Article
Pharmacology & Pharmacy
Yanjuan Huang, Xiuling Dai, Zilin Guan, Di Liu, Lingling Ren, Meixu Chen, Zishan Zeng, Jingwen Jiang, Yong Luo, Yuanfeng He, Min Huang, Chunshun Zhao
Summary: A tailored DNA damage nanoamplifier was developed to induce DNA damage and inhibit DNA repair for efficient triple-negative breast cancer (TNBC) treatment.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Review
Chemistry, Multidisciplinary
Shunzhe Zheng, Guanting Li, Jianbin Shi, Xinying Liu, Meng Li, Zhonggui He, Chutong Tian, Ken-ichiro Kamei
Summary: Due to the severe dose-dependent toxicity and drug resistance, platinum (Pt)-based chemotherapy has limitations. Pt(IV) prodrug nanotherapeutics have emerged as a promising approach to improve the antitumor performance of Pt drugs. This article summarizes the latest advances in Pt(IV) prodrug nano-therapeutics, including their potential for overcoming biological barriers and their synergistic effects with other therapies.
JOURNAL OF CONTROLLED RELEASE
(2023)
Article
Oncology
Nair Hariprasad Haritha, Akbar Nawab, Vinod Vijayakurup, Nikhil Ponnoor Anto, Vijayasteltar B. Liju, Vijai V. Alex, Areekkara Nisthul Amrutha, Sreekumar U. Aiswarya, Mundanattu Swetha, Balachandran S. Vinod, Sankar Sundaram, Maria Guijarro, Thomas Herlevich, Archana Krishna, Nesteena K. Nestory, Smitha Bava, Chittalakkottu Sadasivan, Maria Zajac-Kaye, Ruby John Anto
Summary: A study found that curcumin enhances the sensitivity of breast cancer cells to 5-fluorouracil chemotherapy, particularly in triple-negative breast cancer, providing a new strategy for the treatment of breast cancer.
FRONTIERS IN ONCOLOGY
(2021)
Review
Chemistry, Inorganic & Nuclear
Zoufeng Xu, Zhigang Wang, Zhiqin Deng, Guangyu Zhu
Summary: Platinum-based anticancer drugs have been widely used in clinical practice for over 40 years, with a focus on developing platinum(IV) prodrugs based on traditional platinum(II) anticancer drugs. Recent progress in the field includes synthesizing platinum(IV) prodrugs with new oxidizing reagents, understanding the hydrolysis and stability of platinum(IV) complexes, and exploring reduction processes to achieve controllable intracellular reduction of platinum(IV) prodrugs. This review aims to enhance researchers' understanding of platinum(IV) anticancer prodrugs and inspire new strategies, ideas, and applications in metal-based drugs.
COORDINATION CHEMISTRY REVIEWS
(2021)
Article
Oncology
Kurt W. Evans, Erkan Yuca, Stephen S. Scott, Ming Zhao, Natalia Paez Arango, Christian X. Cruz Pico, Turcin Saridogan, Maryam Shariati, Caleb A. Class, Christopher A. Bristow, Christopher P. Vellano, Xiaofeng Zheng, Ana Maria Gonzalez-Angulo, Xiaoping Su, Coya Tapia, Ken Chen, Argun Akcakanat, Bora Lim, Debu Tripathy, Timothy A. Yap, Maria Emilia Di Francesco, Giulio F. Draetta, Philip Jones, Timothy P. Heffernan, Joseph R. Marszalek, Funda Meric-Bernstam
Summary: Oxidative phosphorylation is a metabolic vulnerability in triple-negative breast cancer, and inhibiting it with IACS-10759 may enhance efficacy of multiple targeted therapies.
Article
Oncology
E. C. de Heer, C. E. Zois, E. Bridges, B. van der Vegt, H. Sheldon, W. A. Veldman, M. C. Zwager, T. van der Sluis, S. Haider, T. Morita, O. Baba, C. P. Schroder, S. de Jong, A. L. Harris, M. Jalving
Summary: The study found that the gene GYS1 is related to tumor growth and therapy resistance in breast cancer, especially in triple-negative breast cancer. Inhibiting GYS1 weakens the proliferation ability of breast cancer cells and makes them more sensitive to inhibition of mitochondrial proteostasis.
JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH
(2023)
Article
Chemistry, Inorganic & Nuclear
Ran Zhang, Yueyue Zhang, Liumei Tang, Yixing Xu, Hao Li, Xueping Jiang, Xiangdong Xin, Zhongzheng Gui
Summary: A series of Pt(IV) prodrugs containing a microtubule inhibitor paclitaxel were synthesized and evaluated for their antitumor activity. One of the prodrugs, named Ptxplatin, effectively entered cancer cells and induced DNA damage, cell cycle arrest, and inhibition of cell migration. Furthermore, Ptxplatin caused mitochondrial dysfunction and triggered endoplasmic reticulum stress, ultimately leading to cancer cell death.
INORGANIC CHEMISTRY FRONTIERS
(2022)
Article
Multidisciplinary Sciences
L. E. Anselmino, M. Baglioni, F. Malizia, N. Cesatti Laluce, C. Borini Etichetti, V. L. Martinez Marignac, V Rozados, O. G. Scharovsky, J. Girardini, M. J. Rico, M. Menacho Marquez
Summary: Drug repositioning accelerates drug development process, finding effective drugs with reduced side effects and lower costs. Combining metformin and propranolol shows potential as adjuvant therapy for both CRC and TNBC, as well as effective alternative for chemo-resistant CRC.
SCIENTIFIC REPORTS
(2021)
Article
Chemistry, Multidisciplinary
Alessandra Barbanente, Valentina Gandin, Chiara Donati, Carmela Ilaria Pierro, Giovanni Natile, Nicola Margiotta
Summary: Platinum-based drugs have been successful in treating solid tumors, but toxicity and resistance limit their outcomes. Natural products, such as 10-HDA found in royal jelly, are being explored as safe and easily available anti-cancer drugs. In this study, the researchers aimed to combine the functionality of 10-HDA with platinum to develop new compounds with potential anti-cancer activity. The synthesized compounds were characterized and tested for their cytotoxicity against human tumor cell lines. The results showed that some of the new compounds exhibited promising activity against specific tumor cell lines.
NEW JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Gang Dong, Yu-heng Li, Jing-si Guo, Qi-qi Lin, Mei-yan Deng, Wen-han Xue, Xin-yan Li, Fan-hao Meng
Summary: Based on previous work, this study focused on the further search for more effective and less damaging inhibitors of thymidylate synthase (TS). A series of (E)-N-(2-benzyl hydrazine-1-carbonyl) phenyl-2,4-deoxy-1,2,3,4-tetrahydro pyrimidine-5-sulfonamide derivatives were synthesized and reported for the first time after structural optimization. The compound DG1 showed potential as a TS inhibitor for treating NSCLC angiogenesis, as it exhibited direct binding to TS proteins, promoted apoptosis in cancer cells, and inhibited cancer tissue proliferation and angiogenesis.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Qiyuan Zhou, Shu Chen, Zoufeng Xu, Gongyuan Liu, Shuyuan Zhang, Zhigang Wang, Man-Kit Tse, Shek-Man Yiu, Guangyu Zhu
Summary: This study reports the synthesis of Pt-IV complexes bearing axial pyridines through ligand exchange reactions. It was discovered that these axial pyridines can be quickly released after reduction, indicating their potential as axial leaving groups. Two multitargeted Pt-IV prodrugs containing bioactive pyridinyl ligands, a PARP inhibitor and an EGFR tyrosine kinase inhibitor, were successfully obtained using this method. These conjugates show great potential for overcoming drug resistance, with the latter inhibiting the growth of Pt-resistant tumor in vivo. This research expands the synthetic methods for Pt-IV prodrugs and increases the range of bioactive axial ligands that can be conjugated to a Pt-IV center.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Inorganic & Nuclear
Sophia Harringer, Michaela Hejl, Eva A. Enyedy, Michael A. Jakupec, Mathea S. Galanski, Bernhard K. Keppler, Paul J. Dyson, Hristo P. Varbanov
Summary: The study revealed that platinum(iv)-DFO prodrugs exhibit moderate in vitro cytotoxicity with slow activation kinetics across various cancer cell models, showing less pronounced differences between chemoresistant and chemosensitive cell lines as well as between 2D and 3D models compared to clinically used platinum(ii) drug carboplatin.
