S-alkylthiolation of O6-methylguanine-DNA-methyltransferase (MGMT) to sensitize cancer cells to anticancer therapy

Détails

ID Serval
serval:BIB_59FC64917E4E
Type
Article: article d'un périodique ou d'un magazine.
Sous-type
Synthèse (review): revue aussi complète que possible des connaissances sur un sujet, rédigée à partir de l'analyse exhaustive des travaux publiés.
Collection
Publications
Institution
Titre
S-alkylthiolation of O6-methylguanine-DNA-methyltransferase (MGMT) to sensitize cancer cells to anticancer therapy
Périodique
Expert Opinion on Therapeutic Targets
Auteur⸱e⸱s
Juillerat  A., Juillerat-Jeanneret  L.
ISSN
1744-7631 (Electronic)
Statut éditorial
Publié
Date de publication
2007
Volume
11
Numéro
3
Pages
349-361
Notes
PT - Journal Article PT - Review
Résumé
O6-methylguanine DNA methyltransferase/O6-alkylguanine DNA alkyltransferase (MGMT/AGT) removes alkyl adducts from the O6-position of guanine in DNA. Expression of MGMT in human cancers has been associated with resistance to therapies using alkylating agents. MGMT promoter methylation regulates its expression and response to alkylating agents. A combination of O6-benzylguanine-based inhibitors of MGMT with alkylating agents improved the efficacy. However, this is associated with enhanced cytotoxicity and the induction of GC to AT transition mutations presumably also in progenitor/stem cells. A few recent studies have described analogs of O6-benzylguanine targeting defined pathways of cancer cells that can be used to improve the selectivity of O6-benzylguanine-based inhibitors for cancer cells. Therefore, MGMT inhibitor targeting represents a reliable strategy for improving cancer therapy with alkylating agents
Mots-clé
Antineoplastic Agents,Alkylating/therapeutic use/Drug Resistance,Neoplasm/drug effects/Enzyme Inhibitors/Guanine/analogs & derivatives/Humans/Mutation/Neoplasms/drug therapy/genetics/metabolism/O(6)-Methylguanine-DNA Methyltransferase/antagonists & inhibitors/chemistry/Protein Conformation
Pubmed
Web of science
Création de la notice
29/01/2008 19:36
Dernière modification de la notice
20/08/2019 15:13
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