What are alkylating agents used to treat?
Alkylating agents are used in treating various forms of cancer, but they tend to work best in slow-growing cancers, such as: , these anticancer drugs were among the first of their kind. Also, they remain the most commonly used chemotherapeutic drug types. How do alkylating agents work? Alkylating agents work by destroying the DNA in cancer cells.
Do alkylating agents kill cancer cells?
Eventually, the cancer cell dies. Alkylating agents were one of the first classes of drugs to be used against cancer. There are five traditional categories of alkylating agents: Nitrogen mustards (eg, bendamustine, chlorambucil, cyclophosphamide, ifosfamide, mechlorethamine, melphalan)
How do alkylating agents prevent cell division?
Alkylating agents prevent cell division primarily by cross-linking strands of DNA. Because of continued synthesis of other cell constituents, such as RNA and protein, growth is unbalanced, and the cell dies. Activity of alkylating agents does not depend on DNA synthesis in the target cells.
Can alkylating drugs cause leukemia?
In rare cases, this can lead to leukemia. The risk of leukemia from alkylating agents is “dose-dependent,” meaning that the risk is small with lower doses, but goes up as the total amount of the drug used gets higher. The risk of leukemia after getting alkylating agents is highest about 5 to 10 years after treatment.
How do alkylating agents work as chemotherapy?
Alkylating agents were among the first anti-cancer drugs and are the most commonly used agents in chemotherapy today. Alkylating agents act directly on DNA, causing cross-linking of DNA strands, abnormal base pairing, or DNA strand breaks, thus preventing the cell from dividing.
What is the role of alkylating agent?
What are Alkylating agents? Alkylating agents are compounds that work by adding an alkyl group to the guanine base of the DNA molecule, preventing the strands of the double helix from linking as they should. This causes breakage of the DNA strands, affecting the ability of the cancer cell to multiply.
How alkylating agents produce anti neoplastic effect?
Some alkylating agents are active under conditions present in cells; and the same mechanism that makes them toxic allows them to be used as anti-cancer drugs. They stop tumor growth by crosslinking guanine nucleobases in DNA double-helix strands, directly attacking DNA.
How does an alkylating agent work and what processes do such agents inhibit?
Alkylating agents involve reactions with guanine in DNA. These drugs add methyl or other alkyl groups onto molecules where they do not belong. This in turn inhibits their correct utilization by base pairing and causes a miscoding of DNA.
What is the mechanism of action for alkylating agents?
Mechanism of action of drugs. Alkylating agents act by cross-linking strands of DNA, particularly at the N-7 position of guanine. They are nonspecific for cell cycle phase and are thus active during most parts of the cell cycle.
Which of the following statements best describes how alkylating agents work as chemotherapy?
Which of the following statements best describes how alkylating agents work as chemotherapy? Alkylating agents work to prevent the cell from replicating its genetic material, preventing cell division.
How do alkylating agents stop the reproduction of cells?
Alkylating agents keep the cell from reproducing (making copies of itself) by damaging its DNA. These drugs work in all phases of the cell cycle and are used to treat many different cancers, including cancers of the lung, breast, and ovary as well as leukemia, lymphoma, Hodgkin disease, multiple myeloma, and sarcoma.
What chemical reaction do alkylating agents participate in?
The alkylating agents are a group of strong disinfecting chemicals that act by replacing a hydrogen atom within a molecule with an alkyl group (CnH2n+1), thereby inactivating enzymes and nucleic acids (Figure 13.3. 11).
What is the importance of bio reductive alkylation?
Most sig- nificantly, it permits the making of pre- dictions of the biologically important structural features of a molecule so that they serve as critical guideposts for a synthetic program whose objectives are the construction of biologically active compounds.
Do alkylating agents suppress the immune system?
Previous work has demonstrated that in addition to mediating antineoplastic effects, alkylating agents deplete specific populations of immune cells.
Why does it make sense that nitrogen mustard is used as an anticancer drug?
The discovery of nitrogen mustard as an alkylating agent in 1942, opened a new era in the cancer chemotherapy. This valuable class of alkylating agent exerts its biological activity by binding to DNA, cross linking two strands, preventing DNA replication and ultimate cell death.
