Agents that arrest cells in MITOSIS, most notably TUBULIN MODULATORS.
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).
Agents that interact with TUBULIN to inhibit or promote polymerization of MICROTUBULES.
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.
An antifungal agent used in the treatment of TINEA infections.
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.
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.
Antitumor alkaloid isolated from Vinca rosea. (Merck, 11th ed.)
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.
A cyclodecane isolated from the bark of the Pacific yew tree, TAXUS BREVIFOLIA. It stabilizes MICROTUBULES in their polymerized form leading to cell death.
Substances that inhibit or prevent the proliferation of NEOPLASMS.
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.
A cell line derived from cultured tumor cells.
An ansa macrolide isolated from the MAYTENUS genus of East African shrubs.
Compounds consisting of chains of AMINO ACIDS alternating with CARBOXYLIC ACIDS via ester and amide linkages. They are commonly cyclized.
Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.
The complex series of phenomena, occurring between the end of one CELL DIVISION and the end of the next, by which cellular material is duplicated and then divided between two daughter cells. The cell cycle includes INTERPHASE, which includes G0 PHASE; G1 PHASE; S PHASE; and G2 PHASE, and CELL DIVISION PHASE.
Changes in the organism associated with senescence, occurring at an accelerated rate.
A group of often glycosylated macrocyclic compounds formed by chain extension of multiple PROPIONATES cyclized into a large (typically 12, 14, or 16)-membered lactone. Macrolides belong to the POLYKETIDES class of natural products, and many members exhibit ANTIBIOTIC properties.
A group of 16-member MACROLIDES which stabilize MICROTUBULES in a manner similar to PACLITAXEL. They were originally found in the myxobacterium Sorangium cellulosum, now renamed to Polyangium (MYXOCOCCALES).
A cyclin-dependent kinase inhibitor that coordinates the activation of CYCLIN and CYCLIN-DEPENDENT KINASES during the CELL CYCLE. It interacts with active CYCLIN D complexed to CYCLIN-DEPENDENT KINASE 4 in proliferating cells, while in arrested cells it binds and inhibits CYCLIN E complexed to CYCLIN-DEPENDENT KINASE 2.
One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.
The two longitudinal ridges along the PRIMITIVE STREAK appearing near the end of GASTRULATION during development of nervous system (NEURULATION). The ridges are formed by folding of NEURAL PLATE. Between the ridges is a neural groove which deepens as the fold become elevated. When the folds meet at midline, the groove becomes a closed tube, the NEURAL TUBE.
Devices which are used in the treatment of orthopedic injuries and diseases.
Two ganglionated neural plexuses in the gut wall which form one of the three major divisions of the autonomic nervous system. The enteric nervous system innervates the gastrointestinal tract, the pancreas, and the gallbladder. It contains sensory neurons, interneurons, and motor neurons. Thus the circuitry can autonomously sense the tension and the chemical environment in the gut and regulate blood vessel tone, motility, secretions, and fluid transport. The system is itself governed by the central nervous system and receives both parasympathetic and sympathetic innervation. (From Kandel, Schwartz, and Jessel, Principles of Neural Science, 3d ed, p766)
A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
A plant genus of the family COMBRETACEAE. Triterpenes and combretastatin have been identified in members of this genus.
Genotypic differences observed among individuals in a population.
Compounds of the general formula R:N.NR2, as resulting from the action of hydrazines with aldehydes or ketones. (Grant & Hackh's Chemical Dictionary, 5th ed)
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.
All of the processes involved in increasing CELL NUMBER including CELL DIVISION.
Exclusive legal rights or privileges applied to inventions, plants, etc.
A condition in which the FORAMEN OVALE in the ATRIAL SEPTUM fails to close shortly after birth. This results in abnormal communications between the two upper chambers of the heart. An isolated patent ovale foramen without other structural heart defects is usually of no hemodynamic significance.
Agents that are capable of inserting themselves between the successive bases in DNA, thus kinking, uncoiling or otherwise deforming it and therefore preventing its proper functioning. They are used in the study of DNA.
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
Acridine antineoplastic agent used in mammary and ovarian tumors. It inhibits RNA synthesis.
Technique that utilizes low-stringency polymerase chain reaction (PCR) amplification with single primers of arbitrary sequence to generate strain-specific arrays of anonymous DNA fragments. RAPD technique may be used to determine taxonomic identity, assess kinship relationships, analyze mixed genome samples, and create specific probes.
A group of replication-defective viruses, in the genus GAMMARETROVIRUS, which are capable of transforming cells, but which replicate and produce tumors only in the presence of Murine leukemia viruses (LEUKEMIA VIRUS, MURINE).
DNA-dependent DNA polymerases found in bacteria, animal and plant cells. During the replication process, these enzymes catalyze the addition of deoxyribonucleotide residues to the end of a DNA strand in the presence of DNA as template-primer. They also possess exonuclease activity and therefore function in DNA repair.
Caustic extract from the roots of Podophyllum peltatum and P. emodi. It contains PODOPHYLLOTOXIN and its congeners and is very irritating to mucous membranes and skin. Podophyllin is a violent purgative that may cause CNS damage and teratogenesis. It is used as a paint for warts, skin neoplasms, and senile keratoses.
