RESUMO
P-glycoprotein(P-gp)- related resistance is one of the major obstacles in treating leukemia patients. Therefore, it is of clinical interest to find new potential modulators and compare their P-gp-modulating efficacy. The present analysis investigated the influence of P-gp modulators, such as verapamil, tamoxifen, droloxifene E, droloxifene Z, SDZ PSC 833 (PSC 833) and dexniguldipine in a leukemic T-cell line (CCRF-CEM) and its P-gp-resistant counterparts (CCRF-CEM/ACT400 and CCRF-CEM/VCR1000). P-gp expression was assessed with an immunocytological technique using the monoclonal antibody 4E3.16. It was characterized as the percentage of P-gp positive cells and also expressed as a D value by using the Kolmogorov Smirnov statistic. The efficacy of P-gp modulators was determined with the rhodamine-123 accumulation test and the MTT test. An in vitro modulator concentration between 0.1 microM and 3 microM was determined, where no genuine antiproliferative effect was apparent. The modulators PSC 833 and dexniguldipine were the significant (pAssuntos
Membro 1 da Subfamília B de Cassetes de Ligação de ATP/antagonistas & inibidores
, Ciclosporinas/farmacologia
, Di-Hidropiridinas/farmacologia
, Resistência a Múltiplos Medicamentos
, Resistencia a Medicamentos Antineoplásicos
, Leucemia de Células T/patologia
, Proteínas de Neoplasias/antagonistas & inibidores
, Tamoxifeno/análogos & derivados
, Tamoxifeno/farmacologia
, Verapamil/farmacologia
, Transportadores de Cassetes de Ligação de ATP/análise
, Anticorpos Monoclonais/imunologia
, Divisão Celular/efeitos dos fármacos
, Ensaios de Seleção de Medicamentos Antitumorais
, Humanos
, Proteínas Associadas à Resistência a Múltiplos Medicamentos
, Células Tumorais Cultivadas/efeitos dos fármacos
, Partículas de Ribonucleoproteínas em Forma de Abóbada