Article
Polymer Science
Jacek J. Walkowiak, Rohit Nikam, Matthias Ballauff
Summary: The effective charge of highly charged polyelectrolytes is significantly lowered by a condensation of counterions. This effect is more pronounced for divalent ions. Our study on dendritic polyglycerol sulfate (dPGS) demonstrates that the interactions between dPGS and divalent ions (Mg2+ and Ca2+) show no ion specificity but clear competition between monovalent and divalent ions. These findings support the latest theoretical studies and indicate the sequential replacement of monovalent ions with divalent ions.
Article
Polymer Science
Felix Reisbeck, Alexander Ozimkovski, Mariam Cherri, Mathias Dimde, Elisa Quaas, Ehsan Mohammadifar, Katharina Achazi, Rainer Haag
Summary: A dual-responsive drug delivery system was synthesized in this study, which exhibited enhanced drug release under different stimuli and efficient inhibition of cancer cell growth. The system showed good biocompatibility and tolerability while achieving targeted drug release and cytotoxic effects on cancer cells.
Review
Polymer Science
Paria Pouyan, Mariam Cherri, Rainer Haag
Summary: Polyglycerols (PG) have remarkable characteristics that make them attractive for biomedical and pharmaceutical applications. The presence of multiple hydroxy groups allows for structure modification, high water solubility, and excellent biocompatibility.
Article
Chemistry, Multidisciplinary
Guangze Yang, Yun Liu, Yue Hui, Tengjisi, Dong Chen, David A. Weitz, Chun-Xia Zhao
Summary: This study compared two types of dye-labeled nanoparticles and found that nanoparticles with dye molecules in a solid state undergo dye quenching, while those in a soluble state do not. To standardize the comparative study, the proposed solutions include using lower dye loading or utilizing medium analysis for quantifying cell uptake of nanoparticles. Valuable insights into selecting valid quantification methods for bio-nano studies are provided.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Chemistry, Organic
Eduardo Izquierdo, Marta L. opez-Corrales, Diego Abad-Montero, Anna Rovira, Gemma Fabria, Manel Bosch, Jose Luis Abad, Vicente Marchan
Summary: Researchers have developed a series of new fluorescent sphingolipid probes with excellent emission quantum yields and different subcellular localization patterns.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Mohamed H. Aboumanei, Ashgan. F. Mahmoud, M. A. Motaleb
Summary: The study successfully developed chitosan-coated colistin nanoliposomes to improve the stability and enhance the oral delivery of colistin. In vivo studies in bacterial infection-bearing mice showed that chitosan-coated nanoliposomes significantly enhanced the bioavailability of colistin. This approach offers a promising tool for enhanced oral delivery of colistin.
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
(2021)
Article
Chemistry, Inorganic & Nuclear
Richard C. Knighton, Thibault Troadec, Valerie Mazan, Patricia Le Saec, Severine Marionneau-Lambot, Thomas Le Bihan, Nathalie Saffon-Merceron, Nathalie Le Bris, Michel Cherel, Alain Faivre-Chauvet, Mourad Elhabiri, Loic J. Charbonniere, Raphael Tripier
Summary: This study presents the preparation and characterization of two novel cyclam-based macrocycles with phosphonate-appended pyridine side arms for the coordination of copper(II) ions in Cu-64 PET imaging. The complexes demonstrated excellent stability and low liver accumulation, paving the way for the use of phosphonated pyridine chelators for in vivo Cu-64-PET imaging.
INORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Esmaeil Gharepapagh, Ashraf Fakhari, Tahereh Firuzyar, Ashkan Shomali, Farzaneh Azimi
Summary: A new Tc-99m N-doped graphene quantum dot Tc-99m-(N-GQD) moiety has been developed for possible radiolabeling of molecules with chelation limitations and poor water solubility. The Tc-99m-(N-GQDs) were synthesized and characterized with high purity, demonstrating high radiochemical purity after radiolabeling and effective elimination by kidneys in biodistribution studies. Dosimetry studies showed kidneys as critical organs for the effective radiation dose of Tc-99m-(N-GQDs).