A lignan (LIGNANS) found in PODOPHYLLIN resin from the roots of PODOPHYLLUM plants. It is a potent spindle poison, toxic if taken internally, and has been used as a cathartic. It is very irritating to skin and mucous membranes, has keratolytic actions, has been used to treat warts and keratoses, and may have antineoplastic properties, as do some of its congeners and derivatives.
Benign epidermal proliferations or tumors; some are viral in origin.
Agents that soften, separate, and cause desquamation of the cornified epithelium or horny layer of skin. They are used to expose mycelia of infecting fungi or to treat corns, warts, and certain other skin diseases.
Diseases of the skin with a genetic component, usually the result of various inborn errors of metabolism.
Sexually transmitted form of anogenital warty growth caused by the human papillomaviruses.
Experimentation on STEM CELLS and on the use of stem cells.
Tumors or cancer of the human BREAST.
An expression of the number of mitoses found in a stated number of cells.
Cyclic hydrocarbons that contain multiple rings and share one or more atoms.

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)

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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 ...
We describe a cell-based assay for antimitotic compounds that is suitable for drug discovery and for quantitative determination of antimitotic activity, In the assay, cells arrested in mitosis as a result of exposure to antimitotic agents in pure form or in crude natural extracts are detected by ELISA using the monoclonal antibody TG-3, The assay was used to screen ,24,000 extracts of marine microorganisms and invertebrates and terrestrial plants and to guide the purification of active compounds from 5 of 119 positive extracts. A new rhizoxin analogue was found in a Pseudomonas species, six new eleutherobin analogues were identified from the octocoral Erythropodium caribaeorum, and two paclitaxel analogues were found in the stem bark of the tree Ilex macrophylla. The assay was also used for quantitative comparison of the antimitotic activity of different analogues. It revealed the importance of the C-11 to C-13 segment of the diterpene core of eleutherobin for its antimitotic activity. The ...
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. ...
Analysis of Mitosis and Antimitotic Drug Responses in Tumors by In Vivo Microscopy and Single-Cell Pharmacodynamics Journal Article ...
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 ...
Although the results of recent cell culture studies have been highly informative, they will not be of great use if they bear no relation to events in an in vivo context. Significantly, a pair of studies that investigated the effect of taxanes on several mouse tumour models also observed wide variation in the response. Tumour regression that was induced by taxane treatment varied widely, and the mitotic index of cells within the tumour did not correlate with either cell death or tumour regression (Milross et al., 1996; Schimming et al., 1999). Similar observations were made in a highly informative clinical study. Eleven women that received neoadjuvant taxol treatment for non-metastatic breast cancer were followed and, at regular intervals post-treatment, biopsies and mammograms were used to determine the mitotic index, apoptotic index and tumour size (Symmans et al., 2000). The authors observed a wide variation in both the mitotic and apoptotic index in response to the drug, with no correlation ...
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 > Tricyclo ring system having the seven-membered hetero ring as one of the ...
The Deacetylation Phosphorylation Regulation of the SIRT2-SMC1A Axis as a Mechanism of the Antimitotic Catastrophe in Early Tumor Development Science Advances
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 ...
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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.
Description: Subject matter wherein the seven-membered hetero ring is attached directly or indirectly by nonionic bonding to an additional nitrogen-containing hetero ring ...
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…
TY - JOUR. T1 - Melampodium leucanthum, a source of cytotoxic sesquiterpenes with antimitotic activities. AU - Robles, Andrew J.. AU - Peng, Jiangnan. AU - Hartley, Rachel M.. AU - Lee, Brigette. AU - Mooberry, Susan L.. PY - 2015/3/27. Y1 - 2015/3/27. N2 - A new tricyclic sesquiterpene, named meleucanthin (1), was isolated from an extract of the leaves and branches of Melampodium leucanthum, along with four known germacranolide sesquiterpene lactones, leucanthin-A (2), leucanthin-B (3), melampodin-A acetate (4), and 3α-hydroxyenhydrin (5). The chemical structure of 1 was elucidated by analysis of 1D and 2D NMR and mass spectrometric data. All compounds exhibited antiproliferative and cytotoxic efficacy against PC-3 and DU 145 prostate cancer cells, as well as HeLa cervical cancer cells, with IC50 values ranging from 0.18 to 9 μM. These compounds were effective in clonogenic assays and displayed high cellular persistence. They were also found to be capable of circumventing ...
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 ...
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 ...
Mental health the nursing actions for additional health information joining a support group meetings here. Action your doctor within 20 hours possible cause blepharitis, inflammation of the following 4 categories: Alkylating agents, antimetabolites, antimitotics, and antibiotics may be required: Stress management development and enhancement of k+ and some other conditions. 5 basic to nursing, ed 3. Cv mosby, st. 4. Potential dysfunctional patterns: The potential for enhancing the intrinsic pacemaker exceeds that of 69 reports, the soleplaints included nausea, vomiting, hepatotoxicity, lactic acidosis in cancer patients with potentially serious adverse effects. *these values were determined in rat smooth muscle cells, secondary to prostate disease include hypersensitivity pneumonitis, medications with prolonged use can result from inhalation of heroin pyrolosate; body packing. Some xenobiotics suppress av nodal conduction cause marked lengthening of night sleep and wakefulness that be saturated ...
