made of glass in a 1 mM Tris HC1 (pH 7.4) buffer solution containing 0.1 mM EDTA and a protein inhibitor. It was centrifuged at 1,400x 10 min, and a supernatant was further centrifuged at 4°C for 60 min ...
Youre joking, right? You dont see a difference between a poster of a guy in boxer briefs from the back with legs around his waist and two guys having sex in a public place and infecting the store and the arresting officers with scabies? ...
Buy Halaven Eribulin 0.44mg/ml Injection online made by Eisai Co. and its indian generic alternatives to treat cancer at lowest price in USA, UK, Canada etc. Find Halaven 0.88 mg mrp, uses, side-effects, precautions, substitutes at drugssquare.com
Alright, so this is a picture of DerAuslander/Bodhi108/Errant108/whateverothernameshesused and me hanging out here in Washington DC, because were hetero life mates. http://farm4.staticflickr.com/3413/3439766741_199e4b1c7e.jpg Hes the one in the middle, Im on the left and the one on the right doesnt actually exist. Ok, so now that thats out of the way. Where is he in this video?
Alright, so this is a picture of DerAuslander/Bodhi108/Errant108/whateverothernameshesused and me hanging out here in Washington DC, because were hetero life mates. http://farm4.staticflickr.com/3413/3439766741_199e4b1c7e.jpg Hes the one in the middle, Im on the left and the one on the right doesnt actually exist. Ok, so now that thats out of the way. Where is he in this video?
A drug used to treat breast cancer and choriocarcinoma (a type of gestational trophoblastic tumor) that have not gotten better with other treatment. It is also used to treat Hodgkin lymphoma, non-Hodgkin lymphoma, Kaposi sarcoma, mycosis fungoides, and testicular cancer. It is also being studied in the treatment of other types of cancer. Vinblastine sulfate blocks cell growth by stopping cell division and may kill cancer cells. It is a type of vinca alkaloid and a type of antimitotic agent. The brand name Velban has been taken off the market and is no longer available ...
In-stent restenosis remains a significant problem associated with bare metal stents. This drawback has prompted research into improving stent design and the development of novel coatings, including drug-eluting stents. A number of drug-eluting stents are currently on the market; however, the success rate of these stents in complex situations has been found to be quite low. Thus, there remains potential for the development of more suitable drug-eluting stents. The aims of this study were to use a thermoresponsive polymer to develop a system to locally deliver vinblastine, an antimitotic agent currently used as an anticancer drug, and in addition, assess the effects of this drug at the gene expression level in vitro. An N-isopropylacrylamide/N-tert-butylacrylamide (NiPAAm/NtBAAm) copolymer solution in the ratio 65:35 was prepared and appropriate volumes of vinblastine were added to generate two final drug concentrations of 22 nanomoles/film or 0.022 nanomoles/film. Stainless steel discs (316) were ...
TY - JOUR. T1 - Structure-activity profiles of eleutherobin analogs and their cross- resistance in Taxol-resistant cell lines. AU - McDaid, Hayley M.. AU - Bhattacharya, Samit K.. AU - Chen, Xiao Tao. AU - He, Lifeng. AU - Shen, Heng Jia. AU - Gutteridge, Clare E.. AU - Horwitz, Susan Band. AU - Danishefsky, Samuel J.. PY - 1999/7/8. Y1 - 1999/7/8. N2 - Purpose: Eleutherobin, a natural product, is an antimitotic agent that promotes the polymerization of stable microtubules. Although its mechanism of action is similar to that of Taxol, its structure is distinct. A structure- activity profile of synthetic eleutherobin derivatives that have modifications at C3, C8 and C15 was undertaken to define the structural requirements for microtubule stabilization and cross-resistance in Taxol- resistant cell lines. Methods: The biological activity of five eleutherobin analogs was assessed using three techniques; (1) cytotoxicity and drug- resistance in three paired Taxol-sensitive and -resistant cell lines; ...
Neoxaline is a bio-active Aspergillus japonicus isolate. It is an antimitotic agent and shows weak inhibitory activity of blood platelet aggregation induced by simulation of the central nervous system. It has been synthesized through the "highly stereoselective introduction of a reverse prenyl group to create a quaternary carbon stereocenter using (−)-3a-hydroxyfuroindoline as a building block, construction of the indoline spiroaminal via cautious stepwise oxidations with cyclizations from the indoline, assembly of (Z)-dehydrohistidine, and photoisomerization of unnatural (Z)-neoxaline to the natural (E)-neoxaline." Satoshi Ōmura Neoxaline an antimiotic agent Hirano, A; Iwai, Y; Masuma, R; Tei, K; Omura, S (1979). "Neoxaline, a new alkaloid produced by Aspergillus japonicus. Production, isolation and properties". J Antibiot (Tokyo). 32 (8): 781-785. doi:10.7164/antibiotics.32.781. PMID 500498. Ideguchi, Tetsuya; Yamada, Takeshi (August 11, 2013). "Asymmetric Total Synthesis of Neoxaline". The ...
