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Kidney Targeting Smart Antibiotic Discovery: Multimechanism Pleuromutilins for Pyelonephritis Therapy.

J Med Chem

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Xi'an Key Laboratory for Antiviral and Antimicrobial-Resistant Bacteria Therapeutics Research, Xi'an 710021, China.

Multidrug-resistant (MDR) bacteria pose a global health threat, underscoring the need for new antibiotics. Lefamulin, the first novel-mechanism antibiotic approved by the FDA in decades, showcases pleuromutilins' promise due to low mutation frequency. However, their clinical use is limited by poor pharmacokinetics and organ toxicity.

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Cyclin-dependent kinases 4 and 6 (CDK4/6) are crucial regulators of cell cycle progression and represent important therapeutic targets in breast cancer. This study employs a comprehensive computational approach to identify novel CDK4/6 inhibitors from marine natural products. We utilized structure-based virtual screening of the CMNPD database and MNP library, followed by rigorous filtering based on drug-likeness criteria, PAINS filter, ADME properties, and toxicity profiles.

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Introduction: This case study presents a rare and fatal instance of Toxic Epidermal Necrolysis (TEN) and Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) syndrome in a 51-year-old male patient diagnosed with Rheumatoid Arthritis (RA).

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Prediction of Potential Risk for Ten Azole and Benzimidazole Fungicides with the Aryl Hydrocarbon Receptor Agonistic Activity to Aquatic Ecosystems.

J Agric Food Chem

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Fujian Engineering Research Center for Green Pest Management/Fujian Key Laboratory for Monitoring and Integrated Management of Crop Pests/East China Branch of the National Center for Agricultural Biosafety Sciences, Institute of Plant Protection, Fujian Academy of Agricultural Sciences, Fuzhou 350013, China.

Azole and benzimidazole fungicides are widely used agrochemicals to prevent and treat fungal growth and are frequently detected in aquatic environments. Here, we aimed to assess the aquatic ecological risks of ten currently used azole and benzimidazole fungicides, which with the aryl hydrocarbon receptor (AhR) agonistic activity, and their transformation products (TPs). We obtained over 400 types of aerobic TPs for ten fungicides.

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The surge in plastic production has spurred a global crisis as plastic pollution intensifies, with microplastics and nanoplastics emerging as notable environmental threats. Due to their miniature size, these particles are ubiquitous across ecosystems and pose severe hazards as they are ingested and bioaccumulate within organisms. Although global plastic production has reached an alarming 400.

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