Articles tagged with Enzyme Inhibitors
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A multidisciplinary team at USC has developed selective compounds that inhibit an enzyme tied to brain inflammation in people at genetic risk for Alzheimer’s. The inhibitors preserve normal brain function and cross the blood-brain barrier, suggesting a promising therapeutic approach for neurodegenerative diseases.
Researchers found that blocking Caspase-2 enzyme in mice increased chronic liver damage and cancer risk as they aged. The study highlights the need for caution when targeting this pathway to treat fatty liver disease.
TGF-β inhibition holds promise for treating liver fibrosis by targeting SMAD-dependent and -independent pathways. Various therapeutic strategies, including direct blockade, receptor inhibitors, antisense oligonucleotides, and natural products from Traditional Chinese Medicine, are being explored to disrupt the TGF-β signaling pathway.
Researchers at IBEC are developing new techniques to study enzymes that erase microtubule modifications, which have shown promise as therapeutic targets. The goal is to understand these mechanisms and develop new treatments for cardiac and neuronal disorders.
Scientists from the University of Bath have identified two new families of chemical compounds that inhibit alpha-methylacyl-CoA racemase (MCR) in Mycobacterium tuberculosis, a key enzyme for TB survival. This breakthrough could lead to new treatments for TB and potentially other diseases like prostate cancer.
Scientists have discovered a novel way to block an enzyme involved in regulating blood pressure, called ACE. Ciprofloxacin binds selectively to a different site, blocking angiotensin I but not inhibiting the enzyme's other functions.
Researchers at University of Seville have discovered patulin and xestoquinol as inhibitors of DNA topoisomerase 1, a key enzyme in DNA metabolism. These natural compounds may provide a new class of anticancer drugs by preventing DNA cuts from being ligated.
The treatment demonstrated early signals of efficacy, with 65.7% of patients experiencing lasting stable disease, and was generally well-tolerated, with most adverse events being mild and manageable.
A new study at Stellenbosch University found that blocking the enzymes involved in glycolysis could cut off the malaria parasite's primary energy source and kill it. This approach has shown promise for developing new malaria drugs, particularly against resistant parasites.
Common prescription medications can disrupt sterol biosynthesis, potentially causing developmental disorders. The editorial highlights the need for mandatory sterol biosynthesis screening in clinical practice.
Researchers at Penn's School of Dental Medicine and Perelman School of Medicine found that ACE inhibitors can inhibit the activity of ACE2, a critical cardioprotective enzyme. This discovery has implications for human patients prescribed these medications, who may benefit from additional ACE2 treatment.
A novel compound ML233 inhibits melanin production with no significant toxic side effects, offering a potential new strategy for treating pigment-related skin conditions. The study demonstrates promising results in reducing melanin synthesis and proliferation of melanoma cells.
Researchers discovered senolytics can target Alzheimer's disease-associated brain enzymes AChE and BChE without affecting healthy ones. This selective approach may lead to safer treatments that improve memory and reduce inflammation in older adults.
Researchers at the Center for Redox Processes in Biomedicine have identified new inhibitors of h15-LOX-2, a protein involved in inflammatory and metabolic processes. These compounds may provide promising candidates for developing new drugs to boost studies on the enzyme's biological role.
Researchers developed CeSPIACE, a 39-amino-acid peptide drug candidate that binds to the spike protein, blocking viral entry. It demonstrates strong binding to major SARS-CoV-2 variants and shows efficacy against multiple strains in vivo and in vitro experiments.
PARP inhibitors have been found to be effective in treating cancers with BRCA1/2 mutations by blocking DNA repair pathways. The combination of PARPis with chemotherapeutic drugs can also improve treatment efficacy, increasing DNA damage and blocking repair processes.
Researchers have identified a new starting point for therapy by targeting SSAT enzyme in psoriasis, restoring regulatory T cell function and breaking inflammation cycle. This approach could lead to a promising alternative treatment option with fewer side effects.
Researchers developed a new method to search through billions of molecules to identify potential anti-inflammatory drug candidates. The method uses computer algorithms to explore vast chemical space and has the potential to speed up the costly drug development process.
A new compound, V-161, has been discovered to effectively inhibit the growth of vancomycin-resistant Enterococci (VRE) by targeting a crucial enzyme. The study reveals that V-161 not only disrupts the enzyme function but also reduces VRE colonization in the mouse small intestine.
Researchers discovered that the protein PIN1 drives bladder cancer by triggering cholesterol synthesis, which fuels out-of-control cell growth. A combination of statins and a PIN1 inhibitor effectively blocks tumor growth in mice, offering a promising therapeutic approach for this deadly disease.
A new Northwestern Medicine study reveals how metformin lowers glucose levels by targeting mitochondrial complex I in cells. The drug also improves COVID outcomes and reduces inflammation, suggesting that mitochondrial complex I inhibition may be a unifying mechanism behind its diverse effects.