Article Title : Targeting Urokinase and the Transferrin Receptor with Novel, Anti-Mitotic N-Alkylisatin Cytotoxin Conjugates Causes Selective Cancer Cell Death and Reduces Tumor ...
Steen, J A J, Steen, H, Georgi, A, Parker, K C, Springer, M, Kirchner, M, Hamprecht, F A and Kirschner, M W (2008). Different Phosphorylation States of the Anaphase Promoting Complex in Response to Anti-Mitotic Drugs: A Quantitative Proteomic Analysis. Proceedings of the National Academy of Sciences. 105 6069-6074 ...
Steen, J A J, Steen, H, Georgi, A, Parker, K C, Springer, M, Kirchner, M, Hamprecht, F A and Kirschner, M W (2008). Different Phosphorylation States of the Anaphase Promoting Complex in Response to Anti-Mitotic Drugs: A Quantitative Proteomic Analysis. Proceedings of the National Academy of Sciences. 105 6069-6074 ...
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. ...
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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.
Children with congenital or acquired immunodeficiency may be vaccinated, keeping in mind that, depending on the state of their immune system, their immune response will be lesser or greater. In children under immunosuppressive treatment (corticotherapy, antimitotic chemotherapy, etc.), it is recommended to postpone vaccination until the end of the treatment ...
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
So some of you may remember that my PANS daughter is compound hetero for 1298 and 677. My husband has one 1298 mutation. My other daughter has one 677 mutation. Of course, being the mom I was more concerned with everyone else and didnt even think to get myself checked! Well I was tested recently as part of a regular physical and it turns out I am homozygous for C677T... and my homacystine levels are already high. I was glad that I somewhat had an understanding of what it meant but now I am in supplement mode and trying to figure out what I have to do to bring my own levels down. Id love ...
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A general redox‐neutral approach into the o‐,o′‐heteroatom‐linked N‐(hetero)aryl‐imidazole family of heteroaromatics has been developed. New types of ...
Additionally, antimitotic agents are not typically recommended during pregnancy. Additionally, it has not been determined if ... and antitumor agents. Podophyllotoxin derived antitumor agents include etoposide and teniposide. These drugs have been ... For example, ring A is not essential to antimitotic activity. Aromatization of ring C leads to loss of activity, possibly from ... Cragg GM, Kingston DG, Newman DJ (2011). Anticancer Agents from Natural Products, Second Edition (2 ed.). CRC Press. p. 97. ...
Characterization of chromosomal aberrations induced in man by various antimitotic agents]". Comptes Rendus des Séances de la ... Amikhelline is an antimitotic drug. It acts as a DNA intercalator and inhibits DNA polymerase. Turchini MF, Geneix A, Perissel ...
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 the penetration of harsh surface sterilizing agents, such as hypochlorite, so ...
... has no anti-mitotic activity. Other anti-tubulin agents used as chemotherapy agents have painful side effects known as ... 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 ...
... 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 the approved drug belantamab mafodotin in ...
Two specific families of antimitotic agents - vinca alkaloids and taxanes - interrupt the cell's division by the agitation of ... Agents that affect the motor protein kinesin are beginning to enter clinical trials. Another type, paclitaxel, acts by ... Even though numerous other spindle proteins exist that could be the target of novel chemotherapeutics, tubulin-binding agents ...
... the potent colchicine site antimitotic agent, with tubulin and effects of analogs on the growth of MCF-7 breast cancer cells". ...
January 1998). "Structure-activity analysis of the interaction of curacin A, the potent colchicine site antimitotic agent, with ...
... 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 ...
... antimitotic agents MeSH D27.505.954.248.150 - antineoplastic agents, alkylating MeSH D27.505.954.248.169 - antineoplastic ... antiviral agents MeSH D27.505.954.122.388.077 - anti-retroviral agents MeSH D27.505.954.122.388.077.088 - anti-hiv agents MeSH ... tocolytic agents MeSH D27.505.954.016 - anti-allergic agents MeSH D27.505.954.122 - anti-infective agents MeSH D27.505.954.122. ... tranquilizing agents MeSH D27.505.696.277.950.015 - anti-anxiety agents MeSH D27.505.696.277.950.025 - antimanic agents MeSH ...
... 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 ...
... 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 ...
As of 2016[update], vinflunine was the only commercially-approved agent in some countries for salvage therapy of urothelial ... Kruczynski A, Barret JM, Etiévant C, Colpaert F, Fahy J, Hill BT (March 1998). "Antimitotic and tubulin-interacting properties ...
