The SLAS Discovery Editor's Top 10 for 2022 showcases articles on COVID-19 drug discovery, 3D organoid systems, and treatments for diseases such as autism spectrum disorder and obesity. These top articles demonstrate the impact of high-throughput screening approaches and innovative technologies in advancing scientific collaboration.
A new protein degrader, AK-2292, shows promise against STAT5, a key player in leukemia and other cancers. By targeting the protein's degradation, researchers have overcome previous challenges in designing small molecule inhibitors.
The 6th Annual Meeting of the Labroots Drug Discovery & Development Virtual Event Series will bring together specialists to discuss ongoing research in drug discovery and development. Keynote speaker Professor Kevin Pfleger will present novel pharmacology findings, while attendees can earn free CE credits.
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A new experimental contraceptive drug has been developed by Weill Cornell Medicine investigators, demonstrating the possibility of an on-demand male contraceptive. The study found that a single dose of the sAC inhibitor TDI-11861 temporarily stops sperm movement and prevents pregnancies in preclinical models.
Researchers from Tokyo University of Science discovered β-damascone, a natural aroma compound found in rose fragrance, modulates dendritic cell functions and reduces inflammatory cytokine production. The study showed β-damascone inhibits antigen-dependent activation and Th1 cell development, as well as ear inflammation in mice models.
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.
A new analysis of NETosis from Dompé farmaceutici puts a spotlight on neutrophils in carcinogenesis. Neutrophils' behavior is modulated by extracellular vesicles and interleukin-8, leading to tumor progression and drug resistance. Targeting IL-8 and EVs may lead to novel drugs to regulate neutrophil biology.
Eleni Tomazou's project aims to create in vitro and in vivo models of pediatric sarcomas to accelerate drug discovery and precision medicine. Her work could lead to a significant impact on the treatment of these deadly cancers.
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UC San Diego scientists developed an AI-based strategy for discovering high-affinity antibody drugs, identifying a new antibody that binds 17 times tighter than an existing one. The approach accelerates the discovery process, reducing failure rates and enabling faster development of novel cancer and COVID-19 treatments.
Researchers have identified a new class of potent antimalarial compounds that target the parasite's sexual phase, preventing it from infecting mosquitoes and subsequently humans. The compounds inhibit the parasitic protein Pfs16, forming the strongest bond with the drug.
Researchers uncover how changing trends in interorganizational deals in the pharmaceutical industry are improving drug discovery and R&D productivity. The study found that M&A-related deals drive revenue growth for large pharmaceutical companies, and academia-owned spinouts of advanced technology are increasing.
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.
Researchers at Rice University have developed a multiplex base-editing platform that significantly improves the pace of new drug discovery by inducing fungi to produce more bioactive compounds. The technique has been deployed as a tool for mining fungal genomes for medically useful compounds, reducing research timeline by over 80%.
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Researchers at UC San Diego School of Medicine identified a novel molecular pathway that causes gout and its progression to joint tissue erosion. The findings position lubricin as a novel therapeutic target for both the prevention and treatment of the disease.
Medical University of South Carolina researchers develop a novel LSD1 inhibitor that shows early promise at fighting neuroblastoma when paired with bortezomib. The combination boosts anti-tumor response and is a viable strategy for targeting high-risk MYCN-amplified neuroblastoma.
A retrospective cohort study of 1,404 subjects with type 2 diabetes found that metformin use reduced the risk of delirium by 50% and decreased 3-year mortality rates. The study suggests that metformin may be a potential benefit for patients with diabetes, particularly in reducing age-related disorders such as dementia.
Researchers from City of Hope identified how a protein receptor targeted by 33% of all federally approved medications works. This discovery could facilitate pharmaceutical research and lead to the creation of innovative medicines with fewer side effects.
Researchers developed an integrated approach to accelerate drug discovery by combining complex datasets from two screening platforms and next-generation metabolomics analysis. The new framework identified known compounds, confirmed mechanisms of action, and discovered novel compounds with unique biological signatures.
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Scientists used AI-driven PandaOmics platform to analyze gene expression datasets from DNA repair diseases, identifying biomarkers associated with treatment response. The study focused on genes that stratify cancer patients by survival outcomes, providing potential targets for personalized therapies.
