Polyplus now part of Sartorius’ Post

A great FREE weekendread: Unveiling Gambogenic Acid as a Promising Antitumor Compound: A Review By Li Mi et al. Read for Free here: https://lnkd.in/ek-8wRHn #PlantaMedica #LetsGrowTogether Fig. 2 A schematic representation of the antitumor activity, pharmacokinetics, nanotechnology-mediated delivery of GNA.

The Mcule Molecular Glue Library is now available, featuring nearly 11,000 carefully selected small molecules with a higher affinity for binding E3 ligase and thus mediate protein-protein interactions between E3 ubiquitin ligase ligands and specific proteins. Explore our library [link to the library in the comments] and unlock the potential of molecular glues. #molecularglue #drugdiscovery #MculeLibraries

Together with John Auchampach’s lab (Medical College of Wisconsin), we introduce the approach of lipid trolling, to derivatize #GPCR ligands that bind at sites in contact with membrane lipids. A3 #adenosine #receptor positive allosteric modulators (#PAMs) occupy a membrane-exposed, cryptic binding site. Analogues that penetrate further into the #phospholipid environment utilize a hydrocarbon (hydrophobic) chain that is functionalized with a terminal cationic group (an amine, guanidino group, etc.), to anchor it to anionic head groups in the membrane inner leaflet. There’s a clear dependence of PAM potency on the chain length (with optima at 10 or 11 carbons). Analogues with uncharged appended chains are essentially inactive, because they lack a stabilizing second anchor (shown by molecular dynamics simulation by Matteo Pavan). In this manner the PAM pharmacological activity is qualitatively enhanced. https://lnkd.in/eEaCvSAy

Further development of adenosine receptor positive allosteric modulators in collaboration with the Jacobson lab at the NIH and introduction of the concept of 'lipid trolling' to optimize molecular interactions with a lipid-exposed transmembrane protein binding site. https://lnkd.in/gmse4VPZ

Delivering a talk in the CSICON 2023 on the benefits of GLP1 analogues and its cardio metabolic effects in reducing vascular events , weight reduction , renal preservation . Semaglutide has the strongest data while more molecules are in pipeline especially the one from Boehringer ingelheim Surviutide. Like for SELECT , I am the NLI of SYNCHRONIZE study . This is the decade of GLP1 analogues

#Cell: #Wnt proteins are enzymatically lipidated by Porcupine (#PORCN) in the ER and bind to Wntless (#WLS) for intracellular transport and secretion. However, How low-solubility Wnts from the #ER to the extracellular space? The study demonstrated that the Wnt7a-WLS complex binds to calreticulin (#CALR), revealing that CALR functions as a chaperone to facilitate Wnt transfer from PORCN to WLS during Wnt biogenesis. In addition, the group proposed a lipidmediated Wnt release mechanism, as well as characterized how Wnt7 coreceptor #RECK binds to Wnt7a for ligandspecific signaling. https://lnkd.in/g_3Qcwe6 For more push, please follow #Twitter: https://lnkd.in/gntQ9qE7 Related Product Recommendation: #Digitonin (https://lnkd.in/gWh25Nc9); #Leupeptin (https://lnkd.in/gVQAwcwG); #Bafilomycin A1 (#BafA1; https://lnkd.in/g4-ZJJtb); #HEPES (https://lnkd.in/gtV978Gk).

Last chance to register for our webinar, tomorrow, where Optibrium CEO Matt Segall will be exploring how in silico approaches can support our understanding of drug metabolism. If you're interested in #DMPK or #MedicinalChemistry, this one's for you! https://lnkd.in/eNtjMEMp #DrugMetabolism #MetabolitePrediction #DrugDevelopment

Challenges with Host Cell Protein Analysis? In this recent paper from scientists at Merck, they utilize the Evosep One coupled to a Bruker timsTOF Pro 2 to overcome the challenges of host cell protein (HCP) analysis. By leveraging diaPASEF, they were able to reveal the presence of more than 600 additional HCPs previously missed by DDA PASEF. In addition to improved characterization of the sample, they were able to increase throughput and eliminate carryover! Taku Tsukidate, Alyssa Stiving, Shannon Rivera, Ansuman Sahoo, Sri Madabhushi, Xuanwen Shawn Li Take a look at the full manuscript 👇 👇👇 https://lnkd.in/e4QkQSyy To learn more about the Evosep One, visit our website evosep.com or reach out to me for additional information. #Evosep, #Bruker, #Hostcellproteins, #hcp,

From the abstract: In this study, we present a comprehensive peptidomimetic structure–activity relationship (SAR) approach, combined with cellular NanoBRET target engagement assays to enhance the existing VHL ligands. Through systematic modifications of the molecule, we identified the 1,2,3-triazole group as an optimal substitute of the left-hand side amide bond that yields 10-fold higher binding activity. Moreover, incorporating conformationally constrained alterations on the methylthiazole benzylamine moiety led to the development of highly potent VHL ligands with picomolar binding affinity and significantly improved oral bioavailability. We anticipate that our optimized VHL ligand, GNE7599, will serve as a valuable tool compound for investigating the VHL pathway and advancing the field of targeted protein degradation.

Competence is one of those things... You often look for it in vain. 👌 Not so with our Mix & Go! E. coli Competent Cells! The 𝗠𝗶𝘅 & 𝗚𝗼! 𝗘. 𝗰𝗼𝗹𝗶 𝗖𝗼𝗺𝗽𝗲𝘁𝗲𝗻𝘁 𝗖𝗲𝗹𝗹𝘀 enable a simple 20 second transformation process that can help you save over 1 hour on transformations. The competent cells have exceptional transformation efficiencies, reaching up to 𝟭𝟬^𝟵 𝘁𝗿𝗮𝗻𝘀𝗳𝗼𝗿𝗺𝗮𝗻𝘁𝘀 𝗽𝗲𝗿 µ𝗴 𝗼𝗳 𝗽𝗹𝗮𝘀𝗺𝗶𝗱 𝗗𝗡𝗔. We have 5 premade strains available, including the renowned DH5 alpha competent cells. 🎯 Find the perfect strain of Mix & Go! Competent Cells for your experiment 🎯 or produce your own using our Mix & Go! E. coli Transformation Kit and Buffer Set. Unlock the pathway to success in your research and therapeutic development endeavors today. #competentcells #Ecoli #celltransformation #transfection #transduction #zymoresearcheurope #innovation