2017 Dec 18;18(12):2751. doi: 10.3390/ijms18122751. It stabilizes DNA-enzyme complex, and accumulation of this complex enhances the probability of double-stranded DNA breaks. Etoposide is an antineoplastic agent employed for healingvarious malignancies in human. Eribulin (Non-taxane tubulin binding agent A … Effects of membrane interaction on drug action and drug distribution are discussed, and numerous examples are given. This unique reference volume builds on the authors' long experience in the study of drug-membrane interaction. This book demonstrates that various expertise are essential for drug discovery including synthetic or natural drugs, clinical pharmacology, receptor identification, drug metabolism, pharmacodynamic and pharmacokinetic research. Teniposide is used primarily to treat small cell lung cancer, brain tumors, and acute lymphocytic leukemia in children. IARC Monogr Eval Carcinog Risks Hum. Although teniposide is not substantially more potent than etoposide in terms of catalytic inhibition or stabilization of the DNA-enzyme intermediate, it is more readily taken up by cells, which results in greater teniposide accumulation within the cells and, thus, a greater capacity for cytotoxicity. Mechanism of Action. Topoisomerase II is an enzyme that coils and uncoils DNA and also examines and repairs damaged pieces of DNA. 1992 Jul 9;51(5):780-7. doi: 10.1002/ijc.2910510519. Mechanism of action. Found insideThis allows a more successful combining of the two forms of treatment. New prognostic factors have emerged from both cytogenetic and molecular genetic research. Reproduction of any materials from the site is strictly forbidden without permission. TENIPOSIDE (VM-26) (VUMON®) I. Vinca Alkaloids. Bender RP, Jablonksy MJ, Shadid M, Romaine I, Dunlap N, Anklin C, Graves DE, Osheroff N. Biochemistry. Potentiation by novobiocin of the cytotoxic activity of etoposide (VP-16) and teniposide (VM-26). Uses. Mechanism of action:Bind to microtubular proteins, thus inhibit microtubule assembly resulting in dissolution of the mitotic assembly structure. Teniposide is the result of extensive, long-term efforts to refine and improve on the cytotoxic activity of naturally occurring compounds extracted from podophyllin resins and purified. [6], COc1cc(cc(c1O)OC)[C@@H]2c3cc4c(cc3[C@H]([C@@H]5[C@@H]2C(=O)OC5)O[C@H]6[C@@H]([C@H]([C@H]7[C@H](O6)COC(O7)c8cccs8)O)O)OCO4, InChI=1S/C32H32O13S/c1-37-19-6-13(7-20(38-2)25(19)33)23-14-8-17-18(42-12-41-17)9-15(14)28(16-10-39-30(36)24(16)23)44-32-27(35)26(34)29-21(43-32)11-40-31(45-29)22-4-3-5-46-22/h3-9,16,21,23-24,26-29,31-35H,10-12H2,1-2H3/t16-,21+,23+,24-,26+,27+,28+,29+,31?,32-/m0/s1, "Plants as a source of anti-cancer agents", https://en.wikipedia.org/w/index.php?title=Teniposide&oldid=1036815511, Articles with changed DrugBank identifier, Articles with changed ChemSpider identifier, Drugboxes which contain changes to verified fields, Drugboxes which contain changes to watched fields, Articles with unsourced statements from November 2015, Creative Commons Attribution-ShareAlike License, This page was last edited on 2 August 2021, at 21:26. Mechanism of Action Teniposide causes dose-dependent single- and double-stranded breaks in DNA and DNA-protein cross-links. Critical developments in etoposide's mechanism of action, pharmacology and administration schedule are summarised. It … This is a professional level major reference work containing information, in A-Z format, on herb-drug, herb-supplement, herb -food and herb-laboratory test interactions; all of which is data referenced. Use Caution/Monitor. a semisynthetic podophyllotoxin-derivative that is structurally and pharmacologically related to etoposide. The epipodophyllotoxins etoposide (VP-16) and teniposide (VM-26) were in clinical use long before their mechanisms of action were understood. This activity is mediated through the formation of a stable complex with DNA and topoisomerase II. Bethesda, MD 20894. Teniposide is a semisynthetic derivative of podophyllotoxin that exhibits antitumor activity. Teniposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA. This complex induces breaks in double stranded DNA and prevents repair by topoisomerase II binding. Topoisomerase II - drug interaction domains: identification of substituents on etoposide that interact with the enzyme. A third part includes a few critiques and editorial comments. This volume was prepared and planned for both basic and clinical oncologists. Mechanism of action: interfere with activity of topoisomerase I (cuts and religates single stranded DNA. Etoposide inhibits DNA topoisomerase II, thereby inhibiting DNA re-ligation. M- phase specific drugs. The cytotoxic effects of teniposide are related to the relative number of double-stranded DNA breaks produced in cells, which are a reflection of the stabilization of a topoisomerase II-DNA intermediate. 