Researchers at the University of Texas at Dallas have developed a computer-based platform for drug discovery using topological data analysis. The approach allows for virtual screening of thousands of compound candidates, narrowing them down to the most promising ones for laboratory and clinical testing.
Researchers at UC San Diego School of Medicine identified PKCα as a potential therapeutic target for Alzheimer's disease. The study found that a subtle increase in PKCα activity was sufficient to produce biochemical, cellular and cognitive impairments in mice, similar to those observed in human AD.
University of Copenhagen researchers made a groundbreaking discovery about the mammalian brain, finding that a vital enzyme that enables brain signals is switching on and off at random intervals. This challenges the long-held assumption that these enzymes are active at all times to convey essential signals continuously.
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The National Institute of Allergy and Infectious Diseases has awarded over $12 million to three institutions for the development of antiviral therapies against pandemic viruses. The funding will support the optimization, development, and clinical testing of promising antiviral candidates.
Scientists at KAUST have identified dynamic regions, called cryptic binding sites, that can be targeted by drugs to treat cancer. The study reveals how molecular motion influences ligand binding to BTB domains, a critical part of many proteins involved in disease.
Researchers at the University of Houston have developed a protocol to reprogram human heart cells into specialized cells that conduct electricity, enabling rhythmic heartbeat and repair diseased hearts. The discovery could lead to improved cardiac function and new pharmacological therapies for heart diseases.
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A recent study found that most Antarctic species' chemical compounds can repel amphipod predators but are ineffective against hermit crabs, which could decimate local populations. This highlights the vulnerability of Antarctic ecosystems to invasive species and underscores the importance of long-term research on the seafloor.
Researchers at University Hospitals and Case Western Reserve University have discovered a small-molecule oral drug that reduces PCSK9 levels and lowers cholesterol by 70% in animal models. This breakthrough could also improve the efficacy of cancer immunotherapies.
Carrying out scientific experiments in space enables faster drug discovery due to lower gravity, speeding up the development of complex medicines. Protein crystallization experiments have been instrumental in designing cancer drugs, while studying aging treatments could lead to breakthroughs in stem cell therapy.
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A research team developed a vaccine targeting synthetic opioid fentanyl to block its entry into the brain, preventing fatal effects. The breakthrough could have major implications for treating Opioid Use Disorder, with potential relapse prevention capabilities.
Researchers found that MK256 induced differentiation and maturation in leukemia stem cells, inhibiting proliferation of AML cell lines. The study also showed dose-dependent inhibition of the STAT pathway in both in vitro and in vivo studies.
Researchers found histamine releases HMGB1 in vascular endothelial cells, leading to severe symptoms. Administering anti-HMGB1 antibody attenuated hypotension and improved recovery rates.
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.
A comparison of two cancer drugs reveals that life cycle management strategy is crucial for a drug's commercial success. The research found that product sales are closely linked to the number of approved indications and inter-organizational alliances.
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Researchers aim to use quantum computer-based AI to accelerate drug discovery, cutting costs and time by exponentially increasing processing power for complex problems. Quantum AI models have higher capability to approximate desired functionality compared to classical neural networks.
A new study in Cell Systems explores the benefits of using multiple data types in drug discovery. Gene expression and cell morphology provide complementary information for drug prioritization, advancing drug discovery, functional genomics, and precision medicine.
Researchers have developed a novel method for antibiotic resistance testing that can analyze bacterial cells in real-time, allowing for faster identification of susceptible and resistant bacteria. This breakthrough technology has the potential to transform microbial screening in clinical and research labs.
Scientists at the University of Florida have identified two small molecules that inhibit precancerous cell progression and reverse a key process involved in pancreatic cancer progression. This discovery could lead to earlier treatments and improved survival rates for patients with pancreatic cancer.
A new AI model called CODE-AE can accurately predict the efficacy of novel drug compounds in humans, addressing a major challenge in drug discovery. The technique has been shown to improve accuracy and robustness over state-of-the-art methods, with potential applications in personalized medicine.
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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.
Researchers have identified a previously unknown biological contributor to postpartum depression: impaired autophagy, which limits the body's ability to clean up old genetic material. This finding may lead to new treatments and early identification of women at risk before they become ill.
