Article
Chemistry, Inorganic & Nuclear
Zoufeng Xu, Long Lin, Binbin Fu, Fu-Ping Huang, Qiyuan Zhou, Guangyu Zhu, Zhigang Wang
Summary: The application of new synthetic methods in platinum(iv) anticancer prodrugs increases the availability of accessible entities that can be conjugated to the platinum(iv) center. These new axial ligands not only endow platinum(iv) complexes with unique properties but also inspire new concepts in prodrug design and development.
INORGANIC CHEMISTRY FRONTIERS
(2023)
Article
Chemistry, Inorganic & Nuclear
Elisabetta Gabano, Marzia Bruna Gariboldi, Giulia Caron, Giuseppe Ermondi, Emanuela Marras, Maura Vallaro, Mauro Ravera
Summary: Octahedral Pt(IV) prodrugs, which combine cisplatin-like moieties and a second drug, are effective in treating glioblastoma. In this study, three Pt(IV) derivatives were synthesized by linking rhein and acetato ligand to a cisplatin core, and they showed higher potency and better blood-brain barrier penetration than the parent drugs. These compounds inhibited tumor progression and reduced cell motility, potentially through the inhibition of MMP2 and MMP9 matrix metalloproteinases.
DALTON TRANSACTIONS
(2022)
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
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)
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
Biochemistry & Molecular Biology
Jorge Leal, Lucia Santos, Diego M. Fernandez-Aroca, J. Vicente Cuevas, M. Angeles Martinez, Anna Massaguer, Felix A. Jalon, M. Jose Ruiz-Hidalgo, Ricardo Sanchez-Prieto, Ana M. Rodriguez, Gregorio Castaneda, Gema Dura, M. Carmen Carrion, Silvia Barrabes, Blanca R. Manzano
Summary: The study synthesized a series of chloride Pt(II) and Pt(IV) compounds, and investigated their cytotoxic properties against different cell lines, revealing a clear relationship between the type of ligand and anti-proliferative properties, demonstrating a positive effect of the NH2 group on activity, and confirming DNA as a target leading to cell death by apoptosis.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2021)
Review
Chemistry, Multidisciplinary
Jingjing Huang, Weize Ding, Xingfan Zhu, Bingbing Li, Fangang Zeng, Kui Wu, Xiaoqin Wu, Fuyi Wang
Summary: This article reviews the development of photoactivatable Pt(IV) anticancer prodrugs, focusing on the coordinated ligands and their effects on the photochemistry and photoactivity of the drugs. These drugs offer higher spatial and temporal controllability and improved safety compared to traditional chemotherapy.
FRONTIERS IN CHEMISTRY
(2022)
Article
Multidisciplinary Sciences
Rita de Cassia Lemos Lima, Ulrike Bocker, Gordon J. McDougall, J. William Allwood, Nils Kristian Afseth, Sileshi Gizachew Wubshet
Summary: A new magnetic ligand fishing probe was developed for discovering DPP-IV inhibitory ligands and tested on lingonberry fruit extract, showing appreciable inhibitory activity. DPP-IV was successfully immobilized on magnetic beads and showed selectivity over a model mixture. Four ligands were successfully fished out and identified using HPLC/HRMS.
Article
Engineering, Biomedical
Kun Shang, Lingpu Zhang, Yingjie Yu, Haihua Xiao, Yajuan Gao, Liu Yang, Jia Huang, Haiqin Song, Hongbin Han
Summary: The study designed composite nanoparticles that encapsulate USP1 inhibitor and platinum (IV) prodrug using a glutathione-sensitive amphiphilic polymer. These nanoparticles can target USP1 to inhibit DNA damage repair, increase the sensitivity of tumor cells to cisplatin, and enhance the anti-cancer efficacy of cisplatin.
