Antimetabolites: Drugs that are chemically similar to naturally occurring metabolites, but differ enough to interfere with normal metabolic pathways. (From AMA Drug Evaluations Annual, 1994, p2033)Antimetabolites, Antineoplastic: Antimetabolites that are useful in cancer chemotherapy.Tetrahydrouridine: An inhibitor of nucleotide metabolism.Floxuridine: An antineoplastic antimetabolite that is metabolized to fluorouracil when administered by rapid injection; when administered by slow, continuous, intra-arterial infusion, it is converted to floxuridine monophosphate. It has been used to treat hepatic metastases of gastrointestinal adenocarcinomas and for palliation in malignant neoplasms of the liver and gastrointestinal tract.Trabeculectomy: Any surgical procedure for treatment of glaucoma by means of puncture or reshaping of the trabecular meshwork. It includes goniotomy, trabeculectomy, and laser perforation.Inosine Monophosphate: Inosine 5'-Monophosphate. A purine nucleotide which has hypoxanthine as the base and one phosphate group esterified to the sugar moiety.Phosphoribosyl Pyrophosphate: The key substance in the biosynthesis of histidine, tryptophan, and purine and pyrimidine nucleotides.Fluorouracil: A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.Mitomycin: An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.6-Mercaptopurine: An antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia.Methotrexate: An antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of TETRAHYDROFOLATE DEHYDROGENASE and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA.Leukemia L1210Folic Acid Antagonists: Inhibitors of the enzyme, dihydrofolate reductase (TETRAHYDROFOLATE DEHYDROGENASE), which converts dihydrofolate (FH2) to tetrahydrofolate (FH4). They are frequently used in cancer chemotherapy. (From AMA, Drug Evaluations Annual, 1994, p2033)Cytarabine: A pyrimidine nucleoside analog that is used mainly in the treatment of leukemia, especially acute non-lymphoblastic leukemia. Cytarabine is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. Its actions are specific for the S phase of the cell cycle. It also has antiviral and immunosuppressant properties. (From Martindale, The Extra Pharmacopoeia, 30th ed, p472)Purines: A series of heterocyclic compounds that are variously substituted in nature and are known also as purine bases. They include ADENINE and GUANINE, constituents of nucleic acids, as well as many alkaloids such as CAFFEINE and THEOPHYLLINE. Uric acid is the metabolic end product of purine metabolism.Antineoplastic Agents: Substances that inhibit or prevent the proliferation of NEOPLASMS.Drug Synergism: The action of a drug in promoting or enhancing the effectiveness of another drug.Drug Screening Assays, Antitumor: Methods of investigating the effectiveness of anticancer cytotoxic drugs and biologic inhibitors. These include in vitro cell-kill models and cytostatic dye exclusion tests as well as in vivo measurement of tumor growth parameters in laboratory animals.DeoxycytidineDrug Evaluation, Preclinical: Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.Cell Survival: The span of viability of a cell characterized by the capacity to perform certain functions such as metabolism, growth, reproduction, some form of responsiveness, and adaptability.Tumor Cells, Cultured: Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely.Neoplasms: New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.Cell Cycle: 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.Cell Division: The fission of a CELL. It includes CYTOKINESIS, when the CYTOPLASM of a cell is divided, and CELL NUCLEUS DIVISION.Cell Line: Established cell cultures that have the potential to propagate indefinitely.Kinetics: The rate dynamics in chemical or physical systems.

High-throughput screening of small molecules in miniaturized mammalian cell-based assays involving post-translational modifications. (1/1229)

BACKGROUND: Fully adapting a forward genetic approach to mammalian systems requires efficient methods to alter systematically gene products without prior knowledge of gene sequences, while allowing for the subsequent characterization of these alterations. Ideally, these methods would also allow function to be altered in a temporally controlled manner. RESULTS: We report the development of a miniaturized cell-based assay format that enables a genetic-like approach to understanding cellular pathways in mammalian systems using small molecules, rather than mutations, as the source of gene-product alterations. This whole-cell immunodetection assay can sensitively detect changes in specific cellular macromolecules in high-density arrays of mammalian cells. Furthermore, it is compatible with screening large numbers of small molecules in nanoliter to microliter culture volumes. We refer to this assay format as a 'cytoblot', and demonstrate the use of cytoblotting to monitor biosynthetic processes such as DNA synthesis, and post-translational processes such as acetylation and phosphorylation. Finally, we demonstrate the applicability of these assays to natural-product screening through the identification of marine sponge extracts exhibiting genotype-specific inhibition of 5-bromodeoxyuridine incorporation and suppression of the anti-proliferative effect of rapamycin. CONCLUSIONS: We show that cytoblots can be used for high-throughput screening of small molecules in cell-based assays. Together with small-molecule libraries, the cytoblot assay can be used to perform chemical genetic screens analogous to those used in classical genetics and thus should be applicable to understanding a wide variety of cellular processes, especially those involving post-transitional modifications.  (+info)

Reactive oxygen species play an important role in the activation of heat shock factor 1 in ischemic-reperfused heart. (2/1229)

BACKGROUND: The myocardial protective role of heat shock protein (HSP) has been demonstrated. Recently, we reported that ischemia/reperfusion induced a significant activation of heat shock factor (HSF) 1 and an accumulation of mRNA for HSP70 and HSP90. We examined the role of reactive oxygen species (ROSs) in the induction of stress response in the ischemic-reperfused heart. METHODS AND RESULTS: Rat hearts were isolated and perfused with Krebs-Henseleit buffer by the Langendorff method. Whole-cell extracts were prepared for gel mobility shift assay using oligonucleotides containing the heat shock element. Induction of mRNA for HSP70 and HSP90 was examined by Northern blot analysis. Repetitive ischemia/reperfusion, which causes recurrent bursts of free radical generation, resulted in burst activation of HSF1, and this burst activation was significantly reduced with either allopurinol 1 mmol/L (an inhibitor of xanthine oxidase) or catalase 2x10(5) U/L (a scavenger of H2O2). Significant activation of HSF1 was observed on perfusion with buffer containing H2O2 150 micromol/L or xanthine 1 mmol/L plus xanthine oxidase 5 U/L. The accumulation of mRNA for HSP70 or HSP90 after repetitive ischemia/reperfusion was reduced with either allopurinol or catalase. CONCLUSIONS: Our findings demonstrate that ROSs play an important role in the activation of HSF1 and the accumulation of mRNA for HSP70 and HSP90 in the ischemic-reperfused heart.  (+info)

Effects of nucleoside analog incorporation on DNA binding to the DNA binding domain of the GATA-1 erythroid transcription factor. (3/1229)

We investigate here the effects of the incorporation of the nucleoside analogs araC (1-beta-D-arabinofuranosylcytosine) and ganciclovir (9-[(1,3-dihydroxy-2-propoxy)methyl] guanine) into the DNA binding recognition sequence for the GATA-1 erythroid transcription factor. A 10-fold decrease in binding affinity was observed for the ganciclovir-substituted DNA complex in comparison to an unmodified DNA of the same sequence composition. AraC substitution did not result in any changes in binding affinity. 1H-15N HSQC and NOESY NMR experiments revealed a number of chemical shift changes in both DNA and protein in the ganciclovir-modified DNA-protein complex when compared to the unmodified DNA-protein complex. These changes in chemical shift and binding affinity suggest a change in the binding mode of the complex when ganciclovir is incorporated into the GATA DNA binding site.  (+info)