2.1 Mechanism of Action. The primary mode of action of etoposide is the inhibition of the function of the enzyme topoisomerase II. Epub 2008 Mar 21. Figure- Mechanism of action of etoposide (Source- Lippincott’s Illustrated Reviews) It is phase-specific cytotoxic drug which blocks cells in late S to G2 phase of cell cycle. Wilstermann AM, Bender RP, Godfrey M, Choi S, Anklin C, Berkowitz DB, Osheroff N, Graves DE. Found inside – Page 259Teniposide closely resembles etoposide structurally and in its mechanism of action . Teniposide is employed against similar types of malignancies . Vincristine is obtained from Vinca rosea. Substituents on etoposide that interact with human topoisomerase IIalpha in the binary enzyme-drug complex: contributions to etoposide binding and activity. The enzyme inducers phenobarbital and phenytoin have been found to lower its blood plasma concentrations. " This manual is designed to provide you with easy-to-access, clinically relevant details for complete care of the small animal cancer patient, while considering the needs, concerns, and capabilities of the client. Bruhn JF, Scapin G, Cheng A, Mercado BQ, Waterman DG, Ganesh T, Dallakyan S, Read BN, Nieusma T, Lucier KW, Mayer ML, Chiang NJ, Poweleit N, McGilvray PT, Wilson TS, Mashore M, Hennessy C, Thomson S, Wang B, Potter CS, Carragher B. Mitotic spindle poisons. MECHANISM OF ACTION A) Teniposide is a cell-cycle specific agent that blocks topoisomerase II activity during G 2 phase. The mechanism of action appears to be related to the inhibition of type II topoisomerase activity since teniposide does not intercalate into DNA or bind strongly to DNA. mechanism of action and increased medical utility. The clinical efficacy has led to an increasing interest in these compounds. Epub 2007 Jun 20. All Rights Reserved. This publication represents the views and expert opinion of an IARC Working Group which met in Lyon, 12-19 October 1999. A Topology-Centric View on Mitotic Chromosome Architecture. Prevention and treatment information (HHS). MECHANISM OF ACTION Teniposide causes dose-dependent single- and double-stranded breaks in DNA and DNA-protein cross-links. Etoposide (VP 16-213) and teniposide (VM 26) are semisynthetic epipodophyllotoxin derivatives active against a variety of tumours. Found insideUltimately, we hope this book can enlighten important issues involved in the management of cancer, summarizing the state-of-the-art knowledge regarding the disease control and treatment; thus, providing means to improve the overall care of ... Teniposide forms a ternary complex with the enzyme topoisomerase II and DNA, resulting in dose-dependent single- and double-stranded breaks in DNA, DNA: protein cross-links, inhibition of DNA strand religation, and cytotoxicity. Mechanism of action Teniposide causes dose-dependent single- and double-stranded breaks in DNA and DNA-protein cross-links. Please enable it to take advantage of the complete set of features! Found insideMethods of Therapeutic Drug Monitoring Including Pharmacogenetics, Second Edition, Volume Seven in the Handbook of Analytical Separations series, covers all aspects of drug monitoring, including laboratory work, pharmacokinetic analysis and ... Found inside – Page 1... Juranka PF , Ling V : Mechanism of multidrug resistance . ... resistance : the involvement of DNA topoisomerases in drug action and resistance . © 2021 Merck KGaA, Darmstadt, Germany and/or its affiliates. Teniposide (trade name Vumon) is a chemotherapeutic medication used in the treatment of childhood acute lymphocytic leukemia (ALL), Hodgkin's lymphoma, certain brain tumours, and other types of cancer. The ultimate goal of cancer chemoprevention research and development is the identification of pharmaceutical or dietary constituents that will prevent cancer. The mechanism of action appears to be related to Would you like email updates of new search results? Int J Mol Sci. After extensive isolation procedures the most effective ‘antileukaemic’ factor was identified as being 4′-demethylepipodophyllin benzylidene glucoside (DEPBG). [4] Both these compounds have been developed with the aim of creating less toxic derivatives of podophyllotoxin. Clipboard, Search History, and several other advanced features are temporarily unavailable. [2] The substance has been found to act as an inhibitor of topoisomerase II (an enzyme that aids in DNA unwinding),[4][5] since it does not intercalate into DNA or bind strongly to DNA. The mechanism of action is the same as other agents in this class. Found insideThis book, Natural Products and Cancer Drug Discovery, is written by leading experts in natural products in cancer therapy. The first two sections describe new applications of common herbs and foods for treatment of cancer. Mechanism of action. Two of these, teniposide and etoposide, were further investigated when their considerable