A study by MedUni Vienna identified a promising therapeutic approach for metabolic liver diseases by targeting fat metabolism inhibition, promoting liver health and reducing liver fat, inflammation and fibrotic remodeling. The approach involves blocking ATGL, an enzyme playing a central role in lipid metabolism.
Researchers found that EZH2 inhibition boosts T-cell immunotherapies' effectiveness by making cancer cells more visible and reducing immunosuppressive regulatory T-cells. This combination therapy showed improved survival rates in mice with lymphomas, suggesting a potential new approach to treating certain cancers.
Researchers have identified UBA1 enzyme as key mediator for immune response to tumors, inhibiting its activity increases T-cell recruitment and lowers tumor resistance. Pairing UBA1 inhibitors with immune checkpoint blockade therapies may make immunotherapy more effective for patients with 'cold' tumors.
A new study by Weill Cornell Medicine scientists reveals that the enzyme EZH2 drives aggressive tumor growth in treatment-resistant prostate cancers. The absence of protein PKCλ/ι enables EZH2's alternative function, promoting cancer progression despite androgen receptor inhibitors.
Researchers at UC Riverside develop a novel method to degrade the Pin1 protein, which is involved in pancreatic cancer development. The 'molecular crowbar' strategy has the potential to target and break down harmful proteins, offering new hope for cancer therapy.
Scientists have discovered a natural compound called sulfuretin that can halt the progression of certain forms of cancer and demyelinating conditions like multiple sclerosis. The study found that sulfuretin blocks the activity of an enzyme involved in these diseases, suggesting its potential as a treatment.
Researchers found that ACLY activity activates the senescence-associated secretory phenotype (SASP), a pro-inflammatory environment associated with chronic inflammation and aging. Blocking ACLY activity reduces inflammation-related genes in aged cells, suggesting a potential strategy for managing aging and age-related diseases.
Researchers from Duke University have discovered the mechanism behind the discrepancies in how resistant infections react to combination treatments. The study found that bacteria with a higher level of 'selfishness' are more likely to thrive after treatment, while less selfish strains benefit more.
Researchers at Umea University have discovered how embryonic stem cells transition into specialized cells, highlighting the importance of LSD1 protein in cancer development. The study suggests that targeting only LSD1's enzymatic activity may not be enough for cancer treatments to be effective.
Researchers found inhibiting ACMSD increases NAD+ levels, reducing inflammation and fibrosis in mouse models of MASLD/MASH. Boosting NAD+ production could protect against severe liver damage and cirrhosis.
Researchers propose a two-pronged attack on the enzyme glutaminase and protein HuR to combat breast cancer. Simultaneous inhibition of both is shown to significantly reduce breast cancer cell growth and invasion by increasing dependence on glutamine.
Researchers discovered that activating the pentose phosphate pathway makes antitumor CD8 T cells more likely to stay in an immature state, leading to better results in animal models and human organoids. This metabolic reprogramming strategy may enhance checkpoint inhibitor therapy by boosting a long-term supply of active cytotoxic T ce...
Researchers at Tokyo Institute of Technology developed a method to precisely control the timing of DNA droplet division, mimicking biological Liquid-Liquid Phase Separation (LLPS) droplets. This breakthrough enables precise control over synthetic droplet dynamics, key to developing bio-inspired systems.
Researchers found that a specific crosslinking mode in the peptidoglycan cell wall inhibits certain cell wall degrading enzymes, protecting bacteria from internal and external damage. This discovery may lead to new treatments for developing antibacterial therapies.
Researchers at WVU are working on a project to inhibit the myeloperoxidase enzyme, which feeds pancreatic cancer growth. By targeting this enzyme, they hope to boost the body's immune system to fight cancer, showing promise in mouse models and potential for future clinical trials.
Researchers at MUSC Hollings Cancer Center discover targeting an immunosuppressive protein on two fronts reduces metastasis and restores sensitivity to immunotherapy in a preclinical model. TNBC cells become resistant to immunotherapy due to membrane instability, enabling PD-L1 protein to drop inside the cell.
A newly developed compound, MOD06051, targets neutrophils and reduces harmful inflammation in rat models. This approach differs from current treatments that may have broader immunosuppressive effects, offering a safer alternative.
Researchers at the University of Bologna have identified a specific location and genomic context where DNA breaks occur due to topoisomerase I inhibition. This discovery could lead to new cancer treatments by inducing DNA damage and genomic instability in cancer cells.
Researchers at Tokyo University of Science discovered a natural tyrosinase inhibitor from Corynebacterium tuberculostearicum that inhibits melanin synthesis and provides an alternative to toxic hydroquinone-based products. The compound, cyclo(L-Pro-L-Tyr), exhibits low toxicity and potential benefits for hyperpigmentation treatment.
