Results 1 to 10 of about 2,218 (114)

Discovery of Novel Biphenyl Carboxylic Acid Derivatives as Potent URAT1 Inhibitors

Molecules, 2023
Urate transporter 1 (URAT1) is a clinically validated target for the treatment of hyperuricemia and gout. Due to the absence of protein structures, the molecular design of new URAT1 inhibitors generally resorts to ligand-based approaches.
Zhiyan Xiao, Yajun Yang, Xianxin Hou
exaly   +3 more sources

URAT1 inhibition in hyperuricemia and gout: from transporter biology to clinical precision therapy [PDF]

Frontiers in Immunology
Impaired renal urate excretion is a major mechanism underlying hyperuricemia and gout, with urate transporter 1 (URAT1), encoded by SLC22A12, playing a central role in proximal tubular urate reabsorption.
Guangtao Li, Yu Wang, Zhuoli Zhang
doaj   +2 more sources

Ectopic expression of Aspergillus flavus uricase and URAT1 in therapeutic cells promotes intracellular degradation of uric acid in hyperuricemic mice. [PDF]

PLoS ONE
Uricase-based drugs excel at treating refractory hyperuricemia and tumor lysis syndrome by directly degrading uric acid but are limited by immunogenicity.
Yuzhong Feng, Jiazhen Cui, Xuan Huang, Yupeng Li, Haolong Dong, Xianghua Xiong, Gang Liu, Qingyang Wang, Huipeng Chen   +8 more
doaj   +2 more sources

Discovery of a Flexible Triazolylbutanoic Acid as a Highly Potent Uric Acid Transporter 1 (URAT1) Inhibitor

Molecules, 2016
In order to systematically explore and understand the structure–activity relationship (SAR) of a lesinurad-based hit (1c) derived from the replacement of the S atom in lesinurad with CH2, 18 compounds (1a–1r) were designed, synthesized and subjected to ...
Guilong Zhao, Lida Tang, Weiren Xu
exaly   +3 more sources

URAT1-Selective Inhibition Ameliorates Insulin Resistance by Attenuating Diet-Induced Hepatic Steatosis and Brown Adipose Tissue Whitening in Mice

Molecular Metabolism, 2022
Objective: Accumulating evidence indicates that high uric acid (UA) is strongly associated with obesity and metabolic syndrome and drives the development of nonalcoholic fatty liver disease (NAFLD) and insulin resistance.
Haruka Kimura, Hirotake Takahashi, Toshikazu Tanaka   +2 more
exaly   +3 more sources

A Case of Idiopathic Renal Hypouricemia with Gene Mutation Showing General Weakness and Incidental Renal Stone [PDF]

Childhood Kidney Diseases, 2021
Idiopathic renal hypouricemia (iRHUC) is a rare hereditary disease caused by a defect in urate handling of renal tubules. Type 1 renal hypouricemia (RHUC1) is diagnosed with confirmation of a mutation in SLC22A12 gene which encodes a renal urate-anion ...
Jin Woon Joung, Young Wha Song, Jong Dae Kim, Eun Jung Cheon   +3 more
doaj   +1 more source

URAT1 is expressed in cardiomyocytes and dotinurad attenuates the development of diet-induced metabolic heart disease

iScience, 2023
Summary: We recently reported that the selective inhibition of urate transporter-1 (URAT1), which is primarily expressed in the kidneys, ameliorates insulin resistance by attenuating hepatic steatosis and improving brown adipose tissue function in diet ...
Yoshiro Tanaka, Tomohisa Nagoshi, Hirotake Takahashi, Yuhei Oi, Rei Yasutake, Akira Yoshii, Haruka Kimura, Yusuke Kashiwagi, Toshikazu D. Tanaka, Masayuki Shimoda, Michihiro Yoshimura   +10 more
doaj   +1 more source

Genetic Basis of the Epidemiological Features and Clinical Significance of Renal Hypouricemia

Biomedicines, 2022
A genetic defect in urate transporter 1 (URAT1) is the major cause of renal hypouricemia (RHUC). Although RHUC is detected using a serum uric acid (UA) concentration
Masayuki Hakoda, Kimiyoshi Ichida
doaj   +1 more source

A Proposal for Practical Diagnosis of Renal Hypouricemia: Evidenced from Genetic Studies of Nonfunctional Variants of URAT1/SLC22A12 among 30,685 Japanese Individuals

Biomedicines, 2021
Background: Renal hypouricemia (RHUC) is characterized by a low serum uric acid (SUA) level and high fractional excretion of uric acid (FEUA). Further studies on FEUA in hypouricemic individuals are needed for a more accurate diagnosis of RHUC.
Yusuke Kawamura, Akiyoshi Nakayama, Seiko Shimizu, Yu Toyoda, Yuichiro Nishida, Asahi Hishida, Sakurako Katsuura-Kamano, Kenichi Shibuya, Takashi Tamura, Makoto Kawaguchi, Satoko Suzuki, Satoko Iwasawa, Hiroshi Nakashima, Rie Ibusuki, Hirokazu Uemura, Megumi Hara, Kenji Takeuchi, Tappei Takada, Masashi Tsunoda, Kokichi Arisawa, Toshiro Takezaki, Keitaro Tanaka, Kimiyoshi Ichida, Kenji Wakai, Nariyoshi Shinomiya, Hirotaka Matsuo   +25 more
doaj   +1 more source

Loss of the Kidney Urate Transporter, Urat1, Leads to Disrupted Redox Homeostasis in Mice

Antioxidants, 2023
High uric acid is associated with gout, hypertension, metabolic syndrome, cardiovascular disease, and kidney disease. URAT1 (SLC22A12), originally discovered in mice as Rst, is generally considered a very selective uric acid transporter compared to other
Neema Jamshidi, Kabir B. Nigam, Sanjay K. Nigam   +2 more
doaj   +1 more source