NEW JOURNAL OF CHEMISTRY
(2021)
Article
Nanoscience & Nanotechnology
Robin Wanka, Florian Koschitzki, Vuk Puzovic, Thorben Pahl, Emily Manderfeld, Kelli Z. Hunsucker, Geoffrey W. Swain, Axel Rosenhahn
Summary: A new dendritic PG-HEMA material was synthesized chemically and compared with commercially available hydrophilic monomers, showing that PPGMA exhibited better resistance to silt incorporation and outperformed PEGMA and PG(4)MA in the DSFE assay.
ACS APPLIED MATERIALS & INTERFACES
(2021)
Article
Pharmacology & Pharmacy
Mahnaz Ahmadi, Mona Khoramjouy, Simin Dadashzadeh, Elham Asadian, Mona Mosayebnia, Parham Geramifar, Soraya Shahhosseini, Fatemeh Ghorbani-Bidkorpeh
Summary: In recent years, there has been growing interest in the use of metal-organic frameworks (MOFs), a new class of highly porous nanomaterials. This study investigated the pharmacokinetics and biodistribution of MOF nanoparticles, specifically ZIF-8 nanoparticles, to track their in vivo fate. The results showed that ZIF-8 nanoparticles exhibited high pulmonary biodistribution and could improve the pharmacokinetics of encapsulated agents for lung targeting.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2023)
Article
Radiology, Nuclear Medicine & Medical Imaging
Christian Gentzsch, Xinyu Chen, Philipp Spatz, Urban Kosak, Damijan Knez, Naoko Nose, Stanislav Gobec, Takahiro Higuchi, Michael Decker
Summary: In this study, a selective and reversible PET tracer targeting AD diagnosis was successfully synthesized, labeled with F-18, and demonstrated promising activity and binding potential in in vitro experiments.
MOLECULAR IMAGING AND BIOLOGY
(2021)
Article
Chemistry, Multidisciplinary
Martin Ullrich, Florian Brandt, Reik Loser, Jens Pietzsch, Robert Wodtke
Summary: The development of novel ligands for G-protein-coupled receptors (GPCRs) involves the characterization of their binding affinity, typically using radioligands in competition or saturation binding assays. GPCRs, being transmembrane proteins, require preparation of receptor samples from tissue sections, cell membranes, cell homogenates, or intact cells for binding assays. In this study, we characterized a series of Cu-64-labeled [Tyr(3)]octreotate (TATE) derivatives in vitro using saturation binding assays to investigate the binding parameters of the somatostatin receptor sub-type 2 (SST2) towards intact mouse pheochromocytoma cells and corresponding cell homogenates. We discuss the observed differences, considering the physiology of SST2 and GPCRs in general, and highlight the advantages and limitations of the methods used.
Article
Oncology
Weijun Wei, Di Zhang, You Zhang, Lianghua Li, Yuchen Jin, Shuxian An, Chun Lv, Haitao Zhao, Cheng Wang, Yanshan Huang, Jiali Dong, Gang Huang, Jianjun Liu
Summary: This study developed three tracers targeting CLDN18.2, which can reliably visualize its expression and show excellent diagnostic value in gastric cancer models and PDX models naturally expressing CLDN18.2.
MOLECULAR THERAPY-ONCOLYTICS
(2022)
Article
Chemistry, Physical
Neha Manhas, Parvesh Singh, Ashona Singh-Pillay, Neil Koorbanally
Summary: A series of quinazoline-4 (3H)-one-tagged triazole conjugates were synthesized using the CuAAC methodology and characterized by various spectroscopic techniques. The antibacterial activities of these compounds against gram-negative strains were evaluated and compared with commercial drugs. SAR analysis demonstrated that the incorporation of a triazole ring significantly enhanced the antibacterial activity, while the position and nature of substituents on the phenyl ring of the triazole ring played important roles in modulating the activity of the conjugates. Molecular docking studies revealed the binding characteristics of these compounds in the DNA gyrase binding site of Staphylococcus aureus.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Medicine, Research & Experimental
Qing Ruan, Cheng Zhou, Qianna Wang, Fei Kang, Yuhao Jiang, Guoquan Li, Junhong Feng, Shu Zong, Junbo Zhang, Jing Wang
Summary: This study aimed to develop a 99mTc-labeled fibroblast activation protein inhibitor (FAPI) tracer, evaluate its imaging efficacy in nude mice, and further explore its biodistribution in healthy volunteers and uptake in tumor patients.
