Articles tagged with Medicinal Chemistry
A team of researchers has uncovered a promising new target for antimalarial drug design, identifying an enzyme called aminopeptidase P from the Plasmodium falciparum parasite. The new inhibitors have been shown to bind more strongly and selectively than existing compounds, demonstrating potential as a new class of drugs to combat malaria.
Scientists at the University of Virginia Health System have developed a suite of AI-powered tools, called YuelDesign, YuelPocket and YuelBond, to transform how new drugs are created. These tools can design drug molecules tailored to fit their protein targets exactly, even accounting for protein flexibility.
Researchers have created a novel monomer that allows for the synthesis of poly(disulfide)s with arbitrary side-chain structures through domino polymerization. The polymers exhibit degradability in reducing environments, including biological systems, making them suitable for drug delivery systems and medical applications.
Researchers developed a machine-learning system that predicts how molecules form, cutting lab work time from months to days and reducing costs. The system uses asymmetric cross-coupling reactions to build complex compounds and can be applied across fields, deepening our understanding of chemistry.
Researchers have identified tyrosine phosphatase 1B (PTP1B) as a key molecular target in immunogenic cell death (ICD), a type of regulated cell death that activates the immune system against cancer cells. Two platinum-containing compounds, Pt-NHC and PlatinER, trigger ICD by blocking PTP1B's enzymatic activity.
Researchers have developed a bacterial system to create millions of potential drug molecules that can target difficult-to-treat cancers. The approach combines chemical peptide stabilisation with the TBS assay to screen for effective peptides, which can then be tested in more complex tissue models and animal studies.
Southwest Research Institute expands manufacturing capabilities to produce safer antidotes to organophosphorus nerve agents and pesticides. The new technique avoids cancer-causing compounds during synthesis of oxime antidotes, supporting kilogram-scale manufacturing for domestic supply and reducing supply chain risks.
Researchers developed antibody–drug conjugates that combine CD4 mimic and neutralizing antibodies to target HIV entry, showing seven times better efficacy than existing approaches. The strategy aims to block HIV before it enters the host cell, offering a more targeted therapeutic profile and potentially reducing adverse effects.
Researchers investigated the binding thermodynamics of doxepin geometric isomers to the histamine H1 receptor, revealing differences in enthalpy and entropy contributions. The study highlights the importance of considering conformational constraints in designing ligands with optimized thermodynamic properties.
Researchers discovered that mycosporine-like amino acids (MAAs) can block a key enzyme involved in blood pressure control and offer antioxidant effects. MAAs are naturally occurring compounds found in algae and cyanobacteria, which also act as natural sunscreens.
Researchers have demonstrated that Janus nanoparticles can disrupt drug-resistant bacteria's defenses, restoring the effectiveness of conventional antibiotics. The approach uses nanoparticles to create pores in bacterial membranes, allowing antibiotics to flood in and execute their killing function.
Computational analysis reveals two strategies: stealthy plasmids pick up new genes first, while manipulative plasmids help them spread rapidly. This 'stealth-first' process can aid in predicting future resistance threats and tracking their emergence.
Polysaccharide-based microneedles have been shown to effectively deliver anti-cancer agents directly into the skin, targeting rich networks of immune cells. The microneedle matrix itself can also modulate these immune cells, creating a powerful dual-action therapy.
Researchers develop experimental drugs that encourage mitochondria in cells to work harder and burn more calories. The findings offer a framework for designing safe and effective weight-loss treatments with potential benefits for metabolic health and neurodegenerative diseases.
In a new study, Northwestern scientists identified a previously unknown toxic sub-species of amyloid beta oligomers that drive brain changes in Alzheimer's disease. NU-9 decreased this toxin and reduced damage in a mouse model, suggesting it could prevent or delay the cascade of toxic events that destroy neurons.
Researchers have discovered a novel natural compound, β-glucose-bound hydroxy mycosporine-sarcosine, produced by thermophilic cyanobacteria that can provide UV protection. The compound's unique biosynthesis pathway and chemical modifications contribute to its enhanced antioxidant potential.
Researchers from Tokyo University of Science developed an efficient strategy to synthesize PROTACs using a three-step click chemistry method. This approach rapidly assembles functional molecules, enabling the easy introduction of ligand components and probe functionalities.
Acute sepsis alters fluid kinetics and creates a 'third space' resistant to adrenergic modulation, leading to maldistribution of crystalloid fluid. Vasoactive drugs have limited effect on fluid distribution in septic sheep compared to healthy animals.
Researchers will examine protein stability mechanisms in Thermus thermophilus to advance treatments for diseases such as Alzheimer's, ALS, and cancer. The team will explore the structure of Rieske proteins and their role in energy production to understand how to restore stability.