A new drug, NMT5, has shown promising results in blocking SARS-CoV-2 infection in animals. The drug coats the virus with chemicals that temporarily alter the human ACE2 receptor, preventing it from infecting cells. In cell culture experiments, the Omicron variant of SARS-CoV-2 was prevented from attaching to human ACE2 receptors by 95%.
Using artificial intelligence, researchers from Tufts University have devised rules for faster and more effective identification of potential new drug cocktails against tuberculosis. The study developed a set of design principles to assemble drug combinations, reducing the amount of testing needed before moving to further study.
Researchers at Tokyo Medical and Dental University identified a compound LAMZ that stimulates muscle cell growth, reduces bone resorption, and promotes bone formation. Administered to mice with locomotor frailty, LAMZ improved muscle and bone health.
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Researchers at Nagoya University have discovered a new treatment for type 1 diabetes that uses leptin to improve insulin-alternative effects in mice. The combination of leptin and a PTP1B inhibitor normalizes blood glucose levels without the need for insulin, reducing hypoglycemia risk.
Researchers found that mTOR inhibition is crucial for p53-mediated tumor suppression, delaying cancer and increasing lifespan. In the absence of mTOR inhibition, cancer-promoting senescent cells drive tumor growth.
A new study from MIT reveals that computer models predicting molecular interactions, like AlphaFold, need improvement to help identify drug mechanisms of action. Researchers improved the performance of these models using machine-learning techniques, but more work is needed.
A KAUST-led research team identified two drug treatments that boost the activity of molecules involved in cell adhesion, enhancing the ability of blood-forming stem cells to enter the bloodstream and produce new blood. This breakthrough could lead to improved bone marrow transplant success for leukemia patients.
Researchers have successfully engineered human immune cells to model an infection common among immunocompromised people, paving the way for new drug testing and treatments. The immune cell type created played a key role in infection, inflammation, and regeneration, but also served as a natural host for germs.
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A study by Japanese researchers from Fujita Health University sheds light on the molecular mechanisms of contact dermatitis, revealing that neutrophil extracellular traps play a key role in the condition. The team's findings suggest that inhibiting NET formation could be a new therapeutic strategy for treating contact dermatitis.
Researchers used x-ray crystallography to study the main protease of SARS-CoV-2 at various temperatures, revealing subtle conformational changes and potential targets for drug design. These findings may inspire the development of new antiviral drugs to counteract COVID-19 and prevent future pandemics.
A team of Chan Zuckerberg Biohub scientists developed a deep-learning method, dubbed
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.
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Researchers at VCU Massey Cancer Center have discovered a new target for treating high-risk neuroblastoma, a deadly pediatric cancer. A novel compound called SHP099 has shown promising results in shrinking tumors and killing cancer cells.
Researchers identified CUDC907 as a dual phosphoinositide-3 kinase/histone deacetylase inhibitor that promotes apoptosis in NF2 schwannoma cells. The compound reduced viability and induced cell cycle arrest in human merlin deficient Schwann cell models.
A new study from MIT and Broad Institute researchers analyzed interactions between nanoparticles and nearly 500 types of cancer cells, revealing thousands of biological traits that influence cell response. The findings could help tailor drug-delivery particles to specific types of cancer.
Researchers have identified 42 host cell proteins that contribute to the replication and spread of Lassa virus, a disease with high morbidity and mortality in Western Africa. One potential drug target, GSPT1, was found to be involved in viral-host interactions and showed antiviral activity against Lassa without cytotoxicity.
Researchers at University of California - San Diego launch nationwide clinical trial to investigate benfotiamine as a metabolic treatment approach for Alzheimer's disease. The trial aims to determine the effectiveness of high doses of benfotiamine in benefiting people with mild AD or mild cognitive impairment.
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Researchers at the University of Birmingham developed a new technique using mass spectrometry to analyze drug-protein interactions in real tissue samples. This allows scientists to predict the therapeutic effect of drugs earlier, enabling more effective treatment options.
Researchers found that men who lose their Y chromosome as they age are more likely to experience deadly heart scarring and earlier death. The study suggests an existing drug may help counteract the effects of this loss, potentially leading to longer, healthier lives for affected men.
Researchers have discovered pairing Spinraza with valproic acid (VPA) can boost its therapeutic effects without increasing toxicity. This approach allows for improved SMN protein production in SMA patients, leading to longer survival and better muscle function.
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