Cyclosporin A and analogues as multidrug resistance modulating agents in tumour cell

Detalhes bibliográficos
Autor(a) principal: Wagner-Souza, Karen
Data de Publicação: 2003
Outros Autores: Meletti-de-Oliveira, Michelle Castro, Maia, Raquel C, Rumjanek, Vivian M
Tipo de documento: Artigo
Idioma: por
Título da fonte: Revista Brasileira de Cancerologia (Online)
Texto Completo: https://rbc.inca.gov.br/index.php/revista/article/view/2112
Resumo: Multidrug resistance (MDR) to chemotherapy is one of the major obstacles in the treatment of cancer patients. The resistance process is multifactorial but the best characterized mechanism involved is the overexpression of Pglycoprotein (Pgp), a plasma membrane protein that functions as an efflux pump leading to a decreased intracellular drug concentration. Circumvention of MDR can be obtained using reversing agents capable of inhibiting the activity of Pgp and other drug efflux pumps. In the present review the use of the immunosupresive agent Cyclosporin A and its analogues as reversing agents is discussed. Aspects such as their combination to cyclophilins, their ability to modify Pgp functional activity and their clinical use, especially in leukemias, are discussed based on the literature and on the authors results.
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spelling Cyclosporin A and analogues as multidrug resistance modulating agents in tumour cellCiclosporina A e seus análogos como reversores da resistência a múltiplas drogas em células tumoraisResistência a Múltiplas DrogasLeucemiaQuimioterapiaCiclosporina AGlicoproteína PBarreira Hemato-EncefálicaAgentes ReversoresAnálogos de Ciclosporina AMultiple Drug ResistanceLeukemiaChemotherapyA-CyclosporineP-GlycoproteinBlood-Brain BarrierReversing AgentsA-Cyclosporine AnaloguesMultidrug resistance (MDR) to chemotherapy is one of the major obstacles in the treatment of cancer patients. The resistance process is multifactorial but the best characterized mechanism involved is the overexpression of Pglycoprotein (Pgp), a plasma membrane protein that functions as an efflux pump leading to a decreased intracellular drug concentration. Circumvention of MDR can be obtained using reversing agents capable of inhibiting the activity of Pgp and other drug efflux pumps. In the present review the use of the immunosupresive agent Cyclosporin A and its analogues as reversing agents is discussed. Aspects such as their combination to cyclophilins, their ability to modify Pgp functional activity and their clinical use, especially in leukemias, are discussed based on the literature and on the authors results.A resistência a múltiplas drogas (MDR) é um dos principais obstáculos no tratamento quimioterápico de pacientes com câncer. O processo de resistência é multifatorial, mas o mecanismo mais bem caracterizado é a superexpressão da glicoproteína P (Pgp), uma proteína de membrana plasmática que funciona como uma bomba de efluxo levando a uma diminuição da concentração intracelular do quimioterápico. A circunvenção da resistência pode ser obtida utilizando-se agentes reversores capazes de inibir a atividade funcional da Pgp e de outras bombas de efluxo relacionadas. Nesta revisão, discutimos o uso do imunossupressor Ciclosporina A (CSA) e de seus análogos como agentes reversores da MDR. Aspectos como sua combinação com ciclofilinas, sua capacidade de inibir a atividade funcional da Pgp e seu uso clínico, especialmente em leucemias, são discutidos baseados tanto na literatura quanto em resultados dos próprios autores.INCA2003-06-30info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionRevisão de literaturaapplication/pdfhttps://rbc.inca.gov.br/index.php/revista/article/view/211210.32635/2176-9745.RBC.2003v49n2.2112Revista Brasileira de Cancerologia; Vol. 49 No. 2 (2003): Apr./May/June; 103-112Revista Brasileira de Cancerologia; Vol. 49 Núm. 2 (2003): abr./mayo/jun.; 103-112Revista Brasileira de Cancerologia; v. 49 n. 2 (2003): abr./maio/jun.; 103-1122176-9745reponame:Revista Brasileira de Cancerologia (Online)instname:Instituto Nacional de Câncer José Alencar Gomes da Silva (INCA)instacron:INCAporhttps://rbc.inca.gov.br/index.php/revista/article/view/2112/1308Wagner-Souza, KarenMeletti-de-Oliveira, Michelle CastroMaia, Raquel C Rumjanek, Vivian M info:eu-repo/semantics/openAccess2021-11-29T20:35:40Zoai:rbc.inca.gov.br:article/2112Revistahttps://rbc.inca.gov.br/index.php/revistaPUBhttps://rbc.inca.gov.br/index.php/revista/oairbc@inca.gov.br0034-71162176-9745opendoar:2021-11-29T20:35:40Revista Brasileira de Cancerologia (Online) - Instituto Nacional de Câncer José Alencar Gomes da Silva (INCA)false