EMP is a dual cytostatic and hence chemotherapeutic agent and a hormonal anticancer agent of the estrogen type. It is a prodrug ... In addition to its antimitotic actions, EMP has also been found to produce other cytostatic effects, including induction of ... or other more marked toxicity associated with such agents. In contrast to most other cytostatic agents, which often cause ... Antineoplastic agents related to EMP, although none of them were marketed, include alestramustine, atrimustine, cytestrol ...
"Anticancer Agent Halaven Approved For Treatment Of Locally Advanced Or Metastatic Breast Cancer In China" (Press release). ... Kawano, S; Asano, M; Adachi, Y; Matsui, J (2016). "Antimitotic and Non-mitotic Effects of Eribulin Mesilate in Soft Tissue ... "U.S. FDA Approves Eisai's Anticancer Agent Halaven For The Treatment Of Advanced Liposarcoma" (Press release). Eisai Co., Ltd. ... In addition to its cytotoxic, antimitotic-based mechanisms, preclinical studies in human breast cancer models have shown that ...
"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, ...
Antimicrobial Agents and Chemotherapy. 4 (3): 294-298. doi:10.1128/AAC.4.3.294. PMC 444544. PMID 4357181. Aphidicolin product ... Cephalosporum aphidicola with antiviral and antimitotic properties. Aphidicolin is a reversible inhibitor of eukaryotic nuclear ...
By acting as a contrast agent and injected into cancerous tumor cells, it would result in a higher dose of the cancerous tissue ... Docetaxel is packed into PEGylated gold nanoparticles Docetaxel is an anti-mitotic chemotherapy medicine which showing great ... Another way in which AuNPs can be used in cancer therapy is as agents for targeted drug delivery. Research shows that AuNPs can ... Jain, S; Hirst, D G; O'Sullivan, J M (2012-02-01). "Gold nanoparticles as novel agents for cancer therapy". The British Journal ...
Available agents[edit]. Main article: List of antineoplastic agents. There is an extensive list of antineoplastic agents. ... 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[edit]. Main article: Alkylating antineoplastic agent. Alkylating agents are the oldest group of ... Siddik ZH (2005). Mechanisms of Action of Cancer Chemotherapeutic Agents: DNA-Interactive Alkylating Agents and Antitumour ...
Agents Chemother. 46 (9): 2772-8. doi:10.1128/AAC.46.9.2772-2778.2002. PMC 127399. PMID 12183227. Muhlradt, P.F.; Sasse, F. ( ... At the higher antimitotic concentrations, paclitaxel appears to act by suppressing microtubule detachment from centrosomes, a ... Due to their better water solubility, cremophors (solubilizing agents used for paclitaxel which can affect cardiac function and ... EMEA/602569/2008 Ojima, I.; Vite, G.D.; Altmann, K.H.; 2001 Anticancer Agents: Frontiers in Cancer Chemotherapy. American ...
... is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin. The ... Monomethyl auristatin E (MMAE) is a synthetic antineoplastic agent. Because of its toxicity, it cannot be used as a drug itself ... These drugs show potency of up to 200 times that of vinblastine, another antimitotic drug used for Hodgkin lymphoma as well as ... It is a potent antimitotic drug derived from peptides occurring in marine shell-less mollusc Dolabella auricularia called ...
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. ...
... s are a set of anti-mitotic and anti-microtubule alkaloid agents originally derived from the periwinkle plant ... leurosine and the chemotherapy agents vinblastine[3] and vincristine,[4] all of which can be obtained from the plant.[5][6][7][ ... 8] The newer semi-synthetic chemotherapeutic agent vinorelbine is used in the treatment of non-small-cell lung cancer[7][9] and ...
2010 The use of 'X-MAN' mutant PI3CA increases the expression of individual tubulin isoforms and promoted resistance to anti-mitotic ... to provide an isogenic system to research disease biology and novel therapeutic agents. They can be used to model any disease ...
"Antimicrobial Agents and Chemotherapy. 54 (6): 2425-30. doi:10.1128/AAC.01599-09. PMC 2876375. PMID 20385860.. ... When the fermentation broth of A. fumigatus was screened, a number of indolic alkaloids with antimitotic properties were ...
"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 ...
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 ...
... and methods of treating infectious disease wherein the infectious agent is particularly susceptible to inhibition by agents ... Estrogenic compounds as anti-mitotic agents. US6051726. Mar 13, 1997. Apr 18, 2000. Pharm-Eco Laboratories, Inc.. Synthesis of ... Estrogenic compounds as anti-mitotic agents. US20050014737 *. May 28, 2004. Jan 20, 2005. Agoston Gregory E.. Antiangiogenic ... Estrogenic compounds as anti-mitotic agents. US5892069. Apr 25, 1997. Apr 6, 1999. The Childrens Medical Center Corporation. ...
Characterization of chromosomal aberrations induced in man by various antimitotic agents]". Comptes Rendus des Séances de la ... Amikhelline is an antimitotic drug. It acts as a DNA intercalator and inhibits DNA polymerase. Turchini MF, Geneix A, Perissel ...
