Research on the molecular targets that drugs act on. Covers new antibiotic mechanisms, drug discovery competitions, bile-acid pathways, and Alzheimer's targets.
A University of Colorado Boulder study suggests that existing PARP inhibitors for hereditary breast and ovarian cancers may not work as intended. The research reveals a previously unknown interaction between the PARP protein and HPF1, which could lead to more effective treatments by targeting this co-protein.
A new study from Boston University School of Medicine has discovered a drug that can inhibit the growth and spread of melanoma in human cells and experimental models. The researchers found that this drug acts through a specific pathway to prevent cancer cell growth and metastasis.
A team of international researchers found that certain FAK inhibitors remain bound to the protein for a long time, causing a structural change that inhibits cancer cell mobility. Computer simulations predicted the kinetics of binding well, allowing for more accurate simulation of drug dissociation rates.
Researchers found that nitisinone is toxic to tsetse flies but harmless to pollinator insects. The study suggests using the approved drug as an eco-friendly strategy to control trypanosomiasis transmission.
OHIO researchers have identified a potential target for anti-viral drugs to battle COVID-19 by disrupting the viral RNA's ability to reproduce. The team found that a specific section of the RNA, called stem-loop II motif, is highly conserved and essential for the virus's replication.
A new drug targeting enzymes involved in myristoylation has shown promise in treating both breast and blood cancers. Researchers found that patients with specific enzyme NMT2 were more likely to die, and the drug slowed tumour growth by 90% in mice with human breast cancer.
A new nasal spray delivery method promises relief from antipsychotic medication's adverse side effects by delivering medication directly to the brain. This approach could reduce required doses by as much as three quarters, sparing patients from debilitating side effects and improving treatment efficacy.
Scientists at Wits University infected mosquitoes with human malaria and identified a new chemical compound that shows promise in treating the disease. The study, published in Nature Communications, aimed to develop a drug that can block both human-to-mosquito transmission and mosquito-to-human transmission.
A new study stratified tumors into 112 subtypes and found Master Regulator proteins control the transcriptional state of each subtype. Targeting these proteins with novel drug classes could benefit a larger fraction of patients. The analysis identified 24 Master Regulator modules, mechanistically controlling cancer cell survival.
Researchers found that decreased activation of gene LEF1 disrupts neuronal function and promotes hyperexcitability in brain cells, a hallmark of bipolar disorder. Increasing LEF1 expression may lead to new drug targets and biomarkers for lithium nonresponsiveness.
Researchers developed a novel method to discover ligands and inhibitors against membrane proteins, which are challenging to target. The method uses DNA-programmed affinity labelling and boosting sequences to improve screening specificity and abundance.
Researchers at UTHealth have discovered a gene signaling pathway linked to schizophrenia using human-induced pluripotent stem cells. The PI3K/GSK3 pathway was found to be dysregulated in neurons from patients with schizophrenia, with SGK1 inhibitor being associated with the condition.
A new study has identified and characterized neurons that regulate nausea-like responses in mice, shedding light on the sensation of nausea. The findings reveal a division of labor between area postrema neurons, with different neuron types responsible for detecting and raising the alarm for various substances.
A study has identified five genes associated with severe COVID-19, which could lead to the development of new treatments. The genes, IFNAR2, TYK2, OAS1, DPP9 and CCR2, are involved in antiviral immunity and lung inflammation processes.
Scientists create peptide-oligourea hybrids that mimic natural peptide structures, enhancing drug efficiency and stability. The hybrids exhibit high binding affinities and resist proteolytic degradation.
Researchers are using cutting-edge technology to analyze immune cell interactions in lupus patients, identifying potential targets for new therapies. The Lupus Mechanisms and Targets Award will support innovative studies aimed at improving diagnostics and treatments for the disease.
Researchers have identified a population of brain cells in the amygdala linked to physiological arousal responses, which can drive symptoms of anxiety disorders. These findings suggest that targeting these neurons may lead to new treatments for psychiatric illnesses.
A novel drug target has been identified for neonatal and infant heart failure, a condition with no specific treatment. The target stimulates cardiac contractility in newborns and infants with minimal side effects, offering new possibilities for pediatric heart failure treatment.
The December special issue of SLAS Discovery focuses on drug discovery efforts for COVID-19, including reviews on repurposing drugs and testing novel proteins necessary for virus replication. The issue also includes articles on the efficacy of existing treatments and potential off-label candidates.
Researchers at Michigan State University have identified a potential genetic target for treating an especially painful and invasive form of endometriosis. They discovered that targeting super-enhancers, altered by a mutation in the ARID1A gene, could lead to effective treatment using epigenetic therapy.
