An antimetabolite is a chemical with a similar structure to a substance (a metabolite) required for normal biochemical reactions, yet different enough to interfere with the normal functions of cells, including cell division. Metabolomics is the "systematic study of the unique chemical fingerprints that specific cellular processes leave behind" - specifically the study of their small-molecule metabolite Cell division is a process by which a cell, called the parent cell divides into two or more cells called daughter cells.
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Function
Cancer treatment
Antimetabolites can be used in cancer treatment, as they interfere with DNA production and therefore cell division and the growth of tumors. Cancer (medical term Malignant Neoplasm) is a class of Diseases in which a group of cells display uncontrolled Because cancer cells spend more time dividing than other cells, inhibiting cell division harms tumor cells more than other cells.
Anti-metabolites masquerade as purine (azathioprine, mercaptopurine) or pyrimidine - which become the building blocks of DNA. Purine ( 1) is a heterocyclic Aromatic Organic compound, consisting of a Pyrimidine ring fused to an Imidazole ring Azathioprine is an immunosuppressant used in Organ transplantation Autoimmune disease such as Rheumatoid arthritis and Pemphigus or inflammatory Mercaptopurine (also called 6-Mercaptopurine 6-MP or its brand name Purinethol) is an Immunosuppressive drug used to treat Leukemia. Pyrimidine is a Heterocyclic Aromatic Organic compound similar to Benzene and Pyridine, containing two Nitrogen Atoms They prevent these substances becoming incorporated in to DNA during the S phase (of the cell cycle), stopping normal development and division. The S phase, short for synthesis phase, is a period in the Cell cycle during Interphase, between G1 phase and the G2 phase. The cell cycle, or cell-division cycle, is the series of events that take place in a eukaryotic cell leading to its replication
They also affect RNA synthesis. However, because thymidine is used in DNA but not in RNA (where uracil is used instead), inhibition of thymidine sythesis via thymidylate synthase selectively inhibits DNA synthesis over RNA synthesis. Thymidine (more precisely called deoxythymidine; can also be labelled deoxyribosylthymine, and thymine deoxyriboside) is a Chemical compound Uracil is a common and naturally occurring Pyrimidine derivative Thymidylate synthetase ( is the enzyme used to generate
Due to their efficiency, these drugs are the most widely used cytostatics. Chemotherapy, in its most general sense refers to treatment of disease by chemicals that kill cells specifically those of micro-organisms or Cancer.
In the ATC system, they are classified under L01B. The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System.
Antibiotics
Antimetabolites may also be antibiotics, such as sulfanilamide drugs, which inhibit dihydrofolate synthesis in bacteria by competing with para-aminobenzoic acid. In modern usage an antibiotic is a Chemotherapeutic agent with activity against Microorganisms such as Bacteria, fungi or Protozoa Sulfanilamide is a molecule containing the sulfonamide functional group attached to an Aniline. Dihydrofolic acid is a Folic acid derivative acted upon by Dihydrofolate reductase to produce Tetrahydrofolic acid. 4-Aminobenzoic acid (also known as para -aminobenzoic acid or PABA) is an Organic compound with the molecular formula C7H7NO2 [1]
Types
Main representatives of these drugs are:
Folic acid analogues
- Methotrexate, a folic acid analogue, prevents the formation of tetrahydrofolate, essential for purine and pyrimidine synthesis, by inhibiting dihydrofolate reductase. Folic acid (also known as Vitamin M and Folacin) and Folate (the Anionic form are forms of the water-soluble Vitamin B9 Folic acid (also known as Vitamin M and Folacin) and Folate (the Anionic form are forms of the water-soluble Vitamin B9 Tetrahydrofolic acid is a Folic acid derivative Metabolism Human synthesis It is produced from Dihydrofolic acid by Dihydrofolate Dihydrofolate reductase, or DHFR, reduces Dihydrofolic acid to Tetrahydrofolic acid, using NADPH as Electron donor, which can be converted This leads to inhibited production of DNA, RNA and proteins (as tetrahydrofolate is also involved in the synthesis of amino acids serine and methionine). Serine (abbreviated as Ser or S) is an Organic compound with the formula H[[oxygen O]]2 CCH NH sub>2CH2OH Methionine ( abbreviated as Met or M) is an α- Amino acid with the Chemical formula HO2CCH(NH2CH2CH2SCH3
Purine analogues