DALTON TRANSACTIONS
(2021)
Article
Chemistry, Multidisciplinary
Javier E. Lopez-Hernandez, Nazia Nayeem, Jose P. Ceron-Carrasco, Afruja Ahad, Aiman Hafeez, Ignacio E. Leon, Maria Contel
Summary: This study describes new heterometallic binuclear and trinuclear platinum(IV)-gold(I) compounds that exhibit cytotoxicity and selectivity against a small panel of cancer cell lines. One trinuclear compound accumulates in the nucleus and mitochondria, induces apoptosis, and shows antimigratory and antiangiogenic properties against triple-negative breast cancer (TNBC) cell lines, as well as potent cytotoxic effect against TNBC 3D spheroids.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Chemistry, Inorganic & Nuclear
Violet Eng Yee Lee, Zhi Chiaw Lim, Suet Li Chew, Wee Han Ang
Summary: A common challenge in Pt(IV) prodrug design is the limited repertoire of linkers available to connect the Pt(IV) scaffold with the bioactive payload. This study introduces a new class of Pt(IV) prodrugs using masked self-immolative 4-aminobenzyl linkers for controlled and traceless codrug delivery, which proved to be more effective than traditional methods in vitro.
INORGANIC CHEMISTRY
(2021)
Article
Engineering, Biomedical
Xiaohui Xiao, Yupeng Wang, Jieyao Chen, Peng Qin, Peiyao Chen, Dongfang Zhou, Yue Pan
Summary: This study presents a self-targeting nano-assembly strategy based on platinum(IV)-lactose amphiphilic prodrug for synergistic and safe chemoradiotherapy of hepatocellular carcinoma (HCC). The nano-assembly targets HCC cells and releases cisplatin to induce DNA damage and cell apoptosis. Under X-ray irradiation, the assembly enhances the cell-killing effect of radiotherapy.
Review
Chemistry, Multidisciplinary
Zhi-Yuan Li, Qing-Hua Shen, Zong-Wan Mao, Cai-Ping Tan
Summary: This review introduces the potential of metal complexes in cancer immunotherapy and summarizes recent discoveries on the immune effects of platinum-based compounds. It also outlines the latest research on metal complexes for cancer immunotherapy, focusing on platinum, ruthenium, iridium, rhenium, and copper complexes. Finally, it discusses research perspectives and unresolved problems in the application of metallo-anticancer agents in cancer immunotherapy.
CHEMISTRY-AN ASIAN JOURNAL
(2022)
Article
Chemistry, Multidisciplinary
Shaokang Jia, Wenjin Wang, Shanshan Qin, Shengjie Xie, Lisi Zhan, Qi Wei, Ziang Lu, Xiaolu Zhou, Cong Chen, Kun Chen, Shen Yan, Caiping Tan, Zongwan Mao, Xiang Zhou
Summary: A phosphorescent probe Ir-PDP containing an Ir(III) complex was designed and synthesized to evaluate the level of G4 in the cytoplasm. Compared with other nucleic acid secondary structures, Ir-PDP exhibited a higher phosphorescence lifetime after interacting with G4. Two-photon phosphorescence lifetime imaging was used to detect the binding events of the probe in the cytoplasm. The addition of G4 binder PDS significantly regulated cytoplasmic phosphorescence lifetime. This project explored a new sensing pathway to observe the binding manners of probes in the cytoplasm through the phosphorescence lifetime of probes.
