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.

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 ...
In general, your oncologist will consider your age and type of leukemia you have to recommend you an appropriate treatment. Leukemia treatment is generally less intensive in patients aged over 60 years.. Chemotherapy. Chemotherapy in the treatment of chronic lymphocytic leukemia is, in many cases, unnecessary. Mild chemotherapy can be used to reduce the number of white blood cells and reduce the size of lymph nodes and spleen.. Treatment of acute, myeloid and lymphoid leukemia is based on Anti-mitotic Drugs (anti-mitotic chemotherapy); certain substances that are often used in the chemotherapy of these types of leukemia include vincristine and vinblastine. Those medications inhibit mitotic cellular division, and prevent the damage of the disease in the body. However, the treatment destroys not only the tumor cells but also the normal cells in your bone marrow, which makes you susceptible to infections, bleeding and anemia. A bone marrow transplant may also be considered. Sometimes the therapy ...
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
がん治療への抵抗は、病気の進行と死亡に貢献します。抵抗性のメカニズムの基盤を決定する治療応答の改善に不可欠です。この原稿の詳細 PC 患者におけるドセタキセル抵抗への進行に関与する経路を解剖するため (PC)...
कैंसर के उपचार के लिए प्रतिरोध रोग प्रगति और मौत के लिए योगदान देता है । प्रतिरोध के यंत्रवत आधार का निर्धारण चिकित्सीय प्रतिक्रिया में ...
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 ...
MCF-7 human breast cancer cells do not express caspase 3, thought by some to be a critical component of the apoptosis cascade. Nonetheless, both mock- and bcl-2-transfected MCF-7 cells undergo apoptosis after treatment with a variety of stimuli, including the DNA-cleaving antimitotic agent, neocarzi …
In the recent years, cancer research succeeded with sensitive detection methods, targeted drug delivery systems, and the identification of a large set of genes differently expressed. However, although most therapies are still based on antimitotic agents, which are causing wide secondary effects, the …
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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. ...
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.
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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 ...
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.
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 ...
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
Nokia sites use cookies to improve and personalize your experience and to display advertisements. The sites may also include cookies from third parties. By using this site, you consent to the use of cookies. Learn more ...
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 ...
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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 ...
... 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". The Journal of Antibiotics. ... January 1986). "Rhizoxin, a macrocyclic lactone antibiotic, as a new antitumor agent against human and murine tumor cells and ... 1999). "In vitro evaluation of antimicrotubule agents in human small-cell lung cancer cell lines". Anticancer Research. 19 (5B ...
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. ...
It can be found in many plants, where it serves as a yellow/ochre colouring agent. It is also found in many fruits and ... In vitro screening has identified fisetin as an antimitotic compound. Rodríguez-García C, Sánchez-Quesada C, Gaforio JJ (2019 ... In lab studies fisetin has been shown to be an anti-proliferative agent, interfering with the cell cycle in several ways. Like ... Fisetin has been shown to be an effective senolytic agent in wild-type mice, with effects of increased lifespan, reduced ...
Paclitaxel (Taxol) was a novel antimitotic agent that promoted microtubule assembly. This agent proved difficult to synthesize ... Later, this agent would also be used to treat lung and ovarian cancers. Cisplatin, a platinum-based compound, was discovered by ... Notably, this agent, although developed by the NCI in partnership with Bristol-Myers Squibb, was exclusively marketed by BMS ( ... Most of these agents caused very severe nausea (termed chemotherapy-induced nausea and vomiting (CINV) in the literature) which ...
Roberts VJ, Gorenstein C (1990). "The effect of antimitotic agents on the intraneuronal distribution of lysosomes". Brain Res. ...
Peloruside A, a novel antimitotic agent with paclitaxel-like microtubule-stabilizing activity. Cancer Research 62: 3356-60 ( ...
"Chromosome doubling effects of selected antimitotic agents in Brassica napus microspore culture" (PDF). Czech Journal of ... Antiparasitic agents, Nitrobenzenes, Sulfonamides, Preemergent herbicides, Anilines, Microtubule inhibitors, All stub articles ...
Antimitotic agents are injected into the cyst and left inside for 5 minutes; after 5 minutes the agents are rinsed out. ... Antimitotic agents stop the mitose of the cells of the cyst by interfering with a particular phase of the cell cycle, which ... Antimitotic agents have the side effect of creating a small inflammation which can easily be treated with topical steroids. ... Depending on the kind of cyst, the clinician will choose either antimitotic agents or AS-OCT, if laser has failed or if laser ...