Cell fate in response to anti-mitotic drug treatment. When cells are exposed to an anti-mitotic agent such as taxol, they ... anti-mitotics - are commonly used to treat a wide variety of cancers. Traditional anti-mitotic agents include the microtubule ... The majority of anti-mitotic agents are administered intravenously, and therapy typically involves treatment cycles of only a ... As we eagerly await the results of clinical trials that will test the next generation of anti-mitotic agents, only now are we ...
Cell-based screen for antimitotic agents and identification of analogues of rhizoxin, eleutherobin, and paclitaxel in natural ... Cell-based screen for antimitotic agents and identification of analogues of rhizoxin, eleutherobin, and paclitaxel in natural ... Cell-based screen for antimitotic agents and identification of analogues of rhizoxin, eleutherobin, and paclitaxel in natural ... AGENT, ANTITUMOR, BINDING, fungus, INHIBITION, MACROCYCLIC LACTONE ANTIBIOTICS, MICROTUBULE-STABILIZING AGENTS, MITOTIC ...
... microtubule disrupting agent. Join researchers using high quality… ... a water soluble plant and parasite-selective antimitotic, ... Plant and parasite-selective antimitotic, microtubule ... Plant and parasite-selective antimitotic, microtubule disrupting agent. Binds to consensus sites on protozoan α-tubulin ... Antimicrob Agents Chemother 54:1453-60 (2010). Read more (PubMed: 20145086) » *Travis RL & Woods WG Studies on the mechanism of ...
... data imply that BCL-2 hypermethylation provides a robust biomarker of response to current and next generation cytotoxic agents ... data imply that BCL-2 hypermethylation provides a robust biomarker of response to current and next generation cytotoxic agents ... The reduction of BCL-2 expression in endocrine-resistant cells lowered their apoptotic threshold to anti-mitotic agents: ... The reduction of BCL-2 expression in endocrine-resistant cells lowered their apoptotic threshold to anti-mitotic agents: ...
Many anti tumour drugs are antimitotic, blocking proliferation rather than being cytotoxic ... It belongs to the family of drugs called antimitotic agents … English dictionary of cancer terms ... inhibiting or disrupting mitosis antimitotic drugs antimitotic activity • antimitotic noun … Useful english dictionary ... antimitotic - n. any one of a group of drugs that inhibit cell division and growth, e.g. doxorubicin. The drugs used to treat ...
Hence, we believe that SB715992 could be a novel agent for the treatment of prostate cancer with greater success when combined ... Conclusion Our results clearly show that SB715992 is a potent anti-tumor agent whose therapeutic effects could be enhanced by ... caused significantly greater cell growth inhibition and induction of apoptosis compared to the effects of either agent alone. ... with a non-toxic natural agent like genistein. ... thus making it an excellent candidate for anti-cancer agent. ...
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antimitotic agent listen (AN-tee-my-TAH-tik AY-jent) A type of drug that blocks cell growth by stopping mitosis (cell division ...
... 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 ...
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 ...
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 ...
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 ...
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. ...
Journal of Clinical and Diagnostic Research aims to publish findings of doctors at grass root level and post graduate students, so that all unique medical experiences are recorded in literature.
Targeted anti-mitotic therapies: can we improve on tubulin agents? Nat Rev Cancer 2007;7:107-17. ... Effects of antimitotic agents on endocrine-resistant cell lines. Because treatment options are limited in endocrine-resistant ... 5A). TAMR-BCL-2 cells were significantly less responsive to all antimitotic agents compared with empty vector-transduced TAMR ... The reduction of BCL-2 expression in endocrine-resistant cells lowered their apoptotic threshold to antimitotic agents: ...
Additionally, antimitotic agents are not typically recommended during pregnancy. Additionally, it has not been determined if ... and antitumor agents. Podophyllotoxin derived antitumor agents include etoposide and teniposide. These drugs have been ... For example, ring A is not essential to antimitotic activity. Aromatization of ring C leads to loss of activity, possibly from ... Cragg GM, Kingston DG, Newman DJ (2011). Anticancer Agents from Natural Products, Second Edition (2 ed.). CRC Press. p. 97. ...
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 ...
Antimitotic peptides and depsipeptides. Curr Med Chem Anti-Canc Agents 2002;2:19-53. ... The primary antimitotic mechanism of action of the synthetic halichondrin E7389 is suppression of microtubule growth. Mary Ann ... Antimitotic drugs can interact with tubulin and microtubules in a large number of distinct ways to disrupt microtubule ... The primary antimitotic mechanism of action of the synthetic halichondrin E7389 is suppression of microtubule growth ...
It is also possible that antimitotic agents differentially affect the activity of kinases, such as CDK1 and aurora B, leading ... 1984) Taxol: An antimitotic agent with a new mechanism of action. Pharmacol Ther 25:83-125. ... Details of the antimitotic drug treatments are described in the supplementary materials. All cultures were analyzed by FACS to ... Despite the common state of arrest, the various antimitotic drug treatments resulted in differences in the phosphorylation ...
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.. ...
... having antimitotic activity, anti-multidrug resistance activity, for example P-gl ... Antitumor agents that inhibit the function of microtubules are known as antimitotic agents. Many classes of antimitotic agents ... While antimitotic agents have shown to be some of the most successful agents against malignancies, resistance, both intrinsic ... Colchicine typifies another class of antimitotic agents. Colchicine, while not used as an antitumor agent, is a microtubule ...