Suppression of replication of multidrug-resistant HIV type 1 variants by combinations of thymidylate synthase inhibitors with zidovudine or stavudine. (4/1229)

The replication of recombinant multidrug-resistant HIV-1 clones modeled on clinically derived resistant HIV-1 strains from patients receiving long-term combination therapy with zidovudine (AZT) plus 2',3'-dideoxycytidine was found to regain sensitivity to AZT and stavudine (D4T) as a consequence of a pharmacologically induced decrease in de novo dTMP synthesis. The host-cell system used was phytohemagglutinin-stimulated peripheral blood mononuclear cells; dTMP and dTTP depletion were induced by single exposures to a low level of the thymidylate synthase inhibitor 5-fluorouracil (5-FU) or its deoxynucleoside, 2'-deoxy-5-fluorouridine. The host-cell response to the latter was biphasic: a very rapid decrease in the rate of de novo dTMP formation and, consequently, in intracellular dTTP pools, followed by slower recovery in both indices over 3 to 24 h. With the additional presence of AZT or D4T, however, replication of the multidrug-resistant HIV-1 strains remained inhibited, indicating dependence of HIV DNA chain termination by AZT-5'-monophosphate or 2',3'-didehydro-2', 3'-dideoxythymidine-5'-monophosphate in these resistant strains on simultaneous inhibition of host-cell de novo synthesis of thymidine nucleotides. No effect on viability of control (uninfected) phytohemagglutinin-stimulated/peripheral blood mononuclear cells was noted on 6-day exposures to 5-FU or 2'-deoxy-5-fluorouridine alone or in combination with AZT or D4T, even at drug levels severalfold higher than those used in the viral inhibition studies. These studies may provide useful information for the potential clinical use of AZT/5-FU or D4T/5-FU combinations for the prevention or reversal of multidrug resistance associated with long-term dideoxynucleoside combination therapy.  (+info)

Capsaicin-sensitive C-fiber-mediated protective responses in ozone inhalation in rats. (5/1229)

To assess the role of lung sensory C fibers during and after inhalation of 1 part/million ozone for 8 h, we compared breathing pattern responses and epithelial injury-inflammation-repair in rats depleted of C fibers by systemic administration of capsaicin as neonates and in vehicle-treated control animals. Capsaicin-treated rats did not develop ozone-induced rapid, shallow breathing. Capsaicin-treated rats showed more severe necrosis in the nasal cavity and greater inflammation throughout the respiratory tract than did control rats exposed to ozone. Incorporation of 5-bromo-2'-deoxyuridine (a marker of DNA synthesis associated with proliferation) into terminal bronchiolar epithelial cells was not significantly affected by capsaicin treatment in rats exposed to ozone. However, when normalized to the degree of epithelial necrosis present in each rat studied, there was less 5-bromo-2'-deoxyuridine labeling in the terminal bronchioles of capsaicin-treated rats. These observations suggest that the ozone-induced release of neuropeptides does not measurably contribute to airway inflammation but may play a role in modulating basal and reparative airway epithelial cell proliferation.  (+info)

Mitochondrial regulation of the cytosolic Ca2+ concentration and the InsP3-sensitive Ca2+ store in guinea-pig colonic smooth muscle. (6/1229)

1. Mitochondrial regulation of the cytosolic Ca2+ concentration ([Ca2+]c) in guinea-pig single colonic myocytes has been examined, using whole-cell recording, flash photolysis of caged InsP3 and microfluorimetry. 2. Depolarization increased [Ca2+]c and triggered contraction. Resting [Ca2+]c was virtually restored some 4 s after the end of depolarization, a time when the muscle had shortened to 50 % of its fully relaxed length. The muscle then slowly relaxed (t = 17 s). 3. The decline in the Ca2+ transient was monophasic but often undershot or overshot resting levels, depending on resting [Ca2+]c. The extent of the overshoot or undershoot increased with increasing peak [Ca2+]c. 4. Carbonyl cyanide m-chlorophenyl hydrazone (CCCP; 5 microM), which dissipates the mitochondrial proton electrochemical gradient and therefore prevents mitochondrial Ca2+ accumulation, slowed Ca2+ removal at high ( > 300 nM) but not at lower [Ca2+]c and abolished [Ca2+]c overshoots. Oligomycin B (5 microM), which prevents mitchondrial ATP production, affected neither the rate of decline nor the magnitude of the overshoot. 5. During depolarization, the global rhod-2 signal (which represents the mitochondrial matrix Ca2+ concentration, [Ca2+]m) rose slowly in a CCCP-sensitive manner during and for about 3 s after depolarization had ended. [Ca2+]m then slowly decreased over tens of seconds. 6. Inhibition of sarcoplasmic reticulum Ca2+ uptake with thapsigargin (100 nM) reduced the undershoot and increased the overshoot. 7. Flash photolysis of caged InsP3 (20 microM) evoked reproducible increases in [Ca2+]c. CCCP (5 microM) reduced the magnitude of the [Ca2+]c transients evoked by flash photolysis of caged InsP3. Oligomycin B (5 microM) did not reduce the inhibition of the InsP3-induced Ca2+ transient by CCCP thus minimizing the possibility that CCCP lowered ATP levels by reversing the mitochondrial ATP synthase and so reducing SR Ca2+ refilling. 8. While CCCP reduced the magnitude of the InsP3-evoked Ca2+ signal, the internal Ca2+ store content, as assessed by the magnitude of ionomycin-evoked Ca2+ release, did not decrease significantly. 9. [Ca2+]c decline in smooth muscle, following depolarization, may involve mitochondrial Ca2+ uptake. Following InsP3-evoked Ca2+ release, mitochondrial uptake of Ca2+ may regulate the local [Ca2+]c near the InsP3 receptor so maintaining the sensitivity of the InsP3 receptor to release Ca2+ from the SR.  (+info)

Mechanisms of hypoxic vasodilatation of isolated rat mesenteric arteries: a comparison with metabolic inhibition. (7/1229)

1. Hypoxia (PO2 < 5 mmHg) decreased vessel tone in isolated rat mesenteric arteries precontracted with either high [K+] or the thromboxane analogue U46619. This response was not altered by N-nitro-L-arginine (L-NA) and indomethacin. 2. Simultaneous measurement of pHi and tension showed that the decrease in vessel tone was accompanied by an intracellular acidification. Similar reductions in tone and pHi were observed with the metabolic inhibitors 2,4-dinitrophenol (DNP) and sodium azide. 3. The presence of the lactate transport inhibitor alpha-cyano-4-hydroxy-cinnamic acid (CHC) increased the magnitude of the acidification and resulted in a significantly faster reduction in tone in response to hypoxia. Addition of CHC to normoxic tissues caused both a vasodilatation and a reduction of pHi. 4. A decrease in pHi induced on washout of ammonium chloride (NH4Cl) resulted in an increase in tone. 5. Relaxation to hypoxia or metabolic inhibition was unaffected when the change in pHi was neutralized by addition of the weak base trimethylamine (TMA). 6. It is concluded that severe hypoxia decreases tone in isolated rat mesenteric arteries by a mechanism which is independent of nitric oxide and prostaglandins. Both severe hypoxia and metabolic inhibition reduced pHi, although this does not appear to be contributing to the changes in tone observed.  (+info)

Cooperative therapeutic effects of androgen ablation and adenovirus-mediated herpes simplex virus thymidine kinase gene and ganciclovir therapy in experimental prostate cancer. (8/1229)

