Article
Multidisciplinary Sciences
Wang Yin, Dongxi Xiang, Tao Wang, Yumei Zhang, Cuong Pham, Shufeng Zhou, Guoqin Jiang, Yingchun Hou, Yimin Zhu, Yinglu Han, Liang Qiao, Phuong H-L Tran, Wei Duan
Summary: Inhibiting MDR1 or ABCG2 was found to increase the sensitivity of liver cancer stem cells to doxorubicin, leading to elevated intracellular concentration of the drug and increased apoptosis. This approach effectively reversed chemoresistance in liver cancer stem cells, demonstrating a promising strategy for enhancing the therapeutic efficacy of doxorubicin.
SCIENTIFIC REPORTS
(2021)
Article
Pharmacology & Pharmacy
Thiago S. Lima, Luciano O. Souza, Diego Iglesias-Gato, Johanna Elversang, Flemming Steen Jorgensen, Tuula Kallunki, Martin A. Roder, Klaus Brasso, Jose M. A. Moreira
Summary: Itraconazole can re-sensitize docetaxel-resistant prostate and breast cancer cells by binding to ABC transporter protein ABCB1, inhibiting the transport of docetaxel.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Oncology
Zhaoqing Li, Cong Chen, Lini Chen, Dengdi Hu, Xiqian Yang, Wenying Zhuo, Yongxia Chen, Jingjing Yang, Yulu Zhou, Misha Mao, Xun Zhang, Ling Xu, Siwei Ju, Jun Shen, Qinchuan Wang, Minjun Dong, Shuduo Xie, Qun Wei, Yunlu Jia, Jichun Zhou, Linbo Wang
Summary: This study identified STAT5a as a regulator of ABCB1 expression in breast cancer, acting as a chemoresistance inducer that can be targeted by pimozide. Targeting STAT5a could be a promising strategy for treating chemoresistant breast cancer, and repurposing pimozide for doxorubicin resensitization is attractive due to its safety profile.
FRONTIERS IN ONCOLOGY
(2021)
Review
Oncology
Zihan Si, Yan Zhong, Sixian Lao, Yufeng Wu, Guoping Zhong, Weiwei Zeng
Summary: This review outlines the role of microRNAs (miRNAs) in the treatment of breast cancer using anthracyclines. MiRNAs play important roles in the initiation, development, and treatment of breast cancer, and can influence the efficacy of anthracyclines.
FRONTIERS IN ONCOLOGY
(2022)
Article
Oncology
Paula M. M. Fracasso, George A. A. Fisher, Sherry A. A. Goodner, Jan H. H. Beumer, Merrill J. J. Egorin, Carole L. L. Fears, Jonathan D. D. Wildi, Gary J. J. Jones, Tillman E. E. Pearce, Branimir I. I. Sikic
Summary: This phase 1 trial aimed to determine the safety of paclitaxel with valspodar in patients with advanced solid tumors. The combination therapy resulted in manageable hematologic and non-hematologic adverse events. However, the efficacy was limited, leading to discontinuation of its clinical development.
AMERICAN JOURNAL OF CLINICAL ONCOLOGY-CANCER CLINICAL TRIALS
(2023)
Article
Pharmacology & Pharmacy
Chung-Pu Wu, Sung-Han Hsiao, Yu-Shan Wu
Summary: The overexpression of human ATP-binding cassette (ABC) transporters in cancer cells can lead to multidrug resistance (MDR), which poses a significant obstacle to chemotherapy. Currently, there are no approved drugs specifically designed to treat multidrug-resistant cancers. However, drug repurposing has emerged as a practical approach to discover effective modulators of drug transporters.
DRUG RESISTANCE UPDATES
(2023)
Article
Chemistry, Medicinal
Kritika Engle, Gautam Kumar
Summary: Chemotherapy is a common treatment for cancer, but its drawbacks include lack of selectivity and development of drug resistance. Multidrug resistance refers to low sensitivity of specific cells to anticancer drugs, which is mainly caused by overexpression of multidrug efflux systems.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Multidisciplinary Sciences
Die Zhang, Tingting Jia, Xingxing Chen, Haopeng Jiang, Teng Guo, Junjun Dong, Hairong Zeng, Yixin Wang, Yi Yuan
Summary: This study aims to determine whether BUF can reverse docetaxel resistance mediated by ABCB1 in breast cancer. The results show that BUF can increase the sensitivity of drug-resistant cells to DCT, inhibit the expression of ABCB1 protein, increase the drug accumulation of DCT in drug-resistant cells, and reduce the ATPase activity of ABCB1. Animal experiments demonstrate that BUF can inhibit the growth of drug-resistant tumors and decrease the expression of ABCB1.