MOLECULAR PHARMACEUTICS
(2023)
Article
Biochemistry & Molecular Biology
Sabine Schulze, Christin Neuber, Stephanie Moeller, Jens Pietzsch, Klaus-Dieter Schaser, Stefan Rammelt
Summary: Although chronic inflammation inhibits bone healing, the healing process is initiated by an inflammatory phase. Pro-inflammatory cytokines are secreted to orchestrate the inflammation response to injury and the recruitment of progenitor cells. sGAG-coated PCL scaffolds have the potential to improve bone healing by inhibiting pro-inflammatory cytokines and promoting regenerative capacity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Florian Brandt, Martin Ullrich, Johanna Wodtke, Klaus Kopka, Michael Bachmann, Reik Loeser, Jens Pietzsch, Hans-Juergen Pietzsch, Robert Wodtke
Summary: The use of radioligands for targeted endoradionuclide therapy is limited due to their toxicity to healthy tissues, specifically the kidneys. However, targeting enzymes in the renal brush border membrane using cleavable linkers that can form fast clearing radionuclide fragments is gaining interest. In this study, a library of 64Cu-labeled cleavable linkers was synthesized and their substrate potentials towards neprilysin (NEP) were quantified, leading to the establishment of structure-activity relationships. It was found that a substrate-based targeting of NEP in the kidneys with small peptides resulted in premature cleavage in the bloodstream, highlighting the importance of additional targeting of albumin for kidney-specific NEP targeting.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Luisa M. Bachmann, Maria Hanl, Felix Feller, Laura Sinatra, Andrea Schoeler, Jens Pietzsch, Markus Laube, Finn K. Hansen
Summary: Multi-target drugs (MTDs) offer a new approach for combination therapies. In this study, a library of dual HDAC-COX inhibitors was designed, synthesized, and evaluated. The synthesized compounds showed significant inhibitory activities against HDAC and COX isoforms. Selected compounds were confirmed to have membrane permeability and inhibition of cellular HDAC activity. The most promising dual inhibitors, C3 and C4, demonstrated antiproliferative effects and increased apoptotic cells. However, simultaneous inhibition of HDAC and COX by these inhibitors or combination treatments did not result in additive or synergistic anticancer activities.
Review
Biotechnology & Applied Microbiology
Rosa Nickl, Sandra Hauser, Jens Pietzsch, Torsten Richter
Summary: The endothelium has a crucial role in maintaining the balance of hemodynamic, humoral, and inflammatory processes in the human body. Dysfunction of the pulmonary endothelium can lead to severe consequences for gas exchange and oxygenation, potentially resulting in multiple organ failure. This review provides a medical context for understanding the dysfunction of the pulmonary endothelium caused by various infections, ventilator-related injury, and aspiration. Emphasis is placed on the interaction between endothelial cells and alveolar macrophages, as well as the induction of cyclooxygenase-2 and related signaling pathways.
BIOENGINEERING-BASEL
(2023)
Article
Pharmacology & Pharmacy
Sebastian Braun, Svetlana Paskas, Markus Laube, Sven George, Bettina Hofmann, Peter Loennecke, Dieter Steinhilber, Jens Pietzsch, Sanja S. Mijatovic, Danijela Maksimovic-Ivanic, Evamarie Hey-Hawkins
Summary: In this study, carborane-containing dual COX-2/5-LO inhibitors were designed by incorporating metabolically stable, sterically demanding, and hydrophobic carboranes into existing inhibitors. Five carborane-containing derivatives showed high inhibitory activities towards COX-2 and 5-LO, with meta-carborane derivative 3 demonstrating higher anticancer activity compared to RWJ-63556. The accumulation of lipid droplets in cells indicated the blockage of COX-2 and 5-LO pathways, suggesting a promising approach for the design of potent dual COX-2/5-LO inhibitors.