Adenovirus-mediated transduction of the herpes simplex thymidine kinase gene (HSV-tk) in conjunction with ganciclovir (GCV) has been shown to result in significant growth suppression and to enhance survival in a model of mouse prostate cancer. However, this therapeutic activity is not sustained, because in most cases tumors eventually regrow and ultimately cause the death of the host. Androgen ablation, an inducer of apoptosis in prostate cells which is used widely as palliative therapy in patients with prostate cancer, was combined with HSV-tk plus GCV using an androgen-sensitive mouse prostate cancer cell line. The combination of castration and HSV-tk plus GCV led to markedly enhanced tumor growth suppression in both subcutaneous and orthotopic models compared with either treatment alone and resulted in an enhanced survival in which combination-treated animals lived twice as long as controls in the subcutaneous model and over 50% longer than controls in the orthotopic model. Further analysis of apoptotic activity demonstrated high levels of apoptosis only in combined androgen ablation and HSV-tk plus GCV-treated tumors after 14 days of growth in an androgen-depleted environment and 8 days after HSV-tk plus GCV therapy. At this time, the apoptotic index, but not the percent of necrotic tissue, was significantly higher for combination therapy-treated tumors relative to control-treated tumors or either treatment alone. These data indicate that the therapeutic effects of androgen ablation and HSV-tk plus GCV are cooperative and that increased apoptosis may, in part, underlie these activities.  (+info)

*Antifolate

... s are a class of antimetabolite medications that antagonise (that is, block) the actions of folic acid (vitamin B9). ...

*Antimetabolite

An antimetabolite is a chemical that inhibits the use of a metabolite, which is another chemical that is part of normal ... Anti-metabolites also affect RNA synthesis. However, because thymidine is used in DNA but not in RNA (where uracil is used ... The presence of antimetabolites can have toxic effects on cells, such as halting cell growth and cell division, so these ... Antimetabolites can be used in cancer treatment, as they interfere with DNA production and therefore cell division and tumor ...

*FM (chemotherapy)

... an antimetabolite; (M)itoxantrone - a synthetic antracycline analogue (an antraquinone) that is able to intercalate DNA and ...

*DAT (chemotherapy)

... an antimetabolite; (T)hioguanine - another antimetabolite. Randomized Comparison of DAT Versus ADE as Induction Chemotherapy in ...

*FCM (chemotherapy)

... an antimetabolite; (C)yclophosphamide - an alkylating antineoplastic agent from the oxazafosforine group; (M)itoxantrone - a ...

*Alanosine

It is an antimetabolite. It is used as one of a few experimental treatments for patients with deadly pancreatic cancer when the ...

*DAM (chemotherapy)

... an antimetabolite; (M)ercaptopurine - another antimetabolite.. ...

*GemOx

... an antimetabolite; (Ox)aliplatin - a platinum-based antineoplastic agent with alkylating mechanism of action. GEMOX-R regimen ...

*Interferon

... enhancement by antimetabolites". Proc. Natl. Acad. Sci. U.S.A. 67 (1): 464-71. doi:10.1073/pnas.67.1.464. PMC 283227 . PMID ...

*Immunosuppressive drug

Antimetabolites interfere with the synthesis of nucleic acids. These include: folic acid analogues, such as methotrexate purine ...

*Chemotherapy

Anti-metabolites are a group of molecules that impede DNA and RNA synthesis. Many of them have a similar structure to the ... Unlike alkylating agents, anti-metabolites are cell cycle dependent. This means that they only work during a specific part of ... Pemetrexed is another anti-metabolite that affects purine and pyrimidine production, and therefore also inhibits DNA synthesis ... Subtypes of the anti-metabolites are the anti-folates, fluoropyrimidines, deoxynucleoside analogues and thiopurines. The anti- ...

*Dilworth Wayne Woolley

Books by Woolley included A Study of Antimetabolites (1952), and The Biochemical Bases of Psychoses (1962). Woolley married ... Dilworth Wayne Woolley, A Study of Antimetabolites (Wiley 1952). Dilworth Wayne Woolley, The Biochemical Bases of Psychoses, or ...

*Tegafur/uracil

Tegafur is a type of antimetabolite. Uracil has also been stated to help protect the gastrointestinal tract from 5-FU toxicity ...

*Trifluridine/tipiracil

Emura, T; Suzuki, N; Yamaguchi, M; Ohshimo, H; Fukushima, M (Sep 2004). "A novel combination antimetabolite, TAS-102, exhibits ... Peters, Godefridus (December 2012). "TAS-102: more than an antimetabolite". The Lancet Oncology. 13 (12): e518-e519. doi: ...

*Enzyme inhibitor

Antimetabolite Pharmacophore Transition state analog Shapiro, R; Vallee, BL (1991). "Interaction of human placental ...

*Ethionine

... is an antimetabolite and methionine antagonist. It prevents amino acid incorporation into proteins and interferes ...

*Squamous cell skin cancer

The antimetabolites azathioprine and mycophenolic acid have an intermediate risk profile. Diagnosis is confirmed via biopsy of ...

*Purine analogue

... s are antimetabolites that mimic the structure of metabolic purines. Azathioprine is the main immunosuppressive ... Parker, William B. (2009). "Enzymology of Purine and Pyrimidine Antimetabolites Used in the Treatment of Cancer". Chem Rev. 109 ... Purine Mercaptopurine Thioguanine Fludarabine Purine antimetabolites are commonly used to treat cancer by interfering with DNA ...

*Tioguanine

... is in the antimetabolite family of medications. It is a purine analogue of guanine and works by disrupting DNA and ...

*Ansamycin

Naphthomycin, an antimetabolite of vitamin K". Arch. Mikrobiol. 65 (4): 303-17. doi:10.1007/bf00412210. PMID 4988744. Sensi, P ...

*Methotrexate

... is an antimetabolite of the antifolate type. It is thought to affect cancer and rheumatoid arthritis by two ...

*Pyrimidine analogue

Parker, William B. (2009). "Enzymology of Purine and Pyrimidine Antimetabolites Used in the Treatment of Cancer". Chem Rev. 109 ... Pyrimidine analogues are nucleoside analog antimetabolites which mimic the structure of metabolic pyrimidines. 5-Fluorouracil ( ... Pyrimidine antimetabolites are commonly used to treat cancer by interfering with DNA replication. ...

*8-Azaguanine

Timmis, G.M.; Williams, Donald Charles (1967). "Chemotherapy of Cancer: the Antimetabolite Approach: The Antimetabolite ...

*Hydroxycarbamide

2015). Hydroxyurea is a monohydroxyl-substituted urea (hydroxycarbamate) antimetabolite. Similar to other antimetabolite anti- ...