Which of the following are commonly used alkylating agents?
Some examples of alkylating agents are nitrogen mustards (chlorambucil and cyclophosphamide), cisplatin, nitrosoureas (carmustine, lomustine, and semustine), alkylsulfonates (busulfan), ethyleneimines (thiotepa), and triazines (dacarbazine).
What are alkylating agents in organic chemistry?
alkylating agent, any highly reactive drug that binds to certain chemical groups (phosphate, amino, sulfhydryl, hydroxyl, and imidazole groups) commonly found in nucleic acids and other macromolecules, bringing about changes in the DNA and RNA of cells.
Which of these are examples of alkylating agents?
Alkylating AgentsClassical alkylatorsAziridine, chlorambucil, cyclophosphamide, estramustine, ifosfamide, mechlorethamine, melphalan, nitrogen mustards, thiotepaPlatinum complexesCarboplatin, cisplatin, oxaliplatinNonclassical alkylatorsAltretamine, dacarbazine, procarbazine
Do alkylating agents suppress the immune system?
Previous work has demonstrated that in addition to mediating antineoplastic effects, alkylating agents deplete specific populations of immune cells.
What chemical reaction do alkylating agents participate in?
The alkylating agents are a group of strong disinfecting chemicals that act by replacing a hydrogen atom within a molecule with an alkyl group (CnH2n+1), thereby inactivating enzymes and nucleic acids (Figure 13.3. 11).
What is the use of alkylating drugs?
Alkylating agents are used to treat various forms of cancer, but they tend to be best for slow-growing cancers, such as:
How does the alkylating agent work?
Alkylating agents work by destroying the DNA in cancer cells. This is achieved by replacing alkyl groups with hydrogen atoms in DNA so that cells cannot repair themselves. Therefore, the lack of functional DNA prevents cancer cells from dividing and replicating.
Types of alkylating agents
There are six categories of alkylating agents, each of which has a specific drug:
Are alkylating agents effective?
Alkylating agents are the most commonly used drugs in chemotherapy and can be used alone or in combination with other therapies. This is because they have a long-term record of effective results.
Limitations and side effects of alkylating agents
Alkylating agents help destroy the DNA in cancer cells. Unfortunately, the same process that prevents cancer cells from multiplying also affects healthy cells in the body. This has led to some notorious side effects of well-known chemotherapy drugs.
Bottom line
Alkylating agents are only one type of chemotherapeutic agent considered in anti-cancer treatment. There are several subtypes of these drugs and related drugs that prevent cancer cells from multiplying by damaging cell DNA.
What is an alkylating agent?
Alkylating agents are a class of antineoplastic or anticancer drugs which act by inhibiting the transcription of DNA into RNA and thereby stopping the protein synthesis. Alkylating agents substitute alkyl groups for hydrogen atoms on DNA, resulting in the formation of cross links within the DNA chain and thereby resulting in cytotoxic, mutagenic, ...
Which cell is most affected by alkylating agents?
Cancer cells are among the most affected because they are among the most rapidly dividing cells. However, hematopoetic, reproductive, and endothelial cells also divide rapidly which accounts for the common side effects of the alkylating agents: anemia, pancytopenia, amenorrhea, impaired spermatogenesis, intestinal mucosal damage, alopecia, ...
What is the role of alkylating agents in cancer?
Alkylating agents play a significant role in the treatment of lymphoma, Hodgkin's disease, breast cancer, multiple myeloma, and other malignancies. In addition to conventional chemotherapy, the linear dose–response curve of alkylating agents expands their role for incorporation into transplant regimens. Table 2.
What alkylating agents are used in chemo?
Cisplatin, oxaliplatin, carboplatin, chlorambucil, cyclophosphamide, mechlorethamine, and melphalan are some of the most important alkylating agents used for chemotherapy. The exposure of cells to alkylating agents causes a specific reduction in DNA synthesis, chromosomal aberrations, and genetic mutations [15].
What are the side effects of alkylating agents?