MATERIALS TODAY BIO
(2023)
Article
Chemistry, Inorganic & Nuclear
Hamid R. Shahsavari, Samira Chamyani, Jiyun Hu, Reza Babadi Aghakhanpour, Arnold L. Rheingold, Sareh Paziresh, Dania Rahal, Miu Tsuji, Bilal Momand, Hudson Beyzavi
Summary: A series of heteroleptic cycloplatinated(II) complexes with greenish-blue phosphorescence in their solid states were synthesized and characterized, with emissions mainly originating from electronic transitions in the dfppy ligand. The emission strengths were significantly affected by the electron density of the phosphine ligands. Density functional theory (DFT) and time-dependent DFT (TD-DFT) calculations were used to rationalize the experimental photophysical data for these complexes.
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
(2021)
Article
Oncology
Xiaoman Mao, Shuang Wu, Pilar Calero-Perez, Ana P. Candiota, Paula Alfonso, Jordi Bruna, Victor J. Yuste, Julia Lorenzo, Fernando Novio, Daniel Ruiz-Molina
Summary: This study reports a new approach for the treatment of glioblastoma, a highly malignant brain tumor, by using a catechol-functionalized Pt(IV) prodrug and intranasal administration. The results show promising therapeutic effects and open up new opportunities in brain tumor treatment.
Article
Chemistry, Medicinal
Bo Fang, Xue Chen, Xingui Zhou, Xindan Hu, Yan Luo, Zhigang Xu, Cheng-He Zhou, Jiang-Ping Meng, Zhong-Zhu Chen, Chunsheng Hu
Summary: This study presents platinum(IV) compounds with multiple-bond ligands, which exhibited superior activity against tumor cells, proliferation, and metastasis compared to cisplatin. Compounds 2 and 5 with meta-substituted groups showed excellent performance. Research further demonstrated that compounds 2 and 5 had appropriate reduction potential and outperformed cisplatin in cellular uptake, reactive oxygen species response, apoptosis regulation, DNA damage-related gene up-regulation, and drug-resistant cell activity. The title compounds displayed better antitumor potential and fewer side effects in vivo compared to cisplatin. Introduction of multiple-bond ligands improved absorption, overcame drug resistance, and exhibited potential for mitochondrial targeting and inhibition of tumor cell detoxification.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Fantao Meng, Benzhi Ju, Zhenzhi Wang, Ronghui Han, Yuang Zhang, Shufen Zhang, Ping Wu, Bingtao Tang
Summary: We present a new synthetic strategy that combines N-carboxyanhydride (NCA) chemistry and photonic crystals for the fabrication of polypeptide structural color films. Through surface-initiated ring-opening polymerization, a di-NCA derivative of L-cystine (Cys) is utilized to replicate functionalized colloidal crystal templates and create freestanding P(Cys) films with adjustable structural color. The feasibility of producing patterned polypeptide photonic films is demonstrated through template microfabrication. The introduction of L-glutamate (Glu) components enables the P(Cys-co-Glu) copolypeptide films to exhibit visual color responsiveness to pH changes. Additionally, the polypeptide photonic films possess on-demand degradability.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Chemistry, Medicinal
Xinguang Cao, Rui Li, Huihua Xiong, Jinfang Su, Changqing Guo, Tianqi An, Hong Zong, Ruihua Zhao
Summary: Among the four Pt(IV) complexes, complex 14 shows promising potential in reversing cisplatin resistance and enhancing anticancer efficiency through multiple mechanisms. Its low systematic toxicity makes it a potential novel P-gp-mediated MDR modulator with increased tumor inhibition compared to cisplatin and oxaliplatin.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Inorganic & Nuclear
Bin-Bin Pan, Hui-Zhong Liu, Wei-Han Meng, Xun-Cheng Su
Summary: This study investigated the interaction between a platinum(iv) complex and alpha-synuclein (α-S) using high-resolution NMR spectroscopy and mass spectrometry. The results showed that the Pt(iv) complex was able to oxidize specific methionine residues in α-S under physiological conditions. These findings are important for understanding the oxidative modification of α-S.
