BroadPharm

🎯 Turning an Unselective Drug into a Precision Weapon Against Cancer! 💊 Huge congratulations to the research scholars at the University of Münster for their latest study, "How to deliver an unselective drug selectively: Novel puromycin-loaded albumin nanoparticles for active targeting and their controllable effectiveness." They introduce an innovative approach to selective cancer treatment using albumin-based nanoparticles. Summary and Conclusions 📊 Traditional chemotherapy often faces the challenge of damaging healthy cells alongside cancerous ones. This study overcomes this limitation by incorporating puromycin into albumin-based nanoparticles, ensuring it is only released in the presence of cathepsin B, an enzyme upregulated in cancer cells. By attaching trastuzumab to the nanoparticle surface, researchers enabled active targeting of HER2/neu-positive cancer cells, leaving HER2/neu-negative cells unharmed. ✅ Selective drug release protects healthy cells. ✅ Enzymatically cleavable linkers control drug activation in tumor environments. ✅ Broad applicability for various drugs and targeting ligands, revolutionizing precision medicine. 🌐 Learn more here: https://lnkd.in/gKHmDEc2 The success of this study was made possible by MC-Val-Ala-NHS ester, supplied by BroadPharm, which played a key role in HLP and HoLP preparation, ensuring precise drug conjugation and controlled release. Looking to enhance your drug delivery research? Explore BroadPharm’s MC-Val-Ala-NHS ester and a wide range of ADC linkers to power your next breakthrough: 🔗  MC-Val-Ala-NHS ester —> https://lnkd.in/gzYx3Sw8 🔗 Other enzymatically cleavable linkers —> https://lnkd.in/gWB-Qdwc 🔗 Other ADC linkers and payloads —> https://lnkd.in/gSinr4CN

Tuberculosis Treatment 🦠 Fluorescent Peptides Pave the Way 🌟 Congratulations to the research scholars at the National Institute of Health for their publication, "Active- and Allosteric-Site Cyclic Peptide Inhibitors of Secreted M. tuberculosis Chorismate Mutase." This innovative study introduces a new class of macrocyclic peptides (MCPs) that effectively inhibit the secreted Chorismate mutase enzyme of Mycobacterium tuberculosis (MtbCM), a promising target in the fight against tuberculosis. Summary and Conclusions 📊 The emergence of antibiotic-resistant strains of Mycobacterium tuberculosis necessitates novel therapeutic strategies. This study focuses on MtbCM, an enzyme implicated in the bacterium's virulence and host interactions. Utilizing the Random Peptides Integrated Discovery (RaPID) system, researchers screened extensive libraries to identify MCPs that bind to MtbCM. Two significant "chorismides" were discovered: one binding to the enzyme's active site and the other to an allosteric site, both demonstrating potent inhibition of MtbCM activity. Structural analysis via X-ray crystallography elucidated their binding modes, providing insights for future drug development. Additionally, the team developed fluorescence-based assays using these peptides, enhancing the evaluation of potential MtbCM inhibitors. The success of this research was bolstered by the use of FAM NHS ester, 6-isomer, and 5-TAMRA NHS Ester from BroadPharm, which facilitated peptide synthesis and fluorophore conjugation. For researchers seeking reliable fluorescent dyes for their projects, explore BroadPharm's extensive selection, including FAM NHS ester, 6-isomer, 5-TAMRA NHS Ester, and more: 🔗 FAM NHS ester, 6-isomer —> https://lnkd.in/gGN9hbjR 🔗 5-TAMRA NHS Ester —> https://lnkd.in/gqEpWZMx 🔗 Other fluorescent dyes —> https://lnkd.in/gqhTUxKF

