Articles tagged with Medicinal Chemistry
A new study published in eLife reveals the folding speed limit of helical membrane proteins using a robust single-molecule tweezer method. The findings provide unprecedented insights into structural states, kinetics, and energy barrier properties, offering valuable guidance for advancing pharmaceutical research and design.
Researchers developed a liver-targeting drug that reversed obesity and lowered cholesterol in obese mice by delivering the drug via nanogel. The treatment, which was administered intraperitoneally, effectively normalized weight and reduced cholesterol levels despite continued high-fat diet consumption.
Researchers at the University of Tokyo have developed a DNA-based anticoagulant that has shown promising results in test mice and may be ready for human trials soon. The treatment could provide a safer alternative to existing medications, such as heparin, which can cause severe bleeding side effects.
Chemists at the University of Basel have developed chromium compounds that can replace osmium and ruthenium in luminescent materials and catalysts. The new materials are nearly as effective as some osmium compounds and are about 20,000 times more abundant and cheaper than their noble metal counterparts.
Researchers at TUM develop an RNA agent for a lung spray that slows macrophage activity, reducing lung inflammation and fibrosis. The active substance RCS-21 is delivered via an inhaler through a special sugar molecule, showing promise in treating acute inflammatory lung damage.
Researchers at the University of Tokyo have developed a continuous-flow manufacturing method for producing cefazolin, an essential antibiotic. This new approach reduces time, cost and waste, making it ideal for flexible production and improving global health access.
Researchers at Penn State have discovered a safe and efficient way to create cyclopropanes, key features in many drugs, using a previously undescribed chemical process. The new method uses visible light and common ingredients to transform alkenes into cyclopropanes with no carbene intermediate.
Researchers at Insilico Medicine discovered novel inhibitors for salt-inducible kinase 2 (SIK2), a potential target for anti-inflammation and anti-cancer therapy. The findings were published in the July 13 edition of Bioorganic & Medicinal Chemistry, demonstrating the power of Insilico's Pharma.AI platform.
Researchers have developed novel molecules that target the membrane of viruses, rather than their proteins, offering a promising new approach for treating infectious diseases. The molecules, inspired by natural peptides, disrupt the protective layers of enveloped viruses like Zika and chikungunya, while sparing human cells.
Researchers at California Polytechnic State University have developed a novel method for storing biological materials such as RNA and proteins in a solid-state, resembling a pill or tablet that dissolves in water for on-demand use. This innovation overcomes current limitations in storage and handling, making it easier to access these m...
Researchers at WVU have developed a way to view synthetic DNA at the atomic level, enabling them to understand how to change its structure for enhanced scissor-like function. This breakthrough could lead to new technology for medical diagnoses and treatments, including potential therapies for diseases like retinal degeneration and cancer.
A new algorithm has been created to search fungal genomes for clusters of genes likely to result in interesting biological compounds. The algorithm, trained on a newly described type of chemistry in fungi, has discovered over 1,300 fungal species with biosynthetic gene clusters centered on isocyanide chemistry.
The study evaluates recent research on artificial intelligence-generated molecular structures from the perspective of medicinal chemists, recommending guidelines for assessing novelty and validity. Insilico Medicine's recommendations aim to improve the process of generating and evaluating novel AI-generated drugs.
Researchers have discovered a novel copper protein binding site that shows promise for use in magnetic resonance imaging (MRI) contrast agents, potentially leading to clearer images and improved diagnoses. The new structure displayed highly effective levels of relaxivity, equal and superior to existing Gd(III) agents used in clinical MRI.
Researchers successfully synthesized isotopic atropisomers based on carbon isotope discrimination, exhibiting high rotational stability and stereochemical purity. The findings hold promise for fundamental understanding of isotopic atropisomers with implications in organic and medicinal chemistry.
Researchers have developed a method to produce pharmaceutical precursors from biorenewable β-pinene, a waste by-product from the paper industry. They successfully created paracetamol and ibuprofen using this compound, presenting a potential alternative to crude oil-based products.
A German federal funding program will support a five-year research collaboration to develop specialty lipids and auxiliaries for mRNA vaccines. The project aims to enhance production capacities and improve the resilience of supply chains for future mRNA therapeutics.
A new study has defined analytical performance specifications for 24,25-dihydroxyvitamin D examinations, which is essential for developing accurate methods to detect this metabolite. The findings show that the variation of 24,25(OH)2D concentration over time was significantly associated with 25(OH)D concentrations and body mass index.
The new method enables the synthesis of BCBs with unprecedented ease through a formal [2+2] cycloaddition, achieving regioselectivity and expanding chemists' access to diverse BCB scaffolds. This breakthrough addresses the challenges of BCB synthesis and offers a promising route for pharmaceutical applications.