- Azathioprine is the main immunosuppressive cytotoxic substance. Folic acid (also known as Vitamin M and Folacin) and Folate (the Anionic form are forms of the water-soluble Vitamin B9 Pemetrexed (brand name Alimta) is a Chemotherapy drug manufactured and marketed by Eli Lilly and Company. Raltitrexed (brand name Tomudex) is an Antimetabolite drug used in cancer Chemotherapy. Trimethoprim ( INN) (traɪˈmɛθəprɪm is a bacteriostatic Antibiotic mainly used in the Prophylaxis and treatment of Urinary tract infections Pyrimethamine ( Daraprim) is a Medication used for Protozoal infections Purine ( 1) is a heterocyclic Aromatic Organic compound, consisting of a Pyrimidine ring fused to an Imidazole ring Azathioprine is an immunosuppressant used in Organ transplantation Autoimmune disease such as Rheumatoid arthritis and Pemphigus or inflammatory It is widely used in transplantations to control rejection reactions. It is nonenzymatically cleaved to 6-mercaptopurine that acts as a purine analogue and an inhibitor of DNA synthesis. Mercaptopurine (also called 6-Mercaptopurine 6-MP or its brand name Purinethol) is an Immunosuppressive drug used to treat Leukemia. By preventing the clonal expansion of lymphocytes in the induction phase of the immune response, it affects both the cell and the humoral immunity. Cell-mediated immunity is an Immune response that does not involve Antibodies or complement but rather involves the activation of Macrophages The Humoral Immune Response (HIR is the aspect of immunity that is mediated by secreted Antibodies (as opposed to Cell-mediated immunity which involves It also successfully suppresses autoimmunity. Autoimmunity is the failure of an organism to recognize its own constituent parts as self, which results in an immune response against its own cells and tissues
- Mercaptopurine
- Thioguanine is used to treat acute leukemias and induction of remissions in acute granulocytic leukemias
- Fludarabine inhibits function of multiple DNA polymerases, DNA primase, DNA ligase I and is S phase-specific (since these enzymes are highly active during DNA replication). Mercaptopurine (also called 6-Mercaptopurine 6-MP or its brand name Purinethol) is an Immunosuppressive drug used to treat Leukemia. Tioguanine ( INN) formerly Thioguanine ( BAN) is a drug that is used in the treatment of Cancer. Fludarabine (marketed as fludarabine phosphate under the trade name Fludara) is a Chemotherapy drug used in the treatment of hematological malignancies A DNA Polymerase is an Enzyme that assists in DNA replication. DNA primase is an Enzyme involved in the replication of DNA by creating an RNA primer In Molecular biology, DNA ligase is a special type of Ligase ( that can link together two DNA strands that have single-strand breaks (a break in both complementary The S phase, short for synthesis phase, is a period in the Cell cycle during Interphase, between G1 phase and the G2 phase.
- Pentostatin and cladribine are adenosine analogs which are primarily used to treat Hairy cell leukemia. Pentostatin (Deoxycoformycin is an anticancer Chemotherapeutic drug Cladribine is a drug commonly used to treat Hairy cell leukemia (leukemic reticuloendotheliosis Hairy cell leukemia is a mature B cell Neoplasm. It is usually classified as a sub-type of Chronic lymphoid leukemia for convenience
Pyrimidine analogues
- 5-fluorouracil (5FU) which inhibits thymidylate synthase. Purine ( 1) is a heterocyclic Aromatic Organic compound, consisting of a Pyrimidine ring fused to an Imidazole ring Mercaptopurine (also called 6-Mercaptopurine 6-MP or its brand name Purinethol) is an Immunosuppressive drug used to treat Leukemia. Tioguanine ( INN) formerly Thioguanine ( BAN) is a drug that is used in the treatment of Cancer. Fludarabine (marketed as fludarabine phosphate under the trade name Fludara) is a Chemotherapy drug used in the treatment of hematological malignancies Pyrimidine is a Heterocyclic Aromatic Organic compound similar to Benzene and Pyridine, containing two Nitrogen Atoms Fluorouracil (5-FU or f5U is a Pyrimidine analog, which is used as a drug in the treatment of Cancer. Thymidylate synthetase ( is the enzyme used to generate
- Floxuridine (FUDR)
- Cytosine arabinoside (Cytarabine)
See also
External links
References
- ^ "The Organic Chemistry of Drug Design and Drug Action" (2nd edition), R. Floxuridine is an Oncology drug that belongs to the class known as Antimetabolites The drug is most often used in the treatment of colorectal cancer Cytarabine, or cytosine arabinoside, is a Chemotherapy agent used mainly in the treatment of hematological malignancies such as Leukemia Pyrimidine is a Heterocyclic Aromatic Organic compound similar to Benzene and Pyridine, containing two Nitrogen Atoms Fluorouracil (5-FU or f5U is a Pyrimidine analog, which is used as a drug in the treatment of Cancer. Floxuridine is an Oncology drug that belongs to the class known as Antimetabolites The drug is most often used in the treatment of colorectal cancer Gemcitabine is a Nucleoside analog used as Chemotherapy. It is marketed as Gemzar by Eli Lilly and Company. A base analog is a chemical that can substitute for a normal Nucleobase in Nucleic acids A common example would be 5-bromouracil (5BU the abnormal The University of Nebraska is the public University system in the state of Nebraska, USA. B. Silverman, 2004.
Dictionary
antimetabolite
-noun
- (medicine) Any substance that competes with, or inhibits the normal metabolic process, often by acting as an analogue of an essential metabolite
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