Modification of alpha-biphenylsulfonamidocarboxylic acids led to potent and selective MMP-13 inhibitors. Compound 16 showed 100% oral bioavailability in rats and demonstrated >50% inhibition of bovine cartilage degradation at 10 ng/mL.
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http://dx.doi.org/10.1016/j.bmc.2005.07.076 | DOI Listing |
NMC Case Rep J
December 2024
Department of Neurosurgery, Graduate School of Biomedical and Health Sciences, Hiroshima University, Hiroshima, Hiroshima, Japan.
Older patients represent a unique and vulnerable subgroup, requiring careful consideration when determining treatment options. Treatment-related leukoencephalopathy is commonly observed in older patients months to years after receiving radiotherapy and/or methotrexate for primary central nervous system lymphoma (PCNSL). Tirabrutinib is an orally available, highly selective, and potent second-generation Bruton's tyrosine kinase inhibitor (BTKi) approved for treating recurrent/refractory PCNSL in Japan.
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January 2025
Department of Chemistry, Virginia Tech, Blacksburg, Virginia 24061, United States.
Millipedes have long been known to produce structurally diverse chemical defenses, including hydrogen cyanide, terpenoid alkaloids, and oxidized aromatics. Although the hydrogen cyanide and oxidized aromatic producing millipedes have been well studied, less than 10% of the terpenoid alkaloid producers have been chemically investigated. Several previous studies have shown that alkaloids disorient predators, but their biochemical target is currently unknown.
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February 2025
National Agri-Food and Biomanufacturing Institute, SAS Nagar, Mohali, India; Institute of Bioresources and Sustainable Development, Regional Centre, Sikkim, India. Electronic address:
Fermented foods of the Indian Himalaya are unexplored functional resources with high nutritional potential. Chhurpi cheese, fermented by defined native proteolytic lactic acid bacteria of Sikkim was assessed for ACE inhibitory, HOCl reducing, and MPO inhibitory, activity across varying stages of gastrointestinal (GI) digestion. The enhanced bioactivity of Lactobacillus delbrueckii WS4 chhurpi was associated with the generation of bioactive and multifunctional peptides during fermentation and GI digestion.
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January 2025
Faculty of Biotechnology, October University for Modern Sciences and Arts, 6th of October, Egypt.
Calcium hydroxide nanoparticles (Ca(OH)NPs) possess potent antimicrobial activities and unique physical and chemical properties, making them valuable across various fields. However, limited information exists regarding their effects on genomic DNA integrity and their potential to induce apoptosis in normal and cancerous human cell lines. This study thus aimed to evaluate the impact of Ca(OH)NPs on cell viability, genomic DNA integrity, and oxidative stress induction in human normal skin fibroblasts (HSF) and cancerous hepatic (HepG2) cells.
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January 2025
Barcelona Institute for Global Health (ISGlobal, Hospital Clínic-University of Barcelona), Rosselló 149-153, Barcelona, 08036, Spain.
We recently characterized the potent antiplasmodial activity of the aggregated protein dye YAT2150, whose presumed mode of action is the inhibition of protein aggregation in the malaria parasite. Using single-dose and ramping methods, assays were done to select Plasmodium falciparum parasites resistant to YAT2150 concentrations ranging from 3× to 0.25× the in vitro IC of the compound (in the two-digit nM range) and performed a cross-resistance assessment in P.
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