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Small Molecule Modulators of AMP-Activated Protein Kinase (AMPK) Activity and Their Potential in Cancer Therapy.
J Med Chem
January 2025
Department of Pharmaceutical Sciences, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of Colorado Anschutz Medical Campus, 12850 East Montview Boulevard, Aurora, Colorado 80045, United States.
AMP-activated protein kinase (AMPK) is a central mediator of cellular metabolism and is activated in direct response to low ATP levels. Activated AMPK inhibits anabolic pathways and promotes catabolic activities that generate ATP through the phosphorylation of multiple target substrates. AMPK is a therapeutic target for activation in several chronic metabolic diseases, and there is increasing interest in targeting AMPK activity in cancer where it can act as a tumor suppressor or conversely it can support cancer cell survival.
View Article and Find Full Text PDFComputational Methods for Modeling Lipid-Mediated Active Pharmaceutical Ingredient Delivery.
Mol Pharm
January 2025
Regional Center of Advanced Technologies and Materials, Czech Advanced Technology and Research Institute (CATRIN), Palacký University Olomouc, Šlechtitelů 27, 779 00 Olomouc, Czech Republic.
Lipid-mediated delivery of active pharmaceutical ingredients (API) opened new possibilities in advanced therapies. By encapsulating an API into a lipid nanocarrier (LNC), one can safely deliver APIs not soluble in water, those with otherwise strong adverse effects, or very fragile ones such as nucleic acids. However, for the rational design of LNCs, a detailed understanding of the composition-structure-function relationships is missing.
View Article and Find Full Text PDFManagement of nausea and vomiting induced by antibody-drug conjugates.
Breast Cancer
January 2025
Advanced Cancer Translational Research Institute, Showa University, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo, 142-8555, Japan.
Antibody-drug conjugates (ADCs) are an emerging class of anticancer therapy that combines the specificity and long circulation half-life of monoclonal antibodies with the cytotoxic potency of the payload connected through a chemical linker. The optimal management of toxicities is crucial for improving quality of life in patients undergoing ADCs and for avoiding improper dose reductions or discontinuations. This article focuses on the characteristics and management of nausea and vomiting (NV) induced by three ADCs: trastuzumab deruxtecan (T-DXd), sacituzumab govitecan (SG), and datopotamab deruxtecan (Dato-DXd).
View Article and Find Full Text PDFTherapeutic potential and underlying mechanisms of phytoconstituents: emphasizing on resveratol, curcumin, quercetin, berberine, and hesperidin in ulcerative colitis.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
University Institute of Pharma Sciences, Chandigarh University, Gharuan, Mohali, Punjab, India.
Ulcerative colitis is a long-term inflammatory colon illness that significantly affects patients quality of life. Traditional medicines and therapies often come with challenges such as side effects, instability, unpredictability, and high costs. This has captured interest in natural products that have huge health benefits.
View Article and Find Full Text PDFThe effect of acetylcysteine on the prothrombin time and international normalized ratio: a narrative review.
Clin Toxicol (Phila)
January 2025
Department of Clinical Pharmacy and Pharmacology, University of Groningen, University Medical Center Groningen, Groningen, The Netherlands.
Introduction: Patients poisoned with paracetamol are treated with acetylcysteine. In patients without hepatocellular injury, an increased prothrombin time or international normalized ratio has been observed during acetylcysteine administration. The international normalized ratio is preferred as it is a standardized calculation of prothrombin time independent of reagents and machinery.
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