Tuberculosis Treatment 🦠 Fluorescent Peptides Pave the Way 🌟 Congratulations to the research scholars at the National Institute of Health for their publication, "Active- and Allosteric-Site Cyclic Peptide Inhibitors of Secreted M. tuberculosis Chorismate Mutase." This innovative study introduces a new class of macrocyclic peptides (MCPs) that effectively inhibit the secreted Chorismate mutase enzyme of Mycobacterium tuberculosis (MtbCM), a promising target in the fight against tuberculosis. Summary and Conclusions 📊 The emergence of antibiotic-resistant strains of Mycobacterium tuberculosis necessitates novel therapeutic strategies. This study focuses on MtbCM, an enzyme implicated in the bacterium's virulence and host interactions. Utilizing the Random Peptides Integrated Discovery (RaPID) system, researchers screened extensive libraries to identify MCPs that bind to MtbCM. Two significant "chorismides" were discovered: one binding to the enzyme's active site and the other to an allosteric site, both demonstrating potent inhibition of MtbCM activity. Structural analysis via X-ray crystallography elucidated their binding modes, providing insights for future drug development. Additionally, the team developed fluorescence-based assays using these peptides, enhancing the evaluation of potential MtbCM inhibitors. The success of this research was bolstered by the use of FAM NHS ester, 6-isomer, and 5-TAMRA NHS Ester from BroadPharm, which facilitated peptide synthesis and fluorophore conjugation. For researchers seeking reliable fluorescent dyes for their projects, explore BroadPharm's extensive selection, including FAM NHS ester, 6-isomer, 5-TAMRA NHS Ester, and more: 🔗 FAM NHS ester, 6-isomer —> https://lnkd.in/gGN9hbjR 🔗 5-TAMRA NHS Ester —> https://lnkd.in/gqEpWZMx 🔗 Other fluorescent dyes —> https://lnkd.in/gqhTUxKF

🛡️ Engineering Dual Integrin Inhibitors for Immunotherapy 🛡️ A round of applause to the research team at Lassogen for their publication: "Overcoming Immune Checkpoint Inhibitor Resistance via Potent and Selective Dual αvβ6/8 Inhibitors Based on Engineered Lasso Peptides" Their work showcases a major leap forward in tackling immune checkpoint inhibitor (ICI) resistance—one of the biggest challenges in oncology today. Summary & Conclusions 📊 Integrins αvβ6 and αvβ8 in the tumor microenvironment (TME) activate TGF-β, a key driver of ICI resistance across multiple cancers. By leveraging the unique structural properties of lasso peptides, researchers engineered potent and highly selective dual αvβ6/8 inhibitors, demonstrating their efficacy in combination with anti-PD-1 therapy. Among them, Lassotide 47, a half-life-extended analog, sensitized resistant tumors, halted tumor growth, and even led to tumor regression in models of triple-negative breast and ovarian cancer. This breakthrough validates αvβ6/8 inhibition as a tumor-specific strategy to enhance immunotherapy. Lasso peptides' stability and selectivity make them a powerful therapeutic modality with potential for improved dosing schedules, enhanced efficacy, and even future oral drug formulations. Continued engineering of ultra-potent lassotides and half-life extensions may drive even greater success in overcoming TGF-β-driven immune evasion. 🌐 Check the full publication here: https://lnkd.in/gUjv2s6m Amino-PEG2-acid, a PEG linker supplied by BroadPharm, enabled the preparation of conjugation intermediate Acyl 50—a crucial step in this study. This underscores the critical role of high-quality PEG linkers in advancing next-generation cancer therapeutics. Discover more about Amino-PEG2-acid and explore BroadPharm’s diverse PEG and PEG amino linkers: 🔗 Amino-PEG2-acid —> https://lnkd.in/g_ARtnhD linker 🔗 More amino PEG linkers —> https://lnkd.in/gMQ4UvFh linker 🔗 More PEG linkers —> https://lnkd.in/g3rFaeq6 linker

