Article
Pharmacology & Pharmacy
Fazhen Luo, Juanjuan Zhao, Shuo Liu, Yuanfei Xue, Dongyun Tang, Jun Yang, Ye Mei, Guowen Li, Yan Xie
Summary: Ursolic acid (UA) enhances the chemosensitivity of drug-resistant breast carcinoma cells to doxorubicin (DOX) by targeting energy metabolism through the AMPK/mTOR/PGC-1 alpha signaling pathway. This leads to inhibition of cellular proliferation and migration, cell cycle arrest, induction of cell apoptosis and DNA damage response.
BIOCHEMICAL PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Tsz Cheung Chong, Iris L. K. Wong, Jiahua Cui, Man Chun Law, Xuezhen Zhu, Xuesen Hu, Jason W. Y. Kan, Clare S. W. Yan, Tak Hang Chan, Larry M. C. Chow
Summary: This study identified Ac15(Az8)(2) as a potent and non-toxic BCRP inhibitor that can reverse BCRP-mediated drug resistance and inhibit tumor growth.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Mohana Krishna Gopisetty, Dora Izabella Adamecz, Ferenc Istvan Nagy, Adam Baji, Vasiliki Lathira, Marton Richard Szabo, Renata Gaspar, Tamas Csont, Eva Frank, Monika Kiricsi
Summary: MDR1 plays a crucial role in multidrug resistance in cancer cells, and inhibiting its activity could potentially improve the success rate of chemotherapy. Novel DHT-derived compounds were found to inhibit MDR1 activity in multidrug-resistant breast adenocarcinoma cells, demonstrating the beneficial effects of efflux pump inhibition in chemotherapy.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Review
Pharmacology & Pharmacy
Sonali Mehendale-Munj, Shivangi Sawant
Summary: Breast Cancer Resistance Protein (BCRP) is an efflux transporter responsible for causing multidrug resistance. BCRP expels potent antineoplastic drugs, leading to resistance and failure in cancer treatment. The regulation and expression of BCRP play important roles in maintaining the balance of xenobiotics and nutrients, impacting cancer therapies.
CURRENT DRUG TARGETS
(2021)
Article
Nanoscience & Nanotechnology
Yousheng Mo, Wei Liu, Piaoxue Liu, Qiao Liu, Zhongyu Yuan, Qi Wang, Dongsheng Yuan, Xiao-Jia Chen, Tongkai Chen
Summary: A multifunctional graphene oxide tumor-targeting drug delivery system was developed, which improved the delivery of paclitaxel, reversed multi-drug resistance, and increased the therapeutic efficacy of breast cancer treatment.
INTERNATIONAL JOURNAL OF NANOMEDICINE
(2022)
Article
Biochemistry & Molecular Biology
Zhanhong Liu, Pengbo Hou, Jiankai Fang, Jingyu Zhu, Juanmin Zha, Rui Liu, Yayun Ding, Muqiu Zuo, Peishan Li, Lijuan Cao, Chao Feng, Gerry Melino, Changshun Shao, Yufang Shi
Summary: Chemotherapy resistance in breast cancer can be induced by mesenchymal stromal cells (MSCs) through reducing the intratumoral accumulation of doxorubicin. This resistance is mediated by hyaluronan (HA), a major extracellular matrix (ECM) product of MSCs, which can bind with doxorubicin and inhibit its entry into breast cancer cells. High levels of HA in the serum are positively associated with chemoresistance in breast cancer patients.
Article
Pharmacology & Pharmacy
Jing-Yi Chen, Chieh-Ju Sung, Ssu-Chi Chen, Yi-Ping Hsiang, Yung-Chia Hsu, Yu-Ning Teng
Summary: Cancer drug resistance is a challenging issue for patients, especially in the later stages of treatment. In this study, researchers investigated the effects of vitamin E TPGS on drug efflux transporters and its ability to reverse multidrug resistance in cancer. The results showed that vitamin E TPGS significantly inhibited the efflux function of transporters P-gp, MRP1, and BCRP, without affecting protein expression levels. It was also found to be a competitive inhibitor on chemotherapeutic drug efflux in different over-expressing cell lines. Furthermore, vitamin E TPGS was able to enhance cell membrane fluidity and reverse multidrug resistance in breast cancer cells. This study suggests that vitamin E TPGS could be a promising modulator for overcoming drug resistance in cancer treatment.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2023)
Article
Agriculture, Dairy & Animal Science
Michela Levi, Luisa Vera Muscatello, Barbara Brunetti, Cinzia Benazzi, Federico Parenti, Francesca Gobbo, Giancarlo Avallone, Barbara Bacci, Elisa Zambon, Paola Valenti, Giuseppe Sarli
Summary: Multidrug resistance in neoplastic cells is primarily mediated by P-glycoprotein and breast cancer resistance protein, with canine mammary carcinomas showing high intrinsic expression levels of both. However, no significant association was found between the expression of these proteins and immunophenotypes, Ki67 index, histological grade, or tumor-related death in this study.