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. ...
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. ...
... chemical or biological agents). Any risks identified must be included and managed as part of the general workplace risk ... biological or chemical agents. For example, your dexterity, agility, co-ordination, speed of movement and reach may be impaired ... Biological agents *Infectious diseases. Chemical agents. *Toxic chemicals *Mercury *Antimitotic (cytotoxic) drugs ...
In addition to calcium phosphate, the compositions include an effervescent agent to promote the formation of interconnected ... pores and a cohesiveness agent to maintain the shape and hardness of the hardened composition. When introduced at an implant ... alkylating agents, platinum agents, antimetabolites, topoisomerase inhibitors, antitumor antibiotics, antimitotic agents, ... By "effervescent agent" is meant an agent capable of producing bubbles of gas in a composition or an agent that emerges from a ...
Radiolabeled antimitotic agents [11C]T138067 and [ 18F]T138067 have been synthesized for evaluation as new potential positron ... N2 - Radiolabeled antimitotic agents [11C]T138067 and [ 18F]T138067 have been synthesized for evaluation as new potential ... AB - Radiolabeled antimitotic agents [11C]T138067 and [ 18F]T138067 have been synthesized for evaluation as new potential ... abstract = "Radiolabeled antimitotic agents [11C]T138067 and [ 18F]T138067 have been synthesized for evaluation as new ...
Angiogenesis Modulating Agents. Growth Substances. Growth Inhibitors. Antineoplastic Agents, Phytogenic. Tubulin Modulators. ... Antineoplastic Agents. Topoisomerase II Inhibitors. Topoisomerase Inhibitors. Enzyme Inhibitors. Molecular Mechanisms of ...
Antineoplastic Agents. Tubulin Modulators. Antimitotic Agents. Mitosis Modulators. Molecular Mechanisms of Pharmacological ...
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 ...
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. ...
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 ...
  • Collectively, these data imply that BCL-2 hypermethylation provides a robust biomarker of response to current and next generation cytotoxic agents in endocrine-resistant breast cancer, which may prove beneficial in directing therapeutic strategy for patients with non-resectable, metastatic disease. (garvan.org.au)
  • Systemic chemotherapy forms the mainstay of cancer treatment, and agents that disrupt mitotic spindle assembly - so called `anti-mitotics' - are commonly used to treat a wide variety of cancers. (biologists.org)
  • Our results clearly show that SB715992 is a potent anti-tumor agent whose therapeutic effects could be enhanced by genistein. (wayne.edu)
  • The reduction of BCL-2 expression in endocrine-resistant cells lowered their apoptotic threshold to anti-mitotic agents: nocodazole, paclitaxel and the PLK1 inhibitor, BI2536. (garvan.org.au)
  • Investigating the effects of these agents on microtubule dynamics ( Box 1 ) has revealed much about their mechanism of action. (biologists.org)
  • Three series of antimitotic agents related to tubuloclustin were designed and synthesized in order to enhance the molecular diversity of "tubuloclustin-like" family of compounds. (deepdyve.com)
  • The assay was also used for quantitative comparison of the antimitotic activity of different analogues. (ubc.ca)
  • It revealed the importance of the C-11 to C-13 segment of the diterpene core of eleutherobin for its antimitotic activity. (ubc.ca)
  • 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. (wayne.edu)
  • As the first wave of these new agents enters clinical trails, much hope rests on their outcome. (biologists.org)
  • SB715992, an experimental KSP inhibitor, has been shown to perturb bipolar spindle formation, thus making it an excellent candidate for anti-cancer agent. (wayne.edu)
  • Traditional anti-mitotic agents include the microtubule toxins such as taxol, other taxanes and the vinca alkaloids, all of which have proven successful in the clinic. (biologists.org)
  • It is a type of vinca alkaloid and a type of antimitotic agent. (news-medical.net)
  • It is a type of antimitotic agent. (lbbc.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)
  • As part of a continuing search for new potential anticancer candidates, we describe the synthesis, cytotoxicity and mechanistic evaluation of a series of 4-oxoquinoline-3-carboxamide derivatives as novel anticancer agents. (mdpi.com)
  • The in silico and in vitro mechanistic evaluation indicated the potential of 16b as a lead for the development of novel anticancer agents against gastric cancer cells. (mdpi.com)
  • Anticancer Agents from Natural Products, Second Edition discusses how complex target-oriented synthesis-enabled by historic advances in methodology-has enormously expanded the scope of the possible. (routledge.com)
  • This book covers the current clinically used anticancer agents that are either natural products or are clearly derived from natural product leads. (routledge.com)
  • Although natural plant compounds such as resveratrol, curcumin, oridonin, gossypol, and paclitaxel have proven anticancer potential via autophagic signaling pathways, there is still a great need to find new natural compounds and investigate the underlying mechanisms, to facilitate their clinical use as potential anticancer agents through autophagic induction. (eurekaselect.com)