Researchers have identified a unique population of CD38hiCD127- CD8 T cells in patients with checkpoint inhibitor-induced arthritis, which are both cytotoxic and proliferating. This discovery could lead to the development of targeted treatments for this side effect.
Researchers discovered that overexpressing protein kinase A (PKA) improves muscle resistance to fatigue in mice by suppressing FoxO proteins and increasing oxidative potential. This study offers a potential solution for treating atrophy and promoting muscle growth without severe side effects.
Researchers have discovered a potential broad-spectrum anti-viral drug target by identifying how encapsulated viruses hijack the protein manufacturing and distribution pathways in cells. This approach offers an attractive alternative to developing individual drugs for each virus, with the same compound targeting multiple viruses.
Centenary Institute scientists discovered that two key proteins involved in blood clotting and immunity exist in multiple disulphide-bonded states. This finding has significant implications for drug development and the fight against disease, as different states of a protein may bind more or less preferentially to drugs.
Professor Robert Prud'homme at Princeton University has been awarded the inaugural Dean for Research Award for Distinguished Innovation for his invention of flash nanoprecipitation, a technique that promises to improve drug delivery. The award recognizes Prud'homme's innovative approach to solving critical challenges in society.
Researchers at Michigan State University have developed a deep learning model to predict the binding sites of known protease inhibitors targeting the SARS-CoV-2 main protease. The model can help drug developers prioritize promising candidates and save time and money in the early stages of drug development.
A real-time tracking system reveals a 15% increase in suspected opioid overdose deaths and a 29% rise in naloxone rescue attempts by EMS since March, coinciding with the pandemic's peak. The System for Opioid Overdose Surveillance (SOS) helps first responders target their efforts and provides critical data for public health authorities.
The D3Targets-2019-nCoV webserver uses molecular docking to predict potential drug targets for SARS-CoV-2 and identifies lead compounds via multi-site docking. The server incorporates various features, including correlated conformations and binding sites, making it a valuable tool for medicinal chemists and clinicians combating COVID-19.
A study published in the Journal of Experimental Medicine identified PKM2 as a critical enzyme involved in immune cell differentiation and exacerbation of inflammation in autoimmune diseases. The findings suggest that targeting PKM2 could lead to more effective treatments, reducing symptoms by over 50%.
Researchers mapped host interactions of MERS-CoV, SARS-CoV-1 and SARS-CoV-2 to identify potential drug targets. Studying patient data showed that COVID-19 patients treated with drugs targeting specific host factors fared better.
Researchers at Purdue University have developed a new type of microrobot that can navigate through the rough terrain of a human colon, enabling potential targeted drug delivery without causing side effects. The microrobots use magnetic fields to tumble and move through the colon, allowing for controlled release of medication.
Researchers have found that a virus-mimicking drug can make certain stealthy melanoma tumors visible to the immune system, allowing for better targeting by immunotherapy. The findings open up new possibilities for personalized therapies in hard-to-treat cancers.
Researchers discovered a potential way to prevent long-lasting brain damage in newborn children by targeting the histamine H2 receptor. A protein known as the histamine H2 receptor inhibits the formation of mature oligodendrocytes, leading to improved recovery from hypoxia-ischemia in mice treated with cimetidine.
Recent advances in nonhormone therapy provide women with more options for managing hot flashes. The new treatments target the KNDy neuron complex, which is activated during menopause, resulting in hot flashes. These innovations include drugs developed for pain control and mood disorders acting via KNDy.
Researchers have made significant breakthroughs in understanding the biology of schistosomes, a parasitic flatworm that causes schistosomiasis. By identifying key vulnerabilities, scientists hope to develop new treatments for this deadly disease, which affects up to 250,000 people annually.
Researchers at Arizona State University have developed a method to examine proteins in keen detail, using surface plasmon resonance (SPR) and innovative microscopy techniques. This new technique resolves single molecules, including proteins, with high sensitivity.
Researchers have developed a comprehensive analysis pipeline using genetic prediction of protein levels to prioritize drug targets. This approach has quantified the potential for reducing drug development failure rates and could help identify novel drug targets.
A study analyzing nearly 900 kidney cancer patients identified novel biomarkers and gene signatures associated with treatment response. These findings could help personalize treatments for patients based on their individual tumor characteristics.
A new algorithm called Ohm predicts allosteric sites in proteins using their structure, which can aid in protein engineering and drug design. The tool may help reduce unintended side effects caused by drugs targeting similar proteins.
A study published in the New England Journal of Medicine found that JAK inhibitors improved developmental milestones in patients with AGS, a rare genetic disorder. The treatment showed promise in improving neurological function, particularly in children who received higher doses.
