Engineering targeted extracellular vesicles loaded with TGF-β inhibitors: in their latest work, Xiaoqian Dang at Xi'an Jiaotong University and collaborators assessed the stability, cytotoxicity, and bone-targeting capability of the BT-EV-G platform, which consists of macrophage-derived extracellular vesicles decorated with targeting peptides and loaded with Galunisertib, a TGF-β inhibitor https://lnkd.in/gVBdzY29 Their findings revealed that BT-EV-G exhibited low toxicity and excellent bone-targeting ability in both in vitro and in vivo studies. An article co-authored by Zhaopu Jing, Guangyang Zhang, Yuanqing Cai, Jialin Liang and Leifeng Lv #extracellularvesicles #exosomes #bioengineering #osteoarthritis #drugdelivery #Vesiculab
Vesiculab’s Post
More Relevant Posts
-
🔬 𝐎𝐩𝐭𝐢𝐦𝐢𝐳𝐞 𝐘𝐨𝐮𝐫 𝐂𝐞𝐥𝐥 𝐁𝐢𝐨𝐥𝐨𝐠𝐲 𝐑𝐞𝐬𝐞𝐚𝐫𝐜𝐡 𝐰𝐢𝐭𝐡 𝐀𝐜𝐜𝐮𝐫𝐚𝐭𝐞 𝐂𝐞𝐥𝐥 𝐏𝐫𝐨𝐥𝐢𝐟𝐞𝐫𝐚𝐭𝐢𝐨𝐧 & 𝐂𝐲𝐭𝐨𝐭𝐨𝐱𝐢𝐜𝐢𝐭𝐲 & 𝐕𝐢𝐚𝐛𝐢𝐥𝐢𝐭𝐲 𝐃𝐞𝐭𝐞𝐜𝐭𝐢𝐨𝐧! Cell proliferation and cytotoxicity assays are essential tools for evaluating cell activity, genotoxicity, and the effects of antitumor drugs. Whether you're assessing cell growth, viability, or mitochondrial function, the right detection kit can make all the difference. At Elabscience, we offer a range of reliable kits, including EdU, Calcein AM/PI, CCK-8, and LDH, to meet your specific experimental needs. Whether you are monitoring cell viability or investigating DNA damage, our solutions are designed to deliver accurate and reproducible results. Discover the ideal kit for your research and ensure precision in every experiment! 🔗 https://lnkd.in/gyAzPD5R #CellBiology #Cytotoxicity #CellProliferation #Elabscience #EdU #CCK8 #CellGrowth #DNA
To view or add a comment, sign in
-
Enjoyed contributing to this study led by old friend and colleague Solomon Gisemba, Ph.D. Here, we (1) synthesized a bicyclic analog of the #opioid #peptide arodyn via sequential RCM, (2) predicted its binding mode to the kappa opioid receptor using molecular modeling, and (3) demonstrated that it retains potent antagonism of the kappa opioid receptor, activity that has shown potential to treat mood disorders and substance abuse. This analog improves our understanding of opioid peptides like arodyn, and it adds to a growing body of work demonstrating that (bi)cyclic peptides are... totally awesome!
