Which of the following best describes the mechanism of action for alkylating agents?

Which of the following terms best describes its mechanism of action? Proflavine acts as an intercalating agent with DNA and binds using van der Waals interactions and ionic bonds. Alkylating agents react with DNA and form covalent bonds. … Busulfan acts as an alkylating agent.

What is the example of 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).

How do alkylating agents cause mutation?

Mutagenicity is related to the ability of alkylating agents to form crosslinks and/or transfer an alkyl group to form monoadducts in DNA. The most frequent location of adducts in the DNA is at guanines. Expressed mutations involve different base substitutions, including all types of transitions and transversions.

What is the role of alkylating agents in cancer treatment?

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 is meant by alkylating agent?

: a substance that causes replacement of hydrogen by an alkyl group especially in a biologically important molecule specifically : one with mutagenic activity that inhibits cell division and growth and is used to treat some cancers.

What do alkylating agents do quizlet?

What do alkylating agents do? Attaches an alkyl group to DNA causing intra/inter-strand cross-linking. Can also modify the structure of guanine and cause ‘depurination’ – excision of the guanine.

What is the major toxicity of the alkylating agents?

The major clinical toxicities of most of the alkylating agents are similar to those of mechloramine, primarily bone marrow depression (including anemia, leukopenia, and thrombocytopenia) and nausea and vomiting. As noted above, alkylating agents generally have low TIs, because they target all dividing cells.

Is bleomycin an alkylating agent?

DNA-damaging agents are among the most effective anticancer agents in clinical use; these include alkylating agents (e.g., cyclophosphamide, cisplatin), antimetabolites (e.g., 5-fluorouracil), topoisomerase inhibitors (e.g., etoposide), and cytotoxic antibiotics (e.g., bleomycin) [16].

What are the three common toxicities caused by alkylating drugs?

Gastrointestinal Toxicity Mucositis, stomatitis, esophagitis, and diarrhea occur with high doses of alkylating agents, particularly after high doses of melphalan and thiotepa or combinations of alkylating agents, including melphalan or thiotepa.

What are DNA alkylating agents?

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.

Are alkylating agents mutagens?

The most commonly used chemical mutagens are alkylating agents such as ethylmethane sulfonate and N-methyl-N-nitrosourea that induce point mutations in DNA.

Why are alkylating agents not used as antiseptics?

The alkylating agent formaldehyde (CH₂OH) is commonly used in solution at a concentration of 37% (known as formalin) or as a gaseous disinfectant and biocide. … Formaldehyde is very irritating to living tissues and is also carcinogenic; therefore, it is not used as an antiseptic.

How do alkylating agents cause cancer?

Alkylating agents induce dose-limiting myelosuppression and cause sublethal DNA damage to hematopoietic progenitors, causing mutational events that lead to malignant transformation to preleukemic and leukemic states.

What is the meaning of alkylating?

: the act or process of introducing one or more alkyl groups into a compound (as to increase octane number in a motor fuel)

Which drug is alkylating anticancer?

Cyclophosphamide — the most widely used alkylating agent of modern times. Chlormethine also known as mechlorethamine or mustine (HN2) — the first alkylating agent to receive regulatory approval.

Why do alkylating agents have short half lives?

As noted above, alkylating agents generally have low TIs, because they target all dividing cells. Individual drugs have additional toxicities.

How do antimetabolites work?

Antimetabolites are called a “cytotoxic” type of drug because they kill cells. They work by mimicking the molecules that a cell needs to grow. Cells are tricked into taking in the drugs and then using the antimetabolites instead of their normal building blocks of genetic material: RNA and DNA.

What are alkylation agents explain with reaction?

Alkylating agents are typically olefin, alcohols, sulfates halides and various nitrogen containing compounds that promote alkylation by enabling alkyl groups to selectively bond to molecules. Often, alkylation requires a catalyst. Common alkylating catalysts are acids, such as HF or H₂SO₄.

What cyclophosphamide is used for?

Cyclophosphamide is used alone or in combination with other medications to treat Hodgkin’s lymphoma (Hodgkin’s disease) and non-Hodgkin’s lymphoma (types of cancer that begin in a type of white blood cells that normally fights infection); cutaneous T-cell lymphoma (CTCL, a group of cancers of the immune system that …

Which residue is susceptible by alkylating agents?

Alkylation of guanine or other bases results in abnormal base pairing as well as the excision of these bases, which in turn leads to strand breakage. Alkylating agents are considered to be cell cycle phase nonspecific, with cells in G₁ and S phases being most susceptible (Figure 20-1).

Is mitomycin C an alkylating agent?

Mitomycin (28.1. 110) is an antineoplastic antibiotic against a wide variety of cancer types produced by Streptomyces caespitosus. It is an important antitumor compound, and being an alkylating agent, has an extraordinary ability to crosslink DNA with high efficiency.

Why do chemotherapy patients lose their hair?

Why does chemotherapy cause hair loss? The reason chemotherapy can cause hair loss is that it targets all rapidly dividing cells — healthy cells as well as cancer cells. Hair follicles, the structures in the skin from which hair grows, include some of the fastest-growing cells in the body.

Is Methotrexate an alkylating agent?

Cyclophosphamide, azathioprine, chlorambucil, and methotrexate are cytotoxic drugs used most commonly for the purpose of immunosuppression. Cyclophosphamide and chlorambucil are alkylating agents, which cause cross-linking of DNA resulting in altered protein production, decreased cell division, and cell death.

Is oxaliplatin an alkylating agent?

Oxaliplatin is classified as an alkylating agent. Alkylating agents are most active in the resting phase of the cell. These drugs are cell-cycle non-specific. There are several types of alkylating agents.

Is an alkylating agent under nitrogen mustard?

Drug type: Nitrogen Mustard is an anti-cancer (antineoplastic or cytotoxic) chemotherapy drug. Nitrogen Mustard is classified as an alkylating agent. (For more detail, see How this drug works section below).

What is the mechanism of action of cyclophosphamide?

MECHANISM OF ACTION: Cyclophosphamide is an alkylating agent of the nitrogen mustard type. 2 An activated form of cyclophosphamide, phosphoramide mustard, alkylates, or binds, to DNA. Its cytotoxic effect is mainly due to cross-linking of strands of DNA and RNA, and to inhibition of protein synthesis.