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 ...
"Effect of different antimitotic agents on polyploid induction of anise hyssop (Agastache foeniculum L.) - PubAg". pubag.nal. ...
... 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 ...
Brentuximab vedotin is a chimeric monoclonal antibody that is complexed to the antimitotic agent, monomethyl auristatin E; the ... These IEL often exhibit natural killer and cytotoxic T-cell cell activation markers, contain various toxic agents (e.g. ... drug binds to the cell-membrane protein CD30 to deliver thereby the antimitotic aged into CD30-bearing target cells. This study ...
... 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 ...
This binding delivers monomethyl auristatin E (MMAE), an antimitotic agent that inhibits mitosis, and leads to anti-tumour ...
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 ...
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 ... Agents which act as inhibitors of tubulin, also act as inhibitors of cell division. A microtubule exists in a continuous ... Antivascular agents are similar to colchicine and bind to the colchicine binding site on β-tubulin so development of novel ...
It is an antimitotic agent and shows weak inhibitory activity of blood platelet aggregation induced by simulation of the ... Ōmura Neoxaline an antimiotic agent Hirano, A.; Iwai, Y.; Masuma, R.; Tei, K.; Omura, S. (August 1979). "Neoxaline, a new ...
... 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 ...
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 ...
... 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. ...
... 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. These ... 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 ...
... migrating neuroblasts and immature precursors are silenced with the anti-mitotic agent and astrocytes are infected with a ...
... 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 ...
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 ...
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 ... chemotherapeutic agents or alkylating agents) as part of a standardized chemotherapy regimen. Chemotherapy may be given with a ... Alkylating agents will work at any point in the cell cycle and thus are known as cell cycle-independent drugs. For this reason ...
"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, ...
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. ...
... is also used as an anti-inflammatory agent for long-term treatment of Behçet's disease. It appears to have limited ... Loss of significant antimitotic activity in human lymphocytes". Arthritis and Rheumatism. 15 (2): 213-217. doi:10.1002/art. ... Portincasa P (2016). "Colchicine, Biologic Agents and More for the Treatment of Familial Mediterranean Fever. The Old, the New ... Antigout agents, Glycine receptor antagonists, Heptalenes, Microtubule inhibitors, Orphan drugs, Peripherally selective drugs, ...
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 ...
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 ...
... (pEHG) is an endogenous tripeptide that acts as a tissue-specific antimitotic and selectively ... "Synthesis and assay for activity of a proposed anorexogenic agent, L -pyroglutamyl- L -histidyl-glycine". Canadian Journal of ...
The bulbs of N. poeticus contain the antineoplastic agent narciclasine. This usage is also found in later Arabian, North ... antimitotic, antiplatelet, hypotensive, emetic, acetylcholine esterase inhibitory, antifertility, antinociceptive, chronotropic ... Pettit, GR; Cragg, GM; Singh, SB; Duke, JA; Doubek, DL (1990). "Antineoplastic agents, 162. Zephyranthes candida". Journal of ... "Antineoplastic Agents. 587. Isolation and Structure of 3-Epipancratistatin from Narcissus cv. Ice Follies". Journal of Natural ...
Allergic reaction: The vehicles (solvent containing the drug) or preservatives are usually the agents causing sensitivity, ... They provide anti-inflammatory, antimitotic, and immune-system suppressing actions through various mechanisms. Topical ... or other agents (e.g. salicylic acid) in vehicle that will raise the absorption rate Placement of occlusive dressing on the ... or medium-potency agents instead of potent or superpotent ones. If potent or superpotent topical glucocorticids are necessary ...
... as well as a companion imaging agent that is created by replacing the potent drug with an imaging agent. "Ultrasound First - ... The most advanced SMDC is vintafolide, a derivative of the anti-mitotic chemotherapy drug vinblastine which is chemically ...
The methods involve the use of at least one anti-cancer agent selected from antimetabolite anti-cancer agents, antimitotic anti ... The methods involve the use of at least one antimitotic anti-cancer agents and a superoxide dismutase mimetic to potentiate the ... The present disclosure relates to methods of treating cancers that are responsive to antimitotic anti-cancer agents. ... disclosure relates to methods of treating cancers that are responsive to antimetabolite or antimitotic anti-cancer agents. ...