ADVANCED THERAPEUTICS
(2023)
Article
Engineering, Biomedical
Yong Xu, Rebecca Rothe, Dagmar Voigt, Ahmed Sayed, Can Huang, Sandra Hauser, Pao-Wan Lee, Meiying Cui, James P. Saenz, Aldo R. Boccaccini, Kai Zheng, Jens Pietzsch, Yixin Zhang
Summary: By incorporating polyphosphate-modified hyaluronic acid and bioactive glass nano-fibril, we can create synthetic hydrogels that mimic the functions of extracellular matrix (ECM). These ECM-like hydrogels can be used for surface modification, 3D cell culture, and in vivo degradation. The system provides a versatile platform for investigating cell-biomatrix interactions.
ACTA BIOMATERIALIA
(2023)
Article
Biochemical Research Methods
Xuan Peng, Zeljko Janicijevic, Sandy Lemm, Markus Laube, Jens Pietzsch, Michael Bachmann, Larysa Baraban
Summary: The functional interaction between cancer cells and the surrounding microenvironment is not well understood, leading to the development of various in vitro tumor models. Factors such as nutrient transport, space availability, and confinement affect the size, shape, and metabolism of tumoroids. A low-cost method based on fluidics is presented to generate alginate and alginate-chitosan microcapsules for growing human hepatoma (HepG2) spheroids of different dimensions and geometries. The composition and thickness of the hydrogel shell are selectively tuned to control the permeability of the microcapsules. The diffusion of benchmark molecules through the shell is systematically investigated using experiments and simulations, ensuring efficient mass transfer and filtering of biochemical species. The metabolic activity of spheroids in microcapsules is confirmed through chromatography studies. Different phenotypic 3D cell assemblies are observed inside capsules based on available space, varying in cell aggregation tightness and shape. Overall, the system with tunable shell thickness and permeability provides a promising platform for studying cancer spheroid formation and their interaction with the surrounding microenvironment.
BIOTECHNOLOGY JOURNAL
(2023)
Article
Immunology
Haidy A. Saleh, Nicola Mitwasi, Martin Ullrich, Manja Kubeil, Magali Toussaint, Winnie Deuther-Conrad, Christin Neuber, Claudia Arndt, Liliana R. Loureiro, Alexandra Kegler, Karla Elizabeth Gonzalez Soto, Birgit Belter, Claudia Roessig, Jens Pietzsch, Marcus Frenz, Michael Bachmann, Anja Feldmann
Summary: Glioblastoma (GBM) is a difficult-to-cure tumor, and current treatment regimes have limited effectiveness. Immunotherapies, particularly chimeric antigen receptor (CAR)-expressing T cells, show promise for targeted therapy of GBM. However, CAR T cells can have serious side effects. In this study, the authors used the switchable RevCAR system to simultaneously target EGFR and GD2, which are expressed in GBM, providing specific and controlled activation of CAR T cells for killing tumor cells. The authors also demonstrated the potential of Dual-RevCAR T cells for gated targeting of GBM.
FRONTIERS IN IMMUNOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Diana Isabel Sandoval Bojorquez, Zeljko Janicijevic, Brenda Palestina Romero, Eduardo Sergio Oliveros Mata, Markus Laube, Anja Feldmann, Alexandra Kegler, Laura Drewitz, Ciaran Fowley, Jens Pietzsch, Juergen Fassbender, Torsten Tonn, Michael Bachmann, Larysa Baraban
Summary: Detection of COVID-19-associated antigens and respective antibodies is achieved using an interdigitated gold nanowire-based impedance nanobiosensor. The sensor devices demonstrate high sensitivity and a low limit of detection for the antibodies and virus antigen. Clinical plasma samples analysis shows the applicability of this platform in determining the infection or immunity status of patients.
Article
Cell Biology
Wonphorn Kandhavivorn, Hannes Glass, Thomas Herrmannsdoerfer, Tobias M. Boeckers, Marc Uhlarz, Jonas Gronemann, Richard H. W. Funk, Jens Pietzsch, Arun Pal, Andreas Hermann
Summary: Amyotrophic lateral sclerosis (ALS) is a devastating motoneuron disease characterized by loss of neuromuscular junctions, degeneration of motoneurons and muscle paralysis. Magnetic stimulation has been found to significantly improve axonal trafficking and regenerative sprouting of motoneurons in vitro, indicating the therapeutic potential of magnetic stimulations in ALS. However, further long-term in vivo studies are needed for validation.