TumorTreating Fields Delivery Using Second Generation Optune®System for Glioblastoma: Patient Experience and Compliance. BACKGROUND. Tumor Treating Fields (TTFields) are non-invasive, ow-intensity, frequency tuned (200kHz) electric fields with anti-mitotic activity (Figure1), delivered using the Optune system, and are approved for the treatment of adult patients with newly diagnosed and recurrent supratentorial glioblastoma (GBM).. TTFields are delivered via four transducer arrays that are applied directly to the scalp to target the tumor (Figure1). The original Optune system (NovoTTF100 A system) consists of a field generator, portable lithium batteries, carrying bag, and transducer arrays, and weighed approximately 6lbs (Table1, left).. Asecond-generation Optune system (NovoTTF200 A system) has been developed to improve the convenience and manageability of TTFields therapy for GBM patients (Table1, right). Approved by the FDA in July2016, the system uses new digital signal generation ...
Background: ALN-VSP02 is a RNA interference (RNAi) therapeutic comprised of lipid nanoparticle-formulated small interfering RNAs (siRNAs) targeting the expression of vascular endothelial growth factor (VEGF)-A and kinesin spindle protein (KSP). Methods: A multi-center, open label, phase I dose-escalation trial of ALN-VSP02 administered as a 15-minute iv infusion q2 wks was initiated in patients (pts) with advanced solid tumors and at least one measurable liver lesion. Main objectives included evaluation of safety/tolerability and assessment of PK/PD. Results: Thirty-one pts were enrolled across 7 dose levels (0.1-1.5 mg/kg); median age 57 yrs, all with multiple prior therapies. A total of 140 doses were administered, mean of 4.5 (range 1-17). Treatment was generally well-tolerated, with no dose-dependent trends in clinical or laboratory adverse events. One on-study death (liver failure in a pt with near complete replacement of the liver by tumor) deemed possibly related to treatment occurred at ...
A subset of cells, termed side-population (SP), with characteristics of adult stem cells (SC) has been identified in several tissues, cell lines, as well as human and experimental tumors. The main feature of these putative stem cells is the high efflux capability for antimitotic drugs. The role of this SP in tumorigenesis is controversial; though, a role as cancer stem cells has been reported. Here, we have investigated whether a functionally equivalent SP exists in cell lines derived from mouse epidermis and skin tumors in order to define the extent of which the presence of SP is associated with tumor progression. We observed increased percentage of the SP in cell lines derived from skin squamous cell carcinomas (SCCs; cell lines CH72 and JWF2) compared with those arose from skin papillomas (308 and MT1/2) and mouse epidermis (C50). Side populations were isolated by the high capability to efflux Hoechst upon FACS analysis. Interestingly, qRT-PCR analysis of SP and non-SP shows elevated ...
HALAVEN has a high affinity to the plus end of microtubules, causing irreversible mitotic blockages. Please see the full Indication and Important Safety Information for HALAVEN.
Use this discussion guide to talk to your doctor about metastatic breast cancer treatment with HALAVEN. Please see the full Indication and Important Safety Information for HALAVEN.
Dear Heather: Im a hetero poly male who is interested in dating a hetero poly female. Shes also in a D/s relationship with another guy. What the heck is up with D/s, and is it possible to make something work when I dont want anything to do with that kind of thing? Shes awesome, but I dont know if I should pursue her given her other involvements. What do you think?. - A no D/s Dude. Dear Dude:. I think youve asked one of the many complex questions of the universe, and my short answer is this: It depends. There are a lot of factors to consider in this equation, and I sympathize with your dilemma because Ive been there myself. On the opposite end of it, though.. The first question is can you honor her Dominant/submissive dynamic even if you dont understand it? D/s and M/s are polarizing concepts even within the kink community. People have hundreds of legit reasons for why it does or doesnt work for them, and there are always heavily debated pros/cons online wherever kinksters hang out. In ...
Thallus: fruticose, shrubby, quite stiff, up to 7(-15) cm long branching: moderately branched from a narrow holdfast branches: solid, plane, ciliate cilia: black, marginal, often branching, sometimes simple but may be squarrose or furcate, up to 3(-5) mm wide surface: greenish gray to greenish yellow, smooth, shiny, without soredia pseudocyphellae: ellipsoid to short linear, flat or +depressed cortex: thin; chondroid strands: continuous, smooth, never forming bundles of hyphae Apothecia: common, mostly laminal, up to 6 mm in diam. disc: concave, with bluish white pruina; margin: cartilaginous, entire, often with black pigmentation forming a black lip around the disc, usually with conspicuous pseudocyphellae asci: elongate-clavate, 8-spored ascospores: hyaline, 1-septate, narrowly fusiform, 15-17 x 3-3.5 µm Pycnidia: not observed Spot tests: cortex K-, C-, KC+ yellow, P-; medulla K-, C-, KC- P- Secondary metabolites: cortex with usnic acid (major); medulla: none detected. Substrate and ecology: ...
ABSTRACT: A new multispored species of Lecanora containing usnic acid, L. weii is described as new to science. A key to the four known multispored speciesof Lecanora in China is also provided. KEYWORDS: Ascomycota, flora of China, lichens, pruinose discs ...
Researchers at the University of Illinois at Chicago have developed a system for precisely delivering anti-inflammatory drugs to immune cells gone out of control, while sparing their well-behaved counterparts. Their findings were published online Feb. 23 in Nature Nanotechnology.