A3-Coupled Linkers Paving the Way for Next-Gen Medicinal PROTACs  🧪 Shoutout to the collaboration between the University of Sussex, University of Dundee, and Reach Separations for their paper: "Use of Aldehyde–Alkyne–Amine Couplings to Generate Medicinal Chemistry-Relevant Linkers." 🔍 Summary & Conclusions: This research highlights how copper-catalyzed aldehyde–alkyne–amine (A3) couplings provide a modular and scalable route to racemic propargylic amines—essential building blocks for medicinal chemistry applications. The study successfully demonstrates chiral purification using HPLC, enabling access to enantiopure compounds critical for designing cellular probes and PROTAC degraders targeting BRD4. Through meticulous analysis, including vibrational circular dichroism (vCD) and X-ray crystallography, the team characterized the stereochemistry and physicochemical properties of these novel linkers. Their work underscores the potential of A3-generated linkers in fine-tuning solubility, binding interactions, and biological stability—key factors in optimizing drug-like properties for targeted protein degradation. With DC50 values <100 nM observed in BRD4 degradation assays, this research lays the foundation for further PROTAC optimization and antibody-drug conjugate applications. 🌐 Read the paper here: https://lnkd.in/gsa7ywgh Integral to this research were PROTAC linkers like Thalidomide-5-(PEG2-acid) and (S,R,S)-AHPC-pentanoic acid, provided by BroadPharm, empowering precise drug design. These linkers played a crucial role in enhancing targeted protein degradation strategies. Explore these PROTAC linkers and take your research further: 🔗Thalidomide-5-(PEG2-acid) —> https://lnkd.in/gVTKgc6W 🔗(S, R, S)-AHPC-pentanoic-acid —> https://lnkd.in/g6_Ren4X 🔗 More PROTAC linkers —> https://lnkd.in/gXXviEwR

Antibody-Oligonucleotide🧬Conjugates (AOCs) are unlocking new frontiers in precision medicine, bridging the power of antibodies with the specificity of oligonucleotides. At BroadPharm, we're proud to contribute to this transformative journey with our unique chemical biology linkers and bioconjugation services. Discover how our solutions can accelerate your AOC research. Explore the latest insights in our blog: 🔗 https://lnkd.in/g2URyuJq #AOC #ADC #ADCLinker #PEGLinker #ValCit #PeptideLinker #Conjugation ##ClickChemistry #ClickChemistryReagent #Bioorthogonal #Chemistry 

Antibody-Oligonucleotide🧬Conjugates (AOCs) are unlocking new frontiers in precision medicine, bridging the power of antibodies with the specificity of oligonucleotides. At BroadPharm, we're proud to contribute to this transformative journey with our unique chemical biology linkers and bioconjugation services. Discover how our solutions can accelerate your AOC research. Explore the latest insights in our blog: 🔗 https://lnkd.in/g2URyuJq #AOC #ADC #ADCLinker #PEGLinker #ValCit #PeptideLinker #Conjugation ##ClickChemistry #ClickChemistryReagent #Bioorthogonal #Chemistry 

🔥🔬Harnessing Dual-Drug Conjugates for Oncology 💡🔥 A huge congratulations to the brilliant researchers from the University of Utah and AstraZeneca for their collaborative work on “Modular Synthesis of Anti-HER2 Dual-Drug Antibody-Drug Conjugates Demonstrating Improved Toxicity.” Summary & Conclusion 📊 ADCs have become a powerful tool for delivering potent chemotherapeutics directly to tumors, but single-drug ADCs often fail due to resistance mechanisms. In this study, researchers developed a modular synthetic strategy to construct a library of 19 dual-drug ADCs, using Diels-Alder and Michael addition chemistries on an anti-HER2 trastuzumab scaffold. By precisely controlling the ratio and position of two drugs, they optimized toxicity, stability, and efficacy—demonstrating that dual-payload ADCs exhibit equal or superior cytotoxicity compared to single-drug ADCs, while leveraging multiple mechanisms of action. This innovation could be a game-changer for treating heterogeneous and resistant tumors. 🌐 Learn more here: https://lnkd.in/gPGfBYbR MC-Val-Cit-Doxorubicin and MC-Val-Cit-PAB-MMAE, offered by BroadPharm, were essential for designing and preparing the dual-drug ADCs. These ADC linker-payloads played a pivotal role in enabling precise conjugation, stability, and enhanced therapeutic outcomes. Explore MC-Val-Cit-Doxorubicin, MC-Val-Cit-PAB-MMAE, and a broad range of ADC linkers & payloads to support your own research: 🔗 MC-Val-Cit-PAB-MMAE —> https://lnkd.in/gmUeu5Js 🔗 MC-Val-Cit-Doxorubicin —> https://lnkd.in/gevv3NzB 🔗 More ADC Linkers —> https://lnkd.in/gG_bCr3J 🔗 More ADC Payloads —> https://lnkd.in/g_NS9T8Q