CHINESE CHEMICAL LETTERS
(2023)
Article
Chemistry, Multidisciplinary
Liu-Yi Liu, Tian-Zhu Ma, You-Liang Zeng, Wenting Liu, Zong-Wan Mao
Summary: This study reveals the structural basis for the specific recognition of G-quadruplex (G4) by pyridostatin (PDS) and its derivatives. The results demonstrate that the rigid aromatic rings of PDS linked by flexible amide bonds match adaptively with G-tetrad planes, enhancing p-p stacking and achieving specific recognition of G4s. The aliphatic amine side chains of PDS adjust conformation to interact with the phosphate backbone via hydrogen bonding and electrostatic interactions, increasing affinity for G4s.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Chemistry, Multidisciplinary
Yu-Yi Ling, Xiao-Yu Xia, Liang Hao, Wen-Jin Wang, Hang Zhang, Liu-Yi Liu, Wenting Liu, Zhi-Yuan Li, Cai-Ping Tan, Zong-Wan Mao
Summary: This study presents two Pt-II complexes as photoactivators of the cGAS-STING pathway, which can activate the pathway and induce pyroptosis under light irradiation, leading to intense anticancer immune responses.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Article
Computer Science, Information Systems
Mingxin Gan, Caiping Tan
Summary: In this study, we proposed a model called MGCAN to incorporate various influential factors into different sequential patterns for next point-of-interest (POI) recommendation. Experimental results showed that the MGCAN model achieved better recommendation performance than benchmark models.
WORLD WIDE WEB-INTERNET AND WEB INFORMATION SYSTEMS
(2023)
Article
Chemistry, Multidisciplinary
Xuxian Su, Bin Liu, Wen-Jin Wang, Kun Peng, Bing-Bing Liang, Yue Zheng, Qian Cao, Zong-Wan Mao
Summary: This study developed a novel cyclometalated Pt-IV-terthiophene complex, Pt3, that disrupts zinc homeostasis and induces cell apoptosis, thereby activating anti-tumor immunity and eliminating tumors.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Multidisciplinary
Wenkai Lin, Yu Liu, Jinhui Wang, Zhennan Zhao, Kai Lu, He Meng, Ruiqi Luoliu, Xiaojun He, Jianliang Shen, Zong-Wan Mao, Wei Xia
Summary: Ir-HEcN is a metal complex decorated bacteria that targets tumor tissues and induces pyroptosis and immunogenic cell death of tumor cells under irradiation. It evokes anti-tumor immune responses and leads to the regression of solid tumors via enhanced photodynamic immunotherapy.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Multidisciplinary
Liu-Yi Liu, Tian-Zhu Ma, You-Liang Zeng, Wenting Liu, Hang Zhang, Zong-Wan Mao
Summary: A novel class of G4-binding organic-platinum hybrids, L-1-cispt and L-1-transpt, were designed with spatial matching for G4 binding and G4 DNA reactivity for binding site locking. The study revealed that L-1-cispt and L-1-transpt mediated genomic dysfunction could activate the RIG-I pathway and induce immunogenic cell death. In vivo experiments demonstrated that using L-1-cispt/L-1-transpt-treated cells as therapeutic vaccines stimulated a robust immune response and effectively inhibited tumor growth. These findings highlight the importance of rational combination of spatial recognition and covalent locking in G4-targeting drug design and their potential in immunotherapy.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Engineering, Environmental
Jia-Ying Zhou, Qing-Hua Shen, Xiao-Jing Hong, Wu-Ya Zhang, Qiao Su, Wu-Guo Li, Bin Cheng, Cai-Ping Tan, Tong Wu
Summary: This study demonstrates the potential of photodynamic therapy (PDT) in oral squamous cell carcinoma (OSCC) by designing two iridium(III) photosensitizers that target the endoplasmic reticulum (ER). The Ir1-mediated PDT treatment adaptively upregulates the expression of programmed death-ligand 1 (PD-L1) and stimulates dendritic cell maturation and T lymphocyte infiltration. It also synergizes with a PD-L1 inhibitor to transform an immune-suppressive cold tumor into an immune-responsive hot tumor.