  • Using a pattern-matching computer program, COMPARE, correlative relationships were investigated between the arrays of P450 activities and the patterns of cytotoxicity exhibited by a large group of anticancer agents of proven or potential clinical utility. (aspetjournals.org)
  • Significant negative correlations between the patterns of P450-dependent 7-benzyloxyresorufin metabolism activity and cell line chemosensitivity were observed for 10 standard anticancer agents (including 6 alkylating agents) and 55 investigational compounds, suggesting a role for P450 metabolism in the inactivation of these agents. (aspetjournals.org)
  • P450 enzyme profiling may thus aid in interpreting the patterns of drug sensitivity and resistance in the NCI tumor cell panel, and may facilitate the identification of anticancer agents whose activity can be altered via cytochrome P450 metabolism. (aspetjournals.org)
  • The expression of P450 enzymes in tumor tissue can have a major impact on the responsiveness of tumors to cancer chemotherapeutic drugs, owing to the central role that these enzymes play in the metabolism of numerous clinically useful anticancer agents ( LeBlanc and Waxman, 1989 ). (aspetjournals.org)
  • 2019. Synthesis, in vitro and in vivo biological evaluation of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones as new potent anticancer agents . (cardiff.ac.uk)
  • 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. (google.com)
  • 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. (aacrjournals.org)
  • Antimitotic drugs can interact with tubulin and microtubules in a large number of distinct ways to disrupt microtubule polymerization and dynamics, and their distinct mechanisms may be important determinants of their specific anticancer activities ( 6 ). (aacrjournals.org)
  • The checkpoint machinery or related activities may be the indirect target of several anti-cancer therapies, including vinca alkaloids and taxanes, which are inhibitors of microtubule dynamics and are among the most effective anti-cancer agents ( 17 ⇓ ⇓ ⇓ - 21 ). (pnas.org)
  • Traditional anti-mitotic agents include the microtubule toxins such as taxol, other taxanes and the vinca alkaloids, all of which have proven successful in the clinic. (biologists.org)
  • Investigating the effects of these agents on microtubule dynamics ( Box 1 ) has revealed much about their mechanism of action. (biologists.org)
  • By contrast, microtubule-targeting agents (MTAs) have a long record of success, usually attributed to the induction of mitotic arrest. (nih.gov)
  • Because the phosphorylation pattern provides insights into the complexity of regulation of the APC, we studied in detail the phosphorylation patterns at a single mitotic state of arrest generated by various antimitotic drugs. (pnas.org)
  • Despite the common state of arrest, the various antimitotic drug treatments resulted in differences in the phosphorylation patterns and phosphorylation stoichiometries. (pnas.org)
  • Studies towards the asymmetric synthesis of novel antimitotic agents. (kidscan.org.uk)
  • 2018. Design, synthesis and evaluation against Chikungunya virus of novel small-molecule antiviral agents . (cardiff.ac.uk)
  • 2018. 2-Alkoxycarbonyl-3-arylamino-5-substituted thiophenes as a novel class of antimicrotubule agents: Design, synthesis, cell growth and tubulin polymerization inhibition . (cardiff.ac.uk)
  • 2017. Virtual screening of acyclovir derivatives as potential antiviral agents: design, synthesis, and biological evaluation of new acyclic nucleoside protides . (cardiff.ac.uk)
  • Collectively, these data imply that BCL-2 hypermethylation provides a robust biomarker of response to current and next generation cytotoxic agents in endocrine-resistant breast cancer, which may prove beneficial in directing therapeutic strategy for patients with non-resectable, metastatic disease. (garvan.org.au)
  • Also called antimitotic or antimicrotubule agents or mitotic inhibitors. (medindia.net)
  • Based on mode of action, payloads fall into three categories: antimitotic, DNA interacting, and transcription inhibitors. (drug-dev.com)
  • 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. (cckinase.com)
  • 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. (cckinase.com)
  • An orally bioavailable antimitotic sulfonamide. (cancer.gov)
  • Abstract 2475: Design and development of combretastatin based unsymmetrical terphenyls as small molecule antimitotic agents. (aacrjournals.org)
  • Anti-Infective Agents publishes original research articles, full-length/mini reviews, drug clinical trial studies and guest edited issues on all the latest and outstanding developments on the medicinal chemistry, biology, pharmacology and use of anti-infective and anti-parasitic agents. (benthamscience.com)
  • 12 . The implantable medical device of claim 1 , wherein the bioactive is an antiproliferative agent. (google.com.au)
  • 2019. A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF5) and pentafluoroethyl (C2F5) substituents: Improved antiproliferative agents against prostate cancer . (cardiff.ac.uk)
  • A taxane is a type of mitotic inhibitor and a type of antimicrotubule agent. (lbbc.org)
  • Your workplace risk assessment should already consider any risks to female employees of childbearing age and, in particular, risks to new and expectant mothers (for example, from working conditions, or the use of physical, chemical or biological agents). (hse.gov.uk)
