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Design and Discovery of Preclinical Candidate LYG-409 as a Highly Potent and Selective GSPT1 Molecular Glue Degraders.
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State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 211100, P. R. China.
Molecular glue degraders induce "undruggable" protein degradation by a proximity-induced effect. Inspired by the clinical success of immunomodulatory drugs, we aimed to design novel molecular glue degraders targeting GSPT1. Here, we report the design of a series of GSPT1 molecular glue degraders.
View Article and Find Full Text PDFAcid sphingomyelinase downregulation alleviates diabetic myocardial fibrosis in mice.
Mol Cell Biochem
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Department of Cardiology, Guangdong Key Laboratory of Vascular Diseases, State Key Laboratory of Respiratory, Disease, Guangzhou Institute of Cardiovascular Disease, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou, 510260, Guangdong, China.
Increased activity of acid sphingomyelinase (ASMase) has been linked to diabetes and organ fibrosis. Nevertheless, the precise influence of ASMase on diabetic myocardial fibrosis and the corresponding molecular mechanisms remain elusive. In this study, we aim to elucidate whether ASMase contributes to diabetic myocardial fibrosis through the phosphorylation mediated by MAPK, thereby culminating in the development of diabetic cardiomyopathy (DCM).
View Article and Find Full Text PDFRhanterium Epapposum Essential Oil and Its Primary Compounds Control Infection, Inflammation, and Serum Electrolyte Imbalance in Mice with Giardiasis.
Acta Parasitol
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Department of Medical Laboratories, College of Applied Medical Sciences, Shaqra University, Ad Dawadimi, Shaqra, 17464, Saudi Arabia.
Purpose: The present experimental study seeks to evaluate the in vitro and in vivo effects, as well as the potential mechanisms of action, of Rhanterium epapposum essential oil (REE) and its main constituents against Giardia lamblia infection.
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Effect of In Vitro Ruminal pH on Zearalenone Degradation and Interaction with Other Mycotoxins in a Static Gastrointestinal Model.
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Department of Food Safety and Quality, Faculty of Veterinary, Lithuanian University of Health Sciences, Tilzes Str. 18, LT-47181 Kaunas, Lithuania.
The degradation of zearalenone (ZEN) in the rumen of dairy cows is influenced by rumen pH, which is a key factor affecting this process. The aim of this study was to investigate the variation of ZEN in interaction with other mycotoxins at different ruminal pH environments (physiological (pH 6.5) and acidic (pH 5.
View Article and Find Full Text PDFGraphene-Based Materials for Bone Regeneration in Dentistry: A Systematic Review of In Vitro Applications and Material Comparisons.
Nanomaterials (Basel)
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Dermatology, Stomatology, Radiology and Physical Medicine, Hospital Morales Meseguer, Medicine School, IMIB-Arrixaca, University of Murcia, 30100 Murcia, Spain.
Introduction: Graphene, a two-dimensional arrangement of carbon atoms, has drawn significant interest in medical research due to its unique properties. In the context of bone regeneration, graphene has shown several promising applications. Its robust structure, electrical conductivity, and biocompatibility make it an ideal candidate for enhancing bone tissue regeneration and repair processes.
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