*Management of ulcerative colitis

Mercaptopurine is a cytostatic drug that is an antimetabolite. The mercaptopurine molecule mimics purine, which is necessary ...
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Two New Antimetabolites of Biotin: α-Methyldethiobiotin and α-Methylbiotin: Two new antimetabolites of biotin were isolated from culture filtrates of Streptomyc
A drug that is similar enough to a natural chemical to participate in a normal biochemical reaction in cells but different enough to interfere with the normal division and functions of cells. So named because the drug inhibits a normal metabolic process. Examples of antimetabolites include 6-mercaptopurine (6MP), methotrexate, and hydroxyurea. Anticancer drugs that closely resemble substances needed by cells for normal growth. The tumor cells uses the drug instead and "starves" for lack of proper substance. ...
Lindner, A and Kutham, T, "Cytochemical effects of antimetabolites and steroids on ascites tumors, a histochemical study. Abstr." (1963). Subject Strain Bibliography 1963. 690 ...
http://www.grandviewresearch.com/industry-analysis/immunomodulators-market. The entire immunomodulators market is bifurcated into immunosuppressants (antimetabolites, antibodies, interferon beta, glucocorticoids and calcineurin inhibitors) and immunostimulators (vaccines, interferon alpha and antibodies). Immunosuppressants have a broader spectrum for drugs in the pipeline such as antiproliferative drugs and antimetabolite drugs. Antimetabolites are expected to gain a wider share in the market as they inhibits induction of hypersensitivity which is a common skin disease. Immunostimulants are anticipated to register greater market share owing to its increased usage in the treatment of multiple sclerosis and increasing incidence rate of cancer and allergies.. Continuous research is going on with respect to immunomodulators in other medical conditions such as diabetes and Alzheimers disease. North America held the highest market share pertaining to factors such as favorable government policies and ...
I cant answer your question entirely but I can tell you how its processed. The liver processes the Imuran in to one of two things: 6MMP and 6TG. Now some people metabolize it entirely into 6MMP-- this is what causes Alkaline Phosphate levels to rise in the blood and causes most people to be taken off for too high liver counts. Some people metabolize it entirely into 6TG and 6TG is what is good for fighting Crohns, but it also lowers the white cells in the body (which is okay if they are being monitored and are at a decent level). 6TG is what controls the T-cells in the body. Most people metabolize Imuran into a mix of both ...
Using the Quick Order field, you can add a product to your shopping cart with just one click. All you have to do: enter the Cat.No. as shown in our catalog in the format xxxxx.yy and click the Go!-Button.. ...
In this article you will know all of the Main drugs used in cancer treatment. Know about Mitotic Inhibitors, Antibiotics, Antimetabolites and Alkylating
Fludara: Fludarabine belongs to the group of cancer-fighting medications known as antineoplastics, and specifically to the family of antineoplastics called antimetabolites.
Read "Genetically modified fibroblasts induce angiogenesis in the 3×6 cm rat epigastric island flap, European Journal of Plastic Surgery" on DeepDyve, the largest online rental service for scholarly research with thousands of academic publications available at your fingertips.
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Looking for online definition of Antimetabolites, antineoplastic in the Medical Dictionary? Antimetabolites, antineoplastic explanation free. What is Antimetabolites, antineoplastic? Meaning of Antimetabolites, antineoplastic medical term. What does Antimetabolites, antineoplastic mean?
In this paper the results of the influence of various metabolic inhibitors on dif- ferent periods of the vernalization process in winter wheat are provided. It was found that the initial period of vernalization is very sensitive to respiratory inhibitors such as azide and 2, 4-nitrophenol. In the middle period, the inhibitor of nucleo-acid metabolism such as 2-thiouracil significantly prolongated the process of vernalization. At the third period the protein metabolic inhibitor such as chloromycetin strongly inhibited the vernalization process. Our experiments demonstrated that a remarkable replacement of metabolic patterns is existed in the course of vernalization of winter wheat. The relative metabolic processes during the time of vernalization not only car- ried on different in rate and in action model of inhibitors but also alternatively. There- fore, we assumed that vernalization process of winter wheat may be divided into several periods (sub-processes) with different metabolic patterns. On the
Furuno, I; Asami, K; and Matsudaira, H, "Inhibition by x-irradiation and antimetabolites of dna synthesis without affecting camp elevation in isoproterenol-stimulated mouse parotid gland." (1974). Subject Strain Bibliography 1974. 2001 ...
Antimetabolite A substance bearing a close structural resemblance to one required for normal physiological functioning, and exerting its effect by interfering with the utilization of the essential metabolite. It competes with, replaces, or antagonizes a particular metabolite; for example, ethionine is an antimetabolite of methionine.methotrexatefolic acidcancerCancercancercancer
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1.Polyfunctional alkylating agents 2.Other Alkylating Drugs 3.Antimetabolites 4.Purine antagonists 5.Pyrimidine antagonists 6.Plant alkaloids 7.Antibiotics 8.Monoclonal Antibodies, 9.Hormonal agents, 10.Miscellaneous anticancer drugs
Gemzar: Gemcitabine belongs to the group of cancer-fighting medications known as antineoplastics, and specifically to the group of antineoplastics known as antimetabolites. Gemcitabine fights cancer by preventing the growth of cancer cells, which eventually results in their destruction. It is used to treat certain types of lung cancer, bladder cancer, breast cancer, and cancer of the pancreas.
Teva-Capecitabine: Capecitabine belongs to the group of cancer-fighting medications known as antineoplastics, and specifically to the group of antineoplastics known as antimetabolites. Capecitabine fights cancer by killing cancer cells and preventing their growth. Capecitabine may be used alone or in combination with other medications to treat certain types of breast cancer and colorectal cancer.
The different types of chemotherapy treatment for cancer including plant alkaloids, antitumor antibiotics, antimetabolites, topoisomerase inhibitors and antineoplastics.
Baseline characteristics were balanced between the arms (E, n = 86; C, n = 88). In the protocol-specified analysis (data cut-off 11 April 2012), the hazard ratio (HR) for OS was 0.92 (95% CI 0.63-1.35, p = 0.68; median OS 22.9 vs 19.6 months for E vs C). When adjusted for baseline factors (age, gender, ECOG PS, smoking history and EGFR mutation type), the HR was 0.86 (95% CI 0.58-1.27). A total of 58% of patients received 2L PST (tyrosine-kinase inhibitors: 31% E, 58% C; platinum compounds: 44% E, 5% C; antimetabolites: 48% E, 19% C). Median time to initiation of 2L PST from time of disease progression (n = 102) was 0.85 months for E and 0.36 months for C. Using method 1, the HR was 0.68 (95% CI 0.37-1.25, p = 0.21; median OS was not reached with E vs 20.8 months with C). The adjusted HR was 0.63 (95% CI 0.34-1.19). Using method 2, the HR was 0.69 (95% CI 0.38-1.26), with an adjusted HR of 0.65 (95% CI 0.35-1.20). ...
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Methotrexate, sold under the trade names Rheumatrex and Trexall, is classified as an antimetabolite medication. This means that it effectively interferes...