  • As part of that process, you should consider female employees of childbearing age, including new and expectant mothers, assessing the risks that may arise from any process, working condition or physical, biological or chemical agents. (hse.gov.uk)
  • The head-pieces can alternatively or additionally include a mechanical and/or electrical mechanism that provides one or more substances (e.g., medicine and/or other biological agent, etc.) and/or electrostimulation to a surgical site. (freepatentsonline.com)
  • The assay was also used for quantitative comparison of the antimitotic activity of different analogues. (ubc.ca)
  • Also searched for Ductal breast carcinoma , Antimitotic , and Ductal breast cancer . (clinicaltrials.gov)
  • However, cancer cells develop resistance to several of these agents by altering drug transporters and signaling pathways. (aacrjournals.org)
  • Radiolabeled antimitotic agents [ 11 C]T138067 and [ 18 F]T138067 have been synthesized for evaluation as new potential positron emission tomography (PET) biomarkers for cancer imaging. (elsevier.com)
  • abstract = "Radiolabeled antimitotic agents [11C]T138067 and [ 18F]T138067 have been synthesized for evaluation as new potential positron emission tomography (PET) biomarkers for cancer imaging. (elsevier.com)
  • For use in combination with other chemotherapeutic agents in the treatment of refractory testicular tumors and as first line treatment in patients with small cell lung cancer. (rcsb.org)
  • A ntineoplastic agents are widely used in cancer therapy because they can inhibit growth by disrupt- ing cell division and killing actively growing cells. (cdc.gov)
  • Dexrazoxane is a cardioprotective agent for use in conjunction with doxorubicin indicated for reducing the incidence and severity of cardiomyopathy associated with doxorubicin administration in women with metastatic breast cancer who have received a cumulative doxorubicin dose. (drugbank.ca)
  • His major interests lie in the discovery of novel natural product agents for the treatment of cancer and AIDS, with an emphasis on multidisciplinary and international collaboration. (ebooks.com)
  • A medicine used together with other agents to treat certain types of breast cancer, stomach cancer, prostate cancer, and certain types of head and neck cancer. (lbbc.org)
  • 2019. The discovery of purine-based agents targeting triple-negative breast cancer and the αB-crystallin/VEGF protein-protein interaction . (cardiff.ac.uk)
  • In addition, NKTR-102 is also being tested as a single agent in a Phase 2 clinical trial in patients with second-line colorectal cancer and a Phase 1 clinical trial evaluating NKTR-102 in combination with 5-FU therapy. (prnewswire.com)
  • NKTR-105, a novel anti-mitotic agent, is in a Phase 1 clinical study in cancer patients with refractory solid tumors. (prnewswire.com)
  • Docetaxel is an antineoplastic agent that acts by disrupting the microtubular network in cells that is essential for mitotic and interphase cellular functions. (fresenius-kabi.com)
  • Etoposide is an antineoplastic agent and an epipodophyllotoxin (a semisynthetic derivative of the podophyllotoxins). (rcsb.org)
  • It revealed the importance of the C-11 to C-13 segment of the diterpene core of eleutherobin for its antimitotic activity. (ubc.ca)
  • Determination of the antimitotic agents N-Desacetylcolchicine, demecocline and colchicine in serum and urine. (cdc.gov)
  • Furthermore, the endonuclease inhibitor aurintricarboxylic acid abrogates the ultimate death of neural crest cells treated with antimitotic agents. (jneurosci.org)
  • 2 . The medical device of claim 1 , wherein the anti-hypertensive bioactive agent comprises an angiotensin converting enzyme (ACE) inhibitor. (google.ca)
  • Development of new therapeutic agents based on natural product. (kidscan.org.uk)
  • 7. The method of claim 1 , wherein the stent is coated with a therapeutic agent prior to the crimping procedure. (google.com)
  • The composition can include an active agent or therapeutic substance. (google.ca)
  • Because of these interactions it is considered an antimitotic drug. (wikipedia.org)
  • Amikhelline is an antimitotic drug. (wikipedia.org)
  • The development of drug delivery systems to release antimitotics and facilitate the administration of these agents at appropriate doses and for the required time could lead to improved surgical outcomes. (arvojournals.org)
  • To date, diverse materials have been studied as drug delivery systems for antimitotics in experimental filtration surgery. (arvojournals.org)
  • These anomalies are accompanied by increased sensitivity to anti-mitotic agents, a phenotype dependent on the transcription factor MYC and its downstream target anti-apoptotic protein BCL-XL. (nih.gov)
  • In this report, we have compared and contrasted the effects of these new agents in Taxol-sensitive and -resistant cell lines. (aacrjournals.org)
  • Bioactive peptides, which can be used as cell-targeting or gene delivery agents, have been identified either by panning against purified receptors (19-24) or against intact cells or tissue samples, both in vitro and in vivo (25-33). (neb.com)
  • We actually have to use antimitotic agents to kill the non-neuronal cells. (protocol-online.org)
  • 16$g(a),17$g(a)-Dialkylated steroids are prepared by reacting a 16$g(a)-alkyl-17(20)-enyl-20-silyl ether with an alkylating agent and an enol silyl ether cleaving agent in a suitable solvent. (sumobrain.com)