Article
Biochemistry & Molecular Biology
Panagiota Pantiora, Veronika Furlan, Dimitris Matiadis, Barbara Mavroidi, Fereniki Perperopoulou, Anastassios C. Papageorgiou, Marina Sagnou, Urban Bren, Maria Pelecanou, Nikolaos E. Labrou
Summary: This study investigated the inhibitory effects of two curcuminoids and eleven monocarbonyl curcumin analogues against human glutathione transferase P1-1 (hGSTP1-1). The results showed that Demethoxycurcumin (Curcumin II) and three monocarbonyl curcumin analogues exhibited the highest inhibitory activity, with IC50 values ranging between 5.45 and 37.72 μM. The most potent inhibitors functioned as non-competitive/mixed-type inhibitors. Structural analysis revealed that the strongest hGSTP1-1 inhibitor, DM96, formed hydrophobic interactions and hydrogen bonds with specific residues, contributing to its superior inhibitory activity. The study highlights the potential of DM96 as a strong hGSTP1-1 inhibitor and its relevance for cancer chemosensitization.
Article
Chemistry, Multidisciplinary
Miae Won, Seyoung Koo, Hao Li, Jonathan L. Sessler, Jin Yong Lee, Amit Sharma, Jong Seung Kim
Summary: This study introduces a new construct, EA-BPS, which induces a synergistic antitumor effect through a combination of ROS production and GST-π inhibition, leading to enhanced cell-killing effect under hypoxic conditions. By making better use of available oxygen in tumor environments, improved therapeutic PDT outcomes can be achieved even in low oxygen conditions.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Biochemistry & Molecular Biology
Oleksii Kupreienko, Fotini Pouliou, Konstantinos Konstandinidis, Irene Axarli, Eleni Douni, Anastassios C. Papageorgiou, Nikolaos E. Labrou
Summary: Multidrug resistance poses a significant barrier to effective anticancer therapies. This study identified iprodione as a potential lead compound with high inhibitory potency against the isoenzyme GSTP1-1 from Mus musculus. The findings shed light on the inhibition mechanism of MmGSTP1-1 and provide a new compound for future drug development.
Article
Chemistry, Multidisciplinary
Hao Lin, Wenxiu Sun, Tao Zeng, Hengda Li, Chenming Xu, Yan Chen, Wu Yin
Summary: This study identified fosaprepitant as a potential GSTP1 inhibitor using structure-based virtual screening in the FDA database, followed by molecular docking and dynamics simulations. Fosaprepitant showed good binding affinity and potent inhibitory activity against GSTP1, with superior toxicity towards A549/DDP cells and the ability to induce cell apoptosis. These findings provide new insights into specific small molecule inhibitors of GSTP1.
NEW JOURNAL OF CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Stefano Zoroddu, Paola Corona, Luca Sanna, Federica Borghi, Valentina Bordoni, Battistina Asproni, Gerard A. Pinna, Luigi Bagella, Gabriele Murineddu
Summary: A library of novel 1,3,4-oxadiazole bioisosteres was synthesized and evaluated for their cytotoxic activity. Several of the new compounds showed potent anticancer activity, surpassing the previously synthesized oxadiazole compound. The nature of the selenadiazole and thiadiazole rings may play a crucial role in the antitumor activity. These compounds exhibited strong cytotoxic effects in tumor cells compared to human primary cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Analytical
Mengying Chen, Lei Wu, Heng Ye, Ning Liang, Longshan Zhao
Summary: A novel nanocomposite sensor was developed for the detection of glutathione and glutathione S-transferase. ZnCo2O4 sheets were synthesized in a deep eutectic solvent and decorated with Au nanoparticles and bovine serum albumin. The sensor showed excellent oxidase-like activity due to the interaction between BSA-AuNP@ZnCo2O4 and dissolved oxygen, resulting in the oxidation of TMB. The method demonstrated high sensitivity and specificity for the detection of glutathione and glutathione S-transferase.
MICROCHEMICAL JOURNAL
(2022)
Article
Biochemistry & Molecular Biology
Hongfei Xu, Zhen Wang, Yalin Wang, Shaobo Pan, Wenting Zhao, Miao Chen, Xiaofan Chen, Tingting Tao, Liang Ma, Yiming Ni, Weidong Li
Summary: This study provides a comprehensive understanding of the protein and mRNA expression changes in human HF tissues. It highlights the importance of GSTM2 in HF progression and proposes it as a potential therapeutic target for HF.
