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FRAX486, a PAK inhibitor, overcomes ABCB1-mediated multidrug resistance in breast cancer cells.
Zhang, Meng; Zeng, Xiaoqi; She, Meiling; Dong, Xingduo; Chen, Jun; Xiong, Qingquan; Qiu, Guobin; Yang, Shuyi; Li, Xiangqi; Ren, Guanghui.
Afiliação
  • Zhang M; Department of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.
  • Zeng X; Department of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.
  • She M; School of Traditional Chinese Medicine, Southern Medical University, Guangzhou, Guangdong, China.
  • Dong X; Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, New York, USA.
  • Chen J; Department of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.
  • Xiong Q; Department of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.
  • Qiu G; Department of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.
  • Yang S; Department of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.
  • Li X; Department of Breast Surgery, The Second Affiliated Hospital of Shandong First Medical University, Tai'an, Shandong, China.
  • Ren G; Department of Thyroid and Breast Surgery, Shenzhen Hospital of Southern Medical University, Shenzhen, Guangdong, China.
Braz J Med Biol Res ; 57: e13357, 2024.
Article em En | MEDLINE | ID: mdl-38958364
ABSTRACT
The overexpression of P-glycoprotein (P-gp/ABCB1) is a leading cause of multidrug resistance (MDR). Hence, it is crucial to discover effective pharmaceuticals that counteract ABCB1-mediated multidrug resistance. FRAX486 is a p21-activated kinase (PAK) inhibitor. The objective of this study was to investigate whether FRAX486 can reverse ABCB1-mediated multidrug resistance, while also exploring its mechanism of action. The CCK8 assay demonstrated that FRAX486 significantly reversed ABCB1-mediated multidrug resistance. Furthermore, western blotting and immunofluorescence experiments revealed that FRAX486 had no impact on expression level and intracellular localization of ABCB1. Notably, FRAX486 was found to enhance intracellular drug accumulation and reduce efflux, resulting in the reversal of multidrug resistance. Docking analysis also indicated a strong affinity between FRAX486 and ABCB1. This study highlights the ability of FRAX486 to reverse ABCB1-mediated multidrug resistance and provides valuable insights for its clinical application.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias da Mama / Resistência a Múltiplos Medicamentos / Resistencia a Medicamentos Antineoplásicos / Subfamília B de Transportador de Cassetes de Ligação de ATP Limite: Female / Humans Idioma: En Revista: Braz J Med Biol Res Ano de publicação: 2024 Tipo de documento: Article País de afiliação: China País de publicação: Brasil
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias da Mama / Resistência a Múltiplos Medicamentos / Resistencia a Medicamentos Antineoplásicos / Subfamília B de Transportador de Cassetes de Ligação de ATP Limite: Female / Humans Idioma: En Revista: Braz J Med Biol Res Ano de publicação: 2024 Tipo de documento: Article País de afiliação: China País de publicação: Brasil