The Medicines for All Institute will work on 14 new global health projects, reducing costs of medicines for tuberculosis, malaria, HIV, and neglected tropical diseases. With the $18.7 million grant, Medicines for All aims to improve access to low-cost medications for people living with these diseases.
Scientists have developed a new method to deliver genetic information to stem cells using nanoparticles coated with a specific polymer, enabling more efficient control over cellular differentiation. This innovation has the potential to improve the efficiency and effectiveness of regenerative medicine treatments.
Researchers at ETH Zurich have decoded details of how cyclic peptides cross cell membranes, providing a new understanding of their mechanism. This knowledge can help speed up drug discovery by identifying ideal side chains for these molecules.
The research team developed a technology that can restore normal peripheral myelin protein 22 distribution in CMT1A cells using electric stimulation, which eliminates protein aggregation and induces myelination. This technology has potential for the development of an electronic medicine with minimal side effects.
Researchers have discovered how TKI cancer drugs cause inflammation, linking it to mitochondrial dysfunction and the NLRP3 inflammasome. The study found that all tested TKIs share a common off-target activity against mitochondrial SFKs.
Researchers at UC San Francisco have created the first molecular-level picture of how an odor molecule activates a human odorant receptor, opening doors to creating novel smells. This achievement paves the way for new insights into biological processes, including fragrances and food science.
Researchers at UC Davis found that engaging serotonin 2A receptors inside neurons promotes growth of new connections, while the same receptors on cell surfaces do not. This discovery guides efforts to develop new treatments for depression and PTSD.
A team of researchers led by Ohio University professor Jennifer Hines has uncovered a new class of compounds that can target RNA and disrupt its function. The discovery identified a chemical scaffold that could be used to develop RNA-targeted medicines for various diseases.
A study by Pusan National University researchers investigates the effects of mild acid hydrolysis on sulfated fucans in sea cucumbers and sea urchins. The results show selective 2-desulfation, leading to an 8-sugar-long oligosaccharide production.
Researchers utilized the Chemistry42 platform to generate novel molecular structures and identified a hit molecule for CDK20, a promising target for hepatocellular carcinoma. The platform's customizable reward function and generative models enabled efficient design and optimization of molecules.
Researchers at Northwestern University developed a sustainable biorefinery that turns organic waste, including lignin, into valuable products. The process involves a microbial electrolysis cell that breaks down lignin into aromatic compounds with medicinal properties.
The researchers aim to create a set of tools to help other chemists select and produce the right crystal structures for new drugs, potentially saving time and cost. By understanding how molecules crystallize, they hope to speed up the development process and lower costs.
Researchers from UTSA and UT Health San Antonio are developing compounds that target the estrogen receptor-beta, which suppresses cancer growth. The goal is to identify a novel ER-beta agonist with potential as a therapeutic strategy for treating GBM in patients.
Researchers at UCLA have created the first synthetic version of lissodendoric acid A, a sea sponge-derived molecule with potential therapeutic benefits for Parkinson’s disease and similar disorders. The team developed a method that employs cyclic allenes to produce only the desired enantiomer of the molecule.
Researchers have identified the genetic secrets behind skullcap's anti-cancer activity, enabling the production of synthetic compounds. The discovery is expected to lead to more sustainable and rapid synthesis of cancer-fighting molecules.
Researchers successfully applied AlphaFold AI to an end-to-end platform, discovering a novel target and developing a potent hit molecule for liver cancer. The study demonstrates the potential of AI-powered drug discovery to accelerate treatment development.
A Cornell University collaboration has made an innovative discovery by incorporating carbon dioxide into organic molecules via electrosynthesis. The team successfully created carboxylated pyridines, which are vital to medicinal chemistry, using a novel electrochemical reactor setup.
Researchers at Scripps Research have developed a general synthesis method for 1,2,3,5-tetrazines, a family of compounds with great promise for making new pharmaceuticals and chemical products. The new method is more efficient than previous approaches, requiring just five reaction steps to produce myriad versions of these compounds.
Researchers used mass spectrometry to analyze complex biological samples, including Salvia miltiorrhiza Bge and Astragali Radix. The studies identified metabolites and compounds with immunoregulatory effects, highlighting the potential for new drugs and improving plant quality.
Researchers investigated Aicardi-Goutières syndrome and found that viral RNA recognition drives uncontrolled interferon production. The immune system mistakenly attacks healthy cells due to the failure of safety mechanisms to distinguish between viral and host genetic material.
Researchers at the University of Missouri have successfully used click chemistry to deliver radiopharmaceuticals specifically to tumors in large dogs with bone cancer, increasing effectiveness and minimizing circulation. This breakthrough could pave the way for click chemistry-based treatments for humans with cancer in the future.
