Articles tagged with Kinase Inhibitors
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A new study reveals that kinase inhibitors can accelerate the degradation of targeted proteins, which is not a rare quirk but a common mechanism. This discovery could help design better drugs that remove kinases altogether or explain unexpected effects of existing therapies.
A new Alliance trial is exploring the effectiveness of a combination of targeted therapy and immunotherapy for patients with advanced adrenocortical carcinoma, a rare and aggressive cancer. The study aims to improve disease control and quality of life for patients with limited treatment options.
A potent new dual lipid kinase inhibitor, RMC-113, selectively inhibits PIKfyve and PIP4K2C, providing a potential strategy to combat emerging viruses. The study reveals that PIP4K2C plays a crucial role in SARS-CoV-2 entry, replication, and assembly/egress, making it an understudied kinase with significant antiviral potential.
A study from The University of Osaka reveals nearly half of patients with extracranial arteriovenous malformations carry mutations in the RAS/RAF/MAPK signaling pathway. These mutations were linked to abnormal vascular morphology and were frequently detected in younger female patients.
Inhibition of Aurora kinases suppresses liver cancer cell proliferation while inducing phenotypic changes resembling normal liver cells. This dual mechanism suggests a promising new approach for liver cancer therapies.
A clinical trial found that LUT014, a topical BRAF inhibitor, significantly reduced the severity of acne-like skin rashes caused by targeted therapy for colorectal cancer. Patients who received LUT014 had improved quality of life and were able to continue receiving their cancer treatment with reduced side effects.
Methyl eugenol has demonstrated notable antioxidant and antiproliferative activity, with potential therapeutic benefits for diseases like Alzheimer's disease and cancer. However, its toxicological risks, including hepatotoxicity and alterations in the gut microbiota, pose concerns for its application.
A USC Stem Cell mouse study has identified shared genes involved in regenerating cells in the ear and eye, which could lead to new treatments for hearing and vision loss. The researchers discovered that inhibiting a specific protein, p27Kip1, can encourage regeneration in both organs.
New guidelines support safe and efficient use of JAK inhibitors for treating chronic inflammatory diseases like rheumatoid arthritis, psoriasis, and Crohn's disease. The updated consensus statement considers safety concerns, including cardiovascular disease and cancer risk, to ensure individualized treatment decisions.
Researchers at Sanford Burnham Prebys have discovered a way to target the energy supply chain of cancer cells. By understanding how enzymes like ubiquitous mitochondrial creatine kinase (uMtCK) function, scientists can design new treatments that slow or stop tumor growth.
Researchers at University of Arizona Cancer Center found that an immunotherapy previously shown to be ineffective against prostate cancer may have therapeutic potential when combined with a specific protein inhibitor. The study's co-author, Noel Warfel, PhD, identified a way to sensitize prostate tumors to immune checkpoint inhibitors ...
Researchers at VCU Massey Comprehensive Cancer Center have identified an innovative combination treatment strategy that collaborates to kill AML cells. The new approach targets the SRC gene and MCL-1 protein, leading to increased cell death in leukemia cells. This discovery offers a promising new direction for leukemia treatment.
Researchers at MD Anderson Cancer Center have identified biomarkers for predicting treatment response in metastatic breast cancer and found a potential target for tumor progression in pancreatic cancer. Additionally, they discovered that abnormal chromosome changes predict survival in patients with secondary acute myeloid leukemia.
Researchers aim to identify key mechanisms and molecular targets to prevent tumor progression in Rhabdomyosarcoma patients. The study focuses on the TAK1 protein, which plays a significant role in regulating cell growth, and its potential inhibition as a therapeutic approach.
The macrocyclization strategy has been widely used to optimize kinase inhibitors, offering improved target selectivity and solubility. Three macrocyclic kinase inhibitors have received FDA approval, addressing limitations of existing molecules and providing substantial clinical benefits for patients with cancer.
Researchers found effective peptidomimetics that can bind to and inhibit Aurora-A's interaction with TACC3 without inhibiting its enzymatic function. This inhibition also showed promise in targeting a different protein-protein interaction between N-Myc and Aurora-A, which is crucial in childhood brain cancers.
A study from Goethe University Frankfurt reveals that venomous crustaceans, specifically remipede crabs in Mexican cenote caves, contain a variety of toxins with pharmacological potential. The xibalbines peptides effectively inhibit potassium channels and activate signaling pathways involved in pain sensitization.
Researchers explore immune activation and tumor-promoting transcription factor FOXM1's role in CDK4/6-MEK resistance. They suggest targeting the oncogenic network of CDK4/6, MEK, PD-L1, and FOXM1 as future treatment options for MPNST patients.