CELL AND BIOSCIENCE
(2023)
Article
Chemistry, Multidisciplinary
Nabil El Brahmi, Abdelmoula El Abbouchi, Said El Kazzouli
Summary: This article introduces the uses and mechanisms of action of the diuretic drug ethacrynic acid, and discusses its potential application value in anticancer chemotherapy.
RESULTS IN CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Saurabh Kumar, Pooja Rani Mina, Ravi Kumar, Anirban Pal, Ateeque Ahmad, Sudeep Tandon, Mahendra P. Darokar
Summary: 4-Chlorothymol demonstrates potential antiplasmodial activity by increasing ROS and RNS levels, modulating enzyme activity, showing synergy with chloroquine, significantly suppressing parasitemia in vivo, and being safe for further exploration of therapeutic properties.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Environmental Sciences
Katarzyna Orlewska, Justyna Klusek, Stanislaw Gluszek, Jolanta Klusek, Bartosz Witczak, Monika Wawszczak, Lukasz Madej, Michal Tomasz Marzec, Ewa Orlewska
Summary: The relationship between GSTP1 gene polymorphism and HbA1c levels in T2D patients was investigated. The study found that GSTP1 gene polymorphism was associated with higher HbA1c levels, suggesting that it may be a risk factor for elevated HbA1c in T2D patients.
INTERNATIONAL JOURNAL OF ENVIRONMENTAL RESEARCH AND PUBLIC HEALTH
(2023)
Article
Chemistry, Analytical
Xiaobin Zhou, Mengke Wang, Xingguang Su
Summary: A new oxidase-like nanozyme Fe/HCS was prepared, which interacts with dissolved oxygen to generate abundant active oxygen species 1O2, leading to a direct and sensitive colorimetric method for detecting glutathione S-transferase activity.
SENSORS AND ACTUATORS B-CHEMICAL
(2021)
Article
Pharmacology & Pharmacy
Ruchi Vyas, Kavindra Kumar Kesari, Petr Slama, Shubhadeep Roychoudhury, Rashmi Sisodia
Summary: This study measured the differential expression of antioxidant enzymes in response to radiation-induced oxidative stress after administration of C. borivilianum root extract. The results indicate a significant increase in glutathione levels and the activity of glutathione-related antioxidant enzymes in mice treated with CRE and CRE-AgNPs. The activity of catalase and superoxide dismutase was also increased in the CRE-AgNPs pretreated irradiated groups.
FRONTIERS IN PHARMACOLOGY
(2022)
Review
Medicine, General & Internal
Petar Simic, Igor Pljesa, Lazar Nejkovic, Djurdja Jerotic, Vesna Coric, Jelena Stulic, Nenad Kokosar, Dunja Popov, Ana Savic-Radojevic, Vladimir Pazin, Marija Pljesa-Ercegovac
Summary: Chemotherapy resistance in ovarian cancer is a complex process involving multiple mechanisms, such as increased activity of efflux transporters, enhanced DNA repair, and altered apoptotic pathways. GSTP1 is recognized as a major enzyme responsible for converting chemotherapy drugs into less effective forms, while miRNAs can regulate drug resistance by targeting GST-mediated drug metabolism.