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.. ...
The most frequently used antimitotic agent in cytogenetic studies is colchicine. We investigated whether the initial treatment ...
Antineoplastic Agents, Phytogenic. Antineoplastic Agents. Tubulin Modulators. Antimitotic Agents. Mitosis Modulators. Molecular ...
Antineoplastic Agents, Phytogenic. Antineoplastic Agents. Tubulin Modulators. Antimitotic Agents. Mitosis Modulators. Molecular ... Antineoplastic Agents, Immunological. Angiogenesis Inhibitors. Angiogenesis Modulating Agents. Growth Substances. Physiological ...
Structure-activity analysis of the interaction of curacin A, the potent colchicine site antimitotic agent, with tubulin and ... Structure-activity analysis of the interaction of curacin A, the potent colchicine site antimitotic agent, with tubulin and ... Structure-activity analysis of the interaction of curacin A, the potent colchicine site antimitotic agent, with tubulin and ... Structure-activity analysis of the interaction of curacin A, the potent colchicine site antimitotic agent, with tubulin and ...
Moreover, further preclinical studies are warranted to explore the molecular mechanisms of these agents in treatment of cancer ... as a potential antitumor agent with particular emphasis on key biosynthesis processes, function of related enzymes and ... Synthesis and antimitotic and tubulin interaction profiles of novel pinacol derivatives of podophyllotoxins.. *A. Abad, J. ... Podophyllotoxin, a medicinal agent of plant origin: past, present and future. *Mounia Guerram, Zhenzhou Jiang, Lu-Yong Zhang ...
Miscellaneous Agent Cholinergic Agonist. Oral. June 20, 2022 In Use. 71335-2122-01. 71335-2122 PREDNISONE. Prednisone. 10.0 mg/ ... Antimitotic Agent Taxane. Intravenous. Sept. 28, 2018 In Use. *1 …. *361. *362 ...
Ko, RJ, Li WY, Koda, RT (1990). Determination of the antimitotic agents N-Desacetylcolchicine, demecocline and colchicine in ... Nerve agentsplus icon *Case Definition: Nerve Agents or Organophosphates. *Toxic Syndrome Description: Nerve Agent and ... Riot control agents/tear gasplus icon *Facts About Riot Control Agents ... Blister agents/vesicantsplus icon *Case Definition: Vesicant (Mustards, Dimethyl Sulfate, and Lewisite) ...
Use as suggested and dosing below is not for antiviral properties but for cellular antimitotic activity at high doses for the ... Antineoplastic agents. Class Summary. These agents inhibit cell growth and proliferation. Useful in the accelerated phase of ... Antiviral agents. Class Summary. These agents inhibit DNA synthesis and viral replication. Nucleoside analogs are initially ... Anti-inflammatory agents. Class Summary. Systemically interfere with events leading to inflammation. ...
Antimitotic agent from plant families Coniferae and Berberidaceae. Interference with microtubular function of the keratinocytes ...
Anti-mitotics (64). *Compounds targeting DNA synthesis and repair (103). *DNA Crosslinking and Alkylating Agents (31) ...
Ko, RJ, Li WY, Koda, RT (1990). Determination of the antimitotic agents N-Desacetylcolchicine, demecocline and colchicine in ... Nerve agentsplus icon *Case Definition: Nerve Agents or Organophosphates. *Toxic Syndrome Description: Nerve Agent and ... Riot control agents/tear gasplus icon *Facts About Riot Control Agents ... Blister agents/vesicantsplus icon *Case Definition: Vesicant (Mustards, Dimethyl Sulfate, and Lewisite) ...
... and anti-mitotic agents (e.g, vincristine and vinblastine). Cytotoxins can be conjugated to a peptide provided herein using ... Such compositions may contain one or more agents such as sweetening agents, flavoring agents, coloring agents and preserving ... emulsifying agents, suspending agents, dispersing agents, solvents, fillers, bulking agents, buffers, vehicles, diluents, and/ ... suspending agent and one or more preservatives. Suitable dispersing or wetting agents and suspending agents are exemplified ...
Natural products (antimitotic agents) (block mitosis and produce metaphase arrest): Vinblastine (Velban) - non-Hodgkins ... make you aware of the adverse health effects of antineoplastic agents; 2. describe how you can be exposed to these agents; and ... The following list contains commonly used antineoplastic agents and some of the cancers treated by these agents [Rogers 1987; ... These agents can also cause health effects among health care workers who work with them. A summary of these health risks and ...
