Article
Plant Sciences
Sara Abdelfatah, Madeleine Boeckers, Maitane Asensio, Onat Kadioglu, Anette Klinger, Edmond Fleischer, Thomas Efferth
Summary: The study identified isopetasin and S-isopetasin as novel P-gp inhibitors, which can overcome multidrug resistance and induce ROS generation and apoptosis in cancer cells.
Article
Biochemistry & Molecular Biology
Diogo Henrique Kita, Gisele Alves de Andrade, Juliana Morais Missina, Kahoana Postal, Viktor Kalbermatter Boell, Francielli Sousa Santana, Ingrid Fatima Zattoni, Isadora da Silva Zanzarini, Vivian Rotuno Moure, Fabiane Gomes de Moraes Rego, Geraldo Picheth, Emanuel Maltempi de Souza, David A. Mitchell, Suresh Ambudkar, Giovana Gioppo Nunes, Glaucio Valdameri
Summary: The study found that polyoxovanadates can serve as inhibitors of ABC drug transporters, selectively inhibiting P-glycoprotein with V-10 and V-18 being the most promising compounds.
Article
Biochemistry & Molecular Biology
Chao-Yun Cai, Qiu-Xu Teng, Megumi Murakami, Suresh V. Ambudkar, Zhe-Sheng Chen, Vijaya L. Korlipara
Summary: A series of 22 quinazolinamine derivatives with potent inhibitory activities on BCRP and P-gp were synthesized. Compound 22 was identified as a dual BCRP and P-gp inhibitor, while compound 33 showed BCRP inhibitory activity. These compounds changed the localization of BCRP and P-gp, inhibiting the efflux of anticancer drugs by the two ABC transporters. Compounds 22 and 33 also stimulated ATP hydrolysis, increasing the accumulation of mitoxantrone in BCRP-overexpressing cells.
Article
Infectious Diseases
Bo Yang, Dongqiang Wang, Mingxiao Liu, Xiaodong Wu, Jigang Yin, Guan Zhu
Summary: The study aimed to generate host cells with resistance to specific anti-cryptosporidial drugs by transiently overexpressing the MDR1 gene. Results showed increased drug tolerance in host cells for certain compounds with varying effects on the anti-parasitic efficacy, highlighting the importance of understanding drug targets in parasite vs. host cells.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
(2022)
Article
Oncology
Lucia Pavlikova, Mario Seres, Albert Breier, Zdena Sulova
Summary: This paper provides an overview of the possible role of miRNAs in the molecular mechanisms that lead to multidrug resistance (MDR). miRNAs regulate post-transcriptional processes in the proteosynthetic pathway and may serve as specific effectors or interesting targets for cancer therapy.
Article
Toxicology
Alicja Zajdel, Joanna Nycz, Adam Wilczok
Summary: Lapatinib can reverse chemoresistance of breast cancer cells to paclitaxel, enhancing its anticancer activity, and thus may have potential benefits in the treatment of HER2-negative breast cancer.
TOXICOLOGY IN VITRO
(2021)
Article
Microbiology
Jan Viglas, Petra Olejnikova
Summary: The ABC transporter superfamily plays a crucial role in transporting various molecules across biological membranes, including antifungal compounds in filamentous fungi. Understanding the physiological substrates and roles of individual subfamilies of ABC transporters in fungi is important for clarifying their significance in clinical and agricultural settings.
MICROBIOLOGICAL RESEARCH
(2021)
Article
Oncology
Chung-Pu Wu, Cheng-Yu Hung, Megumi Murakami, Yu-Shan Wu, Chun-Ling Lin, Yang-Hui Huang, Tai-Ho Hung, Jau-Song Yu, Suresh Ambudkar
Summary: In this study, we investigate the role of P-glycoprotein (P-gp) in the reduced sensitivity of cancer cells to the anaplastic lymphoma kinase (ALK) inhibitor ensartinib. Our results demonstrate that P-gp overexpression decreases the intracellular accumulation and cytotoxic activity of ensartinib in cancer cells. These findings highlight the importance of understanding the mechanisms of ensartinib resistance mediated by P-gp.