Most alkylating agents cause gastrointestinal side effects and dose-limiting toxicity to bone marrow. Most of the alkylating agents produce an acute suppression of the bone marrow, with the major effect being a decreased granulocyte count. Busulfan depresses all blood elements, particularly stem cells. Because both cellular and humoral immunity are suppressed by alkylating agents some are used for the treatment of autoimmune disease. In addition to the effect on the bone marrow, alkylating agents are highly toxic to mucosal cells resulting in oral mucosal ulceration and effects on the intestinal mucosa. Other organ systems affected by some alkylating agents include the lungs (pulmonary fibrosis) and the liver. Cyclophosphamide and ifosfamide cause a severe hemorrhagic cystitis due to their release of acrolein, a metabolite. This condition is manageable with thiol flushing agents. Because the more unstable alkylating agents, such as nitrogen mustard and the nitrosoureas, have strong vesicant properties they damage veins with repeated use and produce ulceration if extravasated. Alkylating agents cause alopecia and have immunosuppressive effects Chabner et al (2001), Pratt et al (1994), Tew et al (2001), Fraiser et al (1991).
Why are alkylating agents toxic?
Because both cellular and humoral immunity are suppressed by alkylating agents some are used for the treatment of autoimmune disease. In addition to the effect on the bone marrow, alkylating agents are highly toxic to mucosal cells resulting in oral mucosal ulceration and effects on the intestinal mucosa.
What is the primary mode of action for most alkylating drugs?
The primary mode of action for most alkylating drugs is via cross-linking of DNA strands. They can be classified as either monofunctional alkylating agents, implying reactions with only one strand of DNA, or bifunctional alkylating agents, which cross-link two strands of DNA.
How do alkylating agents react with DNA?
Alkylating agents react with electron-rich atoms to form covalent bonds. The common alkane transferred by classical alkylating agents is a single-carbon methyl group that also includes longer hydrocarbons. The most important reactions with regard to the agents' antitumor activities are reactions with DNA bases. Some alkylating agents are monofunctional and react with only one strand of DNA. Others are bifunctional and react with an atom on both strands of DNA, producing a cross-link that covalently links the two strands of the DNA double helix. Unless repaired, this lesion will prevent the cell from replicating effectively. The lethality of the monofunctional alkylating agents results from the recognition of the DNA lesion by the cell and by the response of the cell to that lesion.
How do alkylating agents prevent cell division?
Alkylating agents prevent cell division primarily by cross-linking strands of DNA. Because of continued synthesis of other cell constituents, such as RNA and protein, growth is unbalanced, and the cell dies. Activity of alkylating agents does not depend on DNA synthesis in the target cells.
What is the role of alkylating agents in cancer?
These agents act during all phases of the cell cycle, directly on DNA, crosslinking the N-7-guanine residues, causing DNA strand breaks, leading to abnormal base pairing, inhibition of cell division ...
What is an alkylating agent?
Alkylating agents, which prevent cell reproduction through direct deoxyribonucleic acid (DNA) damage, are widely used for the treatment of hematological and solid malignancies, often in combination with other chemotherapy medicines.
What is the role of MRP2 in detoxification?
These findings have implications for the role of MRP2 in detoxification of alkylating agents in the apical epithelium of liver and kidney where it is highly expressed as well as the role of MRP2 in the emergence of alkylating drug resistance in cancer cells.
What is the Cdc25 inhibitor?
one Cdc25 phosphatase inhibitor in combination with. anticancer alkylating agents, antagonists of folic acid, such as. methotrexate and inhibitors of the synthesis of DNA and cell. division such as mitomycin C for the treatment of cancer. A. total of 31 compounds that may be useful in combination.
What is procarbazine used for?
and procarbazine) for the treatment of cancers of breast, ovaries, colon, gastrointestinal (GI) tract, kidneys, bladder, prostate, skin cancer like melanoma, head and neck cancer, lung cancer, such as small-cell lung cancer and. non-small-cell lung cancer, cervix cancer and brain tumours, astrocytoma and glioma.
Is COX-2 inhibitor good for breast cancer?