Researchers from Brigham and Women's Hospital have discovered that senolytic drugs can rejuvenate older organs, reducing inflammation and improving survival rates. The study suggests that these drugs could help close the gap between organ demand and supply, benefiting patients on transplant waitlists.
Researchers at Aarhus University have developed a new equation to describe the activity of enzyme cascades in cells. This breakthrough could lead to a better understanding of how enzymes control cellular signaling and potentially improve drug development for cancer treatment.
Researchers successfully inhibited the P2X4 receptor, which plays a significant role in post-stroke damage and recovery. The study shows that short-term inhibition of this receptor can regulate immune cell activation and improve both acute and chronic stroke recovery.
Biomedical scientists have discovered that diethylcarbamazine directly targets parasitic worms with a temporary paralysis, allowing the host's body to flush out the parasites. This breakthrough could lead to better predictability of resistance development and more effective treatment outcomes for patients.
Researchers at the University of Chicago used computational analysis to identify ebselen as a potential treatment for COVID-19. The study found that ebselen can decrease Mpro's activity in two different ways, making it a promising lead for developing new therapeutic strategies against the virus.
Researchers propose a treatment paradigm targeting leukotrienes, which play a key role in severe COVID-19 cases. The proposed combination of zileuton and montelukast could help reduce inflammation and prevent pulmonary edema.
A new study suggests that repurposing cancer drugs to target human enzymes could lead to effective treatments for COVID-19, while reducing the risk of drug resistance. This approach has the potential to save years of research and millions of dollars in development costs.
Researchers at Sanford Burnham Prebys aim to develop new therapies for schizophrenia, depression, anxiety and substance abuse by identifying potential drug targets in 'orphan' receptors. The team has created an innovative platform called LIFT to screen small molecules and validate these receptors as bonafide drug targets.
Researchers found that beta2-adrenergic receptors in brown fat cells stimulate thermogenesis, a process that burns calories and improves insulin sensitivity. The discovery could lead to new treatments for obesity and type 2 diabetes.
Researchers at UNH identified rare base-flipping events in an RNA virus that could be used to develop new treatments. The study provides insights into how viral RNAs interact with inhibitors, which could lead to the design of better drugs.
A new study has pinpointed the specific brain cells responsible for triggering sugar cravings and overconsumption. The research, led by Matthew Potthoff and Matthew Gillum, reveals that fibroblast growth factor 21 (FGF21) acts on glutamatergic neurons to lower sugar intake and sweet taste preference.
UQ researchers have solved a 50-year-old enzyme mystery, revealing the complete structure of an essential amino acid synthesizing enzyme. This discovery could lead to the development of new herbicides and antimicrobial agents, potentially restoring effective treatment options for infections such as tuberculosis and invasive Candida.
A team of researchers has discovered a new role for a tiny linker in regulating transmembrane ion channels, which could lead to new targets for drugs and treatment in conditions such as hypertension and autism. The study found that the linker plays a more active sensing role than previously thought.
Researchers found that hyperactive immune cells aggravate heart valve disease by activating harmful inflammation due to shear stress. The study identified a potential drug target, Piezo-1, and showed that replacing the aortic valve has an anti-inflammatory effect.
UTEP research reveals a new target for tuberculosis drug development by investigating the mechanisms of Mtb pathogenesis and discovering that Nα-acetylation of EsxA drastically affects the course of infection. The study provides a beautiful story in the prestigious Journal of Biological Chemistry.
Researchers identified seven clinically approved antiviral drugs that could disrupt the mechanisms of SARS-CoV-2 replication and infection. These drugs target kinases, which are potential targets for treating COVID-19, and may alleviate exaggerated inflammatory symptoms.
Scientists discovered a cell signaling pathway that could lead to new treatments for tuberous sclerosis complex, a neurological disorder causing non-cancerous tumors and epilepsy. The heat shock protein cascade restored normal mTOR activity in TSC cells, offering potential drug targets.
A new class of precision medicine targeting cancer's ability to repair its DNA has shown promising results, with half of patients experiencing tumor growth halt. The drug works by stopping cancers from repairing DNA damage and is particularly effective when combined with chemotherapy.
Researchers have found that certain cancer therapeutics concentrate within cells' tiny functional compartments called organelles, known as condensates. This discovery could lead to a new toolset for drug development by tailoring chemicals to seek out and concentrate in specific droplets.
Researchers have gained detailed insights into how a key protein receptor interacts with GABA, providing a clear target for new therapeutic drugs. The study's findings offer promise for improved treatments of neurological disorders such as epilepsy and muscle spasticity.