Document Detail


The cyclin-dependent kinase inhibitor roscovitine and the nucleoside analog sangivamycin induce apoptosis in caspase-3 deficient breast cancer cells independent of caspase mediated P-glycoprotein cleavage: implications for therapy of drug resistant breast cancers.
MedLine Citation:
PMID:  19342873     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Resistance to multiple chemotherapeutic agents is a common clinical problem which can arise during cancer treatment. Drug resistance often involves overexpression of the multidrug resistance MDR1 gene, encoding P-glycoprotein (P-gp), a 170-kDa glycoprotein belonging to the ATP-binding cassette superfamily of membrane transporters. We have recently demonstrated apoptosis-induced, caspase-3-dependent P-gp cleavage in human T-lymphoblastoid CEM-R VBL100 cells. However, P-gp contain many aspartate residues which could be targeted by caspases other than caspase-3. To test whether other caspases could cleave P-gp in vivo, we investigated the fate of P-gp during roscovitine- and sangivamycin- induced apoptosis in MCF7 human breast cancer cells, as they lack functional caspase-3. MCF7 cells were stably transfected with human cDNA encoding P-gp. P-gp was cleaved in vitro by purified recombinant caspase-3, -6 and -7. However, P-gp cleavage was not detected in vivo in MCF7 cells induced to undergoing apoptosis by either roscovitine or sangivamycin, despite activation of both caspase-6 and -7. Interestingly, P-gp overexpressing MCF7 cells were more sensitive to either roscovitine or sangivamycin than wild-type cells, suggesting a novel potential therapeutic strategy against P-gp overexpressing cells. Taken together, our results support the concept that caspase-3 is the only caspase responsible for in vivo cleavage of P-gp and also highlight small molecules which could be effective in treating P-gp overexpressing cancers.
Authors:
Alessandra Cappellini; Francesca Chiarini; Andrea Ognibene; James A McCubrey; Alberto M Martelli
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2009-05-02
Journal Detail:
Title:  Cell cycle (Georgetown, Tex.)     Volume:  8     ISSN:  1551-4005     ISO Abbreviation:  Cell Cycle     Publication Date:  2009 May 
Date Detail:
Created Date:  2009-04-22     Completed Date:  2009-06-03     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  101137841     Medline TA:  Cell Cycle     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1421-5     Citation Subset:  IM    
Affiliation:
Dipartimento di Scienze Motorie e della Salute, Università di Cassino, Cassino, Italy.
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MeSH Terms
Descriptor/Qualifier:
Apoptosis / drug effects*
Breast Neoplasms / drug therapy*,  enzymology,  genetics
Caspase 3 / metabolism*
Cell Line, Tumor
Cyclin-Dependent Kinases / antagonists & inhibitors*
Drug Resistance, Neoplasm / drug effects
Drug Screening Assays, Antitumor
Gene Expression Regulation, Neoplastic / drug effects
Humans
Nucleosides / chemistry
P-Glycoprotein / genetics,  metabolism*
Purines / pharmacology*,  therapeutic use
Pyrimidine Nucleosides / pharmacology*,  therapeutic use
RNA, Messenger / genetics,  metabolism
Grant Support
ID/Acronym/Agency:
R01CA098195/CA/NCI NIH HHS
Chemical
Reg. No./Substance:
0/Nucleosides; 0/P-Glycoprotein; 0/Purines; 0/Pyrimidine Nucleosides; 0/RNA, Messenger; 0/roscovitine; 18417-89-5/sangivamycin; EC 2.7.11.22/Cyclin-Dependent Kinases; EC 3.4.22.-/Caspase 3

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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