Antimitotic Agents 18% * Hypophosphatemia 17% * Response Evaluation Criteria in Solid Tumors 16% ...
"New Aspects of the Pharmacology of Antimitotic Agents" ,Pharmacol. Rev. , 1963,Vol.15 ,pp449~480。 ...
Willwacher, J.; Kausch-Busies, N.; Fürstner, A. Divergent Total Synthesis of the Antimitotic Agent Leiodermatolide. Angewandte ...
Methoxy-2-styrylchromone a novel microtubule-stabilizing antimitotic agent. Biochemical Pharmacology, 75(4), 826 - 835.*Google ... Sousa, E., Paiva, A., Nazareth, N., Gales, L., et al. (2009). Bromoalkoxyxanthones as promising antitumor agents: Synthesis, ...
Anti-mitotics (64). *Compounds targeting DNA synthesis and repair (103). *DNA Crosslinking and Alkylating Agents (31) ...
2-Amino and 2′-aminocombretastatin derivatives as potent antimitotic agents. Chang, J. Y., Yang, M. F., Chang, C. Y., Chen, C. ... 1-Aroylindoline-hydroxamic acids as anticancer agents, inhibitors of HSP90 and HDAC. Ojha, R., Huang, H. L., HuangFu, W. C., Wu ... 2,3-Dimethoxybenzo[i]phenanthridines: Topoisomerase I-targeting anticancer agents. Li, D., Zhao, B., Sim, S. P., Li, T. K., Liu ... 1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase. Lai, M. J., Ojha, R., ...
Thus, this strategy specifically delivers and concentrates a novel class of isatin-based, tubulin destabilizing agents to ... Targeting urokinase and the transferrin receptor with novel, anti-mitotic N-Alkylisatin cytotoxin conjugates causes selective ... Thus, this strategy specifically delivers and concentrates a novel class of isatin-based, tubulin destabilizing agents to ... anti-mitotic N-Alkylisatin cytotoxin conjugates causes selective cancer cell death and reduces tumor growth. Current Cancer ...
Bates D, Eastman A. (2017) Microtubule destabilising agents: far more than just antimitotic anticancer drugs. Br J Clin ... Penna LS, Henriques JAP, Bonatto D. (2017) Anti-mitotic agents: Are they emerging molecules for cancer treatment?. Pharmacol ... 2006) Oxadiazole derivatives as a novel class of antimitotic agents: Synthesis, inhibition of tubulin polymerization, and ... Boiarska Z, Passarella D. (2021) Microtubule-targeting agents and neurodegeneration. Drug Discov Today, 26 (2): 604-615. [PMID: ...
... which is trastuzumab conjugated with the antimitotic agent emtansine (DM1). The clinical application of these targeted agents ... The anti-tumor activity of trastuzumab as a single agent or in combination with cytotoxic agents has been demonstrated in ... In addition to the antibody, a number of small-molecule HER2 kinase inhibitors are available: lapatinib, an approved agent for ... and we characterize their oncogenic properties and sensitivity to anti-HER2 agents. ...
Explants were kept in NB medium and treated with antimitotic agents to eliminate nonneuronal cells. Explants were allowed to ... A cytoskeletal demolition worker: myosin II acts as an actin depolymerization agent. J. Mol. Biol. ... A cytoskeletal demolition worker: myosin II acts as an actin depolymerization agent. J. Mol. Biol. ... recent in vitro studies have shown that myosin II can act as an actin-depolymerizing agent (Haviv et al., 2008), and that at ...
Carboplatin and cisplatin are alkylating agents and belong to the group of platinum-based antineoplastic agents. They interact ... Evaluate epirubicin (an anthracycline) together with vinorelbine (an anti-mitotic drug) in treating patients with stage II, ... Assess the efficacy and safety of single agent olaparib, a PARP inhibitor, vs standard of care based on physicians choice of ... We particularly plan to focus on the role of oxidative stress and one major environmental agent i.e. ionizing radiation ...
