Article
Multidisciplinary Sciences
Hai Wang, Yutong Liang, Yue Yin, Jie Zhang, Wen Su, Alisa M. White, Bin Jiang, Jiangsheng Xu, Yuntian Zhang, Samantha Stewart, Xiongbin Lu, Xiaoming He
Summary: The FSCNO hybrid nanoparticle targets tumor vasculature to release P-gp inhibitor and anticancer drug, improving drug bioavailability inside cells. The nano-onion shows superior light absorption in the NIR region, enabling triggered drug release at low power.
NATURE COMMUNICATIONS
(2021)
Review
Biochemistry & Molecular Biology
Manuel F. Varela, Jerusha Stephen, Deeksha Bharti, Manjusha Lekshmi, Sanath Kumar
Summary: Bacterial pathogens resistant to multiple antimicrobial agents through active efflux pose a serious threat to public health. This review discusses recent molecular studies focused on modulating the antimicrobial efflux transporters to restore the clinical efficacy of infectious disease chemotherapy.
Article
Pharmacology & Pharmacy
Yingqing Du, Yuzhong Zheng, Ciel Xiaomei Yu, Lishan Zhong, Yafang Li, Baomeng Wu, Weihui Hu, Elsa Wanyi Zhu, Venus Wei Xie, Qitian Xu, Xingri Zhan, Yamiao Huang, Liyi Zeng, Zhenxia Zhang, Xi Liu, Jiachuan Yin, Guangcai Zha, Kelvin Chan, Karl Wah Keung Tsim
Summary: Research shows that YPFS can increase intracellular accumulation of cisplatin in lung cancer cells, reduce cell viability, inhibit the activity and expression of ATP-binding cassette transporters and GSTs, resulting in increased apoptosis rate.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Microbiology
Anna Claudia Silva, Daniel Clemente de Moraes, Denilson Costa do Carmo, Giselle Cristina Casaes Gomes, A. Ganesan, Rosangela Sabbatini Capella Lopes, Antonio Ferreira-Pereira, Claudio Cerqueira Lopes
Summary: Azoles are the main antifungal drugs used to treat invasive candidiasis, but their efficacy is limited by fungal resistance mechanisms like overexpression of efflux pumps. A potential strategy to overcome this resistance is to inhibit the efflux process. This study aimed to synthesize altissimacoumarin D and its analogues to evaluate their ability to reverse the resistance phenotype of Candida albicans.
Article
Plant Sciences
Muhammad Aamir Manzoor, Guohui Li, Muhammad Abdullah, Wang Han, Han Wenlong, Zhang Yang, Wang Xinya, Zhao Yu, Feng Xiaofeng, Jin Qing, Muhammad Sohaib Shafique, Yongping Cai
Summary: In this study, 404 MATE genes from six Rosaceae genomes were identified and classified into eight main subfamilies based on structural and phylogenetic analysis. The results suggest that whole-genome duplication events may have played a vital role in the expansion of the MATE genes family. The analysis revealed functional divergence among different subfamilies, providing insights into the functions, expansion complexity, and evolutions of the MATE genes in Chinese pear and five Rosaceae species.
PHYSIOLOGIA PLANTARUM
(2021)
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
Infectious Diseases
Wen-Jung Lu, Pang-Hung Hsu, Chun-Ju Chang, Cheng-Kuan Su, Yan-Jyun Huang, Hsuan-Ju Lin, Margaret Lai, Gui-Xia Ooi, Jing-Yi Dai, Hong-Ting Victor Lin
Summary: The study found that the seaweed compound diphenylmethane (DPM) has potential efflux pump inhibitory activity against drug-resistant Escherichia coli, enhancing the antibacterial activity of antibiotics without damaging E. coli membranes. Cell toxicity tests showed that DPM has mild toxicity towards human cells.
Review
Pharmacology & Pharmacy
Tushar Khare, Uttpal Anand, Abhijit Dey, Yehuda G. Assaraf, Zhe-Sheng Chen, Zhijun Liu, Vinay Kumar
Summary: Antibiotic resistance is a serious threat to human healthcare, with multidrug-resistant strains posing major hurdles. Inappropriate use of antibiotics in various fields leads to evolution and spread of resistance. Plant phytochemicals show potential in combating drug-resistant pathogens.