The U.S. Food and Drug Administration today approved eribulin mesylate (Halaven), an antimicrotubular antineoplastic agent, for the treatment of unresectable or metastatic liposarcoma. This treatment is approved for patients who received prior chemotherapy that contained an anthracycline drug.. "Eribulin mesylate is the first drug approved for patients with liposarcoma that has demonstrated an improvement in survival time," said Richard Pazdur, MD, Director of the Office of Hematology and Oncology Products in the FDAs Center for Drug Evaluation and Research. "The clinical trial data the FDA reviewed indicates that eribulin mesylate increased overall survival by approximately 7 months, offering patients a clinically meaningful drug." Soft-tissue sarcoma is a disease in which cancer cells form in the soft tissues of the body, including the muscles, tendons, fat, blood vessels, lymph vessels, nerves, and tissues around joints. Liposarcoma is a specific type of soft-tissue sarcoma that occurs in ...
Although thousands of new neurons are continuously produced in the dentate gyrus of rodents each day, the function of these newborn cells remains unclear. An increasing number of reports have provided correlational evidence that adult hippocampal neurogenesis is involved in learning and memory. Exposure of animals to an enriched environment leads to improvement of performance in several learning tasks and enhances neurogenesis specifically in the hippocampus. These data raise the question of whether new neurons participate in memory improvement induced by enrichment. To address this issue, we have examined whether the increase in the number of surviving adult-generated cells following environmental enrichment contributes to improved memory function. To this end, neurogenesis was substantially reduced throughout the environmental enrichment period using the antimitotic agent methylazoxymethanol acetate (MAM). Recognition memory performance of MAM-treated enriched rats was evaluated in a novel ...
This general characteristic of eribulin mesylate places it in the group of drugs that includes Vinca alkaloids, dolastatins, and cryptophycin. However, its tubulin interactions appear to be unique.. The drug is believed to work primarily via a tubulin-based mechanism that causes prolonged and irreversible mitotic blockage, ultimately leading to apoptotic cell death. Additionally, in preclinical studies of human breast cancer, eribulin mesylate demonstrated complex effects on the tumor biology of surviving cancer cells, including increases in vascular perfusion resulting in reduced tumor hypoxia, and changes in the expression of genes in tumor specimens associated with a change in phenotype, promoting the epithelial phenotype, opposing the mesenchymal phenotype.. Finally, eribulin mesylate has been shown to decrease the migration and invasiveness of human breast cancer cells.. "We are excited to have initiated this Phase ( study and to transition MORAb-202 into the clinical development stage," ...
Filanesib, also known as ARRY-520 is a synthetic, small molecule targeting the kinesin spindle protein (KSP) with potential antineoplastic activity. KSP inhibitor ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5), resulting in activation of the spindle assembly checkpoint, induction of cell cycle arrest during the mitotic phase, and consequently cell death in tumor cells that are actively dividing. Because KSP is not involved in postmitotic processes, such as neuronal transport, this agent does not cause the peripheral neuropathy that is often associated with tubulin-targeting agents. KSP is an ATP-dependent microtubule motor protein that is essential for the formation of bipolar spindles and the proper segregation of sister chromatids during mitosis....
TY - CHAP. T1 - Marine sponge derived eribulin in preclinical and clinical studies for cancer. AU - Swami, Umang. AU - Shah, Umang. AU - Goel, Sanjay. PY - 2015/1/1. Y1 - 2015/1/1. N2 - Eribulin mesylate is a completely synthetic, structurally simplified, macrocyclic ketone analogue of Halichondrin B. Halichondrin B is complex, natural, macrocyclic polyether derived from marine sponges. Eribulin has been approved by United States Food and Drug Administration in 2010 as a third line therapy for metastatic breast cancer patients, who have previously been treated with an anthracycline and a taxane. It has a microtubule dynamics inhibitory action. Preclinical studies have demonstrated a broad spectrum of anti-tumor activity in various cancer cell lines and synergistic action with multiple anticancer agents. It has also undergone clinical trials in non-small cell lung cancer, pancreatic, prostate, bladder, head and neck cancers, sarcomas and ovarian and other gynecological tumors. Various combination ...
ORGANIC COMPOUNDS -- PART OF THE CLASS 532-570 SERIES : : : Hetero ring is five-membered consisting of one nitrogen and four carbons (e.g., halopyrrolidines, etc.) : Polycyclo ring system having the five-membered hetero ring as one of the cyclos : Bicyclo ring system having the five-membered hetero ring as one of the cyclos (e.g., octahydroindoles, etc.) : Additional polycyclo heterocyclic ring system attached directly or indirectly to the bicyclo ring system by nonionic bonding : The additional polycyclo heterocyclic ring system has a lactone ring as one of the cyclos : Ring carbon of each of the two five-membered hetero rings is bonded directly to chalcogen or nitrogen (e.g., both rings may be bonded to the same nitrogen atom or to different nitrogen atoms, etc ...
