Article
Pharmacology & Pharmacy
Sofija Jovanovic Stojanov, Epole N. Ntungwe, Jelena Dinic, Ana Podolski-Renic, Milica Pajovic, Patricia Rijo, Milica Pesic
Summary: Coleon U, a natural compound not recognized as a substrate of P-glycoprotein, has equal efficacy against sensitive and multidrug-resistant cancer cells. It delays the decrease in P-glycoprotein activity by decreasing mitochondrial membrane potential and inhibiting P-glycoprotein expression.
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
Chemistry, Medicinal
Samer S. Daher, Miseon Lee, Xiao Jin, Christiana N. N. Teijaro, Pamela R. R. Barnett, Joel S. S. Freundlich, Rodrigo B. B. Andrade
Summary: The increasing bacterial drug resistance calls for the development of novel antibacterials with new mechanisms of action. This study explores the design and synthesis of a novel series of solithromycin analogs, with a focus on their structure-activity relationship. Two analogs are found to exhibit improved activity against resistant strains, showing potential for further pre-clinical studies.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
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
Biochemistry & Molecular Biology
Wenqin Sun, Iris L. K. Wong, Helen Ka-Wai Law, Xiaochun Su, Terry C. F. Chan, Gege Sun, Xinqing Yang, Xingkai Wang, Tak Hang Chan, Shengbiao Wan, Larry M. C. Chow
Summary: Tea polyphenol derivative EC31 is a potent and nontoxic P-gp inhibitor that can reverse multidrug resistance and enhance the efficacy of anticancer drugs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Aobulikasimu Hasan, Dan Tang, Dilaram Nijat, Hequn Yang, H. A. Aisa
Summary: The study isolated several new diterpenoids from Euphorbia glomerulans, with compound 5 showing high efficacy in reversing multidrug resistance in cancer by inhibiting P-gp transport function. Molecular docking predicted the recognition mechanism of compound 5 and verapamil with P-gp.
BIOORGANIC CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Balint Racz, Annamaria Kincses, Krisztian Laczi, Gabor Rakhely, Enrique Dominguez-alvarez, Gabriella Spengler
Summary: Recently, the anticancer activity of symmetrical selenoesters was investigated in sensitive and resistant human colon adenocarcinoma cells. The compounds showed synergistic interaction with doxorubicin and exhibited ABCB1 inhibitory and apoptosis-inducing effects. Transcriptome analysis revealed that symmetrical selenoesters may influence the redox state of cells and interfere with metastasis formation.
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
Multidisciplinary Sciences
Jiong Zhang, Xiangxiang Zhao, John R. Cappiello, Yi Yang, Yunfei Cheng, Guang Liu, Wenjing Fang, Yinzhu Luo, Yu Zhang, Jiajia Dong, Lixin Zhang, K. Barry Sharpless
Summary: A series of arylfluorosulfates synthesized via SuFEx, including compounds 3, 81, and 101, showed potent antibacterial activity, the ability to overcome multidrug resistance, and a lack of susceptibility to resistance development. These compounds also demonstrated rapid bactericidal potency, selectivity against gram-positive bacteria, and the capability to disrupt bacterial biofilms and kill persisters. Additionally, compound 3 exhibited synergy with streptomycin and gentamicin, while their anti-MRSA activity was evaluated using the Caenorhabditis elegans model.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2021)
Article
Chemistry, Medicinal
Elisa Frederico Seneme, Daiane Carla dos Santos, Carolina Afonso de Lima, Icaro Augusto Maccari Zelioli, Juliana Mozer Sciani, Giovanna Barbarini Longato
Summary: The combination of myristicin with chemotherapeutic agents enhances their cytotoxic effects by blocking P-glycoprotein, allowing the drugs to enter cells and function properly. This study suggests myristicin as a potential reverser of multidrug resistance.
Retraction
Oncology
S. Mohana, M. Ganesan, N. Rajendra Prasad, D. Ananthakrishnan, D. Velmurugan
Summary: A correction to this paper has been published and is accessible through the original article.
Article
Biophysics
Xiaolin Zhang, Lanlan Jia, Nanxin Liu, Ying Zhao, Tingting Zhang, Xiaoyu Xie
Summary: The use of inside-out oriented extracellular vesicles coated magnetic nanoparticles enables the discovery of low-toxicity and high-efficiency P-gp inhibitors from natural products. This method provides an effective tool for the screening of novel P-gp inhibitors, expanding the application field of cell membrane biomimetic magnetic nanoparticles.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2023)
Article
Biochemistry & Molecular Biology
Pradhapsingh Bharathiraja, David S. P. Cardoso, N. Rajendra Prasad, Silva Mulhovo, Deepa S. Lakra, Maria-Jose U. Ferreira
Summary: This study found that derivatives of N-alkylated monoterpene indole alkaloids, particularly N-(para-bromobenzyl) (NBBT), can reverse P-gp-mediated multidrug resistance in cancer cells. NBBT exhibited the highest P-gp inhibitory activity and reduced P-gp overexpression by inhibiting the nuclear translocation of the nuclear factor kappa B p-50 subunit. Additionally, NBBT showed synergistic effects with doxorubicin, decreasing the cellular migration and increasing apoptotic incidence in drug-resistant cells.
JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Manuela Labbozzetta, Paola Poma, Monica Notarbartolo
Summary: Acute myeloid leukemia (AML) is difficult to treat due to the development of resistance to both traditional chemotherapy and new drugs in some patients. Multidrug resistance (MDR) in AML is often caused by the overexpression of P-glycoprotein (P-gp), which is an efflux pump. This mini-review focuses on the advantages of using natural substances as inhibitors of P-gp, including phytol, curcumin, lupeol, and heptacosane, and their mechanisms of action in AML.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Qianqian Qiu, Feng Zou, Huilan Li, Wei Shi, Daoguang Zhou, Ping Zhang, Teng Li, Ziyu Yin, Zilong Cai, Yuxuan Jiang, Wenlong Huang, Hai Qian
Summary: Compound 21 is a dual inhibitor that can block both P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), showing potential in overcoming multidrug resistance and improving the oral bioavailability of specific drugs.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Lin Yan, Jingjie Wang, Miaobo Pan, Qianqian Qiu, Wenlong Huang, Hai Qian
CHEMICAL BIOLOGY & DRUG DESIGN
(2016)
Article
Biochemistry & Molecular Biology
Lin Yan, Miaobo Pan, Mian Fu, Jingjie Wangb, Wenlong Huang, Hai Qian
BIOORGANIC & MEDICINAL CHEMISTRY
(2016)
Article
Biochemistry & Molecular Biology
Zheng Li, Miaobo Pan, Xin Su, Yuxuan Dai, Mian Fu, Xingguang Cai, Wei Shi, Wenlong Huang, Hai Qian
BIOORGANIC & MEDICINAL CHEMISTRY
(2016)
Article
Chemistry, Medicinal
Zheng Li, Qianqian Qiu, Xue Xu, Xuekun Wang, Lei Jiao, Xin Su, Miaobo Pan, Wenlong Huang, Hai Qian
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2016)
Article
Chemistry, Medicinal
Zheng Li, Chunxia Liu, Xue Xu, Qianqian Qiu, Xin Su, Yuxuan Dai, Jianyong Yang, Huilan Li, Wei Shi, Chen Liao, Miaobo Pan, Wenlong Huang, Hai Qian
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2017)
Article
Chemistry, Medicinal
Qianqian Qiu, Baomin Liu, Jian Cui, Zheng Li, Xin Deng, Hao Qiang, Jieming Li, Chen Liao, Bo Zhang, Wei Shi, Miaobo Pan, Wenlong Huang, Hai Qian
JOURNAL OF MEDICINAL CHEMISTRY
(2017)
Article
Chemistry, Medicinal
Qianqian Qiu, Wei Shi, Zheng Li, Bo Zhang, Miaobo Pan, Jian Cui, Yuxuan Dai, Wenlong Huang, Hai Qian
JOURNAL OF MEDICINAL CHEMISTRY
(2017)
Article
Materials Science, Biomaterials
Mian Fu, Chenyu Zhang, Yuxuan Dai, Xue Li, Miaobo Pan, Wenlong Huang, Hai Qian, Liang Ge
BIOMATERIALS SCIENCE
(2018)
Article
Biochemistry & Molecular Biology
Mutta Kairuki, Qianqian Qiu, Miaobo Pan, Qifei Li, Jiaqi Zhou, Hesham Ghaleb, Wenlong Huang, Hai Qian, Cheng Jiang
BIOORGANIC & MEDICINAL CHEMISTRY
(2019)
Article
Chemistry, Physical
Ananya Sathanikan, Giacomo Ceccone, Jorge Banuls-Ciscar, Miaobo Pan, Fadwa Kamal, Talia Bsaibess, Anne Gaucher, Damien Prim, Rachel Meallet-Renault, Pascal Colpo, Sonia Amigoni, Frederic Guittard, Thierry Darmanin
Summary: The study aims to control the surface wetting and fluorescence properties of conducting polymer nanotubes through post-grafting. Findings suggest that surface hydrophobicity and fluorescence depend on the substituent, while surface morphology remains unchanged after grafting.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2022)
Article
Biochemistry & Molecular Biology
Yuxuan Dai, Xingguang Cai, Wei Shi, Xinzhou Bi, Xin Su, Miaobo Pan, Huilan Li, Haiyan Lin, Wenlong Huang, Hai Qian
Article
Biochemistry & Molecular Biology
Miaobo Pan, Jian Cui, Lei Jiao, Hesham Ghaleb, Chen Liao, Jiaqi Zhou, Mutta Kairuki, Haiyan Lin, Wenlong Huang, Hai Qian
BIOORGANIC & MEDICINAL CHEMISTRY
(2017)
Article
Biochemistry & Molecular Biology
Wei Shi, Miaobo Pan, Hao Qiang, Qianqian Qiu, Wenlong Huang, Haiyan Lin, Hai Qian, Liang Ge
CHEMICAL BIOLOGY & DRUG DESIGN
(2017)