Article
Chemistry, Multidisciplinary
Xuan Liang, Shan Qian, Zhizheng Lou, Renming Hu, Yuchen Hou, Peng R. Chen, Xinyuan Fan
Summary: The development of a biocompatible photocatalytic technology termed CAT-NIR enables the spatiotemporal manipulation of biological processes in living animals using external near infrared light (NIR). This system utilizes Os(II) terpyridine complex as an efficient NIR photocatalyst for deboronative hydroxylation reactions, resulting in the release of bioactive molecules. CAT-NIR also allows for the regulation of affibody binding to cell surface receptors through genetic code expansion and computer-aided screening, providing a selective cell tagging technology with external NIR light.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Multidisciplinary
Mengyang Chang, Feng Gao, Devin Pontigon, Giri Gnawali, Hang Xu, Wei Wang
Summary: A bioorthogonal on-demand prodrug strategy was developed to selectively activate and release PROTACs in cancer cells. The strategy utilizes a Tetrazine-modified RGD peptide as an activation component for targeted degradation of proteins of interest (POIs) in cancer cells. The results demonstrate selective activation of the PROTACs in an integrin alpha(v)beta(3)-dependent manner for protein degradation in cancer cells.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2023)
Article
Chemistry, Physical
Valerio Sabatino, V. B. Unnikrishnan, Goncalo J. L. Bernardes
Summary: Bioorthogonal chemistry provides powerful tools for studying and manipulating biological systems without interfering with biological processes. The possibility of using bioorthogonal tools for prodrug activation is a promising area of research, which is currently progressing towards clinical trials. Metal-mediated bioorthogonal cleavage reactions have limitations in biological media, but they have been engineered for applications such as the release of small molecules.
Article
Chemistry, Inorganic & Nuclear
Olga Krasnovskaya, Daniil Spector, Alexander Erofeev, Peter Gorelkin, Roman Akasov, Dmitry Skvortsov, Alexander Trigub, Ksenia Vlasova, Alevtina Semkina, Nikolay Zyk, Elena Beloglazkina, Alexander Majouga
Summary: Researchers reported two multispecific Pt-IV complexes, DNP and NP, with the non-steroidal anti-inflammatory drug naproxen (NPX) as the axial ligand(s). The study clarified the mechanism of action of DNP, its therapeutic target, and intracellular redox-status.
DALTON TRANSACTIONS
(2021)
Article
Biochemistry & Molecular Biology
Patrick Keppel, Barbara Sohr, Walter Kuba, Marion Goldeck, Philipp Skrinjar, Jonathan C. T. Carlson, Hannes Mikula
Summary: Bond-cleavage reactions triggered by bioorthogonal tetrazine ligation have been used to chemically control the function of (bio)molecules and activate prodrugs. However, current methods for releasing phenols are limited. To address this issue, we developed a self-immolative linker that connects cleavable amines and phenols, allowing for controlled release of prodrugs.
Article
Chemistry, Organic
Yayue Wang, Guohua Shen, Jie Li, Wuyu Mao, Hongbao Sun, Ping Feng, Haoxing Wu
Summary: This study reports the bioorthogonal cleavage of methylene tetrazines with ether or ester linkages in the presence of trans-cyclooctene. This approach allows for the controlled release of molecules with phenol or carboxylic acid moieties and has potential applications in various biomedical fields.
Article
Chemistry, Multidisciplinary
Ha Rin Kim, Young Seok Cho, Seung Woo Chung, Jeong Uk Choi, Yoon Gun Ko, Seong Jin Park, Sang Yoon Kim, Youngro Byun
Summary: This article describes a tumoral caspase-3 mediated peptide-doxorubicin conjugates (PDC) switch therapy for targeting metastatic triple-negative breast cancer. The therapy utilizes two different caspase-3 cleavable PDCs to induce apoptosis in tumor cells and target tumor sites, resulting in enhanced tumor-specific apoptosis amplification and potent therapeutic efficacy.
JOURNAL OF CONTROLLED RELEASE
(2022)
Article
Materials Science, Multidisciplinary
Yoshinori Arisaka, Nobuhiko Yui
Summary: In this study, photo-crosslinkable polyrotaxanes (PRXs) via riboflavins were synthesized for anchoring to biological tissues. These PRXs could form hydrogels in the presence of RBFs and showed excellent biocompatibility and adhesion properties.