Article
Materials Science, Multidisciplinary
Sinan Cheng, Zheng Lu, Yang Feng, Xuewei Zhao, Ruixia Zhao, Zuchun Qiu, Chenshuang Jia, Lirong Chen, Yue Yuan, Xinyao Li, Qian Gao, Jie Xu, Zhan Shu, Wei Duan, Yingchun Hou, Guochao Nie, Li Xiao
Summary: Breast cancer is the most common cancer and leading cause of death in women. Current chemotherapy has low efficacy and high side effects, necessitating the development of a novel targeted drug delivery formulation. The study discovered a new drug formulation that showed satisfactory therapeutic efficacy for breast cancer, particularly for drug resistant cases.
MATERIALS TODAY ADVANCES
(2022)
Review
Biochemistry & Molecular Biology
Ji He, Erika Fortunati, Dong-Xu Liu, Yan Li
Summary: Chemotherapeutics are a main therapy for metastatic breast cancers, but multidrug resistance due to ABC transporters remains a challenge. Targeting ABCB1 to reverse drug resistance in clinical trials has been disappointing, but ABC transporters may play roles in breast cancer development and metastasis beyond efflux function. Understanding the functions and regulations of ABC transporters in breast cancer biology may lead to more targeted and novel therapies.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
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
Oncology
Hee-Jeong Lee, Cheol-Hee Choi
Summary: New resistant breast cancer cell lines overexpressing BCRP were established by gradually increasing SN38 concentration, and genes and mechanisms associated with multidrug resistance were discovered.
Article
Biology
Absarul Haque, Ghazanfar Ali Baig, Abdulelah Saleh Alshawli, Khalid Hussain Wali Sait, Bilal Bin Hafeez, Manish Kumar Tripathi, Badrah Saeed Alghamdi, Hani S. H. Mohammed Ali, Mahmood Rasool
Summary: This study determined the binding affinity and potential interaction sites of the multidrug resistance protein 1 (MRP1) with various anticancer drugs using homology modelling and molecular docking analysis. The results suggested that Carboplatin could be an appropriate therapeutic choice against MRP1 in ovarian cancer, and combining Carboplatin with Gemcitabine may overcome multidrug resistance phenotype.
Review
Biochemistry & Molecular Biology
Shiwen Yu, Jinling Zheng, Yan Zhang, Dandan Meng, Yujue Wang, Xiaoyu Xu, Na Liang, Shayibai Shabiti, Xu Zhang, Zixi Wang, Zehua Yang, Pengbing Mi, Xing Zheng, Wenjun Li, Hongfei Chen
Summary: Chemotherapy is the primary treatment for breast cancer, but side effects and multidrug resistance (MDR) are major challenges. Research is focused on finding new drugs and understanding the mechanisms and inhibition of MDR.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Oncology
Wenting Ni, Hui Fan, Xiuqin Zheng, Fangming Xu, Yuanyuan Wu, Xiaoman Li, Aiyun Wang, Shile Huang, Wenxing Chen, Shijun Wang, Yin Lu
Summary: The study found that cryptotanshinone (CPT) has a reversal effect on drug resistance in breast cancer by inhibiting the oligomer formation of breast cancer resistance protein (BCRP). The inhibitory effect of CPT on BCRP is related to the expression level of estrogen receptor alpha (ER alpha) in breast cancer cells, and it is also sensitive in ER alpha-negative breast cancer cells.