Article
Chemistry, Analytical
Yanyan Ma, Zhanchen Guo, Chuanwen Fan, Jingran Chen, Shuxin Xu, Zhen Liu
Summary: This study developed aptamers that can target ABCG2 and reverse multidrug resistance, showing great potential in cancer diagnosis and treatment. The aptamers can specifically bind to human colorectal cancer stem cells and effectively reverse drug resistance in liver cancer cells.
ANALYTICAL CHEMISTRY
(2022)
Review
Biology
Maria Bucci-Munoz, Aldana Magali Gola, Juan Pablo Rigalli, Maria Paula Ceballos, Maria Laura Ruiz
Summary: Cancer multidrug resistance (MDR) is a major cause of therapy failure and mortality, often caused by the overexpression of drug transporters. Extracellular vesicles (EVs) play a role in cell-cell communication and can transfer various biomolecules, including transporter molecules and noncoding RNAs, leading to MDR or drug-sensitive phenotype. This article reviews the regulation of ABC transporters by EV-mediated cell-cell communication and discusses the potential for novel therapeutic strategies.
Article
Biochemistry & Molecular Biology
Eric Chekwube Aniogo, Blassan P. George, Heidi Abrahamse
Summary: The study utilized photodynamic therapy to treat MCF-7 cells overexpressed with P-glycoprotein, resulting in cell apoptosis with increased externalisation of phosphatidylserine protein and changes in apoptotic protein expression.
Article
Chemistry, Physical
Damian Krzyzanowski, Marcin Kruszewski, Agnieszka Grzelak
Summary: Silver nanoparticles (AgNPs) have unique properties that have attracted significant attention, showing antibacterial, antifungal, and anticancer properties. However, they can also exhibit cytotoxic effects and modulate the activity and expression of ABC transporters.
Article
Chemistry, Physical
Linna Liang, Wendi Huo, Bei Wang, Lingzhi Cao, Haoran Huo, Yixin Liu, Yi Jin, Xinjian Yang
Summary: Tumor multidrug resistance is a major cause of chemotherapy failure, and reversing tumor multidrug resistance is crucial for increasing the sensitivity of tumor cells to chemodrugs. The self-assembled DNAzyme nanoflowers can efficiently reverse multidrug resistance, enhance drug loading capacity, and suppress P-glycoprotein expression.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2022)
Article
Cell Biology
Chung-Pu Wu, Megumi Murakami, Yu-Shan Wu, Ya-Chen Chi, Sung-Han Hsiao, Yang-Hui Huang, Tai-Ho Hung, Suresh Ambudkar
Summary: The study explored the potential of using branebrutinib to resensitize P-gp-overexpressing multidrug-resistant cancer cells to chemotherapy by inhibiting the drug transport function of P-gp. Results showed that branebrutinib could reverse P-gp-mediated MDR at sub-toxic concentrations while maintaining cytotoxicity against drug-sensitive parental cell lines and P-gp-overexpressing multidrug-resistant variants. This new pharmacological action of branebrutinib against P-gp activity warrants further investigation in future drug combination studies.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2021)
Article
Pharmacology & Pharmacy
Gangyang Wang, Lingling Cao, Yafei Jiang, Tao Zhang, Hongsheng Wang, Zhuoying Wang, Jing Xu, Min Mao, Yingqi Hua, Zhengdong Cai, Xiaojun Ma, Shuo Hu, Chenghao Zhou
Summary: This study demonstrates that anlotinib can reverse multidrug resistance in osteosarcoma cells by inhibiting the efflux function of P-glycoprotein 1 (PGP1) and increasing the intracellular accumulation of chemotherapeutic agents. Anlotinib also stimulates the ATPase activity of PGP1. In animal studies, anlotinib combined with doxorubicin shows a significant decrease in tumor growth rate and tumor size.
FRONTIERS IN PHARMACOLOGY
(2022)