WuXi Discovery Services’ Post

Despite the success of delivery technologies such as lipid nanoparticles and trivalent GalNAc conjugation, targeted delivery of oligonucleotides to extra hepatic tissues remains a challenge. WuXi AppTec recently presented a poster showing the utilization of our peptide-based DNA-encoded library screening platform to identify endocytosis receptor-binding peptides. The binding affinity of hit peptides was confirmed through biophysical assays, and target-based delivery efficiency in breast cancer cells was evaluated by flow cytometry. These results highlight the potential of this approach for developing peptide-oligonucleotide conjugates for peptide-based drug delivery. Curious to learn more? Click 👇 to view our poster. Questions? Contact us by clicking here: https://lnkd.in/eG97YXCs #Biotech #Biopharma #DrugDiscovery #DEL #Endocytosis #Peptides #PeptideConjugates https://lnkd.in/gvKx75-J

🚀 Unlock the Future of Biomedical Research with Assay Genie’s 3D Organoid Cell Viability Assay! 🧬 Take your research to the next level with our cutting-edge 3D Organoid Cell Viability Assay. Designed to provide accurate and reliable results, our kit is perfect for researchers looking to: Assess cell viability in complex 3D structures Enhance drug screening processes Improve cancer research outcomes 🔬 Why Choose Assay Genie? Precise and reliable results User-friendly protocol Versatile applications Elevate your research and discover more about how our 3D Organoid Cell Viability Assay can benefit your studies. Visit Assay Genie for more information! https://lnkd.in/gb3nMuUV #BiomedicalResearch #CellViability #OrganoidResearch #AssayGenie #DrugDiscovery

The RAS family of small GTPases are among the most frequently mutated oncogenes in human cancer. Previously viewed as undruggable, the recent FDA approval of two KRAS G12C-selective inhibitors has offered real promise to the development of anti-RAS therapies, including mutation-specific strategies. To support the discovery of novel RAS inhibitors, WuXi AppTec offers a comprehensive panel of ready-to-go biophysical assays, nucleotide exchange assays, and established X-ray crystallography protocols. Our RAS protein production platform encompasses a broad range of KRAS variants, including G12C, G12D, G12V, and “Cys-light” variants to study covalent inhibitors. Click ⬇️ to learn more https://lnkd.in/e48wNQVF #Biophysical #Crystallography #StructuralBiology #Biochemical #KRAS #NRAS #G12C #MST #nanoDSF #SPR

The RAS family of small GTPases are among the most frequently mutated oncogenes in human cancer. Previously viewed as undruggable, the recent FDA approval of two KRAS G12C-selective inhibitors has offered real promise to the development of anti-RAS therapies, including mutation-specific strategies. To support the discovery of novel RAS inhibitors, WuXi AppTec offers a comprehensive panel of ready-to-go biophysical assays, nucleotide exchange assays, and established X-ray crystallography protocols. Our RAS protein production platform encompasses a broad range of KRAS variants, including G12C, G12D, G12V, and “Cys-light” variants to study covalent inhibitors. Click ⬇️ to learn more https://lnkd.in/e48wNQVF #Biophysical #Crystallography #StructuralBiology #Biochemical #KRAS #NRAS #G12C #MST #nanoDSF #SPR

Congratulations to Ms. Tianqi Wang, a graduate student of Associate Professor Matthias Wacker, for winning the Best Presenter Award (1st Prize) in the Poster Competition at the Asian Drug Delivery & Formulation Summit 2024! Her poster is titled "Elucidating Peptide-Biopolymer Interactions for the Design of Nanoscale Assemblies of the Anticancer Peptide FFW." Additionally, we congratulate Ms. Shaista Shabbir Jasdanwala, a graduate student of Assistant Professor Shruti Bhatt, who received recognition in the Poster Competition for the 3rd Prize at the AACR-Frontiers in Cancer Science 2024! Her poster is titled "Integrating Genomic And Functional Phenotypes To Refine Risk Assessment In Acute Myeloid Leukemia Across The Age Spectrum: Insights from Singapore” Well done all! #NationalUniversityofSingapore #NUSPharmacyandPharmaceuticalSciences #NUSPharmacyResearch #NUSResearch