Researchers identified protein kinase N as a key regulator of heart fibrosis, which threatens heart function. Deleting this enzyme reduced cardiac dysfunction, suggesting anti-PKN treatments may protect against heart failure.
Researchers at Purdue University have received an additional $95,000 from the Trask Innovation Fund to further de-risk their technology for patent-pending drought-resistant soybean plants. Herman Sintim's team aims to develop novel compounds that potentially inhibit TAK1, a protein kinase shown to play key roles in arthritis.
A team of researchers from Penn State College of Medicine identified KDR, a tyrosine kinase, as a potential drug target for treating diseases caused by human T-cell leukemia virus type 1 (HTLV-1). By blocking KDR, the viral protein Tax is degraded, leading to cell death and disruption of cancer-causing signaling pathways.
Researchers at Purdue University have developed a patent-pending compound called HSN748 to treat drug-resistant acute myeloid leukemia (AML). The compound has been validated in tests with IU School of Medicine and demonstrated 100% survivability after 120 days. AML is a cancer that begins in bone marrow and can be difficult to treat du...
Researchers have identified a potent and unique way to kill drug-resistant bacteria using a repurposed compound called LEI-800. The compound targets the bacterial enzyme DNA gyrase, which is essential for bacterial growth and has not been targeted by existing antibiotics.
Researchers from Juntendo University discover that canagliflozin, an SGLT2 inhibitor, eliminates senescent cells and improves glucose metabolism in mice with dietary obesity. The study highlights the potential of this novel senolytic strategy for managing aging-related disorders.
A new study reveals TNIK's role in various diseases, including fibrosis, cancer, obesity, and Alzheimer's. The protein has been found to drive cancer cell proliferation and treatment resistance, while also regulating metabolic processes.
Scientists at Sanford Burnham Prebys and Vanderbilt University have identified phosphatidylinositol-5-phosphate 4-kinases (PI5P4Ks) as a key regulator of the hippo pathway, which is dysregulated in cancer. The study suggests that targeting PI5P4Ks may lead to new treatments for cancers with abnormal hippo signaling.
A novel, non-hormonal sperm-specific approach offers a promising option for reversible human male contraception. Researchers identified a small molecule inhibitor that targets serine/threonine kinase 33 (STK33), a protein essential for fertility in both men and mice.
The study investigates the anticancer potential of CLK kinase inhibitors 1C8 and GPS167, which inhibit CLOCK kinases and affect cancer cell proliferation. The compounds also alter the expression and alternative splicing of transcripts involved in EMT and antiviral immune response.
Research found that RAMP1 protects liver cells from damage caused by ischemia-reperfusion injury. The protein inhibited the ERK/YAP pathway, leading to reduced cell death and inflammation. This study highlights RAMP1's potential as a therapeutic target for treating this condition.
Scientists at German Cancer Research Center have discovered a combination therapy that improves treatment response and delays resistance in lung cancer cells. The therapy, which combines ALK and SRC inhibitors, blocks key protein expression changes that lead to resistance.
Scientists at St. Jude Children's Research Hospital found that ruxolitinib, a drug inhibiting both Janus Kinase 1 (JAK1) and JAK2, is a safe and potentially more effective therapy for Hemophagocytic lymphohistiocytosis (HLH), a rare and aggressive syndrome of hyperactive inflammation. The study showed that ruxolitinib increased surviva...
Researchers at University at Buffalo propose a new approach to developing cancer drugs by determining the optimal placement of molecular linkers earlier in the process, reducing trial and error and increasing potency, according to a study published in Communications Chemistry.
GFH009 inhibits tumor growth and induces apoptosis in various HHM-derived cell lines. The compound's mechanism of action involves rapid 'on-off' inhibition of CDK9, which exerts a proapoptotic effect on cancer cells.
Researchers have identified a novel mechanism leading to motor neuron degeneration in SMA, which can be stopped by a Cdk5 inhibitor. This discovery offers a new treatment approach that could benefit all patients with SMA, including those ineligible for gene therapy.
Researchers have developed a new method, SECRE, to identify genetic regulators of cytokine secretion in autoimmune diseases. The technique has been validated on cells known to play a crucial role in inflammatory bowel disease (IBD) and shows promising results for treating conditions with few therapeutic options.
A multicenter, retrospective study of Japanese patients treated with JAK inhibitors found impressive remission rates and low disease activity. The study's results contradict previous concerns about the effectiveness of these drugs, suggesting they may be a viable option for patients with other health problems.
The Cusack group at EMBL Grenoble has provided insights into the interactions of XIAP and RIPK2 molecules involved in gut signalling pathways. This research sheds light on how these molecules interact, revealing a promising drug target for treating inflammatory bowel diseases.