Researchers found that rapamycin treatment during developmental growth phase decelerates aging rate and extends lifespan in animals. A transient late-life treatment is not effective, but a transient early-life treatment can reprogram aging.
Researchers at the University of Illinois developed an AI-powered system that uses a molecule-making machine to find optimal reaction conditions for synthesizing chemicals. The system doubled the average yield of a challenging class of reactions, paving the way for faster innovation and automation in biomedical and materials research.
Scientists are conducting a first-of-its-kind study to investigate the origin of psychedelic compounds in fungi, including psilocybin found in 'magic mushrooms'. The research aims to understand the evolution of these compounds and their potential applications in medicine and conservation.
A search of the Cambridge Structural Database found nearly 1,800 conglomerate crystal structures with spontaneous enriched chirality, augmenting synthetic building blocks for medicinal chemists. This discovery introduces a new pool of chiral molecules outside of natural sources, potentially leading to more effective treatments.
Scientists have designed compounds that activate the 5HT2a receptor, producing antidepressant and antianxiety effects in mice. The compounds' mechanism of action differs from psychedelics like LSD, offering a potential new approach to developing effective antidepressants with fewer side effects.
Researchers at Washington University in St. Louis found that cancer cells metabolize glucose in their mitochondria, following conventional biochemical patterns. The study suggests that limiting glucose uptake may not be an effective strategy to target cancer cells, and glucose metabolism may need to be reevaluated as a therapeutic target.
Researchers at Kyoto University have developed a new protocol for synthesizing dialkyl ethers using three catalysts that hydroxylate alkenes quickly and cheaply. This method enables the precise control of electrons and protons to convert unactivated alkenes into reactive carbocation equivalents under mild reaction conditions.
Researchers at Ohio State University have developed a new method to synthesize medicines using carbenes, reducing the need for explosive intermediates. This breakthrough could enable faster production of cyclopropanes, a key ingredient in COVID-19 treatments and other medications.
Researchers at Nanyang Technological University in Singapore have developed a series of chemical-based compounds that could be potential drug candidates for treating pulmonary tuberculosis. The compounds were licensed by US-based Neuro-Horizon Pharma LLC for commercialization.
Researchers developed a mathematical model to predict the efficiency of nanoparticle delivery into cells, particularly in stem cells. They found that nanoparticles become trapped in bubble-like vesicles, preventing them from reaching their targets.
Researchers from Tokyo University of Science developed novel complex-peptide hybrids that induce programmed cell death in apoptosis-resistant cancer cells through paraptosis. The compounds, syn-6 and anti-6, inhibit cell death by uncoupling mitochondrial calcium uptake and inducing cytoplasmic vacuolization, leading to cell death.
Researchers at Aarhus University have developed an easy and inexpensive method for linking molecules to DNA sequences with desired functions. The method uses sulfonyl azides to introduce various functionalities, avoiding the need for expensive and unstable special phosphoramidites.
Despite advances in biology and medicinal chemistry, research on schistosomiasis and other parasitic worm diseases remains at an early stage. Novel molecular targets and parasite signaling pathways may contribute to the development of new treatments.
Researchers have developed a new therapeutic agent from Brazilian lapacho tree bark that targets acute myeloid leukemia cells while minimizing toxic effects on healthy cells. The compound is attached to an antibody that binds specifically to cancer cells, delivering the drug directly to its target.
Rensselaer researchers will use a five-year grant to develop novel inhibitors of the SARS-CoV-2 virus's CLpro and PLpro proteases. The team aims to create an orally bioavailable drug that can be administered at home, with the potential for improved antiviral activity when combined with other drugs like remdesivir.
A study published in Journal of Pharmaceutical Analysis found that the quality of mistletoe, a traditional Chinese medicine, is affected by its host plant. The researchers used metabolomics to investigate the influence of host plants and environmental factors on mistletoe's medicinal qualities. The results show that both host plants an...
A new study suggests that supplementing a diet with Ascidiacea, also known as sea squirts, reverses some main signs of aging in animal models. The researchers found that plasmalogens, vital to body processes, decrease with age and contribute to neurodegenerative diseases like Alzheimer's and Parkinson's.
Researchers developed a deep learning-based model to predict drug-drug interactions using gene expression data. The DeSIDE-DDI model can identify potentially dangerous pairs and act as a drug safety monitoring system, helping establish the correct usage of drugs in the development phase.
Professor Holger Frey's innovative research aims to preserve PEGylation benefits while avoiding immune system recognition. His project RandoPEGMed seeks to create modified polymers for medicinal agents, potentially solving the problem of increasing antibody resistance.
Researchers at Aarhus University have developed improved DNA nanostructures that can assemble biomolecules with multiple functions, increasing the effectiveness of cancer treatment. The new structures are more stable, non-toxic, and immune system-friendly than previous versions.