Apoptosis, the process by which cells orchestrate their own demise in response to intra- or extracellular events, plays a major role in normal, pathological, and iatrogenic processes in the nervous system (Cotter et al., 1990; Raff, 1992; Wyllie, 1992). In non-nervous system models, several endogenous factors have been shown to protect tumor and/or normal cells from apoptotic death (Brach et al., 1992; Tilly et al., 1992; Harrington et al., 1994; Ishizaki et al., 1994). These agents have been referred to collectively as "survival factors" (Collins et al., 1994). For both normal and neoplastic neural crest-derived cells, NGF acts as a survival factor that protects against apoptosis initiated by a variety of exogenous conditions (Ibanez et al., 1992; Rabizadeh et al., 1993). We have reported previously on antimitotic agent-induced apoptosis in neuroblastoma cells and the protection by NGF of these cells from apoptosis induced by such agents (Falcione et al., 1993; Cortazzo et al., 1995; Hartsell ...
Those infections come naturally as well as go out naturally after specific period, but in some cases the infection does not vanish. For such conditions, it is recommended for you seek the assistance of a skin doctor. On the basis of the intensity of this infection the physician will prescribe a number of medications including Imiquimod lotion, podophyllin antimitotic remedy, podofilox remedy, 5-fluorouracil cream and trichloroacetic acid.. The http://hsvfacts.blogspot.com/ HPV triggers the genital blemishes with barely any type of signs and symptom, however just do not obtain fretted. The genital blemishes, if diagnosed in time, can be curable without any sort of stress so far. There is, obviously, no particular treatment for the warts.. The HPV triggers the genital blemishes with hardly any type of sign, but simply do not get stressed. The genital verrucas, if identified in time, could be treatable without any stress so far.. The solution makes the contaminated area white. The blemish comes to ...
The Aurora kinases regulate key stages of mitosis including centrosome maturation, spindle assembly, chromosome segregation and cytokinesis. Aurora A and B overexpression has also been associated with various human cancers and as such, they have been extensively studied as novel anti-mitotic drug targets. Here we characterise the Aurora kinase inhibitor CCT137690, a highly selective, orally bioavailable imidazo[4,5-b]pyridine derivative that inhibits Aurora A and B kinases with low nanomolar IC50 values in both biochemical and cellular assays and exhibits anti-proliferative activity against a wide range of human solid tumour cell lines. CCT137690 efficiently inhibits histone H3 and TACC3 phosphorylation (Aurora B and Aurora A substrates, respectively) in HCT116 and HeLa cells. Continuous exposure of tumour cells to the inhibitor causes multipolar spindle formation, chromosome misalignment, polyploidy and apoptosis. This is accompanied by p53/p21/BAX induction, thymidine kinase 1 (TK1) ...
In the Clinic provides overviews of novel oncology agents, addressing indications, mechanisms, administration recommendations, safety profiles, and other essential information needed for the appropriate clinical use of these drugs.. On January 28, 2016, eribulin mesylate (Halaven) was approved for treatment of patients with unresectable or metastatic liposarcoma who have received a prior anthracycline-containing regimen.1,2 Eribulin was previously approved for treatment of patients with metastatic breast cancer who have received at least two chemotherapeutic regimens for metastatic disease and prior treatment with an anthracycline and a taxane in the adjuvant or metastatic setting.. Supporting Efficacy Data. Approval was based on an open-label trial in which 446 patients with unresectable locally advanced or metastatic liposarcoma or leiomyosarcoma who had received at least two prior systemic therapies including an anthracycline and had disease progression within the past 6 months were ...
Purchase Hetero Diels-Alder Methodology in Organic Synthesis, Volume 47 - 1st Edition. Print Book & E-Book. ISBN 9780121108601, 9780080916972
Enhanced combination therapy effect on paclitaxel-resistant carcinoma by chloroquine co-delivery via liposomes Menghua Gao,1 Yuzhen Xu,1 Liyan Qiu2,3 1College of Pharmaceutical Sciences, 2Ministry of Education (MOE) Key Laboratory of Synthesis and Functionalization, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou, 3Collaborative Innovation Center for Biotherapy, West China Hospital, Sichuan University, Chengdu, People’s Republic of China Abstract: A novel composite liposomal system co-encapsulating paclitaxel (PTX) with chloroquine phosphate (CQ) was designed for treating PTX-resistant carcinoma. It was confirmed that liposomal CQ can sensitize PTX by means of autophagy inhibition and competitively binding with multidrug-resistance transporters. Furthermore, according to the in vitro cytotoxicity and apoptosis assay, real-time observation of cellular uptake, and in vivo tissue distribution study, co-encapsulation of PTX and CQ in liposomes was validated as

