etoposide(Zinc03978073)

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Search Term: etoposide (treatment: Zinc03978073)

Overview

Description:	A semisynthetic derivative of podophyllotoxin that exhibits antitumor activity. Etoposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA. This complex induces breaks in double stranded DNA and prevents repair by topoisomerase II binding. Accumulated breaks in DNA prevent entry into the mitotic phase of cell division, and lead to cell death. Etoposide acts primarily in the G2 and S phases of the cell cycle. [PubChem]
Drug Type:	Small Molecule; Approved
Pharmacology:	Etoposide is an antineoplastic agent and an epipodophyllotoxin (a semisynthetic derivative of the podophyllotoxins). It inhibits DNA topoisomerase II, thereby inhibiting DNA synthesis. Etoposide is cell cycle dependent and phase specific, affecting mainly the S and G2 phases. Two different dose-dependent responses are seen. At high concentrations (10 µg/mL or more), lysis of cells entering mitosis is observed. At low concentrations (0.3 to 10 µg/mL), cells are inhibited from entering prophase. It does not interfere with microtubular assembly. The predominant macromolecular effect of etoposide appears to be the induction of DNA strand breaks by an interaction with DNA-topoisomerase II or the formation of free radicals.
Mechanism of Action:	Etoposide inhibits DNA topoisomerase II, thereby inhibiting DNA synthesis at the premitotic stage of cell division. Etoposide is cell cycle dependent and phase specific, affecting mainly the S and G2 phases of cell division.
Indication:	For use in combination with other chemotherapeutic agents in the treatment of refractory testicular tumors and as first line treatment in patients with small cell lung cancer. Also used to treat other malignancies such as lymphoma, non-lymphocytic leukemia, and glioblastoma multiforme.
Half Life:	4-12 hours

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Data Correlations | 5 studies

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Genes

Score

TOP2A

100

Mbl1

100

SEMA5A

FBXW5

C1orf210

RPL18

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Biogroups

Score

NAD(P)-binding

100

Cell Cycle

Activation of Src by Protein-tyrosi…

MAPK Signaling Pathway

PTC1 (Sonic Hedgehog Receptor) Path…

ERBB Signaling Pathway

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Individual Studies
Drug target sets for approved compounds Homo sapiens \| Therapeutic The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information. Authors: David S Wishart, Craig Knox, An Chi Guo et al. Organization: Department of Computing Science, Univers…	Liver Pharmacology and Xenobiotic Response Repertoire Rattus norvegicus \| RNA Expression A definition of RNA expression changes that correlate with liver response programs and an understanding of the similarities and differences in responses to different classes of chemicals would aid in new chemical or drug characterization and add to our understanding of liver biology. Authors: Natsoulis G, Pearson CI, Gollub J et al. Organization: Iconix Biosciences 325 E. Middlefield Rd…

Individual Studies

Drug target sets for approved compounds

Homo sapiens | Therapeutic

The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information.

Authors: David S Wishart, Craig Knox, An Chi Guo et al.

Organization: Department of Computing Science, Univers…

Liver Pharmacology and Xenobiotic Response Repertoire

Rattus norvegicus | RNA Expression

A definition of RNA expression changes that correlate with liver response programs and an understanding of the similarities and differences in responses to different classes of chemicals would aid in new chemical or drug characterization and add to our understanding of liver biology.

Authors: Natsoulis G, Pearson CI, Gollub J et al.

Organization: Iconix Biosciences 325 E. Middlefield Rd…