Proven and potential clinical benefits of washing red blood cells before transfusion: current perspectives Amy E Schmidt, Majed A Refaai, Scott A Kirkley, Neil Blumberg Department of Pathology and Laboratory Medicine, University of Rochester Medical Center, Rochester, NY, USA Abstract: Red blood cells (RBCs) are washed for a variety of reasons such as to remove excess potassium, cytokines, and other allergen proteins from the supernatant and/or to mitigate the effects of the storage lesion. The storage lesion is a product of RBC aging and include leakage of potassium and chloride from the RBCs, depletion of 2,3-diphosphoglycerate and adenosine triphosphate, loss of phospholipids and cholesterol, exposure of phosphatidylserine, elaboration of lipid mediators, loss of glutathione, autoxidation of hemoglobin to methemoglobin contributing to decreased blood flow viscosity and adherence to endothelial cells, increased microparticle formation, and disruption of NO-mediated vasodilation. A
BACKGROUND: Infliximab withdrawal in patients with Crohns disease on concomitant antimetabolite therapy is considered to be superior if obtained after a maintenance therapy period compared to induction alone.. METHODS: We retrospectively analyzed the outcome of Crohns disease patients treated with infliximab and an antimetabolite after infliximab was withdrawn using induction alone or induction plus at least 1-year of maintenance therapy. The time to relapse was analyzed using univariate and multivariate analyses. The model was adjusted according to the period of infliximab withdrawal.. RESULTS: A total of 92 patients were included, 54 in the induction alone group. The patient characteristics were identical in the two groups except for the period of infliximab withdrawal. After a median follow-up period of 47.1 (interquartile range=4.4-110.2) months, 66 patients (72%) experienced a relapse. After a year-adjustment, no significant difference was observed between the two groups. Based on ...
VACUETTE Glycolytic Inhibitor, Potassium Oxalate and Sodium Fluoride 4 ml, 13 x 75 mm case of 1200 for use in glucose and lactate determinations. Buy Now!
The purpose of this study is to compare whether there is a delay or prevention of recurrence or death in subjects with surgically removed pancreatic cancer who then take nab-paclitaxel in combination with gemcitabine compared to those who take gemcitabine alone.. ...
Specializing in Buying and selling widely in the areas of Childrens, Art, Scholarly, Photography, Sports, Bindings. Have been actively selling for over 25 years and, though were more generalists than specialists, we do place a particular focus on books and ephemera in the above areas. Will travel far and wide to look at interesting collections and always welcome inquiries. ...
Pseudomonas syringae is pathogenic in a wide variety of plants, causing diseases with economic impacts. Pseudomonas syringae pathovars produce several toxins that can function as virulence factors and contribute to disease symptoms. These virulence factors include antimetabolite toxins, such as tabtoxin, phaseolotoxin and mangotoxin, which target enzymes in the pathways of amino acid metabolism. The antimetabolite toxins are generally located in gene clusters present in the flexible genomes of specific strains. These gene clusters are typically present in blocks of genes that appear to be integrated into specific sites in the P. syringae core genome. A general overview of the genetic organization and biosynthetic and regulatory functions of these genetic traits of the antimetabolite toxins will be given in the present work.
firm role in the growth development and heredity of living organisms (Nurse 2000). During this phase DNA is synthesised from the original DNA template (replication kratom tincture for sale richardson origins) to yield two DNA strands and duplication of chromosomes (sister chromatids) which Kratom Herb Store Cross involves protein synthesis and packaging of the DNA into chromosomes.. The effect of chloroform and MSE on clonogenicity 2. Chapter 2 2. Chapter 3 3. Effect of metabolic inhibitors on the cytotoxicity of MSE and MIT in metabolically competent MCL-5 cells Discussion Genotoxic potential of MSE and MIT Introduction Materials and methods 3. Cell line and conditions 3.. Cell lines and culture conditions 2. Resuscitation of frozen cells 2. Cell quantification and viability 2. Preparation and analysis of methanol-chloroform extract of Mitragyna speciosa Korth (MSE) 2.. A ridiculous waste of money. Wen you find it at head shops in Seattle it looks like loose-leaf tea or powder (sold either in a ...
Take this medicine exactly as directed by your doctor. You may be told to take a higher dose to start, then reduce as your thyroid levels become normal, but your doctor will work out the best dose for you. Propylthiouracil should be taken with a glass of water. The total daily dose may be taken in divided doses over the day or as a single daily dose. Try to get into the habit of taking this medicine at the same times each day to avoid missing any doses. If you forget to take a dose, take it as soon as you remember. Do not take two doses together. If it is almost time to take the next dose, wait until then and then carry on as before. Treatment with propylthiouracil may continue for up to two years. If you suspect that you or someone else has taken an overdose of propylthiouracil contact your doctor or go to the accident and emergency department of your local hospital at once. Always take the container with you if possible, even if it is empty. This medicine is for you. Never give it to others ...
Cancer drugs can be divided into two general classes: CELL CYCLE SPECIFIC DRUGS (CCS; esp. plant alkaloids and antimetabolites), and CELL CYCLE NON-SPECIFIC DRUGS (CCNS; esp. alkylating agents and some natural products). Antineoplastic agents can also be organized according to their chemical class, mechanism of action, therapeutic use or their toxicities ...
Research and Markets: Investigation Report on Chinas Pemetrexed Market, 2009-2018: A Multi-Targeted Antimetabolite Antitumor Drug
Nucleoside analouges belong to the fmalily of antimetablits that resemble the neleosieds for uptake and metaolism that inibitr dna sytnse and couase cain termination. It is a durg target for cacner and viral infcations. ...
The IUPHAR/BPS Guide to Pharmacology. D-cycloserine ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
Raltitrexed (Tomudex, TDX, ZD 1694) is an antimetabolite drug used in cancer chemotherapy. It is an inhibitor of thymidylate synthase, and is manufactured by AstraZeneca. Used in treatment of colorectal cancer since 1998. It may also be used in the treatment of malignant mesothelioma. Raltitrexed is chemically similar to folic acid and is in the class of chemotherapy drugs called folate antimetabolites, which inhibit one or more of three enzymes that use folate and derivatives as substrates: DHFR, GARFT and thymidylate synthase. Raltitrexed is fully active after polyglutamylation, which allows cellular retention of the drug. By inhibiting Thymidylate synthase (TS), thus formation of precursor pyrimidine nucleotides, raltitrexed prevents the formation of DNA and RNA, which are required for the growth and survival of both normal cells and cancer cells. Inhibition of L1210 cell growth in culture IC50 = 9 nM, is one of the strongest antimetabolites in use. Structure and phase I clinical trial of the ...
Get a Sample of D-Cycloserine (CAS 68-41-7) Sales market research report from- http://www.marketreportsworld.com/enquiry/request-sample/10312763. Market Segment by Regions, this D-Cycloserine (CAS 68-41-7) Sales market report splits Global into several key Regions, with sales (consumption), revenue, market share and growth rate of D-Cycloserine (CAS 68-41-7) Sales Market from 2011 to 2022 (forecast), like:. 1. North America. 2. China. 3. Europe. 4. Japan. 5. Southeast Asia. 6. India. No. of Report Pages: 121. Price (Single User Licence): $4000. Buy the D-Cycloserine (CAS 68-41-7) Sales market Report at: http://www.marketreportsworld.com/purchase/10312763. This D-Cycloserine (CAS 68-41-7) Sales Industry report also takes into account the past price of 2011-2015 and future price of 2016-2021 as per the supply-demand relation along with perspectives and D-Cycloserine (CAS 68-41-7) Sales market forecasts. Additionally, the D-Cycloserine (CAS 68-41-7) Sales Market report also discusses the data on ...