Antimitotic agents such as mitomycin C and 5-fluorouracil are administered to reduce the extent of postoperative scarring and ... Moreover, this agent lowered IOP in a rat model of glaucoma filtration surgery in vivo. RARγ agonists might thus prove ... Brennan B, Chiu Y, Berthelon L, Kolis S, Davies B. Effect of age and gender on the pharmacokinetics of R667, a novel agent for ... Chiu YY, Roth M, Kolis S, Rogovitz D, Davies B. Pharmacokinetics of a novel agent, R667, in patients with emphysema. Br J Clin ...
  • An agent that prevents or interferes with cell division (mitosis). (cdc.gov)
  • Sustancias que bloquean las células en MITOSIS, especialmente los MODULADORES DE LA TUBULINA. (bvsalud.org)
  • Agents that arrest cells in MITOSIS , most notably TUBULIN MODULATORS . (bvsalud.org)
  • Purified podophyllotoxin that is antimitotic, cytotoxic, and available for patient's home use. (medscape.com)
  • This invention allows for the use of drugs that include Formula (I). Formula (I) drugs can be combined with other drugs including anti-proliferative, antiplatelet, antiinflammatory, antithrombotic, cytotoxic, agents that inhibit cytokine binding, cell dedifferentiation inhibitors and anti-lipaemic agents, matrix metaloproteinase inhibitors or cytostatic drugs. (patentpc.com)
  • Metabolic Imaging to Assess Treatment Response to Cytotoxic and Cytostatic Agents. (environmed.pl)
  • However, the linker should efficiently release the cytotoxic agent upon ADC internalization. (creativebiolabs.net)
  • The most frequently used antimitotic agent in cytogenetic studies is colchicine. (nysed.gov)
  • Determination of the antimitotic agents N-Desacetylcolchicine, demecocline and colchicine in serum and urine. (cdc.gov)
  • They are exploited for therapeutic gain in cancer chemotherapy as targets for agents derived from a variety of natural products: taxanes, colchicine and vinca alkaloids. (guidetopharmacology.org)
  • OncoSec uses its OncoSec Medical System electroporation device for up-regulation of IL-12, and ablation of tumors combined with bleomycin (an approved chemotherapy agent). (onemedplace.com)
  • DM1 is also 24-270 times more potent than agents used in conventional chemotherapy, such as paclitaxel. (creativebiolabs.net)
  • Thus, this strategy specifically delivers and concentrates a novel class of isatin-based, tubulin destabilizing agents to tumors in vivo and warrants further detailed preclinical investigation. (edu.au)
  • 2008). 4′-Methoxy-2-styrylchromone a novel microtubule-stabilizing antimitotic agent . (up.pt)
  • Bates D, Eastman A. (2017) Microtubule destabilising agents: far more than just antimitotic anticancer drugs. (guidetopharmacology.org)
  • Boiarska Z, Passarella D. (2021) Microtubule-targeting agents and neurodegeneration. (guidetopharmacology.org)
  • GRAPHICS] Six new antimitotic diterpenes, 2-7, have been isolated from the Caribbean octocoral Erythropodium caribaeorum, Structural variations encountered in this group of natural products test recently proposed pharmacophore models for microtubule stabilizing compounds. (ubc.ca)
  • DM1 is an antimitotic agent that inhibits microtubule assembly leading to cell cycle arrest and apoptosis. (creativebiolabs.net)
  • Objective: The aim of the present review is to give an overview about the role, biosynthesis, and characteristics of Podophyllotoxin (PTOX) as a potential antitumor agent with particular emphasis on key biosynthesis processes, function of related enzymes and characterization of genes encoding the enzymes. (semanticscholar.org)
  • Nerve agents inhibit the action of this enzyme. (cdc.gov)
  • Antineoplastic agents are widely used in cancer therapy because they can inhibit growth by disrupting cell division and killing actively growing cells. (cdc.gov)
  • There is a need for therapeutic agents that inhibit CXCR3 function. (justia.com)
  • Antineoplastic agents - occupational hazards in hospitals. (cdc.gov)
  • Some of these antineoplastic agents are also being used for other purposes such as the treatment of nonmalignant diseases. (cdc.gov)
  • provide and identify control methods and work practices to prevent or reduce your exposure to antineoplastic agents. (cdc.gov)
  • 2009). Bromoalkoxyxanthones as promising antitumor agents: Synthesis, crystal structure and effect on human tumor cell lines . (up.pt)
  • Acetaminophen and hydrocodone is a combination of non-opioid and narcotic or sleep-inducing agents used to treat moderate to severe pain associated with inflammation. (medindia.net)
  • A comprehensive review of topoisomerase inhibitors as anticancer agents in the past decade. (semanticscholar.org)
