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antimetabolite

 
Dictionary: an·ti·me·tab·o·lite   (ăn'tē-mĭ-tăb'ə-līt', ăn'tī-) pronunciation
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n.
A substance that closely resembles an essential metabolite and therefore interferes with physiological reactions involving it.

antimetabolic an'ti·met'a·bol'ic (-mĕt'ə-bŏl'ĭk) adj.

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Britannica Concise Encyclopedia: antimetabolite
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Substance that competes with, replaces, or inhibits a specific compound within a cell, whose functioning is thereby disrupted. Because its structure resembles the compound's, it is taken up by the cell, but it does not react in the same way with the enzyme that acts on the usual compound. It may inhibit the enzyme or be converted into an aberrant chemical. Many antimetabolites are useful in treating disease, including sulfa drugs, which disrupt bacterial but not human metabolism for bacterial diseases, and others (e.g., methotrexate, 5-fluorouracil) for various cancers.

For more information on antimetabolite, visit Britannica.com.

Food and Nutrition: antimetabolite
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Compound that inhibits a normal metabolic process, acting as an analogue of a normal metabolite. Some are useful in chemotherapy of cancer, others are naturally occurring toxins in foods, frequently causing vitamin deficiency diseases by inhibiting the normal metabolism of the vitamin. See also antivitamin.

Veterinary Dictionary: antimetabolite
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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.

Wikipedia: Antimetabolite
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The drug methotrexate (right) is an antimetabolite that interferes with the metabolism of folic acid (left).

An antimetabolite is a chemical that inhibits the use of a metabolite, which is another chemical that is part of normal metabolism.[1] Such substances are often similar in structure to the metabolite that they interfere with, such as the antifolates that interfere with the use of folic acid. The presence of antimetabolites can have toxic effects on cells, such as halting cell growth and cell division, so these compounds are used as chemotherapy for cancer.[2]

Contents

Function

Cancer treatment

Antimetabolites can be used in cancer treatment,[3] as they interfere with DNA production and therefore cell division and the growth of tumors. Because cancer cells spend more time dividing than other cells, inhibiting cell division harms tumor cells more than other cells.

Anti-metabolites masquerade as a purine (azathioprine, mercaptopurine) or a 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.[4]

They also affect RNA synthesis. However, because thymidine is used in DNA but not in RNA (where uracil is used instead), inhibition of thymidine synthesis via thymidylate synthase selectively inhibits DNA synthesis over RNA synthesis.

Due to their efficiency, these drugs are the most widely used cytostatics.

In the ATC system, they are classified under L01B.

Antibiotics

Antimetabolites may also be antibiotics, such as sulfanilamide drugs, which inhibit dihydrofolate synthesis in bacteria by competing with para-aminobenzoic acid.[5]

Types

Main representatives of these drugs are:

See also

References

  1. ^ Smith, A. L. (1997). Oxford dictionary of biochemistry and molecular biology. Oxford [Oxfordshire]: Oxford University Press. pp. 43. ISBN 0-19-854768-4. 
  2. ^ Peters GJ, van der Wilt CL, van Moorsel CJ, Kroep JR, Bergman AM, Ackland SP (2000). "Basis for effective combination cancer chemotherapy with antimetabolites". Pharmacol. Ther. 87 (2-3): 227–53. PMID 11008002. 
  3. ^ MeSH Antineoplastic+Antimetabolites
  4. ^ Takimoto CH, Calvo E. "Principles of Oncologic Pharmacotherapy" in Pazdur R, Wagman LD, Camphausen KA, Hoskins WJ (Eds) Cancer Management: A Multidisciplinary Approach. 11 ed. 2008.
  5. ^ "The Organic Chemistry of Drug Design and Drug Action" (2nd edition), R. B. Silverman, 2004.

External links

v • d • e
Intracellular chemotherapeutic agents/antineoplastic agents (L01)
SPs/MIs
(M phase)
Block microtubule assembly
Block microtubule disassembly
DNA replication
inhibitor
DNA precursors/
antimetabolites
(S phase)
Photosensitizers/PDT
Other
Other/ungrouped

This entry is from Wikipedia, the leading user-contributed encyclopedia. It may not have been reviewed by professional editors (see full disclaimer)

 
 

 

Copyrights:

Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved.  Read more
Britannica Concise Encyclopedia. Britannica Concise Encyclopedia. © 2006 Encyclopædia Britannica, Inc. All rights reserved.  Read more
Food and Nutrition. A Dictionary of Food and Nutrition. Copyright © 1995, 2003, 2005 by A. E. Bender and D. A. Bender. All rights reserved.  Read more
Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.  Read more
Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Antimetabolite".  Read more