FRONTIERS IN PHARMACOLOGY
(2021)
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.
Review
Pharmacology & Pharmacy
Suman Panda, Oishika Chatterjee, Laboni Roy, Subhrangsu Chatterjee
Summary: This review discusses the involvement of calcium signaling in cancer progression and multidrug resistance, as well as the possibilities and challenges of targeting calcium channels, transporters, and pumps for cancer treatment through structure-based drug design.
DRUG DISCOVERY TODAY
(2022)
Article
Biochemistry & Molecular Biology
Igor D. D. Zlotnikov, Natalia V. V. Dobryakova, Alexander A. A. Ezhov, Elena V. V. Kudryashova
Summary: A strategy is proposed to enhance the efficacy and selectivity of cytotoxic agents against cancer cells by utilizing the differences in morphology and microenvironment between tumor and healthy cells. The developed enhanced formulations of cytotoxic agents, including efflux inhibitors and ion channel inhibitors, demonstrate increased permeability in A549 cells and a protective effect on healthy HEK293T cells.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Microbiology
Seiji Yamasaki, Naoki Koga, Martijn Zwama, Keisuke Sakurai, Ryosuke Nakashima, Akihito Yamaguchi, Kunihiko Nishino
Summary: This study found that different Trp mutations at different locations in the structure of MexB can affect the inhibitory effect of EPIs, without affecting the function of the efflux pumps.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Article
Oncology
Yingfang Fan, Tian Tao, Zhixing Guo, Kenneth Kin Wah To, Da Chen, Shaocong Wu, Chuan Yang, Jinsui Li, Min Luo, Fang Wang, Liwu Fu
Summary: The study demonstrates that lazertinib effectively reverses MDR by inhibiting drug efflux activities of ABCB1 and ABCG2, leading to increased intracellular accumulation of transporter substrate anticancer drugs. Additionally, lazertinib competitively binds to the ATP-binding site of the transporters and stimulates their ATPase activity, showing potential for overcoming MDR in cancer cells overexpressing ABCB1/ABCG2.
MOLECULAR THERAPY-ONCOLYTICS
(2022)
Article
Chemistry, Medicinal
Sandra Kovachka, Giuliano Malloci, Meline Simsir, Paolo Ruggerone, Stephane Azoulay, Isabelle Mus-Veteau
Summary: This review focuses on the biological evaluation and molecular mechanistic insights of inhibitors of the drug efflux activity of the Hedgehog receptor Patched1 (Ptch1). Ptch1 is known to be over-expressed in many types of cancers and plays a role in the resistance to chemotherapy of cancer cells. Inhibition of Ptch1 has been shown to improve the efficacy of chemotherapy without toxicity for healthy cells or potential side effects.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Food Science & Technology
Natalie Rauber Kleinubing, Tassiana Ramires, Simone de Fatima Rauber Wurfel, Louise Haubert, Leticia Klein Scheik, Frederico Schmitt Kremer, Graciela Volz Lopes, Wladimir Padilha da Silva
Summary: The study found that in the broiler production chain in Southern Brazil, 82.2% of Campylobacter jejuni isolates showed resistance to at least one antimicrobial, with 46.4% being multidrug resistant. Among the resistant isolates, 91.3% had genes encoding multidrug efflux pumps, 81.2% of tetracycline-resistant isolates had the tet(O) gene, and all kanamycin-resistant isolates had the aphA-3 gene. Furthermore, 66.7% of ampicillin-resistant isolates had the bla(oxa-61) gene. This highlights the importance of prudent use of antimicrobial agents in animal production in Brazil to combat antimicrobial resistance.