Review
Biochemistry & Molecular Biology
Monika Stompor-Goracy, Maciej Machaczka
Summary: Ferulic acid, a derivative of 4-hydroxycinnamic acid, has beneficial properties but faces challenges in its intracellular transport, leading to the development of new nanotechnological approaches; this review aims to summarize the past decade's research on the biological properties of ferulic acid and innovative delivery methods to support pharmacological therapy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Multidisciplinary
Mingjie Rong, Jian Liu, Zhen Sun, Tong Li, Yang Li, Chunhuan Jiang, Lehui Lu
Summary: This study proposes an innovative strategy using black phosphorous nanosheets (BPNSs) to enhance Pd-mediated bioorthogonal catalytic activity. The electron-donor properties of BPNSs enable the in situ growth of Pd nanoparticles (PdNPs) on their surface. Additionally, the superb capability of reducing Pd-II and the lone pair electrons of BPNSs contribute to accelerating the transmetallation in the decaging reaction process and firmly anchoring PdNPs via Pd-P bonds. This design endows Pd/BP with the capability to activate prodrugs and retard tumor growth, providing new insights into the design of heterogeneous transition-metal catalysts (TMCs) for bioorthogonal catalysis.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Article
Chemistry, Physical
Danjun Mao, Shuxue Yang, Yuan Hu, Huan He, Shaogui Yang, Shourong Zheng, Cheng Sun, Zhifeng Jiang, Xiaolei Qu, Po Keung Wong
Summary: By fabricating freestanding ultrafine Bi5O7Br nanowires with abundant oxygen vacancies, this study successfully optimized the critical processes of CO2 photocatalysis and improved the reaction efficiency. The findings may inspire the future design of ultrafine catalysts for artificial photosynthesis.
APPLIED CATALYSIS B-ENVIRONMENT AND ENERGY
(2023)
Article
Engineering, Environmental
Zheng Lian, Ting Wu, Xining Zhang, Shuangfei Cai, Youlin Xiong, Rong Yang
Summary: By preparing a Mo2C/MoOx thin film via one-step chemical vapor deposition (CVD), the redox cycles of multiple Mo valence states and staggered bandgap structures of Mo-based components in the film synergistically promote PMS activation and visible-light photocatalysis, generating reactive oxygen species that efficiently degrade the uneasily degradable antibiotic tetracycline. The film also exhibits promising reusability, maintaining the degradation capability for at least 10 cycles. This work provides feasible approaches to develop easily prepared AOP thin film materials for antibiotic pollutant degradation.
CHEMICAL ENGINEERING JOURNAL
(2023)
Article
Multidisciplinary Sciences
Fan Mo, Chunlin Song, Qixing Zhou, Wendan Xue, Shaohu Ouyang, Qi Wang, Zelin Hou, Shuting Wang, Jianling Wang
Summary: TiO2@Fe -N -C catalysts with Fe atomic clusters and Fe-N-4 active sites were fabricated for efficient peroxymonosulfate oxidation reactions. The charge redistribution induced by atomic clusters strengthened the interaction between single atoms and peroxymonosulfate. The reaction efficiency was enhanced by optimizing the oxidation and desorption steps, resulting in rapid degradation of tetracycline in the Vis/TiFeAS/PMS system.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2023)
Article
Polymer Science
Alex Abramov, Binoy Maiti, Ina Keridou, Jordi Puiggali, Oliver Reiser, David Diaz Diaz
Summary: A novel methodology for pH-triggered degradation of polymers or drug release under visible light irradiation is described, based on the cyclization of ortho-hydroxy-cinnamates (oHC) to coumarins. The key oHC structural motif can be easily incorporated into the rational design of novel photocleavable polymers via click chemistry, with rapid photocleavage under 455 nm light irradiation when a suitable base is added.
MACROMOLECULAR RAPID COMMUNICATIONS
(2021)
Article
Biochemistry & Molecular Biology
Xiao Liu, Marie-Christin Barth, Klaudia Cseh, Christian R. Kowol, Michael A. Jakupec, Bernhard K. Keppler, Dan Gibson, Wolfgang Weigand
Summary: Three new Pt(IV) lipoate complexes were synthesized and characterized, showing anticancer activity and generation of reactive oxygen species in tested cell lines. The monosubstituted complex can be reduced by ascorbic acid and forms adducts that facilitate the formation of DNA-crosslinks in cells.