Astrocytic glutamine synthetase plays a key role in regulating glutamate signaling, contributing to nicotine-induced brain changes and locomotor sensitization. A custom-designed peptide inhibits this process, demonstrating the importance of astrocyte communication in nicotine addiction.
Researchers at the University of Virginia Health System have developed a new treatment for acute myeloid leukemia, a deadly form of blood cancer. The FDA-approved medication works by disrupting cellular protein interactions that drive leukemia cell growth and survival, offering patients a potential cure.
Researchers at Martin Luther University Halle-Wittenberg develop PROTAC molecule MA203, specifically binding to tumor protein CHK1, leading to its breakdown in cancer cells. This triggers a chain reaction destroying other tumor proteins, ultimately killing the cancer cells.
The Alliance for Clinical Trials in Oncology will host a public webinar showcasing key findings from the 2025 ASCO Annual Meeting. Researchers will discuss latest information on colorectal, squamous cell, and renal cell cancers.
A new study published in Clinical Chemistry and Laboratory Medicine has developed a practical tool to support harmonization and quality improvement in vitamin D testing. The multicentre study evaluates the measurement uncertainty of various 25-(OH)D assays and their ability to detect physiologically relevant changes over time.
Researchers analyzed 5 years of Yellow Card data on 13 drugs containing fluorine and found no significant correlation between fluorine content and adverse drug reactions. The study suggests that the way a drug acts is more likely to result in an adverse reaction, rather than the presence of fluorine.
Researchers at Beijing University of Chemical Technology developed a new reconfigurable information code using macroscopic hydrogels that respond to external stimuli. The system can store over 800 billion distinct configurations, opening up potential applications in smart labels, biomedical tags and secure data encoding.
A new treatment for corneal scarring is being developed by University of Houston optometry researcher Tarsis G. Ferreira. The treatment uses a natural protein called decorin to block scarring and unwanted blood vessel growth, offering hope for people with injured corneas.
Researchers at Shibaura Institute of Technology have developed a scalable and safer method to generate hydrogen fluoride, eliminating the need for pressurized HF gas and corrosive liquid reagents. The new fluorinating complexes can be used for pharmaceuticals, functional materials, and molecular probes.
Researchers at King's College London used cryo-electron microscopy to study the flagellum in unprecedented detail, revealing its architecture and identifying potential drug targets. This breakthrough could lead to the development of new treatments for bacterial infections without driving resistance.
A study from Waseda University reveals distinct differences between enantiomeric and racemic thalidomide crystals, with asymmetric and uniform thermal responses attributed to dimer symmetry. This research provides insights into chiral compound behavior and supports rational drug design.
Researchers review nanozymes derived from Chinese herbs, including their catalytic properties, biomedical applications, and potential challenges in developing herbzymes for practical use. The review highlights three main types of herbzymes: herb carbon dot enzymes, polyphenol-metal nanozymes, and herb extract nanozymes.
Researchers discovered novel small-molecule inhibitors targeting the WDR5-MYC protein-protein interaction, demonstrating improved inhibitory activity compared to reference compounds. The lead compound, 9c-1, showed a 35-fold enhancement in activity and sub-micromolar binding affinity.
The Center for Research Innovation in Biotechnology (CRIB) has developed a comprehensive database of active pharmaceutical ingredients with evidence of clinical testing. The database provides valuable information on drug discovery and development, including pricing, sponsors, and intended clinical applications.
Researchers developed a topical antibiotic gel that cured middle ear infections in chinchillas within 24 hours. The gel, containing negatively charged liposomes, was more effective than previous formulations in delivering antibiotics across infected eardrums.
Researchers at Northwestern University propose a new approach to therapeutic development using structural precision in nanomedicine. By fine-tuning the interaction between nanomedicines and the human body, scientists can design interventions that are more effective, targeted, and beneficial for patients.
A UT Health San Antonio-led discovery could redefine drug discovery by turning IV medications into orally administered treatments for brain cancer, Alzheimer’s disease, and other complex conditions. The new strategy uses a protein receptor called CD36 to efficiently deliver large molecules into cells.
Insilico Medicine's Pharma.AI Day 2025 will showcase the latest AI breakthroughs and updates, including precision target discovery engine PandaOmics and generative biologics platform Generative Biologics. The company aims to accelerate drug discovery and advance life sciences research with its proprietary platform.
University of California researchers developed a new drug, JRT, with reduced hallucinogenic potential compared to LSD. The compound has shown promise in treating the negative and cognitive symptoms of schizophrenia, including anhedonia and cognitive function.
A recent study reveals that tropical forests are home to an incredible diversity of chemical compounds, including terpenoids and alkaloids, which could have practical implications for human health. The researchers found that tree species in higher elevations tend to use similar chemicals to protect themselves from enemies.
Researchers created an anchoring-borrowing strategy to form artful single-atom catalysts, overcoming traditional oxidative addition steps in cross-coupling reactions. The new catalysts achieve high yields, excellent stability, and set a benchmark for turnover numbers.