Methotrexate is an antineoplastic anti-metabolite. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the "S" phase (of the cell cycle), stopping normal development and division. Methotrexate inhibits folic acid reductase which is responsible for the conversion of folic acid to tetrahydrofolic acid. At two stages in the biosynthesis of purines and at one stage in the synthesis of pyrimidines, one-carbon transfer reactions occur which require specific coenzymes synthesized in the cell from tetrahydrofolic acid. Tetrahydrofolic acid itself is synthesized in the cell from folic acid with the help of an enzyme, folic acid reductase. Methotrexate looks a lot like folic acid to the enzyme, so it binds to it quite strongly and inhibits the enzyme. Thus, DNA synthesis cannot proceed because the coenzymes needed for one-carbon transfer reactions are not produced from tetrahydrofolic acid ...
In order to understand antimetabolites and how they work, it is necessary to briefly discuss the processes that are being targeted by these agents. The term metabolism refers to the many chemical reactions that take place in our bodies. We are constantly breaking down food into usable components and using those components to build our proteins, DNA and other cellular structures. Metabolite is a general term for the organic compounds that are synthesized, recycled, or broken down in cells. Materials that provide us with key metabolites enter our body as food. These compounds can be broken down into simpler structures that can be re-used in our cells. Examples include vitamins and amino acids. Metabolites that are the end products of a process or pathway may be excreted by the body. An example is urea, the end product of protein metabolism, excreted by the body as a component of urine. ...
I found out that glyphosate is an aminophosphonic analogue of glycine. First question: How is it different? Is there a phosphate group added onto it? What does being an aminophosphonic analogue entail?Now, the analogues act as antimetabolites, which interefere, at least in this case, with the production of the plants amino acids. They compete with normal substrates at the active site, denaturing the enzyme, and making it useless for its original purpose. So here lies my second question: Is there a substrate that is non-competitive to do this same thing OR are there even allosteric sites on such enzymes?Many thanks ...
Looking for Antitumour antibiotic? Find out information about Antitumour antibiotic. any one of a group of synthetic or natural substances used in the treatment of malignant tumors. Antineoplastics include alkylating agents , antimetabolites... Explanation of Antitumour antibiotic
293649200 - EP 0987265 A1 2000-03-22 - Interleukin-5 inhibiting 6-azauracil derivatives - The present invention is concerned with the compounds of formula CHEM the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein p is 0 to 4; X is O, S, NR 5 or a direct bond; Y is O, S, NR 5 or S(O)2; R 1 independently is C1-6alkyl, halo, polyhaloC1-6alkyl, hydroxy, mercapto, C1-6alkyloxy, C1-6alkylthio, C1-6alkylcarbonyloxy, aryl, cyano, nitro, Het 3 , R 6 , NR 7 R 8 or substituted C1-4alkyl; R 2 is Het 1 , C3-7cycloalkyl or optionally substituted C1-6alkyl and if X is O, S or NR 5 , then R 2 may also represent aminocarbonyl, aminothiocarbonyl, C1-4alkylcarbonyl, C1-4alkylthiocarbonyl, arylcarbonyl, arylthiocarbonyl, Het 1 carbonyl or Het 1 thiocarbonyl; R 3 and R 4 independently are hydrogen, C1-6alkyl or C3-7cycloalkyl; R 3 and R 4 form a C2-6alkanediyl; R 5 is hydrogen or C1-4alkyl; R 6 a sulfonyl or sulfinyl derivative; R 7 and R 8 are
In a small randomised, prospective study, OBrart and co-workers1 attempted to prove that trabeculectomy (n=25) provided better intraocular pressure (IOP) control than viscocanalostomy (n=23). However, we have serious concerns about the methodology of this study that need to be addressed.. Viscocanalostomy is characterised by the injection of viscoelastic into Schlemms canal.2 However, this was not performed in half of the patients randomised to this group. This would be as inappropriate as using an antimetabolite in only half the patients in the trabeculectomy group, and then comparing this entire group to the viscocanalostomy group. Although the authors do state that the subgroup of patients with intracanalicular viscoelastic injection was inferior to trabeculectomy, this cohort consisted only of 12 patients and it is not known how many had completed follow up after 18 months. Surely, these small numbers are insufficient to draw such conclusions.. We are also concerned that the use of ...
IKKbeta is the key kinase in the TNFalpha-NF-kB pathway that phosphorylates IkBalpha and targets it for polyubiquitination and degradation. As a result, NF-kB is released and moves into the nucleus, where it binds to the promoters of target genes and activates transcription that increases cell proliferation or prevents apoptosis. In the chapter two of this dissertation, a novel role for the TNFalpha-IKK-NF-kB signaling pathway in anti-cancer drug resistance is described. Contrary to its physiological function, TNFalpha induced G0-G1 cell cycle arrest through IKK in cancer cells, which provided a mechanism for developing drug resistance to the purine and pyrimidine antimetabolites. A specific IKKbeta inhibitor prevented TNFalpha-induced drug resistance. Thus IKK inhibitors can enhance the effectiveness of antimetabolites in chemotherapy.; Phosphorylation regulates the kinase activity of IKKbeta. In chapters three and four of this dissertation, mass spectrometry-based proteomic methods was ...
Trade Name: Xeloda®. For which conditions is this drug approved? Capecitabine is FDA approved for initial treatment for metastatic colorectal cancer, stage III colorectal cancer, treatment for metastatic breast cancer in addition to the chemotherapy agent docetaxel (Taxotere®) after cancer progression following anthracycline chemotherapy, and treatment for metastatic breast cancer in patients who have been treated with both anthracycline and paclitaxel (Taxol®) chemotherapy. It is important for patients to remember that physicians have the ability to prescribe medication for conditions other than those for which the drug has been approved by the FDA. Patients who have received a prescription of this drug for a condition other than which it is approved may wish to discuss this issue with their physician.. What is the mechanism of action? Capecitabine belongs to a group of drugs called antimetabolites. Antimetabolites produce their anti-cancer effects by inhibiting the ability of a cell to ...
Hearts isolated from 11- and 12-day rat embryos were incubated in a simple salt solution to which was added the metabolic inhibitors iodoacetate, malonate, 2, 4-dinitrophenol or trypan blue. Comparisons were made between the two age-groups and it was observed that both 11- and 12-day hearts exhibited depressed contractile activity with the glycolytic inhibitor iodoacetate. Malonate did not depress contraction rate in the younger hearts but significantly depressed the rate in the older hearts. A greater inhibitory action on the older hearts as compared with the younger hearts was also produced by 2, 4-dinitrophenol. These results were interpreted as further evidence of a shift in dependence on pathways other than glycolysis between days 11 and 12 of development.. The teratogenic agent trypan blue was shown to depress contraction rate when added to the incubation medium. This effect could be reversed by adding glycolytic intermediates such as fructose-1, 6-diphosphate or alpha glycerophosphate. ...
Definition of tioguanine in the Definitions.net dictionary. Meaning of tioguanine. What does tioguanine mean? Information and translations of tioguanine in the most comprehensive dictionary definitions resource on the web.
The purpose of this work was to determine the role of metabolic energy [adenosine triphosphate (ATP)] in the expression of cytotoxicity of the antitumor drug, Adriamycin (ADRM), in Chinese hamster fibroblasts. When ADRM-sensitive V79 cells or an ADRM-resistant variant, 77A, were pretreated with either 6 mm 2-deoxy-d-glucose or 0.2 mm 2,4-dinitrophenol for 18 hr and then exposed to ADRM for 1 hr at 37°, we observed a substantial increase in cellular survival. In the case of V79 cells pretreated with deoxyglucose, as much as a 1000-fold increase in survival was measured. The maximum dose of ADRM for V79 cells was 3 µg/ml, and for 77A cells it was 15 µg/ml.. The effects of metabolic inhibitors on intracellular ATP content, ADRM uptake, mitotic indices, cellular multiplication, and plating efficiency were measured in untreated as well as in inhibitor-treated cells. The same concentrations of deoxyglucose (6 mm) and dinitrophenol (0.2 mm) that were used for cytotoxicity studies were also used in ...