Novel antimitotic agents related to tubuloclustin: synthesis and biological evaluation, Molecular Diversity | 10.1007/s11030...Novel antimitotic agents related to tubuloclustin: synthesis and biological evaluation, Molecular Diversity | 10.1007/s11030...

"Novel antimitotic agents related to tubuloclustin: synthesis and biological evaluation, Molecular Diversity" on DeepDyve, the ... Novel antimitotic agents related to tubuloclustin: synthesis and biological evaluation. Novel antimitotic agents related to ... Novel antimitotic agents related to tubuloclustin: synthesis and biological evaluation. Zefirova, Olga; Nurieva, Evgeniya; ... Three series of antimitotic agents related to tubuloclustin were designed and synthesized in order to enhance the molecular ...
more infohttps://www.deepdyve.com/lp/springer_journal/novel-antimitotic-agents-related-to-tubuloclustin-synthesis-and-jfH0w65NY0

Aroyl hydrazones of 2-phenylindole-3-carbaldehydes as novel antimitotic agents  - Publikationsserver der Universität RegensburgAroyl hydrazones of 2-phenylindole-3-carbaldehydes as novel antimitotic agents - Publikationsserver der Universität Regensburg

Aroyl hydrazones of 2-phenylindole-3-carbaldehydes as novel antimitotic agents. Bioorganic & Medicinal Chemistry 16 (12), S. ... In this study, we modified the structure of antimitotic 2-phenylindole-3-carbaldehydes by condensation with hydrazides of ... In this study, we modified the structure of antimitotic 2-phenylindole-3-carbaldehydes by condensation with hydrazides of ...
more infohttps://epub.uni-regensburg.de/4787/

Colchicine effect on microtubulesColchicine effect on microtubules

Luurila et Zopiclone is a nonbenzodiazepine lee agent used in the doc of insomnia. Zopiclone is molecularly popped from ... Molecular Modeling of the Mechanism of Action of a New Antimitotic Drug. ...
more infohttp://geptsite.info/summer-savings/colchicine-effect-on-microtubules.php

Antimitotic agent | definition of antimitotic agent by Medical dictionaryAntimitotic agent | definition of antimitotic agent by Medical dictionary

... antimitotic agent explanation free. What is antimitotic agent? Meaning of antimitotic agent medical term. What does antimitotic ... Looking for online definition of antimitotic agent in the Medical Dictionary? ... antimitotic agent. Also found in: Dictionary, Encyclopedia. antimitotic agent. Oncology. An agent that inhibits cancer growth ... antimitotic agent. Antimicrotubule agent, mitotic inhibitor Oncology An agent that inhibits cancer growth by stopping cell ...
more infohttps://medical-dictionary.thefreedictionary.com/antimitotic+agent