Acta Pharmaceutica Sinica B publishes original research articles and reviews on pharmaceutical sciences, including a retrospective cohort study on elderly COVID-19 patients and the use of machine learning to predict cytotoxicity, as well as studies on liver regeneration and cancer immunotherapy.
Four UTA faculty members - Cameron, Dias, Shiakolas, and Yuan - recognized by the National Academy of Inventors for their outstanding research discoveries. Their innovations have made a tangible impact on society through patents, licensing, and commercialization.
A comprehensive review article highlights emerging strategies that enable environmentally benign coupling reactions, reducing reliance on rare metals and lowering energy consumption. The hypervalent iodine approach facilitates selective bond formation with high functional group tolerance and broad substrate scope.
Xiamen University has joined the Bentham Science Institutional Membership Program to enable researchers to publish Open Access at concessionary rates in Bentham Science journals. The program promotes open research and fosters scientific advancements globally.
A new consensus paper emphasizes the role of bone turnover markers (BTMs) in diagnosing and managing osteoporosis. BTMs, such as procollagen type I N propeptide (PINP) and β-isomerized C-terminal telopeptide of type I collagen (β-CTX-I), are invaluable tools for predicting fracture risk and monitoring treatment adherence.
Avelino Corma, John Hartwig, and Helmut Schwarz received the BBVA Foundation Frontiers of Knowledge Award for their fundamental advances in catalysis. They have improved efficiency and reduced energy consumption in various industrial processes through their innovative catalysts.
Researchers uncovered two electron-transfer mechanisms producing hydroxyl radicals, crucial in atmospheric chemistry. The findings reshape our understanding of acid-base chemistry and have implications for air quality, climate science, and biomedical processes.
A new technology called in vivo antibody painting enables sustained weight loss and prolonged blood sugar management with a lower dose of GLP-1 receptor agonist. The system, developed by MIT professor Bradley Pentelute, attaches peptides directly to antibodies, overcoming the limitation of peptide degradation.
Researchers at Indiana University and Wuhan University developed a novel light-driven reaction to produce tetrahydroisoquinolines, a crucial group in medicinal chemistry. This approach enables the creation of new structural patterns in molecules, offering a more efficient way to make complex compounds.
Researchers at the University of Texas at El Paso have developed a portable, blood-based device that can detect colon cancer using a biomarker called CCSP-2. The device has the potential to provide early detection and treatment options for this second-deadliest US cancer, making it a significant advancement in colorectal cancer screening.
Dr. Ronald Newbold has been appointed as the permanent CEO of Empire Discovery Institute (EDI), a non-profit drug discovery and development accelerator. With over 30 years of business development experience, Dr. Newbold will lead EDI's growth and expansion, including the addition of new programs and partnerships.
Researchers used X-ray light to analyze the structure of 2-thiouracil, a substance with medically relevant properties. The study found that UV radiation causes the molecule to bend, resulting in the protrusion of the sulfur atom and making it reactive.
Richard Willson, a University of Houston professor, has been elected Fellow of the Royal Society of Chemistry for his contributions to the chemical sciences. He has developed innovative methods to detect viruses and other biological threats using glow-in-the-dark nanoparticles.
Researchers have developed a palladium-mediated reaction to precisely modify peptides and proteins, overcoming challenges in bioconjugation. The method targets dehydroalanine-containing peptides and proteins, enabling efficient synthesis of structurally unique peptides.
CrySyst's QbC framework addresses crystallization monitoring, modeling and control using research from Purdue University. The software provides guided experiment selection, semiautomated model development and reliable solutions to reduce time and material usage.
Researchers from NUS have pioneered a new catalytic transformation that converts epoxides into fluorinated oxetanes, a coveted class of drug molecules. The discovery potentially opens the door to new medicines and offers a reliable route to incorporate these motifs into the design of novel small-molecule therapeutics.
A team from Tokyo University of Science developed a novel trivalent platform for triple click chemistry, allowing for the efficient synthesis of complex compounds. The approach utilizes simple initial materials and promotes sustainable pharmaceutical synthesis.
Biomedical engineers at Duke University have developed a new technique that traps together cellular machinery to increase protein production rates. This approach uses synthetic disordered proteins to form compartments called biological condensates, which enhance the rate of protein production by bringing together biomolecular machinery...
Researchers at UC Davis have successfully synthesized ibogaine and its related compounds using a new, efficient method. The study's findings suggest that these analogues may be useful in treating substance use disorders and other conditions, and highlight the potential for safer and more effective medicines.
Daniel Armstrong, a renowned UTA chemist, has been honored with the prestigious 2025 Pittcon Analytical Chemistry Award for his pioneering work in analytical chemistry. His research focuses on developing new approaches to identify chiral disease biomarkers, peptide epimers, and isotopic compounds.