INORGANIC CHEMISTRY FRONTIERS
(2022)
Article
Chemistry, Multidisciplinary
N. Kolevzon, D. Hashoul, S. Naik, A. Rubinstein, E. Yavin
CHEMICAL COMMUNICATIONS
(2016)
Article
Chemistry, Multidisciplinary
Meital B. D. Bloch, Eylon Yavin, Aviram Nissan, Ilana Ariel, Ron Kenett, Dovrat Brass, Abraham Rubinstein
JOURNAL OF CONTROLLED RELEASE
(2017)
Article
Chemistry, Multidisciplinary
Orit Amsalem, Taher Nassar, Sandrine Benhamron, Philip Lazarovici, Simon Benita, Eylon Yavin
JOURNAL OF CONTROLLED RELEASE
(2017)
Article
Biochemistry & Molecular Biology
Ofrah Faust, Dana Grunhaus, Odelia Shimshon, Eylon Yavin, Assaf Friedler
Article
Biochemistry & Molecular Biology
Galia Tiram, Shiran Ferber, Paula Ofek, Anat Eldar-Boock, Dikla Ben-Shushan, Eilam Yeini, Adva Krivitsky, Roni Blatt, Nava Almog, Jack Henkin, Orit Amsalem, Eylon Yavin, Gadi Cohen, Philip Lazarovici, Joo Sang Lee, Eytan Ruppin, Michael Milyavsky, Rachel Grossman, Zvi Ram, Marcelo Calderon, Rainer Haag, Ronit Satchi-Fainaro
Article
Biochemistry & Molecular Biology
Maxim Mogilevsky, Odelia Shimshon, Saran Kumar, Adi Mogilevsky, Eli Keshet, Eylon Yavin, Florian Heyd, Rotem Karni
NUCLEIC ACIDS RESEARCH
(2018)
Article
Oncology
Vadim V. Maximov, Rania Akkawi, Saleh Khawaled, Zaidoun Salah, Lina Jaber, Ahlam Barhoum, Omer Or, Marco Galasso, Kyle C. Kurek, Eylon Yavin, Rami Aqeilan
INTERNATIONAL JOURNAL OF CANCER
(2019)
Article
Biophysics
Dina Hashoul, Rachel Shapira, Maria Falchenko, Odelia Tepper, Vera Paviov, Aviram Nissan, Eylon Yavin
BIOSENSORS & BIOELECTRONICS
(2019)
Article
Multidisciplinary Sciences
Polina Denichenko, Maxim Mogilevsky, Antoine Clery, Thomas Welte, Jakob Biran, Odelia Shimshon, Georgina D. Barnabas, Miri Danan-Gotthold, Saran Kumar, Eylon Yavin, Erez Y. Levanon, Frederic H. Allain, Tamar Geiger, Gil Levkowitz, Rotem Karni
NATURE COMMUNICATIONS
(2019)
Article
Chemistry, Multidisciplinary
Terese Soudah, Saleh Khawaled, Rami Aqeilan, Eylon Yavin
Editorial Material
Biochemistry & Molecular Biology
Eylon Yavin
Article
Chemistry, Multidisciplinary
Odelia Tepper, Itamar Peled, Yair Fastman, Adina Heinberg, Vera Mitesser, Ron Dzikowski, Eylon Yavin
Summary: In this study, FIT-PNAs were used as molecular probes to detect SNPs associated with artemisinin and chloroquine drug resistances in Plasmodium falciparum. The results showed that FIT-PNAs could effectively discriminate between wild-type and mutant strains of the parasite. FIT-PNAs were able to penetrate infected red blood cells and the difference in fluorescence signals could be detected using FACS analysis and confocal microscopy.
Article
Chemistry, Multidisciplinary
Odelia Tepper, Hongchao Zheng, Daniel H. Appella, Eylon Yavin
Summary: The cpFIT-PNA probes are highly emissive RNA sensors with improved mismatch discrimination compared to FIT-PNAs.
CHEMICAL COMMUNICATIONS
(2021)
Article
Chemistry, Multidisciplinary
Itamar Peled, Eylon Yavin
Article
Biochemical Research Methods
Terese Soudah, Maxim Mogilevsky, Rotem Karni, Eylon Yavin
BIOCONJUGATE CHEMISTRY
(2017)