Vesiculab’s Post

🔬 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

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!

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 

🔬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

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

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

A masterpiece in enzymology, what a pleasure to see this in the publication landscape!

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

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

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.