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Gout is a disease caused by the deposit of monosodium urate (MSU) crystals that produce joint inflammation and subcutaneous nodules (tophi). The treatment of gout aims to reduce serum uric acid (sUA) levels by administering urate-lowering therapies (ULT) such as xanthine oxidase inhibitors (XOI: allopurinol, febuxostat) or uricosurics (e.g.
View Article and Find Full Text PDFhURAT1 Transgenic Mouse Model for Evaluating Targeted Urate-Lowering Agents.
Int J Rheum Dis
January 2025
Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing, China.
Background: Urate transporter 1 (URAT1) is a well-known therapeutic target for reducing urate levels in the treatment of hyperuricemia and gout. However, current pharmacological studies have failed to evaluate the efficacy of URAT1 inhibitors in non-primate animal models. We established a human URAT1 (hURAT1) transgenic knock-in (KI) mouse model to assess uricosuric agents' effectiveness and characterize URAT1-caused pathogenesis.
View Article and Find Full Text PDFAn update on the pharmacotherapy of gout.
Expert Opin Pharmacother
January 2025
Department of Rheumatology, Royal Free London NHS Foundation Trust, London, UK.
Introduction: Gout is a common form of acute inflammatory arthritis caused by the deposition of monosodium urate crystals within synovium of joints. This leads to severe pain, reducing quality of life for patients with this condition.
Areas Covered: This review summarizes the treatment of both acute flares of gout and urate-lowering therapy based on guidance from various major international societies.
Identification of N-phenyl-N-(quinolin-4-yl) amino carboxylic acids as URAT1 inhibitors with hypouricemic effects.
Bioorg Med Chem Lett
March 2025
Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China; State Key Laboratory of Digestive Health, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. Electronic address:
Urate transporter 1 (URAT1) is a therapeutic target for the treatment of hyperuricemia and gout. However, the application of currently marketed URAT1 inhibitors is hampered by insufficient efficacy and poor safety profiles. A series of N-phenyl-N-(quinolin-4-yl) amino carboxylic acids were designed by adopting strategies of molecular hybridization, scaffold hopping, and functional variation.
View Article and Find Full Text PDFOptimizing gout treatment: A comprehensive review of current and emerging uricosurics.
Joint Bone Spine
November 2024
Division of Rheumatology, Department of Medicine, Spencer Fox Eccles School of Medicine, University of Utah, Salt Lake City, 84132 Utah, United States; Department of Medicine, Spencer Fox Eccles School of Medicine, University of Utah, Salt Lake City, 84132 Utah, United States.
Gout is the most common inflammatory arthritis, affecting approximately 5.1% of adults in the United States (US) population. Gout is a metabolic and autoinflammatory disease.
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