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Discovery of D-Ring-Contracted Artemisinin as a Potent Hydrophobic Tag for Targeted Protein Degradation.
J Med Chem
January 2025
Key laboratory of Plant Resource Conservation and Germplasm Innovation in Mountainous Region (Ministry of Education), Guizhou Engineering Laboratory for Synthetic Drugs, School of Pharmaceutical Sciences, Guizhou University, Guiyang 550025, PR China.
The relentless pursuit of innovative hydrophobic tags remains a formidable challenge within the realm of targeted protein degradation. Herein, we have uncovered the remarkable potential of D-ring-contracted artemisinin as a potent hydrophobic tag that demonstrates exceptional degradation efficiency. We have crafted a series of conjugates by fusing D-ring-contracted artemisinin with raloxifene, and among these, has emerged as a promising candidate for degrading estrogen receptor α (ERα).
View Article and Find Full Text PDFBrain organoid methodologies to explore mechanisms of disease in progressive multiple sclerosis.
Front Cell Neurosci
December 2024
Department of Clinical Neurosciences and NIHR Biomedical Research Centre, University of Cambridge, Cambridge, United Kingdom.
Multiple sclerosis (MS), a debilitating autoimmune disorder targeting the central nervous system (CNS), is marked by relentless demyelination and inflammation. Clinically, it presents in three distinct forms: relapsing-remitting MS (RRMS), primary progressive MS (PPMS), and secondary progressive MS (SPMS). While disease-modifying therapies (DMTs) offer some relief to people with RRMS, treatment options for progressive MS (pMS) remain frustratingly inadequate.
View Article and Find Full Text PDFLight People: Prof. Henry Snaith's (FRS) perovskite optoelectronics journey.
Light Sci Appl
January 2025
Executive Management College of CHN ENERGY, No.7 Binhe Avenue, North District of Future Science City, Changping District, Beijing, 102211, China.
In 2012, Prof. Henry Snaith demonstrated the first solid-state perovskite solar cell (PSC) with an efficiency of 10.9%, igniting a surge of interest and research into perovskite materials for their potential to revolutionize the photovoltaic (PV) industry.
View Article and Find Full Text PDFDecoding Neurodegeneration: A Review of Molecular Mechanisms and Therapeutic Advances in Alzheimer's, Parkinson's, and ALS.
Int J Mol Sci
November 2024
Department of Anatomy, "Carol Davila" University of Medicine and Pharmacy, 050474 Bucharest, Romania.
Neurodegenerative diseases, such as Alzheimer's, Parkinson's, ALS, and Huntington's, remain formidable challenges in medicine, with their relentless progression and limited therapeutic options. These diseases arise from a web of molecular disturbances-misfolded proteins, chronic neuroinflammation, mitochondrial dysfunction, and genetic mutations-that slowly dismantle neuronal integrity. Yet, recent scientific breakthroughs are opening new paths to intervene in these once-intractable conditions.
View Article and Find Full Text PDF2'-O-Galloylhyperin Prevents Tissue Remodeling in Thyroid Eye Disease: Prospects as a Thyrotropin Receptor Antagonist.
J Clin Endocrinol Metab
December 2024
Department of Endocrinology and Diabetes Center, The First Affiliated Hospital, Sun Yat-sen University, Guangzhou, Guangdong, 510080, China.
Context: Thyroid eye disease (TED) is a challenging condition owing to relentless orbital tissue remodeling, with thyrotropin receptor (TSHR) in orbital fibroblasts (OFs) serving as a promising therapeutic target.
Objective: This study seeks to discover potential TSHR inhibitors among US Food and Drug Administration (FDA)-approved drugs and evaluate their effects on TED-OFs.
Methods: Adipose tissues were sourced from the patients with or without TED.
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