𝗣𝗵𝗮𝗿𝗺𝗮𝗰𝗼𝗸𝗶𝗻𝗲𝘁𝗶𝗰𝘀 𝟮.𝟬 𝘀𝗽𝗼𝘁𝗹𝗶𝗴𝗵𝘁 | 𝟮𝟬𝟮𝟰 - 𝗪𝗲𝗲𝗸 𝟭𝟱    Today we are happy to release the inaugural edition of our pharmacokinetics 2.0 spotlight. On a biweekly basis we will use the spotlight to present three recent papers from the cellular and molecular pharmacokinetics field that got our attention. In this edition we present a study demonstrating a the nanocarrier-based cytosolic peptide delivery approach in cancer cells, exploiting the endolysosomal pathway. In a second paper, we highlight an alternative use of the endolysosomal pathway to mediate the transepithelial delivery of nanoparticles. Finally, the use of a dual ABC transporter expressing cell line is presented as a useful to obtain insights into a drug’s unbound brain concentration.     Are you struggling with endolysosomal escape of your compound? Do want to know more about the cellular trafficking of your compound or advanced delivery platform? Or would you be interested to know the unbound concentration in (brain) cells? Feel free to contact us: https://lnkd.in/e2vMReau.   𝘙𝘦𝘧𝘦𝘳𝘦𝘯𝘤𝘦𝘴: 1. Chen et al. 2024 https://lnkd.in/e-6bc6cS     2. Colclough et al. 2024 https://lnkd.in/e83ebD7y 3. Wang et al. 2024 https://lnkd.in/eiU_g_nD     #endolysosomal #nanoparticles #peptidedrugs #advanceddeliveryplatform #ABCtransporters #Kpuu #BBB #subcellulartargetting

This research focuses on the development of mixed ligand copper(II) complexes with diamines (phenanthroline or 4-methyl phenanthroline) and various carboxylate ligands as potential anticancer agents. The complexes were synthesized and characterized in the solid state, including a new crystal structure of [Cu2(3-(4-hydroxyphenyl)propanoate)3(phenanthroline)2]Cl·H2O. Various stoichiometries were observed, and partial dissociation of the complexes into Cu-diimine complexes was noted in solution. DNA binding studies revealed that the complexes interacted with DNA through partial intercalation and groove binding. In vitro cytotoxicity testing on multiple cancer cell lines (MDA-MB-231, MCF-7, A549) and non-tumor cells (MCF-10A, MRC-5) showed higher activity than cisplatin but lower selectivity. The results suggest that these mixed ligand copper(II) complexes exhibit promising anticancer activity and warrant further investigation for potential therapeutic applications. This study contributes to the ongoing research on coordination compounds as anticancer agents, which was initially sparked by the success of cisplatin. https://lnkd.in/dNjtGfm6 #bioinorganichemistry #inorganicbiochemistry #Article_Summary #cancerresearch

New advancements in epigenetic technologies are transforming clinical application research! Check out this article on how researchers are leveraging DNA methylation and histone modifications for potential cancer classification, anti-obesity drug development, and reversing age-related diseases. Learn about the cutting-edge potential of nanopore sequencing and programmable mRNA-based epigenomic medicines that could pave the way for novel therapeutic approaches, in the future Read more here: https://bit.ly/44NX933

🔬 Excited to share our latest breakthrough in medicinal chemistry! 🎉 Our article, titled "A Potent Solution for Tumor Growth and Angiogenesis Suppression via ELR+CXCLCXCR1/2 Pathway Inhibitor," has been published in ACS Med Chem Letters. 💡 We're particularly thrilled to announce that our innovative work has been selected for the front cover of the journal! 📚 Our study explores a groundbreaking pathway inhibitor that shows promise in suppressing tumor growth and angiogenesis, paving the way for more effective cancer therapies. 🌟Congratulations to all authors: Grytsai, O., Dufies, M., Le Du, J., Rastoin, O., Pires Gonçalves, L. C., Mateo, L., Lacas-Gervais, S., Cao, Y., Demange, L., Pagès, G., Benhida, R., and Ronco, C. 🎉Check out the article to learn more about our groundbreaking approach and its potential impact on the field of medicine. #MedicinalChemistry #Innovation #Research #ACS #TargetedTherapies #ScienceCommunity

Inositol-requiring enzyme 1α (IRE1α) is a sensor protein that plays a key role in multiple myeloma (MM) and is considered a potential therapeutic target for this type of blood cancer. IRE1α is activated by ER stress, which is common in MM cells due to their high protein synthesis. WuXi AppTec recently contributed to a study which identified a potent and selective IRE1α inhibitor, designated G-5758, that was well tolerated following multiday oral administration. Significantly, G-5758 demonstrated comparable pharmacodynamic effects to induced IRE1 knockdown in a KMS-11 multiple myeloma model. Click this link 👇 to view the abstract: https://lnkd.in/eq4YGias #Biotech #DrugDiscovery #IRE1 #MultipleMyeloma #IRE1alpha