FRONTIERS IN ONCOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Aktan Alpsoy, Emily C. Dykhuizen
JOURNAL OF BIOLOGICAL CHEMISTRY
(2018)
Article
Oncology
Aparna Shinde, Sarah Libring, Aktan Alpsoy, Ammara Abdullah, James A. Schaber, Luis Solorio, Michael K. Wendt
MOLECULAR CANCER RESEARCH
(2018)
Article
Pharmacology & Pharmacy
Monica Soto-Velasquez, Michael P. Hayes, Aktan Alpsoy, Emily C. Dykhuizen, Val J. Watts
MOLECULAR PHARMACOLOGY
(2018)
Article
Medicine, Research & Experimental
Aktan Alpsoy, Seda Yasa, Ufuk Gunduz
BIOMEDICINE & PHARMACOTHERAPY
(2014)
Article
Cell Biology
Eliana F. Torres-Zelada, Robert E. Stephenson, Aktan Alpsoy, Benjamin D. Anderson, Selene K. Swanson, Laurence Florens, Emily C. Dykhuizen, Michael P. Washburn, Vikki M. Weake
JOURNAL OF CELL SCIENCE
(2019)
Article
Biochemistry & Molecular Biology
Katelyn E. Connelly, Tyler M. Weaver, Aktan Alpsoy, Brian X. Gu, Catherine A. Musselman, Emily C. Dykhuizen
NUCLEIC ACIDS RESEARCH
(2019)
Article
Biochemistry & Molecular Biology
Rhushikesh A. Kulkarni, Daniel W. Bak, Darmood Wei, Sarah E. Bergholtz, Chloe A. Briney, Jonathan H. Shrimp, Aktan Alpsoy, Abigail L. Thorpe, Arissa E. Bavari, Daniel R. Crooks, Michaella Levy, Laurence Florens, Michael P. Washburn, Norma Frizzell, Emily C. Dykhuizen, Eranthie Weerapana, W. Marston Linehan, Jordan L. Meier
NATURE CHEMICAL BIOLOGY
(2019)
Article
Chemistry, Multidisciplinary
Bo Cai, Dongwook Kim, Saeed Akhand, Yixing Sun, Robert J. Cassell, Aktan Alpsoy, Emily C. Dykhuizen, Richard M. Van Rijn, Michael K. Wendt, Casey J. Krusemark
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2019)
Article
Oncology
Aktan Alpsoy, Sagar M. Utturkar, Benjamin C. Carter, Alisha Dhiman, Sandra E. Torregrosa-Allen, Melanie P. Currie, Bennett D. Elzey, Emily C. Dykhuizen
Summary: The SWI/SNF chromatin-remodeling complexes, particularly the GBAF subcomplex, play a critical role in prostate cancer by interacting with AR and CTCF, modulating AR-dependent gene expression, and exhibiting overlapping genome localization and transcriptional targets with BET proteins. Targeting the BRD9 subunit of GBAF complex may provide a promising alternative for treating AR-positive prostate cancers, including those resistant to androgen deprivation therapies, by coordinating SWI/SNF-BET cooperation.
Article
Biochemistry & Molecular Biology
Sijie Wang, Aktan Alpsoy, Surbhi Sood, Sandra Carolina Ordonez-Rubiano, Alisha Dhiman, Yixing Sun, Guanming Jiao, Casey J. Krusemark, Emily C. Dykhuizen
Summary: Polycomb group (PcG) proteins regulate embryonic development and cancer progression by forming Polycomb repressive complexes. Among them, CBX2 is upregulated in various cancers, especially advanced prostate cancer. A selective CBX2 chromodomain probe, SW2_152F, has been discovered to inhibit CBX2 chromatin binding and block neuroendocrine differentiation in prostate cancer cells.
Review
Biology
Aktan Alpsoy, Surbhi Sood, Emily C. Dykhuizen
Summary: The packaging of DNA in the nucleus plays a crucial role in gene expression, with long-range interactions through physical loops in the genome influencing transcription. The hierarchy of chromatin folding in the nucleus is tightly regulated, allowing for dynamic shifts to accommodate changes in transcription, DNA replication, and repair. Chromatin remodeling is essential for maintaining and regulating the 3D genome organization, particularly in relation to the regulation of architectural proteins CTCF and cohesin.
Article
Biology
Rouhollah Khodadust, Aktan Alpsoy, Gozde Unsoy, Ufuk Gunduz
TURKISH JOURNAL OF BIOLOGY
(2020)