To view or add a comment, sign in
-
Medicinal Chemistry - Project Leader; Technology Innovation & External Platforms presso Alfasigma - parla di #scienze #farmaci #farmaceutico #ricerca #innovazione #sociale
NEW PARP-1 INHIBITORS THROUGH A DNA-ENCODED LIBRARIE (DEL) PLATFORM, AND A PARP1 CATALYTIC MODEL WITHOUT THE AUTOINHIBITORY HELICAL DOMAIN Inhibition of poly (ADP-ribose) polymerase-1 (PARP1), a DNA repair enzyme, has proven to be a successful strategy for the treatment of various cancers. The first drugs PARP-1 inhibitor have been available for over 10 years, e.g. Olaparib (Lynparza®); Rucaparib (Rubraca®). Poly(ADP-ribose) polymerase inhibitors (PARPi) are approved by the US FDA as monotherapy for ovarian, breast and pancreatic tumors harboring BRCA1/2 mutations, as well as castration-resistant prostate cancers with homologous recombination repair (HRR) mutations. Other PARP-Is are currently investigated in clinical trials. Inhibition of poly (ADP-ribose) polymerase-1 (PARP1) has proven to be a successful strategy for the treatment of various cancers. However, despite the successes of medicinal chemistry in this field, difficulties remain in developing new generations of PARP-1 inhibitors due to non-specific interactions between protein-DNA. To overcome this, authors of a just accepted ChemMedChem (Chemistry Europe) article, have used a DNA-encoded library (DEL) platform, comprising ~5 billion molecules, to screen multiple PARP1 protein constructs, including one with the autoinhibitory helical domain removed to mimic a biologically relevant conformation. https://lnkd.in/ehuKSk8q Thanks to this approach, new and potent PAPR-1 inhibitors with single-digit nanomolar potency have been designed, that do not exhibit toxic DNA-trapping properties, a property that could be advantageous in the clinic. #PARP1 #DEL
Full professor of Medicinal Chemistry & Chemical Biology at the University of Salerno; Secretary of the EFMC Executive Committee; Chair of the Editorial Board of ChemMedChem
Inhibition of poly (ADP-ribose) polymerase-1 (PARP1), a DNA repair enzyme, has proven to be a successful strategy for the treatment of various cancers. In a just accepted ChemMedChem (Chemistry Europe) article by Valo Health, the authors used a DNA-encoded library platform, comprising ~5 billion molecules, to screen multiple PARP1 protein constructs, including one with the autoinhibitory helical domain removed to mimic a biologically relevant conformation. The experimental design allowed them to find novel and potent isoindolinone PARP1 inhibitors that do not exhibit toxic DNA-trapping properties Discovery of Potent Isoindolinone Inhibitors That Target an Active Conformation of PARP1 Using DNA-Encoded Libraries Kelly A McCarthy, Douglas J Marcotte, Sangram Parelkar, Crystal L McKinnon, Lindsay E Trammell, Eric L Stangeland, Rachael Jetson https://lnkd.in/en4Qw7a6
To view or add a comment, sign in
-
🔬Citation Break!📖 This citation investigates the relationship between CDK5 and Alpha-Synuclein, and the role the enzyme might have in Synuclein neurotoxicity. Our Alpha-Synuclein and Beta-Synuclein were used in cytotoxicity assays after the authors’ cell culture experiments. rPeptide offers a wide range of Synuclein products including full length proteins, fragments, mutants, preformed fibrils, and more. Paper: https://t.ly/wT4L_ Alpha-Synuclein: https://t.ly/Dv6WF Beta-Synuclein: https://t.ly/p-oSZ #Research #Development #rPeptide #Experiment #Synuclein #Alpha #Beta
Extracellular alpha-synuclein induces calpain-dependent overactivation of cyclin-dependent kinase 5 in vitro
sciencedirect.com
To view or add a comment, sign in
-
Oncology Discovery | Precision Medicine | Cancer Dependency | Pharmacology | DNA Damage & Oncogenic signaling | Functional Genomics & Epigenomics
Exploring the structure-activity relationship (SAR) of a small molecule has led to the creation of SJ3149. This degrader of CK1α protein has shown to be effective and selective in both in vitro and in vivo settings. The co-crystal structure of SJ3149 with CK1α + CRBN + DDB1 has shed light on its enhanced degradation properties. Check out the full article for more information on this exciting breakthrough! #drugdiscovery #drugdevelopment #degrader #molecularglue https://lnkd.in/eEg-uf8h
Selective CK1α degraders exert antiproliferative activity against a broad range of human cancer cell lines - Nature Communications
nature.com
To view or add a comment, sign in
-
Yong Chen synthesized dual-ligand PROTACs that incorporate two copies of a protein-binding ligand and two copies of an E3 ligase-binding ligand. Despite their high molecular weight (> 3 kDa), these molecules demonstrate superior performance compared to conventional PROTACs, both in vitro and in vivo, in terms of target protein degradation and therapeutic activity. We hypothesize that dual-ligand PROTACs form more stable ternary complexes, which may prevent PROTACs from leaving the cell. https://lnkd.in/eXKNuEKn
To view or add a comment, sign in
-
A masterpiece in enzymology, what a pleasure to see this in the publication landscape!