CHEMICAL ENGINEERING JOURNAL
(2023)
Article
Chemistry, Medicinal
Zhennan Zhao, Xinyu Wang, Jinhui Wang, Yiyi Li, Wenkai Lin, Kai Lu, Jun Chen, Wei Xia, Zong-Wan Mao
Summary: In this study, a nanobody-catalyst conjugate Ru-PD-L1 was developed by fusing a ruthenium catalyst to an anti-PD-L1 nanobody. Ru-PD-L1 disrupts the PD-L1/PD-1 interaction and catalyzes the release of the DOX prodrug, leading to reduced toxicity and immunogenic cell death. The combination of chemo-immunotherapy significantly increases tumor-infiltrating T-cells and exhibits high antitumor activity in murine models.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Yue Zheng, Xiao-Xiao Chen, Dong-Yang Zhang, Wen-Jin Wang, Kun Peng, Zhi-Yuan Li, Zong-Wan Mao, Cai-Ping Tan
Summary: We report a highly emissive rhodium(III) complex (Rh-Mito) as the mtDNA intercalator that specifically binds to mtDNA, causing cytoplasmic release of mtDNA fragments to activate the cGAS-STING pathway. Rh-Mito also activates mitochondrial retrograde signaling and alters nuclear genome methylation landscape to influence genes related to immune signaling pathways. Furthermore, ferritin-encapsulated Rh-Mito elicits potent anticancer activities and immune responses in vivo. This study provides insights into the development of biomacromolecule-targeted immunotherapeutic agents.
Article
Chemistry, Inorganic & Nuclear
Yu-Yi Ling, Ya-Jie Kong, Liang Hao, Zheng-Yin Pan, Zong-Wan Mao, Cai-Ping Tan
Summary: In this study, three Ir(iii) photosensitizers (Ir1-Ir3) targeting carbonic anhydrase IX (CAIX) were designed, and they exhibited potent antiproliferative activities in colon cancer cells upon irradiation with visible light (425 nm). The most active complex Ir3 can photodegrade CAIX under hypoxia, downregulating the expression of HIF-1a and VEGF to improve cancer immune microenvironments. Furthermore, Ir3 can induce pyroptosis of cancer cells through lipid peroxidation, causing immunogenic cell death (ICD) under hypoxia.
INORGANIC CHEMISTRY FRONTIERS
(2023)
Review
Chemistry, Multidisciplinary
Kun Peng, Yue Zheng, Wei Xia, Zong-Wan Mao
Summary: The article discusses the important role of metal complexes in human cancer therapy and the problems of targeting and drug resistance. It focuses on the development and action mechanisms of anti-tumor organometallics, targeting tumor intracellular processes and disrupting tumor energy/redox/metal/immune homeostasis. The article also reviews the nine cell death pathways induced by organometallics and their morphological and biochemical features.
CHEMICAL SOCIETY REVIEWS
(2023)
Article
Chemistry, Multidisciplinary
Lu-Si Rao, Liang Hao, Liu-Yi Liu, You-Liang Zeng, Bing-Bing Liang, Wenting Liu, Zong-Wan Mao
Summary: A TTPP probe has been developed for distinguishing G-quadruplexes (G4s) from other nucleic acid topologies, allowing visualization of cytoplasmic G4s in live cells using fluorescence lifetime imaging microscopy. It also shows potential for detecting cell apoptosis and ferroptosis by tracking cytoplasmic G4s.
CHEMICAL COMMUNICATIONS
(2023)
Article
Chemistry, Multidisciplinary
Liang Hao, Jie Wang, Zheng-Yin Pan, Zong-Wan Mao, Cai-Ping Tan
Summary: In this study, a CAIX targeting and binding-enhanced ruthenium-based photodegrader was constructed, which effectively inhibited the catalytic activity of CAIX. This research provides a new approach for the development of tools for protein functional studies.
CHEMICAL COMMUNICATIONS
(2022)