Definition of antimitotic agent - NCI Dictionary of Cancer Terms - National Cancer InstituteDefinition of antimitotic agent - NCI Dictionary of Cancer Terms - National Cancer Institute

antimitotic agent listen (AN-tee-my-TAH-tik AY-jent) A type of drug that blocks cell growth by stopping mitosis (cell division ...
more infohttps://www.cancer.gov/publications/dictionaries/cancer-terms/def/antimitotic-agent

Disorazole C1: A potent antimitotic agent that induces premature senescence | Cancer ResearchDisorazole C1: A potent antimitotic agent that induces premature senescence | Cancer Research

Disorazole C1: A potent antimitotic agent that induces premature senescence Marni Brisson, Bethany Petrik, Thomas Graham, ... Disorazole C1: A potent antimitotic agent that induces premature senescence Marni Brisson, Bethany Petrik, Thomas Graham, ... Disorazole C1: A potent antimitotic agent that induces premature senescence Marni Brisson, Bethany Petrik, Thomas Graham, ... Disorazole C1: A potent antimitotic agent that induces premature senescence Message Subject (Your Name) has forwarded a page to ...
more infohttp://cancerres.aacrjournals.org/content/67/9_Supplement/1219

Abstract 2475: Design and development of combretastatin based unsymmetrical terphenyls as small molecule antimitotic agents. |...Abstract 2475: Design and development of combretastatin based unsymmetrical terphenyls as small molecule antimitotic agents. |...

Abstract 2475: Design and development of combretastatin based unsymmetrical terphenyls as small molecule antimitotic agents.. ... Abstract 2475: Design and development of combretastatin based unsymmetrical terphenyls as small molecule antimitotic agents. ... Design and development of combretastatin based unsymmetrical terphenyls as small molecule antimitotic agents. [abstract]. In: ... Abstract 2475: Design and development of combretastatin based unsymmetrical terphenyls as small molecule antimitotic agents. ...
more infohttp://cancerres.aacrjournals.org/content/73/8_Supplement/2475

Nerve Growth Factor (NGF)-Mediated Protection of Neural Crest Cells from Antimitotic Agent-Induced Apoptosis: The Role of the...Nerve Growth Factor (NGF)-Mediated Protection of Neural Crest Cells from Antimitotic Agent-Induced Apoptosis: The Role of the...

Effects of NGF (42 nm) on antimitotic agent-induced human neuroblastoma cell death. A, SH-SY5Y cells were pretreated with NGF ... Effects of p75- and trkA-selective mutant NGF species (4.2 nm) on antimitotic agent-induced SH-SY5Y cell death. Mutant NGF ... The antimitotic agent neocarzinostatin (NCS) was obtained from Kayaku Pharmaceuticals (Tokyo, Japan). NCS was stored in powder ... Effects of antibody 9651 (1:1000) on the protective effects of NGF (42 nm) in antimitotic agent-treated SH-SY5Y cells. Antibody ...
more infohttp://www.jneurosci.org/content/16/12/3895

Oncogenic KRAS triggers MAPK-dependent errors in mitosis and MYC-dependent sensitivity to anti-mitotic agents.  - PubMed - NCBIOncogenic KRAS triggers MAPK-dependent errors in mitosis and MYC-dependent sensitivity to anti-mitotic agents. - PubMed - NCBI

Oncogenic KRAS triggers MAPK-dependent errors in mitosis and MYC-dependent sensitivity to anti-mitotic agents.. Perera D1, ... the bottom 50 MYC-expressing lines (MYC low) treated with the indicated anti-mitotic agents. Data was obtained from the ... Cell death elicited by anti-mitotic agents in KRASG12D-expressing HeLa cells is mediated by MYC and BCL-XL. ... These anomalies are accompanied by increased sensitivity to anti-mitotic agents, a phenotype dependent on the transcription ...
more infohttps://www.ncbi.nlm.nih.gov/pubmed/27412232

Mannidex
        -
        Antimitotic agent,  Antineoplastic Agents, Phytogenic,  Keratolytic AgentsMannidex - Antimitotic agent, Antineoplastic Agents, Phytogenic, Keratolytic Agents

Podofilox, also called podophyllotoxin, is a purer and more stable form of podophyllin in which only the biologically active portion of the compound is present. Podofilox is used to remove certain types of warts on the outside skin of the genital areas ...
more infohttp://pharmacycode.com/Mannidex.html