MEDICINA-LITHUANIA
(2022)
Article
Biochemistry & Molecular Biology
Sarah A. P. Pereira, A. Catarina L. Baptista, Lorenzo Biancalana, Fabio Marchetti, Paul J. Dyson, M. Lucia M. F. S. Saraiva
Summary: A novel automated method based on sequential injection analysis was developed to evaluate the activity of GST P1-1 in organometallic complexes with potential anticancer activity. The method is simple, robust, reliable, and efficient, requiring only 5 minutes per analysis with fewer reagents used.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Giuseppina Chianese, Annalisa Lopatriello, Carmina Sirignano, Alessandro Andreani, Andrea Gambini, Eric De Combarieu, Mariano Stornaiuolo, Orazio Taglialatela-Scafati
Summary: Two unprecedented cyclopamine analogues, 18-hydroxycyclopamine and 24R-hydroxycyclopamine, with modifications on rings D-F, were isolated from the mother liquors obtained from crystallization of cyclopamine extracted from corn lily. The stereostructures of these new natural compounds were determined through detailed MS and 1D/2D NMR investigation. Their inhibition of the hedgehog pathway was evaluated using the dual-luciferase bioassay, providing new insights into the structure-activity relationships for this class of compounds.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Review
Chemistry, Medicinal
Fansheng Ran, Hualu Xing, Yang Liu, Daoguang Zhang, Pengzhan Li, Guisen Zhao
ARCHIV DER PHARMAZIE
(2015)
Article
Oncology
Jianzhen Liu, Bo Liu, Yongkui Jing, Guisen Zhao
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2016)
Article
Oncology
Guangzhu Guo, Jianzhen Liu, Guanjie Wang, Daoguang Zhang, Jinjie Lu, Guisen Zhao
Article
Chemistry, Medicinal
Yang Liu, Yanzhen Yin, Jingya Zhang, Krystle Nomie, Liang Zhang, Dezhi Yang, Michael L. Wang, Guisen Zhao
ARCHIV DER PHARMAZIE
(2016)
Review
Oncology
Jingya Zhang, Linna Zhang, Yuanyou Wang, Guisen Zhao
CANCER CHEMOTHERAPY AND PHARMACOLOGY
(2016)
Article
Chemistry, Medicinal
Yang Liu, Yanzhen Yin, Zhen Zhang, Carrie J. Li, Hui Zhang, Daoguang Zhang, Changying Jiang, Krystle Nomie, Liang Zhang, Michael L. Wang, Guisen Zhao
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2017)
Review
Chemistry, Medicinal
Zhen Zhang, Daoguang Zhang, Yang Liu, Dezhi Yang, Fansheng Ran, Michael L. Wang, Guisen Zhao
ARCHIV DER PHARMAZIE
(2018)
Article
Biochemistry & Molecular Biology
Daoguang Zhang, Solomon Asnake, Jingya Zhang, Per-Erik Olsson, Guisen Zhao
CHEMICAL BIOLOGY & DRUG DESIGN
(2018)
Article
Biochemistry & Molecular Biology
Daoguang Zhang, Dongdong Tong, Dezhi Yang, Jing Sun, Fenghe Zhang, Guisen Zhao
Article
Chemistry, Medicinal
Fansheng Ran, Yang Liu, Daoguang Zhang, Meixia Liu, Guisen Zhao
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2019)
Review
Chemistry, Multidisciplinary
Kaiwen Guo, Wendi Tang, Huijun Zhuo, Guisen Zhao
Article
Oncology
Xin Chen, Changqing Xu, Yuxia Li, Xiaoming Duan, Guisen Zhao
Summary: A series of 1-methyl-1H-pyrazole-5-carboxamide derivatives were synthesized and compound H24 was found to exhibit significant inhibitory activities against both PSA expression and growth of prostate cancer cell lines, suggesting its potential as a therapeutic agent for prostate cancer treatment.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Medicinal
Fansheng Ran, Yun Liu, Chen Wang, Zhongyuan Xu, Yanan Zhang, Yang Liu, Guisen Zhao, Yong Ling
Summary: Bruton's tyrosine kinase (BTK) plays a crucial role in the treatment of hematologic malignancies, but current therapies have limitations. Therefore, researchers are exploring new treatment strategies, such as next-generation BTK inhibitors, BTK-PROTACs, and combination therapies.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Fansheng Ran, Yang Liu, Guisen Zhao
Summary: The development of Bruton's tyrosine kinase (BTK) inhibitors holds great value and significance in the treatment of B-cell malignancies and autoimmune diseases. In this study, a novel class of pyrazolopyrimidine-based BTK inhibitors were designed and evaluated in mantle cell lymphoma (MCL) cell lines. The target compounds showed improved antiproliferative activity compared to the lead compound, and specific compound 13l demonstrated effective antiproliferative activity in MCL cells lines. Furthermore, compound 13l induced cell apoptosis through the caspase 3-mediated apoptotic pathway in Z138 cells.
MEDICINAL CHEMISTRY RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Dezhi Yang, Dongdong Tong, Qian Zhang, Yongtao Wang, Jing Sun, Fenghe Zhang, Guisen Zhao
CHEMICAL BIOLOGY & DRUG DESIGN
(2017)