Fludarabine (NSC 118218) is a DNA synthesis inhibitor, which also inhibits phosphorylation of STAT1. Fludarabine, a pro-drug, is converted metabolically by dephosphorylation to the antimetabolite, F-ara-A. - Mechanism of Action & Protocol.
Resistance to bacteriostasis by 2-thiazole alanine develops rapidly; however, such resistance is lost during growth in the absence of the analog. This induced resistance is accompanied by increased formation of an enzyme sensitive to 2-thiazole alanine. Maintenance of the elevated enzyme levels in growing cells, like resistance, requires the presence of the analog. ...
Due to inconsistencies between the drug labels on DailyMed and the pill images provided by RxImage, we no longer display the RxImage pill images associated with drug labels. We anticipate reposting the images once we are able identify and filter out images that do not match the information provided in the drug labels. ...
Analysis of turnover of Treg by BrdU incorporation. BALB/c mice were treated with BrdU administered continuously for 7 d using osmotic pumps. Then, peripheral L
Specificity of the deficit in BrdU incorporation in D2 KO mouse brain. (a) The WT mice displayed significant (P | 0.05), over twofold, increase in the number
Regional delivery of an adenovirus vector containing the Escherichia coli cytosine deaminase gene to provide local activation of 5-fluorocytosine to suppress the growth of colon carcinoma metastatic to liver Academic Article ...
Trade Name: Rheumatrex®, TrexallTM. How is this drug used? Methotrexate is FDA approved for the following cancers: gestational choriocarcinoma, chorioadenoma destruens and hydatidiform mole, acute lymphocytic leukemia, meningeal leukemia, breast cancer, epidermoid cancers of the head and neck, advanced mycosis fungoides, lung cancer, advanced non-Hodgkins lymphomas, and osteosarcoma. It is important for patients to remember that physicians have the ability to prescribe medication for conditions other than those for which the drug has been approved by the FDA. Patients who have received a prescription of this drug for a condition other than which it is approved may wish to discuss this issue with their physician.. What is the mechanism of action? Methotrexate belongs to a group of agents classified as antimetabolites. Antimetabolites produce their anti-cancer effects by inhibiting the ability of a cell to produce or repair DNA, thereby making the cell unable to replicate or repair itself and ...
Abstract: : Purpose: To compare trabeculectomy with viscocanulostomy for the control of intraocular pressure (IOP) in open angle glaucoma (OAG) uncontrolled by medical therapy. Methods: 45 patients (50 eyes) were randomised to trabeculectomy (25 eyes) or viscocanulostomy (25 eyes). Eyes in both groups were graded on the basis of risk factors for drainage failure and given intraoperative antimetabolites (5-Fluoruracil 25mg/ml (5-FU), Mitomycin-C (MMC) 0.2mg/ml & 0.4 mg/ml) according to a protocol. Results: There were no differences between the groups in age, sex, type of OAG, preoperative medications, risk factors for drainage failure and preoperative IOP. Mean follow-up was 16 months (range 3-24 months). At the last follow-up visit, complete success (IOP ,21 mmHg without anti-glaucoma medications) was seen in 19 eyes (76%) undergoing trabeculectomy, but in only 43% of eyes undergoing viscocanulostomy (p,0.05). At the last follow-up visit, the average number of anti-glaucoma medications was 0.32 ...
The best-studied example of genetic variation within a DME and its effect on toxicity is the interaction between variants in thiopurine methyltransferase (TPMT) and toxicity with the thiopurine antimetabolites 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG). 6-MP is used as an immunosuppressant for some nonmalignant conditions, such as inflammatory bowel diseases (12, 13), and is one of the backbones of treatment in the most frequent pediatric malignancy, acute lymphoblastic leukemia [ALL (14)]. The thiopurines are prodrugs that are converted by multiple enzymes into thioguanine nucleotides (TGN), which are then incorporated into DNA. Inactivation of TGN occurs by 2 main mechanisms: oxidation by xanthine oxidase and methylation by TPMT. Xanthine oxidase activity is negligible in hematopoietic tissues, so these cells rely on TPMT for TGN inactivation (15).. Struck by the wide interpatient variability in both response and toxicity observed in patients treated with 6-MP, Weinshilboum and Sladek ...
Interferons (IFN) are glycoproteins that, among other products, are released from virus-infected cells. In neighboring cells, interferon stimulates the production of antiviral proteins. These inhibit the synthesis of viral proteins by (preferential) destruction of viral DNA or by suppressing its translation. Interferons are not directed against a specific virus, but have a broad spectrum of antiviral action that is, however, species-specific. Thus, interferon for use in humans must be obtained from cells of human origin, such as leukocytes (IFN-a), fibroblasts (IFN-P), or lymphocytes (IFN-y). Interferons are also used to treat certain malignancies and autoimmune disorders (e.g., IFN-a for chronic hepatitis C and hairy cell leukemia; IFN-p for severe herpes virus infections and multiple sclerosis).. Virustatic antimetabolites are false DNA building blocks (B) or nucle-osides. A nucleoside (e.g., thymidine) consists of a nucleobase (e.g., thymine) and the sugar deoxyribose. In ...
A composition is described for use in memory and learning enhancement or for treatment of a cognitive disorder or a psychotic disorder. This composition contains the compound D-cycloserine and D-alanine and provides reduced adverse side effects typically associated with chronic D-cycloserine use.
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How would the volume of the urine production be altered if the proximal convulated tubules were experimentally subjected to 1)Cooling 2)metabolic inhibitors...
MeSH-minor] Acute Disease. Adolescent. Antimetabolites, Antineoplastic / administration & dosage. Antimetabolites, Antineoplastic / therapeutic use. Child. Child, Preschool. Combined Modality Therapy. Cytarabine / administration & dosage. Cytarabine / therapeutic use. Disease-Free Survival. Down Syndrome / complications. Doxorubicin / administration & dosage. Doxorubicin / analogs & derivatives. Drug Administration Schedule. Etoposide / administration & dosage. Female. Hematopoietic Stem Cell Transplantation. Humans. Hydrocortisone / administration & dosage. Infant. Infection / etiology. Infection / mortality. Japan / epidemiology. Kaplan-Meier Estimate. Male. Methotrexate / administration & dosage. Mitoxantrone / administration & dosage. Remission Induction. Survival Analysis. Transplantation, Autologous. Transplantation, Homologous. Treatment Outcome. Tretinoin / administration & dosage. Vincristine / administration & ...
Looking for online definition of viscocanalostomy in the Medical Dictionary? viscocanalostomy explanation free. What is viscocanalostomy? Meaning of viscocanalostomy medical term. What does viscocanalostomy mean?
The thiopurine drugs are purine antimetabolites that are useful in the treatment of acute lymphoblastic leukemia, autoimmune disorders (e.g., Crohn disease, rheumatoid arthritis), and organ transplant recipients. The thiopurine drugs, 6-mercaptopurine (6-MP), 6-thioguanine (6-TG), and azathioprine (AZA) are prodrugs that require intracellular activation to 6-thioguanine nucleotides (6-TGN). This activation is catalyzed by multiple enzymes. The cytotoxic effects of thiopurine drugs are achieved mainly through incorporation of 6-TGN into DNA and RNA. The pathway that leads to synthesis of active cytotoxic 6-TGN is in competition with inactivation pathways catalyzed by thiopurine methyltransferase (TPMT). Evaluation of this pathway is important because the level of 6-TGN measured in red blood cells have been correlated with both thiopurine therapeutic efficacy and toxicity such as myelosuppression.. TPMT activity is inherited as a monogenic codominant trait, and variable TPMT activity is associated ...