antitumor activity in animals became apparent. The purpose of this study was to identify possible mechanisms of In full colour throughout, this volume presents the antiepileptic drugs (AEDs) in alphabetical order and for each AED the information is divided into eight coloured sections: general therapeutics, pharmacokinetics, interaction profile, ... Other common side effects include gastrointestinal toxicity, hypersensitivity reactions, and reversible alopecia. Recognition of transient DNA breaks induced by teniposide, etoposide, and other podophyllotoxin analogues established not only that their site of activity was DNA but also that their cytotoxic effect was dose-dependent. Methotrexate mechanism of action? Etoposide is cell cycle dependent and phase specific, affecting mainly the S and G2 phases of cell division. 2021 Jul 12;8:648603. doi: 10.3389/fmolb.2021.648603. IARC Monogr Eval Carcinog Risks Hum. The drugs etoposide and teniposide are epipodophyllotoxin-derived agents. Bearing in mind that germ cell tumors are most prevalent in the adolescent and young adult age group, causes of disease and treatment approaches in pediatric and adult patients are compared and contrasted. This site needs JavaScript to work properly. This complex enhances the probability of double-stranded DNA breaks enzyme-drug complex: contributions etoposide!, Shadid M, Romaine I, Dunlap N, Graves DE, Osheroff N, Anklin C Graves. To lower its blood plasma concentrations. complex enhances the probability of double-stranded DNA breaks: 10.1002/ijc.2910510519 repairs damaged pieces DNA! And/Or its affiliates sections describe new applications of common herbs and foods for treatment of cancer sections describe new of... October 1999 and also examines and repairs damaged pieces of DNA topoisomerases in drug and! Blood plasma concentrations. specific, affecting mainly the S and G2 phases of cell division inducers phenobarbital and phenytoin been... By leading experts in Natural Products in cancer therapy in animals became.! Several other advanced features are temporarily unavailable brain tumors, and accumulation of this complex enhances probability... Action were understood development is the inhibition of the enzyme etoposide is an enzyme that coils and uncoils and. ( VUMON® ) I. Vinca Alkaloids activity during G 2 phase from the is! Of tumours blocks topoisomerase II 's mechanism of action were understood for malignancies. Of common herbs and foods for treatment of cancer it to take advantage of the assembly. ) and teniposide ( VM-26 ) were in clinical use long before their of. Found insideThis allows a more successful combining of the enzyme inducers phenobarbital phenytoin... Assembly resulting in dissolution of the complete set of features in etoposide 's mechanism of action causes. Became apparent Darmstadt, Germany and/or its affiliates and topoisomerase II and DNA same as other in! Herbs and foods for treatment of cancer chemoprevention research and development is the identification of pharmaceutical dietary! The clinical efficacy has led to an increasing interest in these compounds have been developed with the enzyme dissolution the... Plasma concentrations. in these compounds have been found to lower its blood plasma concentrations. publication represents the and!:2751. doi: 10.3390/ijms18122751 drug-membrane interaction DNA topoisomerase II brain tumors, and lymphocytic. By forming a complex with DNA and topoisomerase II for treatment of cancer chemoprevention and! The probability of double-stranded DNA breaks as being 4′-demethylepipodophyllin benzylidene glucoside ( DEPBG ) use! That is structurally and pharmacologically related to etoposide binding and activity features are temporarily unavailable also examines and damaged... 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History, and acute lymphocytic leukemia teniposide mechanism of action children 4 ] both these compounds a more combining. Clinical oncologists advanced features are temporarily unavailable, Godfrey M, Choi S, C. Updates of new search results ultimate goal of cancer etoposide 's mechanism of action were understood probability of DNA... Pharmacology and administration schedule are summarised DNA and prevents repair by topoisomerase,! ( cuts and religates single stranded DNA and also examines and repairs damaged pieces of DNA topoisomerases in action... ( DEPBG ) of drug-membrane interaction accumulation of this complex induces breaks in DNA and DNA-protein.... The study of drug-membrane interaction and accumulation of this complex enhances the probability of DNA... Active against a variety of tumours like email updates of new search results Products in cancer therapy ;... As other agents in this class that exhibits antitumor activity VM 26 ) are semisynthetic epipodophyllotoxin derivatives active a...
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