Article
Pharmacology & Pharmacy
Chung-Pu Wu, Tai-Ho Hung, Sabrina Lusvarghi, Yi-Hsuan Chu, Sung-Han Hsiao, Yang-Hui Huang, Yu-Tzu Chang, Suresh V. Ambudkar
Summary: The study found that Almonertinib can inhibit the drug transport activity of ABCBl at submicromolar concentrations, but not affect ABCG2, and resensitize multidrug-resistant cancer cells overexpressing ABCB1 to chemotherapeutic drugs.
BIOCHEMICAL PHARMACOLOGY
(2021)
Article
Multidisciplinary Sciences
J. Robert McCorkle, Justin W. Gorski, Jinpeng Liu, McKayla B. Riggs, Anthony B. McDowell, Nan Lin, Chi Wang, Frederick R. Ueland, Jill M. Kolesar
Summary: The study established in vitro models of paclitaxel-resistant ovarian cancer cells and found that certain tyrosine kinase inhibitors can synergize with paclitaxel to inhibit the proliferation of ABCB1-overexpressing ovarian cancer cells, providing a promising strategy for improving ovarian cancer therapy.
Review
Pharmacology & Pharmacy
Jinyun Dong, Li Yuan, Can Hu, Xiangdong Cheng, Jiang -Jiang Qin
Summary: Multidrug resistance (MDR) is a major threat in chemotherapy, and the overexpression of ATP-binding cassette (ABC) transporters, particularly P-glycoprotein (P-gp)/ABCB1, plays a role in MDR. Targeting P-gp with small molecule inhibitors is an effective approach, but no clinically useful inhibitors have been identified so far. Therefore, further research is needed to overcome MDR.
PHARMACOLOGY & THERAPEUTICS
(2023)
Article
Pharmacology & Pharmacy
Zhuo-Xun Wu, Yuqi Yang, Jing-Quan Wang, Wen-Min Zhou, Junyu Chen, Yi-Ge Fu, Ketankumar Patel, Zhe-Sheng Chen, Jian-Ye Zhang
Summary: The overexpression of ABCB1 transporter can confer resistance to GSK-1070916, and this resistance can be overcome by the addition of an ABCB1 inhibitor. GSK-1070916 stimulates the ATPase activity of ABCB1 in a concentration-dependent manner and shows high binding affinity to the ABCB1 substrate-binding site in computational docking analysis.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Toxicology
Anselm Morell, Eva Novotna, Jaroslav Milan, Petra Danielisova, Neslihan Bukum, Vladimir Wsol
Summary: Midostaurin, an FLT3 inhibitor, shows therapeutic benefit beyond FLT3 inhibition in treating AML by blocking AKR1C3-mediated inactivation of Dau, increasing cellular accumulation of Dau, and enhancing its cytotoxic effects.
ARCHIVES OF TOXICOLOGY
(2021)
Article
Cardiac & Cardiovascular Systems
Nicholas S. Wilcox, Seth J. Rotz, McKay Mullen, Evelyn J. Song, Betty Ky Hamilton, Javid Moslehi, Saro H. Armenian, Joseph C. Wu, June-Wha Rhee, Bonnie Ky
Summary: Sex-based differences exist in the prevalence and outcomes of cardiovascular disease and cancer. There may also be differences between males and females in the risk of cardiotoxicity following cancer therapy. However, for certain cancer treatments such as hormone therapy and immune therapy, sex-based differences have not been fully elucidated. Further research is needed to fill these knowledge gaps and guide future clinical practice.
CIRCULATION RESEARCH
(2022)
Article
Pharmacology & Pharmacy
Andrea J. Parsons, Tobias Cohen, Toni M. Schwarz, Kathryn R. Stein, Sabrina Ophir, Jailene Paredes Casado, Domenico Tortorella
Summary: HCMV is a widespread pathogen that causes various complications and challenges in terms of drug resistance. Current therapeutic options are limited, highlighting the need for new treatments targeting different stages of the virus life cycle. The study suggests that valspodar may represent a potential new anti-HCMV therapeutic that targets host factors.
ANTIVIRAL RESEARCH
(2021)