🩺 Next-Gen Pain Relief: siRNA Nanoparticle Therapy Shows Promising Results Huge congratulations to the dedicated research scholars at Harvard for their collaborative efforts on "Lipid Nanoparticle Delivery of siRNA to Dorsal Root Ganglion Neurons to Treat Pain." Summary and Conclusions 📊 This study demonstrates a pioneering approach using lipid nanoparticles (LNPs) to deliver small interfering RNA (siRNA) directly to DRG neurons, effectively silencing the transient receptor potential vanilloid 1 (TRPV1) ion channel, a key player in pain perception. The research highlights the ability of LNPs to enable precise gene silencing, providing a reversible and targeted analgesic effect while mitigating off-target impacts. The team systematically optimized LNP formulations by varying lipid-PEG compositions, particle sizes, and surface charges to enhance siRNA delivery efficiency. Their findings revealed that smaller, negatively charged LNPs (55 nm) coated with DMG-PEG achieved the highest siRNA accumulation in DRG neurons, leading to robust and temporary TRPV1 silencing. Behavioral assessments confirmed that this intervention significantly reduced pain responses to heat, capsaicin, and inflammation while maintaining safety profiles in vivo. 🌐 Learn more here: https://lnkd.in/gSY4jPqk   Notably, D-Lin-MC3-DMA, provided by BroadPharm, played a crucial role in achieving the optimal LNP formulation, ensuring enhanced stability and delivery efficiency. Interested in optimizing your own LNP formulations? Check out BroadPharm’s high-quality lipids designed for drug delivery applications! 🔗 D-Lin-MC3-DMA & Analogs —> https://lnkd.in/gacpT6Ps 🔗 Other PEG azide linkers —> https://lnkd.in/gqQ3uDKG 🔗 Other PEG linkers —> https://lnkd.in/gQH2TCEH

🛑➡️ Stop-and-Go DNA Motors: A New Frontier in Molecular Motion! Huge congratulations to Emory University and Georgia Institute of Technology on their publication, “On-demand photoactivation of DNA-based motor motion.” Summary and Conclusions 📊 The team has developed a cutting-edge approach to dynamically control DNA-based synthetic motors with light, mimicking the precise, on-demand motion of biological motor proteins. By employing photocleavable systems to create "fuel" and "brake" mechanisms, the researchers enabled stop-and-go control with spatiotemporal precision. This breakthrough includes dual-input systems that function as "AND" gates, laying the groundwork for optically controlled bio-nanotechnological devices. This innovation overcomes limitations of earlier light-driven motors, achieving both dynamic track formation and active, directional motion. With further advancements, this research could inspire transformative applications in DNA nanotechnology, from medical devices to programmable nanomachines. 🌐 Check the full publication here: https://lnkd.in/gAphKbuG We’re thrilled that azidoacetic acid NHS ester played a critical role in synthesizing azide-functionalized motors, serving as an enabler of this system. Interested in exploring similar solutions for your projects? Discover our comprehensive portfolio of PEG linkers: 🔗 Azidoacetic acid NHS Ester —> https://lnkd.in/gD6ZZq5x linker 🔗 Other PEG azide linkers —> https://lnkd.in/gXQkU9RE linker 🔗 Other PEG linkers —> https://lnkd.in/gGTTHHgk linker