Here we consider the potential utility of selective COX-2 inhibitors for the prevention and treatment of breast cancer. Data for cancers of the colon and breast are compared where possible. In addition, the mechanisms by which COX-2 is upregulated in cancers and contributes to tumorigenesis are discussed.
Is albumin a drug carrier?
Taking cancer, an age-associated disease, as an example, the use of albumin nanoparticles as a drug carrier overcomes some of the limitations of chemotherapy such as severe side effects, nonspecific targeting, insolubility in aqueous solutions, short-term retention in bloodstream, and damage to normal cells.
What are Alkylating agents?
Alkylating agents are compounds that work by adding an alkyl group to the guanine base of the DNA molecule, preventing the strands of the double helix from linking as they should. This causes breakage of the DNA strands, affecting the ability of the cancer cell to multiply. Eventually, the cancer cell dies.
Further information
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How do alkylating agents work?
Alkylating agents. Alkylating agents keep the cell from reproducing (making copies of itself) by damaging its DNA. These drugs work in all phases of the cell cycle and are used to treat many different cancers, including cancers of the lung, breast, and ovary as well as leukemia, lymphoma, Hodgkin disease, multiple myeloma, and sarcoma.
What are the other treatments for cancer?
Other types of drugs used to treat cancer. Other drugs and biological treatments are used to treat cancer, but aren’t considered chemotherapy . They often have different side effects than chemotherapy . Many are used along with surgery, chemo, or radiation therapy.
How are chemo drugs grouped?
Types of chemo drugs. Chemo drugs can be grouped by how they work, their chemical structure, and their relationships to other drugs. Some drugs work in more than one way, and may belong to more than one group. (Note: not all chemotherapy drugs are listed here.)
What is chemo used for?
Many different kinds of chemotherapy or chemo drugs are used to treat cancer – either alone or in combination with other drugs or treatments. These drugs are very different in their chemical composition (what they are made of), how they are prescribed and given, how useful they are in treating certain types of cancer, ...
What are alkaloids used for?
(Enzymes are proteins that cause chemical reactions in living cells.) Topoisomerase inhibitors are used to treat certain leukemias, as well as lung, ovarian, gastrointestinal, colorectal, and pancreatic cancers.
How does chemo work?
Chemotherapy works with the cell cycle. Every time any new cell is formed, it goes through a usual process to become a fully functioning (or mature) cell. The process involves a series of phases and is called the cell cycle. Chemotherapy drugs target cells at different phases of the cell cycle. Understanding how these drugs work helps doctors ...
What does it mean when you get chemo?
Each time chemo is given, it means trying to find a balance between killing the cancer cells (in order to cure or control the disease) and sparing the normal cells (to lessen side effects).
What Is The Use of Alkylating Drugs?
How Does The Alkylating Agent Work?
- Alkylating agents work by destroying the DNA in cancer cells. This is achieved by replacing alkyl groups with hydrogen atoms in DNA so that cells cannot repair themselves. Therefore, the lack of functional DNA prevents cancer cells from dividing and replicating. To help minimize the risk of side effects, oncologists usually provide the lowest and m...
Are Alkylating Agents Effective?
- Alkylating agents are the most commonly used drugs in chemotherapy and can be used alone or in combination with other therapies. This is because they have a long-term record of effective results. Your doctor will recommend a course based on the type and stage of your cancer. The overall efficacy and side effects of anti-cancer drugs will also be considered. It is important to di…
Limitations and Side Effects of Alkylating Agents
- Alkylating agents help destroy the DNA in cancer cells. Unfortunately, the same process that prevents cancer cells from multiplying also affects healthy cells in the body. This has led to some notorious side effects of well-known chemotherapy drugs. The most common side effects of alkylating agents include: 1. Alopecia (hair loss) 2. anemia 3. Decreased blood count (pancytope…
Bottom Line
- Alkylating agents are only one type of chemotherapeutic agent considered in anti-cancer treatment. There are several subtypes of these drugs and related drugs that prevent cancer cells from multiplying by damaging cell DNA. Your doctor can help you determine whether an alkylating agent is right for you based on the type and stage of cancer, as well as potential risks and side e…