LWT-FOOD SCIENCE AND TECHNOLOGY
(2021)
Review
Pharmacology & Pharmacy
Luca Andrei, Sandor Kasas, Ignacio Ochoa Garrido, Tijana Stankovic, Monica Suarez Korsnes, Radka Vaclavikova, Yehuda G. Assaraf, Milica Pesic
DRUG RESISTANCE UPDATES
(2020)
Review
Pharmacology & Pharmacy
Silpa Narayanan, Chao-Yun Cai, Yehuda G. Assaraf, Hui-Qin Guo, Qingbin Cui, Liuya Wei, Juan-Juan Huang, Charles R. Ashby, Zhe-Sheng Chen
DRUG RESISTANCE UPDATES
(2020)
Review
Pharmacology & Pharmacy
Linzhi Yan, Min Lin, Shuya Pan, Yehuda G. Assaraf, Zhi-wei Wang, Xueqiong Zhu
DRUG RESISTANCE UPDATES
(2020)
Review
Pharmacology & Pharmacy
Wenxiao Jiang, Jun Xia, Shangdan Xie, Ruanmin Zou, Shuya Pan, Zhi-wei Wang, Yehuda G. Assaraf, Xueqiong Zhu
DRUG RESISTANCE UPDATES
(2020)
Review
Pharmacology & Pharmacy
Elise Lepeltier, Patricia Rijo, Flavio Rizzolio, Rachela Popovtzer, Vilma Petrikaite, Yehuda G. Assaraf, Catherine Passirani
DRUG RESISTANCE UPDATES
(2020)
Review
Pharmacology & Pharmacy
Luyao Long, Yehuda G. Assaraf, Zi-Ning Lei, Hongwei Peng, Lin Yang, Zhe-Sheng Chen, Simei Ren
DRUG RESISTANCE UPDATES
(2020)
Review
Nutrition & Dietetics
Yarden Golan, Yehuda G. Assaraf
Article
Oncology
David G. J. Cucchi, Costa Bachas, Marry M. van den Heuvel-Eibrink, Susan T. C. J. M. Arentsen-Peters, Zinia J. Kwidama, Gerrit J. Schuurhuis, Yehuda G. Assaraf, Valerie de Haas, Gertjan J. L. Kaspers, Jacqueline Cloos
Article
Cell Biology
Michal Stark, Tomas F. D. Silva, Guy Levin, Miguel Machuqueiro, Yehuda G. Assaraf
Article
Rheumatology
Ittai B. Muller, Marry Lin, Willem F. Lems, Marieke M. ter Wee, Anna Wojtuszkiewicz, Michael T. Nurmohamed, Jacqueline Cloos, Yehuda G. Assaraf, Gerrit Jansen, Robert de Jonge
Summary: This study investigated the association between FPGS 8PR levels and lack of responsiveness to MTX treatment in RA patients, finding a correlation between high baseline 8PR/8WT ratios and disease activity scores as well as treatment outcomes.
Article
Oncology
May Levin, Michal Stark, Yishai Ofran, Yehuda G. Assaraf
Summary: The study explored chemoresistance mechanisms in AML patients and found that each patient displayed unique resistance mechanisms following similar treatment protocols. Standardized evaluation of key drug transport and metabolism genes is necessary as an integral component of routine AML management for selecting treatment of choice for individual patients.
CANCER CELL INTERNATIONAL
(2021)
Article
Biochemical Research Methods
Michal Stark, Shachar Raz, Yehuda G. Assaraf
Summary: The study reveals that cytoplasmic FPGS is associated with the cytoskeleton and unconventional myosin-1c, supporting the dynamic channeling of polyglutamylated folates to metabolon compartments. This novel finding enhances folate-dependent de novo biosynthesis of nucleotides and DNA/protein methylation.
JOURNAL OF PROTEOMICS
(2021)
Article
Chemistry, Medicinal
Vinay K. Sharma, Michal Stark, Natalia Fridman, Yehuda G. Assaraf, Zeev Gross
Summary: PC-Im is a theranostic agent with pH-sensitive properties that selectively targets and kills tumor cells through endogenous and exogenous stimuli, ensuring its cytotoxicity occurs upon lysosomal accumulation and light activation.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biology
Michal Stark, May Levin, Igor Ulitsky, Yehuda G. Assaraf
Summary: This study reveals that the localization of cFPGS mRNA and protein at cell protrusions is mediated by two G-quadruplex (GQ) motifs in the 3 ' UTR of FPGS. Upon folate stimulation, the FPGS 3 ' UTR GQ motifs induce an invasive phenotype in cancer cell migration and invasion.