  • Biotechnological approaches to the production of plant-derived promising anticancer agents: An update and overview. (semanticscholar.org)
  • Mono-ester, di-ester derivatives and rapamycin (esterification at position 31 and 42) have been proven to be effective as antifungal agents (U.S. Patent. (patentpc.com)
  • In these cases, treatment of the disease may need to include systemic antifungal agents, which can interfere or interact with other prescribed medications (eg, ketoconazole, fluconazole, itraconazole) or compromise liver function in patients with liver disease. (medscape.com)
  • The purpose of this literature review is to highlight the antitumour activity of Solanaceae extracts-single isolated compounds and nanoparticles with extracts-and their synergistic effect with chemotherapeutic agents in various in vitro and in vivo cancer models. (semanticscholar.org)
  • Fürstner, A. Divergent Total Synthesis of the Antimitotic Agent Leiodermatolide. (mpg.de)
  • The present disclosure relates to methods of treating cancers that are responsive to antimitotic anti-cancer agents. (epo.org)
  • Folic acid inhibited the antimitotic activity of aqueous extract of R. aquatica in a dose dependent manner. (who.int)
  • The pre-treatment of soybean seeds with antimitotic agents to establish improved genetic pool may also contribute to the enhancement of germination, seedling development, morpho-physiological growth and yield. (journaltocs.ac.uk)
  • The methods involve the use of at least one antimitotic anti-cancer agents and a superoxide dismutase mimetic to potentiate the therapeutic effect of the anti-cancer agent(s). (epo.org)
  • This agent also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2 (B-cell Leukemia 2). (nih.gov)
  • Although N-Mannich bases of amides, imides, hydantoins and various other NH-acidic compounds have been known for a long time, and several drug substances and other compounds bearing an NH-acidic group have been modified by N-aminomethylation and tested as potential medicinal agents, the facile decomposition of several N-Mannich bases in aqueous solution has not been generally recognized. (researchgate.net)
  • The results obtained were compared with methotrexate--a known drug available in market as anti-cancer agent. (who.int)
  • At various concentrations (up to 80%), these agents rapidly penetrate and cauterize skin, keratin, and other tissues. (medscape.com)
  • Greater porosity means the pre-injected anti-cancer agent can penetrate the tumor cells without affecting the surrounding healthy tissue. (onemedplace.com)
  • These agents can also cause health effects among health care worker s who work with them. (cdc.gov)
  • This is soon followed by bone marrow suppression due to the antimitotic effects of T-2 toxin. (medscape.com)
  • Docetaxel is a chemotherapeutic antimitotic agent that works by interfering with cell division. (mpc-pharma.com)
  • When the current is removed, the tumor cells reseal rapidly and trap most of the anti-cancer agent. (onemedplace.com)
  • 1996. Threshold limit values for chemical substances and physical agents and biological indices for 1995/1996. (cdc.gov)
  • We particularly plan to focus on the role of oxidative stress and one major environmental agent i.e. ionizing radiation inducing DNA damage and chromosomal instability. (intechopen.com)
  • IMSEAR at SEARO: Evaluation of antimitotic activity of Rotula aquatica (Lour): a traditional herb used in treatment of cancer. (who.int)
  • In the present study, an attempt has been made to evaluate the antimitotic activity of R. aquatica. (who.int)
  • The different fractions obtained by successive extraction of R. aquatica using solvents of increasing polarity were also evaluated for their antimitotic activity. (who.int)
  • Acenocoumarol is a blood thinner agent prescribed to treat or prevent the formation of blood clots or thrombus in the blood vessels helps by dissolving the blood clots and reducing the complication of thromboembolic disorders. (medindia.net)
  • Expect cure rate of 20-50% if used as single agent. (medscape.com)
  • This characteristic supports its use as an agent to treat rheumatoidarthritis. (patentpc.com)
  • A case in which a potentially exposed person is being evaluated by health-care workers or public health officials for poisoning by a particular chemical agent, but no specific credible threat exists. (cdc.gov)
  • The case can be confirmed if laboratory testing was not performed because either a predominant amount of clinical and nonspecific laboratory evidence of a particular chemical was present or the etiology of the agent is known with 100% certainty. (cdc.gov)