Article
Chemistry, Multidisciplinary
Martin Ullrich, Florian Brandt, Reik Loser, Jens Pietzsch, Robert Wodtke
Summary: The development of novel ligands for G-protein-coupled receptors (GPCRs) involves the characterization of their binding affinity, typically using radioligands in competition or saturation binding assays. GPCRs, being transmembrane proteins, require preparation of receptor samples from tissue sections, cell membranes, cell homogenates, or intact cells for binding assays. In this study, we characterized a series of Cu-64-labeled [Tyr(3)]octreotate (TATE) derivatives in vitro using saturation binding assays to investigate the binding parameters of the somatostatin receptor sub-type 2 (SST2) towards intact mouse pheochromocytoma cells and corresponding cell homogenates. We discuss the observed differences, considering the physiology of SST2 and GPCRs in general, and highlight the advantages and limitations of the methods used.
Article
Pharmacology & Pharmacy
Liridona Useini, Teodora Komazec, Markus Laube, Peter Loennecke, Jonas Schaedlich, Sanja Mijatovic, Danijela Maksimovic-Ivanic, Jens Pietzsch, Evamarie Hey-Hawkins
Summary: Nonsteroidal anti-inflammatory drugs (NSAIDs) are widely used for pain, fever, and inflammation, and have reported antitumor properties. Selectivity for the COX-2 isoform of NSAIDs is of high interest to reduce off-target effects. Modified NSAIDs using carborane clusters show altered selectivity profile and isonimesulide and its carborane derivatives exhibit stronger antitumor potential compared to nimesulide and isonimesulide. Additionally, replacement of the phenyl ring with a carborane moiety shifts the COX activity from nonactive to active compounds.
ADVANCED THERAPEUTICS
(2023)
Review
Chemistry, Medicinal
Reik Loeser, Manuela Kuchar, Robert Wodtke, Christin Neuber, Birgit Belter, Klaus Kopka, Lakshmi Santhanam, Jens Pietzsch
Summary: The understanding of the contribution of the tumour microenvironment to cancer progression and metastasis, in particular the interplay between tumour cells, fibroblasts and the extracellular matrix has grown tremendously over the last years. Lysyl oxidases are increasingly recognised as key players in this context, in addition to their function as drivers of fibrotic diseases.
Article
Cell Biology
Anne Krueger-Genge, Susanne Koehler, Markus Laube, Vanessa Haileka, Sandy Lemm, Karolina Majchrzak, Sarah Kammerer, Christian Schulz, Joachim Storsberg, Jens Pietzsch, Jan-Heiner Kuepper, Friedrich Jung
Summary: Cancer patients have a high risk of thrombotic events, possibly due to tumor cell detachment or the effects of chemotherapeutic agents. Cyclophosphamide (CPA) is a commonly used drug that requires activation by cytochrome P450 enzymes (CYP). We hypothesize that CPA could induce thrombosis by damaging endothelial cells (EC) through metabolization or direct damage. In our study, HUVECs were treated with CPA and showed DNA damage, reduced EC layer formation, and increased release of prothrombotic substances. This suggests that CPA treatment may contribute to the risk of thrombus formation.
Article
Radiology, Nuclear Medicine & Medical Imaging
Thu Hang Lai, Barbara Wenzel, Sladjana Dukic-Stefanovic, Rodrigo Teodoro, Lucie Arnaud, Aurelie Maisonial-Besset, Valerie Weber, Rares-Petru Moldovan, Sebastian Meister, Jens Pietzsch, Klaus Kopka, Tareq A. Juratli, Winnie Deuther-Conrad, Magali Toussaint
Summary: This study developed an F-18-labeled ligand for non-invasive assessment of the IDH1R132H variant using positron emission tomography (PET) imaging. In vitro and in vivo experiments demonstrated a target-specific internalization of [F-18]AG-120, a high metabolic stability, and slightly higher accumulation in IDH1R132H-glioma compared to IDH1-glioma.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2023)