dc.title.none.fl_str_mv Cyclosporin A and analogues as multidrug resistance modulating agents in tumour cell
Ciclosporina A e seus análogos como reversores da resistência a múltiplas drogas em células tumorais
title Cyclosporin A and analogues as multidrug resistance modulating agents in tumour cell
spellingShingle Cyclosporin A and analogues as multidrug resistance modulating agents in tumour cell
Wagner-Souza, Karen
Resistência a Múltiplas Drogas
Leucemia
Quimioterapia
Ciclosporina A
Glicoproteína P
Barreira Hemato-Encefálica
Agentes Reversores
Análogos de Ciclosporina A
Multiple Drug Resistance
Leukemia
Chemotherapy
A-Cyclosporine
P-Glycoprotein
Blood-Brain Barrier
Reversing Agents
A-Cyclosporine Analogues
title_short Cyclosporin A and analogues as multidrug resistance modulating agents in tumour cell
title_full Cyclosporin A and analogues as multidrug resistance modulating agents in tumour cell
title_fullStr Cyclosporin A and analogues as multidrug resistance modulating agents in tumour cell
title_full_unstemmed Cyclosporin A and analogues as multidrug resistance modulating agents in tumour cell
title_sort Cyclosporin A and analogues as multidrug resistance modulating agents in tumour cell
author Wagner-Souza, Karen
author_facet Wagner-Souza, Karen
Meletti-de-Oliveira, Michelle Castro
Maia, Raquel C
Rumjanek, Vivian M
author_role author
author2 Meletti-de-Oliveira, Michelle Castro
Maia, Raquel C
Rumjanek, Vivian M
author2_role author
author
author
dc.contributor.author.fl_str_mv Wagner-Souza, Karen
Meletti-de-Oliveira, Michelle Castro
Maia, Raquel C
Rumjanek, Vivian M
dc.subject.por.fl_str_mv Resistência a Múltiplas Drogas
Leucemia
Quimioterapia
Ciclosporina A
Glicoproteína P
Barreira Hemato-Encefálica
Agentes Reversores
Análogos de Ciclosporina A
Multiple Drug Resistance
Leukemia
Chemotherapy
A-Cyclosporine
P-Glycoprotein
Blood-Brain Barrier
Reversing Agents
A-Cyclosporine Analogues
topic Resistência a Múltiplas Drogas
Leucemia
Quimioterapia
Ciclosporina A
Glicoproteína P
Barreira Hemato-Encefálica
Agentes Reversores
Análogos de Ciclosporina A
Multiple Drug Resistance
Leukemia
Chemotherapy
A-Cyclosporine
P-Glycoprotein
Blood-Brain Barrier
Reversing Agents
A-Cyclosporine Analogues
description Multidrug resistance (MDR) to chemotherapy is one of the major obstacles in the treatment of cancer patients. The resistance process is multifactorial but the best characterized mechanism involved is the overexpression of Pglycoprotein (Pgp), a plasma membrane protein that functions as an efflux pump leading to a decreased intracellular drug concentration. Circumvention of MDR can be obtained using reversing agents capable of inhibiting the activity of Pgp and other drug efflux pumps. In the present review the use of the immunosupresive agent Cyclosporin A and its analogues as reversing agents is discussed. Aspects such as their combination to cyclophilins, their ability to modify Pgp functional activity and their clinical use, especially in leukemias, are discussed based on the literature and on the authors results.
publishDate 2003
dc.date.none.fl_str_mv 2003-06-30
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
Revisão de literatura
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv https://rbc.inca.gov.br/index.php/revista/article/view/2112
10.32635/2176-9745.RBC.2003v49n2.2112
url https://rbc.inca.gov.br/index.php/revista/article/view/2112
identifier_str_mv 10.32635/2176-9745.RBC.2003v49n2.2112
dc.language.iso.fl_str_mv por
language por
dc.relation.none.fl_str_mv https://rbc.inca.gov.br/index.php/revista/article/view/2112/1308
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv INCA
publisher.none.fl_str_mv INCA
dc.source.none.fl_str_mv Revista Brasileira de Cancerologia; Vol. 49 No. 2 (2003): Apr./May/June; 103-112
Revista Brasileira de Cancerologia; Vol. 49 Núm. 2 (2003): abr./mayo/jun.; 103-112
Revista Brasileira de Cancerologia; v. 49 n. 2 (2003): abr./maio/jun.; 103-112
2176-9745
reponame:Revista Brasileira de Cancerologia (Online)
instname:Instituto Nacional de Câncer José Alencar Gomes da Silva (INCA)
instacron:INCA
instname_str Instituto Nacional de Câncer José Alencar Gomes da Silva (INCA)
instacron_str INCA
institution INCA
reponame_str Revista Brasileira de Cancerologia (Online)
collection Revista Brasileira de Cancerologia (Online)
repository.name.fl_str_mv Revista Brasileira de Cancerologia (Online) - Instituto Nacional de Câncer José Alencar Gomes da Silva (INCA)
repository.mail.fl_str_mv rbc@inca.gov.br
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