👀 😀 Always gratifying to witness the impact of the crucial role of #bindingkinetics in efficacy prediction! In this impresive publication, researchers provide mechanistic insights for the largest cohort of EZH2 inhibitors reported to date, demonstrating that 𝙧𝙚𝙨𝙞𝙙𝙚𝙣𝙘𝙚 𝙩𝙞𝙢𝙚 values obtained from biochemical assays are the 𝗯𝗲𝘀𝘁 𝗽𝗿𝗲𝗱𝗶𝗰𝘁𝗼𝗿 𝗼𝗳 𝗰𝗲𝗹𝗹𝘂𝗹𝗮𝗿 𝗲𝗳𝗳𝗶𝗰𝗮𝗰𝘆. AUC values obtained from a cellular washout assay together with endpoint IC50’s from the same assay were also good predictors for antiproliferative activity. https://lnkd.in/ddaKgxgU #DrugDiscovery #Screening #HTS #MedChem #Drugdesign #epigenetics
A miniaturized mode-of-action profiling platform enables high throughput characterization of the molecular and cellular dynamics of EZH2 inhibition - Scientific Reports
nature.com
To view or add a comment, sign in
-
Interest in metabolomic and lipidomic biomarkers from clinical samples is on the rise, but conventional extraction methods present notable time and complexity challenges. Our BeatBox® boffins took on the challenge, and the result? A new high-throughput processing workflow for targeted metabolomic and lipidomic analysis of limited tissue specimens. Learn more about the application: https://ow.ly/M2Ux50RBHZY #BeatBox #lipids #biomarkers #homogenization #MassSpec #samplepreparation #LCMS #metabolomics #lipidomics
AppNote | Expanding the BeatBox for low-input high-throughput targeted metabolomics and lipidomics
go.preomics.com
To view or add a comment, sign in
-
These timelapse imaging videos show the results of two experimental conditions with THP1-ASC-GFP cells, a THP1 monocyte cell line in which GFP is expressed as a fusion protein with ASC, an integral component of the NLRP3 inflammasome. In both cases, the cells were previously primed with LPS to induce rapid expression of inflammasome components. In the video on the right, the inflammasome was activated with nigericin, which elicits the rapid assembly of the NLRP3 inflammasome protein complex and is observed as the condensing of ASC-GFP into a single green "speck" in each cell. This ultimately results in secretion of inflammatory cytokines, including IL-1beta. Conversely, in the video on the left, LPS was co-applied to the cells with a drug that inhibits the inflammasome activation process. This experimental approach demonstrates how we can test compounds for their anti-inflammatory potential and mechanism of action, in this case inhibiting the NLRP3 inflammasome activation step. #CellImaging #TimelapseVideos #ExperimentalConditions #THP1Cells #ASCProtein #NLRP3Inflammasome #Lipopolysaccharide #Nigericin #InflammasomeActivation #IL1Beta #AntiInflammatory
To view or add a comment, sign in
-
Discovery and Hit to Lead Optimization of Macrocyclic Peptides as Novel Tropomyosin Receptor Kinase A Antagonists The peptides described here can serve as a new class of analgesics, and the structure optimization methods reported provide a strategy for discovering new peptide drugs.
Discovery and Hit to Lead Optimization of Macrocyclic Peptides as Novel Tropomyosin Receptor Kinase A Antagonists
pubs.acs.org
To view or add a comment, sign in
8,325 followers
--
3moThank you for displaying a very outstanding information or article.