Researchers discovered a new role for extracellular signal-regulated kinase (ERK) in a pathway activated by interferon-gamma that leads to cancer cell death. Hyperactivation of ERK causes stress in cells, triggering cell death through specific proteins DR5 and NOXA.
A new study published in Exp. Mol. Med. has identified Thrap3 as a key player in exacerbating non-alcoholic fatty liver disease (NAFLD) by inhibiting AMPK, a crucial regulator of fat metabolism. Inhibiting Thrap3 expression presents a promising avenue for treating NAFLD.
Researchers explore CDK9 inhibitors as a promising combination partner in treating hematological malignancies. They discuss the role of cyclin-dependent kinases (CDKs) in these diseases and highlight the potential synergism with other drugs.
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 identified anti-malarial properties in cancer drugs, offering a potential solution to the growing crisis of drug-resistant malaria. The study found that certain protein kinase inhibitors exhibited strong anti-malarial effects, highlighting a new approach to accelerating drug discovery.
Researchers identified five previously unknown CaMKII inhibitors, including ruxolitinib, which was found to be the most effective at inhibiting CaMKII activity in cell and mouse models of arrhythmias. The study provides a promising new approach for treating heart conditions.
Researchers discovered that cancer cells can adapt to novel CDK2 inhibitors in as little as one to two hours, but adding a second drug can squelch this workaround. Combining CDK2 inhibitors with existing drugs may treat resistant breast cancers more effectively
Researchers found that MALAT1 inhibition decreased BRAF RNA and protein levels, while increasing correlation with MAPK-associated genes. MALAT1-ASO treatment also reduced melanoma cell growth and tumor size in xenograft models.
Scientists have identified a key event controlling the timing of biological clocks, which could lead to therapies for sleep disorders and clock disruption. The study found that a genetic mutation shortens the clock cycle in people with Familial Advanced Sleep Phase Syndrome.
Researchers found that p21 knockout mice experienced reduced senescent cell presence, alleviated chronic lung inflammation, and improved fitness. Resident epithelial and endothelial cells played a significant role in mediating the p21-dependent inflammatory response.
A new review paper suggests that selective protection of normal cells from chemotherapy could increase the therapeutic window and improve outcomes for cancer patients. The authors propose using antagonistic drug combinations to kill drug-resistant cancer cells, reducing side effects and improving quality of life.
Researchers found that gatekeeper mutations in kinases can destabilize the inactive form, making them more active and prone to cancer recurrence. This could inform which drugs oncologists use as a first-line treatment.
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 USC Keck School of Medicine have identified two new avenues for treating diverse forms of ALS by suppressing genes and inhibiting proteins. The findings suggest that targeting SYF2 gene suppression and PIKFYVE kinase inhibition may lead to broadly effective treatments for the disease.
Scientists have mapped out over 300 protein kinases and their targets, which could yield new leads for cancer drugs. The comprehensive atlas helps researchers identify signaling pathways that differ between normal and cancerous cells, or between treated and untreated cancer cells.
Researchers discovered that 15-deoxy-prostamide-J2 induces ER stress-mediated apoptosis selectively in tumor cells, reducing melanoma growth. The molecule activates PERK, IP3R, and the mitochondrial permeability transition pore, leading to cell death.
A Mount Sinai study found that certain inflammatory markers can predict which patients are more likely to respond to COVID-19 immunotherapies. The researchers identified a subtype of COVID-19 patients with hyperinflammation who could benefit from pacritinib, an anti-cancer drug.
A new chemical probe selectively inhibits human COQ8A in cells, targeting ubiquinone biosynthesis and providing a potential therapeutic strategy for diseases such as cancer. The inhibition of COQ8 has been linked to increased lifespan in certain organisms, suggesting its role in metabolic processes.
Opaganib, an oral small molecule pill, shows potential as a nuclear radiation injury therapeutic for homeland security medical countermeasures and antitumor radiotherapy. The compound protects normal tissue from radiation damage and improves antitumor activity and response to chemoradiation.
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.
A new experimental drug has shown promising results in treating liver cancer, with two patients experiencing a partial response to the treatment. The drug, NMS-01940153E, targets an enzyme that plays a critical role in cell division and growth, and its side effects are manageable.
Researchers found that CaMKII β promotes sleep onset and inhibits awakening, with its phosphorylation state controlling the transition from wakefulness to sleep. The study provides clues for ideal sleep control methods, aiming to maintain sleep duration.
Researchers found that sapanisertib can kill the malaria parasite at several stages during its life cycle, including in the liver and red blood cells. The study's findings offer new hope against a disease that kills over half a million people annually.