Actinomycin
From Wikipedia, the free encyclopedia
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Actinomycin
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| Systematic (IUPAC) name | |
| (Dactinomycin ) | |
| Identifiers | |
| CAS number | |
| ATC code | L01 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C62H86N12O16 |
| Mol. mass | 1255.42 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | 5% |
| Metabolism | ? |
| Half life | 36 hours |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status | |
| Routes | ? |
Actinomycin is any of a class of polypeptide antibiotics isolated from soil bacteria of the genus Streptomyces.
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[edit] Mechanism
Actinomycin-D is primarily used as an investigative tool in cell biology to inhibit transcription. It does this by binding DNA at the transcription initiation complex and preventing elongation by RNA polymerase.[1]
As it can bind DNA duplexes, it can also interfere with DNA replication, although other chemicals such as hydroxyurea are better suited for use in the laboratory as inhibitors of DNA synthesis.
[edit] Clinical use
[edit] As chemotherapy
Actinomycin-D is marketed under the trade name Dactinomycin. Actinomycin-D is one of the older chemotherapy drugs which has been used in therapy for many years.
It is a clear, yellow liquid which is administered intravenously and most commonly used in treatment of a variety of cancers, including:
[edit] As an antibiotic
It was the first antibiotic shown to have anti-cancer activity, but is not normally used as such, as it is highly toxic, causing damage to genetic material.
It was the first antibiotic ever isolated by Selman Waksman.
[edit] Research use
Actinomycin-D and its fluorescent derivative, 7-amino-actinomycin D, are used as stains in microscopy and flow cytometry applications. The affinity of these stains compounds for GC-rich regions of DNA strands makes them excellent markers for DNA.
7-amino-actinomycin D (7-AAD) is used as a DNA stain. 7-AAD binds to single stranded DNA. Therefore it is a useful tool in determining apoptosis and distinguishing between dead cells and live ones. (Source)
[edit] References
- ^ Sobell H (1985). "Actinomycin and DNA transcription". Proc Natl Acad Sci U S A 82 (16): 5328–31. doi:. PMID 2410919.
- ^ Turan T, Karacay O, Tulunay G, Boran N, Koc S, Bozok S, Kose M. "Results with EMA/CO (etoposide, methotrexate, actinomycin D, cyclophosphamide, vincristine) chemotherapy in gestational trophoblastic neoplasia". Int J Gynecol Cancer 16 (3): 1432–8. doi:. PMID 16803542.
- ^ Abd El-Aal H, Habib E, Mishrif M (2005). "Wilms' Tumor: The Experience of the Pediatric Unit of Kasr El-Aini Center of Radiation Oncology and Nuclear Medicine (NEMROCK)". J Egypt Natl Canc Inst 17 (4): 308–11. PMID 17102824.
- ^ Khatua S, Nair C, Ghosh K (2004). "Immune-mediated thrombocytopenia following dactinomycin therapy in a child with alveolar rhabdomyosarcoma: the unresolved issues". J Pediatr Hematol Oncol 26 (11): 777–9. doi:. PMID 15543019.