CHEMISTRY & BIODIVERSITY
(2022)
Review
Biochemistry & Molecular Biology
Tom Miclot, Aurane Froux, Luisa D'Anna, Emmanuelle Bignon, Stephanie Grandemange, Giampaolo Barone, Antonio Monari, Alessio Terenzi
Summary: In this review, the important studies on the interactions between G4s and peptides are examined, and the strengths and limitations of current analytic approaches are highlighted. It is found that the combined use of high-level molecular simulation techniques and experimental spectroscopy is the best way to design specifically tuned and selective peptides, thus controlling important biological functions.
Article
Chemistry, Inorganic & Nuclear
Luisa D'Anna, Simona Rubino, Candida Pipitone, Graziella Serio, Carla Gentile, Antonio Palumbo Piccionello, Francesco Giannici, Giampaolo Barone, Alessio Terenzi
Summary: Five metal complexes were synthesized and characterized for their interactions with DNA G-quadruplex structures. The copper complex showed the highest selectivity towards G-quadruplexes and exhibited dose-dependent cytotoxic activity in cancer cells.
DALTON TRANSACTIONS
(2023)
Correction
Pharmacology & Pharmacy
M. S. Galanski, V. B. Arion, M. A. Jakupec, B. K. Keppler
CURRENT PHARMACEUTICAL DESIGN
(2023)
Correction
Pharmacology & Pharmacy
F. Dufrasne, M. S. Galanski
CURRENT PHARMACEUTICAL DESIGN
(2023)
Article
Chemistry, Multidisciplinary
Paul Strasser, Bianca Montsch, Silvia Weiss, Haider Sami, Christoph Kugler, Sonja Hager, Hemma Schueffl, Robert Mader, Oliver Brueggemann, Christian R. R. Kowol, Manfred Ogris, Petra Heffeter, Ian Teasdale
Summary: The design and synthesis of novel bottlebrush polymers (PPz-g-PGA) with exceptional control over their structure and molecular dimensions have been reported. These polymers show outstanding aqueous solubility, ultra-high multivalency, and biodegradability, making them ideal as nanomedicines. They exhibit enhanced cellular uptake, pharmacokinetics, and tumor accumulation, offering valuable insights into the influence of architecture on the in vivo performance of nanomedicines.
Article
Pharmacology & Pharmacy
Yvonne Lerchbammer-Kreith, Nadine S. Sommerfeld, Klaudia Cseh, Xian Weng-Jiang, Uchechukwu Odunze, Andreas G. Schaetzlein, Ijeoma F. Uchegbu, Mathea S. Galanski, Michael A. Jakupec, Bernhard K. Keppler
Summary: A new class of anticancer prodrugs was developed by combining platinum(IV) complexes with glycol chitosan polymers as drug carriers. The platinum(IV) complexes were synthesized and conjugated with degraded glycol chitosan (dGC) polymers of different chain lengths. These conjugates exhibited higher cytotoxicity and antiproliferative activity in cancer cell lines compared to platinum(IV) counterparts. In particular, a cisplatin(IV)-dGC conjugate showed the highest cytotoxicity, being 33 times more potent than the corresponding platinum(IV) complex and twice as potent as cisplatin. Biodistribution studies of an oxaliplatin(IV)-dGC conjugate also showed increased accumulation in the lung, suggesting potential for further activity studies.
Article
Pharmacology & Pharmacy
Yvonne Lerchbammer-Kreith, Michaela Hejl, Petra Vician, Michael A. Jakupec, Walter Berger, Mathea S. Galanski, Bernhard K. Keppler
Summary: Based on their drug delivery properties and activity against tumors, PAMAM dendrimers were combined with platinum(IV) complexes to improve anticancer treatment. The conjugates showed faster reduction behavior compared to the platinum(IV) complexes and exhibited significantly increased cytotoxic activity in human cell lines. In vivo experiments demonstrated tumor growth inhibition and prolonged animal survival.