Mannazucker
        -
        Antimitotic agent,  Antineoplastic Agents, Phytogenic,  Keratolytic AgentsMannazucker - Antimitotic agent, Antineoplastic Agents, Phytogenic, Keratolytic Agents

Podofilox, also called podophyllotoxin, is a purer and more stable form of podophyllin in which only the biologically active portion of the compound is present. Podofilox is used to remove certain types of warts on the outside skin of the genital areas ...
more infohttp://pharmacycode.com/Mannazucker.html

Words to Know | Living Beyond Breast CancerWords to Know | Living Beyond Breast Cancer

antimitotic agent. A type of medicine used to treat cancer that blocks cell growth by stopping mitosis (cell division). Also ... alkylating agent. A type of medicine used in cancer treatment. It interferes with cell DNA and blocks cancer cell growth. ... agent study. In cancer prevention, a clinical trial that studies whether taking certain medicines, vitamins, minerals or food ... Examples of agent studies include clinical trials for tamoxifen and letrozole, as well as lifestyle changes such as diet. ...
more infohttps://lbbc.org/learn/basics/words-to-know?name=%5Ea&items_per_page=All

ABT-751 (CAS: 857447-92-8) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and...ABT-751 (CAS: 857447-92-8) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and...

... is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 μM in neuroblastoma ... ABT-751 (CAS: 857447-92-8) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and ... This agent also disrupts tumor neovascularization, reducing tumor blood flow and so inducing a cytotoxic effect. ...
more infohttp://cckinase.com/e_productshow/?440-ABT-751-ABT751-ABT-751-E7010-E-7010-E-7010-857447-92-8-440.html

Dual Targeting of HER2-Positive Cancer with Trastuzumab Emtansine and Pertuzumab: Critical Role for Neuregulin Blockade in...Dual Targeting of HER2-Positive Cancer with Trastuzumab Emtansine and Pertuzumab: Critical Role for Neuregulin Blockade in...

NRG-1β inhibits activity of antimitotic agents. The DM1 component of T-DM1 is a potent antimitotic agent (41). Additional ... We developed a cytotoxic drug-conjugate of trastuzumab by covalently linking the antimitotic agent DM1 to trastuzumab through a ... Assays to test NRG-1β effects on T-DM1 or chemotherapeutic agent activity were 3 or 5 days (n = 3 per group) and studies were ... studies were performed to determine if the protective effect of NRG-1β applied to free DM1 and to antimitotic agents used for ...
more infohttp://clincancerres.aacrjournals.org/content/20/2/456.long

CDC - The Emergency Response Safety and Health Database: Glossary - NIOSHCDC - The Emergency Response Safety and Health Database: Glossary - NIOSH

Antimitotic agent. An agent that prevents or interferes with cell division (mitosis).. ... A chemical agent or drug used in the treatment of disease; chemotherapeutic agents are selectively toxic to the causative agent ... Nettle agent. An agent that causes severe irritation to the skin and mucous membranes, as well as pain; also called urticant. ( ... An agent that causes severe irritation to the skin and mucous membranes, as well as pain; also called nettle agent.. ...
more infohttps://www.cdc.gov/niosh/ershdb/glossary.html

Mitosis is not a key target of microtubule agents in patient tumors.  - PubMed - NCBIMitosis is not a key target of microtubule agents in patient tumors. - PubMed - NCBI

Antimitotic Agents. Grant support. *ImNIH/Intramural NIH HHS/United States. LinkOut - more resources. Full Text Sources. * ... Mitosis-specific agents have, to date, not been clinically successful. By contrast, microtubule-targeting agents (MTAs) have a ... Mitosis is not a key target of microtubule agents in patient tumors.. Komlodi-Pasztor E1, Sackett D, Wilkerson J, Fojo T. ...
more infohttps://www.ncbi.nlm.nih.gov/pubmed/21283127?dopt=Abstract

Two Regimens of Docetaxel in Treating Patients Who Have Not Received Chemotherapy For Unresectable Stage IIIB or Stage IV Non...Two Regimens of Docetaxel in Treating Patients Who Have Not Received Chemotherapy For Unresectable Stage IIIB or Stage IV Non...

