Amino ketone warheads were explored as alternatives to the nitrile group of a potent and selective cathepsin K inhibitor. The resulting compounds were potent and selective inhibitors of cathepsin K and these nitrile replacements had a significant effect on metabolism and pharmacokinetics.
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http://dx.doi.org/10.1016/j.bmcl.2008.12.053 | DOI Listing |
Int J Mol Sci
December 2024
Plant Breeding and Acclimatization Institute-National Research Institute, Radzikow, 05-870 Blonie, Poland.
Int J Mol Sci
December 2024
School of Biological Sciences, Nanyang Technological University, Singapore 637551, Singapore.
Host defense antimicrobial peptides (AMPs) are promising lead molecules with which to develop antibiotics against drug-resistant bacterial pathogens. Thanatin, an inducible antimicrobial peptide involved in the host defense of insects, is gaining considerable attention in the generation of novel classes of antibiotics. Thanatin or thanatin-based analog peptides are extremely potent in killing bacterial pathogens in the Enterobacteriaceae family, including drug-resistant strains of and .
View Article and Find Full Text PDFPolymers (Basel)
January 2025
Facultad de Farmacia-Centro de Innovación en Química Avanzada (ORFEO-CINQA), Unidad nanoDrug, Departamento de Química Inorgánica, Orgánica y Bioquímica, Universidad de Castilla-La Mancha, 02071 Albacete, Albacete, Spain.
The compounds targeting the bromo and extra terminal domain proteins (BET), such as the JQ1, present potent anti-cancer activity in preclinical models, however, the application of JQ1 at the clinical level is limited by its short half-life, rapid clearance, and non-selective inhibition of BET family proteins, leading to off-target effects and resistance. To address these challenges, the optimization of JQ1 delivery has been accomplished through polylactide (PLA) nanoparticles. PLA derivatives with varying molecular weights were synthesized via ring-opening polymerization using a zinc-based initiator and characterized using thermogravimetric analysis, differential scanning calorimetry, and infrared spectroscopy.
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December 2024
Department of Zoology, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
Nocturnal asthma (NA) is a high-prevalence disease that causes severe respiratory issues, leading to death from early midnight to early morning. In this research, nanoparticulate drug delivery system of methylprednisolone (MP) was developed using chitosan (CH) and pectin (PEC). MP is a synthetic corticosteroid medication widely used for its potent anti-inflammatory activity.
View Article and Find Full Text PDFMolecules
January 2025
Institute of Modern Physics, Chinese Academy of Sciences, Lanzhou 730000, China.
More than 70% of cancer patients receive radiotherapy during their treatment, with consequent various side effects on normal cells due to high ionizing radiation doses despite tumor shrinkage. To date, many radioprotectors and radiosensitizers have been investigated in preclinical studies, but their use has been hampered by the high toxicity to normal cells or poor tumor radiosensitization effects. Genistein is a naturally occurring isoflavone found in soy products.
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