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Unique features of ...
Unique features of the mode of action of ET-743.
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D'Incalci, Maurizio (författare)
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Erba, Eugenio (författare)
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Damia, Giovanna (författare)
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visa fler...
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Galliera, Emanuela (författare)
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Carrassa, Laura (författare)
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Marchini, Sergio (författare)
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Mantovani, Roberto (författare)
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- Tognon, Gianluca, 1976 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för invärtesmedicin,Institute of Internal Medicine
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Fruscio, Robert (författare)
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Jimeno, José (författare)
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Faircloth, Glynn T (författare)
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visa färre...
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(creator_code:org_t)
- 2002
- 2002
- Engelska.
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Ingår i: The oncologist. - 1083-7159. ; 7:3, s. 210-6
- Relaterad länk:
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https://gup.ub.gu.se...
Abstract
Ämnesord
Stäng
- This paper describes the current knowledge of the primary mode of action of a natural product, ecteinascidin 743 (ET-743), derived from the marine tunicate Ecteinascidia turbinata. ET-743 was initially selected for preclinical development because of its potent antitumor activity observed against several human solid tumor types. In vitro, the drug is cytotoxic in the nanomolar range, and in the case of some very sensitive cell lines, in the picomolar range. The large potency differences observed among several solid tumor types indicate that this compound possesses some tumor selectivity, but the molecular basis of these differential effects remains to be elucidated. The present studies were undertaken to evaluate the mechanism of action of ET-743 in this context. The available information on ET-743 binding to DNA and its effects on transcriptional regulation point to a unique behavior of this drug, as it independently affects specific gene transcription in a promoter-dependent way. In addition, ET-743 shows a peculiar pattern of selectivity in cells with different defects in their DNA-repair pathways. These results highlight a unique property of ET-743, possibly explaining why it possesses antitumor activity against tumors that are refractory to standard anticancer drugs, all of which certainly act by mechanisms that are different from that of ET-743.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)
Nyckelord
- Antineoplastic Agents
- Alkylating
- pharmacology
- DNA Damage
- DNA Repair
- DNA-Binding Proteins
- drug effects
- Dioxoles
- pharmacology
- Humans
- Isoquinolines
- pharmacology
- Structure-Activity Relationship
- Tetrahydroisoquinolines
- Transcription
- Genetic
- drug effects
- Tumor Cells
- Cultured
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- ref (ämneskategori)
- for (ämneskategori)
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D'Incalci, Mauri ...
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Erba, Eugenio
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Damia, Giovanna
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Galliera, Emanue ...
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Carrassa, Laura
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Marchini, Sergio
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visa fler...
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Mantovani, Rober ...
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Tognon, Gianluca ...
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Fruscio, Robert
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Jimeno, José
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Faircloth, Glynn ...
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visa färre...
- Om ämnet
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- MEDICIN OCH HÄLSOVETENSKAP
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MEDICIN OCH HÄLS ...
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och Medicinska och f ...
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och Farmakologi och ...
- Artiklar i publikationen
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The oncologist
- Av lärosätet
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Göteborgs universitet