Because alterations in cell membrane sialoglycoconjugates can affect the behavior of neoplastic cells, we investigated the effects of in vitro treatment with antimetabolites used in cancer therapy on the expression of membrane sialic acid in cultured HL-60 leukemic cells. In these studies, cells were incubated with Vibrio cholerae neuraminidase to remove surface sialic acid. Reappearance of membrane sialic acid during drug treatment was followed (a) by measuring changes in radioactive surface labeling of viable cells with sodium metaperiodate-sodium[3H]-borohydride, (b) by measuring the decline in accessible surface galactosyl receptor sites which occurred coincident with membrane sialic acid replacement, and (c) by measuring the incorporation of [3H]glucosamine into membrane-associated neuraminidase-labile sialic acid.. We were especially interested in learning whether drugs that affect intracellular pools of cytidine triphosphate (CTP), an important nucleotide intermediate in sialylation ...
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... molecular features. and regular cells. Curiously, inhibitors of mitochondrial breathing do not really considerably impact viability, but had been capable to boost level of sensitivity of sarcomas to inhibition of glycolysis. Additionally, inhibition of glycolysis considerably decreased intracellular ATP amounts, and level of sensitivity to 2-DG-induced development inhibition was related to respiratory prices and glycolytic addiction. Our results demonstrate book human relationships between sarcoma bioenergetics and level of sensitivity to metabolic inhibitors, and recommend that inhibition of metabolic paths in sarcomas should become additional looked into as a potential restorative technique. < 0.05, indicating that WHI-P 154 IC50 cells that are more reliant on glycolysis possess WHI-P 154 IC50 lower ATP-linked respiration rates. Level of sensitivity of human being sarcoma cells to glycolysis inhibition To examine ...
Synonyms for 5-fluorouracil in Free Thesaurus. Antonyms for 5-fluorouracil. 1 word related to fluorouracil: antimetabolite. What are synonyms for 5-fluorouracil?
6-mercaptopurine monohydrate testing. Laboratory testing for CAS number 6112-76-1. . This chemical is light yellow crystalline powder
Background: To determine the effect of scleral flap size on the medium-term intraocular pressure control and complication rates after augmented trabeculectomy.. Design: Prospective randomized clinical trial.. Participants: Glaucoma patients undergoing primary trabeculectomy. Exclusion criteria included previous ocular surgery apart from cataract surgery, secondary glaucoma and age under 18.. Methods: Patients were randomized to either standard trabeculectomy (4 × 4 mm scleral flap) or microtrabeculectomy (2 × 2 mm scleral flap), both with adjustable sutures and antimetabolites. Bleb needling was performed as required. Patients were evaluated at day 1, weeks 1, 3, 6 and months 3, 6, 12, 18 and 24 postoperatively.. Main Outcome Measures: Vision, intraocular pressure, complications and failure (intraocular pressure ≥ 21 mmHg or not reduced by ≥20% from baseline, intraocular pressure ≤ 5 mmHg, repeat glaucoma surgery and no light perception vision).. Results: Forty-one patients were ...
Efudix (Fluorouracil) is a type of topical cream which is applied to the skin as a treatment for skin growths such as solar keratoses or actinic keratoses. It is also used to treat a type of skin cancer known as superficial basal cell carcinoma. The active ingredient in this cream is in a class of drugs known as antimetabolites.
Significant pharmaceutical innovations and progresses have occurred in oncology treatments and patients management. Recent signal transduction inhibitor agents having a strong anti-tumour specificity are able to disrupt signal pathways mediating cancer cell proliferation and efficiently prevent tumour growth. Signal transduction inhibitors include imatinib, sunitinib, nilotinib, dasatinib, sorafenib and other tyrosine kinase blockers currently under investigation. But other chemotherapeutic drugs such as antimetabolites (methotrexate, 5-Fluorouracil), mitotic spindle inhibitors (vincristine, vinorelbine), antibiotic inhibitors of topoisomerases (etoposide, topotecan) etc. are also increasingly used in oncology. As a consequence, cancer patients are living longer, and the amount of consumption of these classes of drugs has grown accordingly. In parallel, the amount of anticancer drug residues released into the environment has increased. Indeed, most anticancer drugs are eliminated by urines or ...
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 ...
Authors: Nurgalieva Z, Liu CC, Du XL. Title: Chemotherapy use and risk of bone marrow suppression in a large population-based cohort of older women with breast and ovarian cancer.. Journal: Med Oncol 28(3):716-25. Date: 2011 Sep. Abstract: We studied 65,521 women with breast cancer and 7,420 women with ovarian cancer aged ≥ 65 identified from the 16 areas of the Surveillance, Epidemiology and End Results program linked with Medicare data during 1991-2002. Bone marrow toxicity associated with chemotherapy was defined using diagnosis codes from Medicare inpatient, outpatient and physician claims. The time to event Cox regression was utilized to estimate the risk of bone marrow toxicity. Use of anthracyclines, taxanes or platinums was associated with increased risks of short- (≤3 months) and long-term (>3 months) anemia and neutropenia in patients with breast cancer. Alkylating agents or antimetabolites were additional significant predictors of anemia in women with ovarian cancer. Patients who ...
We talked to him about the fact that when I get my injections (Friday) I then spend between 2 and 5 days basically bed ridden. I can get up and move about but I get very sore/sick very quickly unless I stay laying down/reclining. The tiredness is indescribable - I quite literally will fall asleep at the kitchen table. Were going to change chemo days so that I can feel well for the weekends and sleep away a tuesday or wednesday instead but some weeks (like last week) it drags on all week... I was finally feeling a bit better and realized it was Friday - chemo day - again. This week however went MUCH better - I slept off Sunday but otherwise was in decent shape. Anyways - the bad news is his advice was (while he was very sympathetic about it and did say some people just get wiped out - something about it being an antimetabolite and at that point his words got too big even for me) that its most likely something I will just have to cope with. I didnt expect a here this pill will fix it! reply ...
We talked to him about the fact that when I get my injections (Friday) I then spend between 2 and 5 days basically bed ridden. I can get up and move about but I get very sore/sick very quickly unless I stay laying down/reclining. The tiredness is indescribable - I quite literally will fall asleep at the kitchen table. Were going to change chemo days so that I can feel well for the weekends and sleep away a tuesday or wednesday instead but some weeks (like last week) it drags on all week... I was finally feeling a bit better and realized it was Friday - chemo day - again. This week however went MUCH better - I slept off Sunday but otherwise was in decent shape. Anyways - the bad news is his advice was (while he was very sympathetic about it and did say some people just get wiped out - something about it being an antimetabolite and at that point his words got too big even for me) that its most likely something I will just have to cope with. I didnt expect a here this pill will fix it! reply ...
Alimta infusion contains the active ingredient pemetrexed disodium, which is a type of chemotherapy medicine for cancer called a cytotoxic antimetabolite.
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  • The purpose of this study was to examine the role of Fas-mediated apoptosis in mediating cell death in response to the antimetabolite drugs 5-FU, RTX, and MTA and to assess the effect of TS induction and p53 status on drug-induced activation of this pathway. (aacrjournals.org)
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  • Because of this mode of action, most antimetabolites have high cell cycle specificity and can target arrest of cancer cell DNA replication. (wikipedia.org)
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