A new study finds that combining an inhibitor of a metabolic pathway with chemotherapy could improve treatment outcomes in triple negative breast cancer brain metastases. Inhibiting fatty acid synthase, an enzyme critical for cancer cell survival, shows promise in improving chemotherapy efficacy.
Researchers at Ohio State University are exploring the role of caspase 11 in SARS-CoV-2 infection, aiming to prevent inflammation and tissue injury. They will use human cell samples and experimental inhibitors to develop new treatment strategies for long COVID.
Scientists have identified a critical genetic mechanism driving cardiac fibrosis and found a novel target for its reversal. The discovery sheds light on the role of transforming growth factor-beta (TGFβ) and ATP-citrate lyase (ACLY) in promoting excessive tissue scarring, providing hope for new heart failure treatments.
Researchers at Tampere University analyzed the molecular activity of over 10,000 genes to investigate the efficacy of ZED1227, a transglutaminase 2 inhibitor. The study found that ZED1227 effectively prevented gluten-induced intestinal mucosal damage and inflammation in celiac patients.
Researchers found that combining the immunosuppressive drug ruxolitinib with existing checkpoint inhibitor therapies boosts their effectiveness in fighting cancer. The treatment results in an increase in functional T cells and a reduction in myeloid suppressor cells, which are tied to poor prognosis of several cancers.
A recent study suggests that inhibiting epigenetic control enzymes in immune cells, specifically HDAC1, improves anti-tumor immunity and tumor surveillance. This finding could lead to new therapeutic strategies in cancer immunotherapy.
The study reveals that the binding sites of USP28 and USP25 inhibitors are identical, leading to non-specific effects. Researchers now aim to develop precise inhibitors targeting either enzyme site to reduce side effects.
Research suggests that altered lipid signaling in brain cells contributes to mental disorders, with specific inhibitors showing promise in rebalancing this mechanism. The study found similar changes in both human patients and healthy relatives, as well as mice with genetic disorders, opening up new treatment opportunities.
Researchers developed a novel approach to block cancer cell growth by targeting specific proteins, reducing side effects and increasing treatment efficacy. The method uses antibody-peptide inhibitor conjugates, which deliver inhibitors specifically to cancer cells,
Researchers at Okayama University developed a novel AAK1 inhibitor using Kinobeads technology, shedding light on its inhibitory mechanism and targeting various neurological disorders and viral infections. This breakthrough paves the way for rapid and cost-effective enzyme inhibitors with clinical applications.
Scientists at St. Jude Children's Research Hospital have designed novel PXR inhibitors that can block the activity of pregnane X receptor, a key regulator of drug metabolism. The study provides new insights into the relationship between compounds that activate and inhibit PXR, with implications for designing more effective therapeutics.
Researchers at Kobe University have discovered a new method to inhibit streptococcal infections by using aggregates of the non-toxic molecule Mn007. The study found that aggregates of Mn007 significantly reduce bacterial growth, suggesting potential as an effective treatment for toxic shock syndrome.
Researchers at Insilico Medicine have identified a new class of Polθ inhibitors featuring central scaffolding rings, designed using Chemistry42, with significant enzymatic and cellular potency. The discovery showcases the potential of AI in medicinal chemistry for precise molecular modifications.
Scientists at Sanford Burnham Prebys have identified promising links between common HIV drugs and a reduced incidence of Alzheimer's disease. The study analyzed over 225,000 medical records and found that RT inhibitor exposure was associated with a statistically significant reduced incidence and prevalence of AD.
Researchers from the University of Cincinnati presented findings on the effectiveness of a two-component enzyme replacement therapy for late-onset Pompe disease. The study showed that patients treated with this regimen experienced improvement or stability in motor function, pulmonary function, and muscle strength. Additionally, experts...
Researchers unveil innovative strategies to overcome metabolic constraints in CAR-T cell therapy, aiming to boost its efficacy in treating solid tumors. Metabolic interventions targeting immunosuppressive metabolites, metabolite uptake, and mitochondrial metabolism are proposed to enhance anti-tumor activity.
Researchers have identified five LpxC inhibitors that can bind to and inhibit the enzyme, leading to accumulation of inactive enzyme and bacterial cell death. Compound-specific differences were observed in membrane composition and stress responses.
Researchers developed a novel concept to control chemical reactions during catalytic processes by employing light. They proposed an innovative nanosystem that enables rapid and efficient catalyst deactivation without additional chemicals, facilitating controlled reaction rates.
Rumbaugh's lab aims to understand the effects of dispersing bacteria from a biofilm on their susceptibility to antibiotics and on the host. They will use enzymes as tools to break up biofilms, allowing researchers to better comprehend the relationship between bacterial dispersal and infection outcomes.
Researchers at the Francis Crick Institute and UCL have identified a gene that causes heart defects in Down syndrome, a condition resulting from an extra copy of chromosome 21. Reducing the overactivity of this gene partially reversed these defects in mice, setting the scene for potential future therapies.