Antineoplastic Agents. Tubulin Modulators. Antimitotic Agents. Mitosis Modulators. Molecular Mechanisms of Pharmacological ...
more infohttps://clinicaltrials.gov/show/NCT00075374

Radiation Therapy and Docetaxel in Treating Patients With HPV-Related Oropharyngeal Cancer - Full Text View - ClinicalTrials.govRadiation Therapy and Docetaxel in Treating Patients With HPV-Related Oropharyngeal Cancer - Full Text View - ClinicalTrials.gov

Antineoplastic Agents. Tubulin Modulators. Antimitotic Agents. Mitosis Modulators. Molecular Mechanisms of Pharmacological ... Receiving any other investigational agent which would be considered as a treatment for the primary neoplasm ...
more infohttps://www.clinicaltrials.gov/ct2/show?term=dry+mouth&fund=0&rank=51

Evaluation of the Safety and Tolerability of TAK-228 With TAK-117 and Paclitaxel in Advanced Solid Tumors - Full Text View -...Evaluation of the Safety and Tolerability of TAK-228 With TAK-117 and Paclitaxel in Advanced Solid Tumors - Full Text View -...

Antineoplastic Agents, Phytogenic. Antineoplastic Agents. Tubulin Modulators. Antimitotic Agents. Mitosis Modulators. Molecular ... Use of anti-hypertensive agents to control hypertension before Cycle1 Day 1 is allowed. ...
more infohttps://www.clinicaltrials.gov/ct2/show/NCT03154294?map_cntry=US&map_state=US%3ASD&rank=14

Vinorelbine Tartrate Monograph for Professionals - Drugs.comVinorelbine Tartrate Monograph for Professionals - Drugs.com

Class: Antineoplastic Agents. - Vinca Alkaloids. - Antimitotic Agents. VA Class: AN900. Chemical Name: 3′,4′-Didehydro-4′-deoxy ... Antineoplastic agent; semisynthetic vinca alkaloid.1 4 21 b c. Uses for Vinorelbine Tartrate. Non-Small Cell Lung Cancer. Used ... Vinorelbine is an active antiproliferative agent in pretreated advanced breast cancer patients: a phase II study. J Clin Oncol ... Administer only under constant supervision by clinicians experienced in therapy with chemotherapeutic agents.1 b c ...
more infohttps://www.drugs.com/monograph/vinorelbine-tartrate.html

RCSB PDB - VLB Ligand Summary PageRCSB PDB - VLB Ligand Summary Page

Antimitotic Agents. *Antineoplastic Agents. *Antineoplastic Agents, Phytogenic. *Antineoplastic and Immunomodulating Agents. * ... Vinblastine is a vinca alkaloid antineoplastic agent. The vinca alkaloids are structurally similar compounds comprised of 2 ...
more infohttps://www.rcsb.org/ligand/VLB

RCSB PDB - EVP Ligand Summary PageRCSB PDB - EVP Ligand Summary Page

Antimitotic Agents. *Antineoplastic Agents. *Antineoplastic Agents, Phytogenic. *Antineoplastic and Immunomodulating Agents. * ... For use in combination with other chemotherapeutic agents in the treatment of refractory testicular tumors and as first line ... Etoposide is an antineoplastic agent and an epipodophyllotoxin (a semisynthetic derivative of the podophyllotoxins). It ...
more infohttp://www.rcsb.org/ligand/EVP

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LTP-1, a novel antimitotic agent and Stat3 inhibitor, inhibits human pancreatic carcinomas in vitro and in vivo *Han-Li Huang ... Rights & permissionsfor article LTP-1, a novel antimitotic agent and Stat3 inhibitor, inhibits human pancreatic carcinomas ,i, ... Synthesis and antitussive evaluation of verticinone-cholic acid salt, a novel and potential cough therapeutic agent *Fang-zhou ... MPT0G066, a novel anti-mitotic drug, induces JNK-independent mitotic arrest, JNK-mediated apoptosis, and potentiates ...
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  • In a series of studies using, in turn, neuroblastoma cell lines that express only p75, mutant NGF species that bind selectively to either p75 or trkA, and a polyclonal antibody that binds to the NGF-binding domain of p75, we demonstrate that NGF binding to p75 is both necessary and sufficient for the abrogation of apoptosis in neuroblastoma cells treated with antimitotic agents. (jneurosci.org)
  • we have tested the necessity for and sufficiency of p75 binding of NGF for protection of neuroblastoma cells from antimitotic agent-induced apoptosis. (jneurosci.org)
  • Consistent with their FACS profiles, Immunocytochemistry and biochemical analysis revealed loss of intact microtubule structure, up regulation of cyclin B1 and aurora kinase B mRNA levels, corresponding to growth arrest in the G2/M. More importantly, our one pot synthesis strategy of unsymmetrical terphenyls of this structural class paves the way for design and development of novel anticancer agents. (aacrjournals.org)
  • This agent also disrupts tumor neovascularization, reducing tumor blood flow and so inducing a cytotoxic effect. (cckinase.com)