Article
Chemistry, Multidisciplinary
Martin Schaier, Sarah Theiner, Dina Baier, Gabriel Braun, Walter Berger, Gunda Koellensperger
Summary: In this study, a workflow combining low-dispersion laser ablation with inductively coupled plasma time-of-flight mass spectrometry (LA-ICP-TOFMS) was presented, enabling spatial single-cell metallomics in tissue to decode cellular heterogeneity. The toolbox of single-cell metallomics was expanded by integrating the concepts of imaging mass cytometry (IMC) to utilize metal-labeled antibodies for cellular tissue profiling.
Correction
Oncology
Mathea Sophia Galanski, Bernhard K. K. Keppler
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2023)
Article
Oncology
Monika Caban, Bettina Koblmueller, Diana Groza, Hemma H. Schueffl, Alessio Terenzi, Alexander Tolios, Thomas Mohr, Marlene Mathuber, Kushtrim Kryeziu, Carola Jaunecker, Christine Pirker, Bernhard K. Keppler, Walter Berger, Christian R. Kowol, Petra Heffeter
Summary: Through chemical modifications, KP2187 has similar activity and action as other clinically used EGFR inhibitors, without interfering with EGFR binding. In vitro and in vivo experiments have shown that KP2187 can significantly inhibit tumor cell proliferation and activate the EGFR signaling pathway. Moreover, KP2187 has a high synergistic effect with VEGFR inhibitors, indicating its potential as a hypoxia-activated prodrug.
Article
Chemistry, Applied
Alexia Tialiou, Zahraa H. Athab, Robert T. Woodward, Veronika Biegler, Bernhard K. Keppler, Ahmed F. Halbus, Michael R. Reithofer, Jia Min Chin
Summary: A novel hydroxypropyl cellulose (gHPC) hydrogel with graded porosity was successfully synthesized by cross-linking different parts of the hydrogel at different temperatures. The pore size in the hydrogel decreased from top to bottom. The hydrogel also showed graded mechanical properties, with the top layer being able to withstand 50% compression before fracture, while the middle and bottom layers could withstand 80% compression.
CARBOHYDRATE POLYMERS
(2023)
Correction
Biochemistry & Molecular Biology
Mathea Sophia Galanski, Michael A. Jakupec, Bernhard K. Keppler
CURRENT MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Xiao Liu, Dominik Wenisch, Philipp Dahlke, Paul M. Jordan, Michael A. Jakupec, Christian R. Kowol, Phil Liebing, Oliver Werz, Bernhard K. Keppler, Wolfgang Weigand
Summary: In recent decades, the close connection between inflammation and cancer has been recognized, leading to extensive studies on joint strategies involving chemotherapeutic and anti-inflammatory agents. In this study, novel Pt(IV) complexes based on cisplatin and oxaliplatin were synthesized, incorporating non-steroidal anti-inflammatory drugs (NSAIDs) and their carboxyl ester analogues. Certain cisplatin-based Pt(IV) complexes 22-30 exhibited increased cytotoxicity in human cancer cell lines compared to the Pt(II) drug. Complex 26, containing two aceclofenac moieties, displayed potent anticancer effects combined with anti-inflammatory properties.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Polymer Science
M. Ali Aboudzadeh, Vanessa Rodriguez-Fanjul, Alessio Terenzi, Estibaliz Gonzalez de San Roman, Jose I. Miranda, Ana M. Pizarro, Luca Salassa, Fabienne Barroso-Bujans
Summary: We synthesized a macrocyclic poly(ethyleneoxide) (PEO) connected with a [Ru(bpy)(3)](2+) unit, which is a photoactive metal complex with potential biomedical applications. The PEO chain provides biocompatibility, water solubility, and topological play. The macrocycles were successfully synthesized by copper-free click cycloaddition and exhibited higher fluorescence lifetime compared to their linear analogues.
Article
Chemistry, Inorganic & Nuclear
Alexander Kastner, Theresa Mendrina, Florian Bachmann, Walter Berger, Bernhard K. Keppler, Petra Heffeter, Christian R. Kowol
Summary: In this study, oxaliplatin(iv)-based complexes were developed as platinum(iv) prodrugs to release aspirin, which has shown antitumor activity against colon cancer. The newly synthesized complex demonstrated increased reduction stability compared to a cisplatin analog and exhibited desired prodrug properties in cell culture. A derivative with albumin-binding properties showed improved pharmacokinetics and tumor accumulation, leading to enhanced antitumor activity and overall survival in tumor-bearing mice.
INORGANIC CHEMISTRY FRONTIERS
(2023)