Results 151 to 160 of about 2,667 (184)

FRI0389 RDEA3170, a novel, high affinity URAT1 inhibitor binds to a central domain within URAT1

Annals of the Rheumatic Diseases, 2012
Background URAT1 inhibitors, used for the treatment of gout, lower serum urate levels by blocking uric acid reabsorption in the kidney proximal tubule through inhibition of the uric acid transporter URAT1. We have identified a URAT1 inhibitor RDEA3170 that specifically binds to and inhibits URAT1 with nanomolar potency.
J.N. Miner, P. Tan
openaire   +1 more source

Continuous flow synthesis of the URAT1 inhibitor lesinurad

Reaction Chemistry & Engineering, 2020
A 5-steps continuous flow synthesis of lesinurad is provided and delivers this API in 68% overall yield.
Mariana C. F. C. B. Damião, Henrique M. Marçon, Julio Cezar Pastre   +2 more
openaire   +1 more source

Overview of the pharmacokinetics and pharmacodynamics of URAT1 inhibitors for the treatment of hyperuricemia and gout

Expert Opinion on Drug Metabolism & Toxicology, 2023
Hyperuricemia is a common metabolic disease, which is a risk factor for gouty arthritis and ureteral stones and may also lead to cardiovascular and chronic kidney disease (CDK). Therefore, hyperuricemia should be treated early. Xanthine oxidase inhibitors (XOIs) and uricosuric agents (UAs), which target uric acid, are two types of medications that are ...
Zihan Hou, Aijinxiu Ma, Jiale Mao, Danni Song, Xu Zhao   +4 more
openaire   +2 more sources

Prevalence of URAT1 allelic variants in the Roma population

Nucleosides, Nucleotides & Nucleic Acids, 2016
The Roma represents a transnational ethnic group, with a current European population of 8-10 million. The evolutionary process that had the greatest impact on the gene pool of the Roma population is called the founder effect. Renal hypouricemia (RHUC) is a rare heterogenous inherited disorder characterized by impaired renal urate reabsorption.
Blanka, Stiburkova, Dana, Gabrikova, Pavel, Čepek, Pavel, Šimek, Pavol, Kristian, Elizabeth, Cordoba-Lanus, Felix, Claverie-Martin   +6 more
openaire   +2 more sources

Urate Transporter URAT1 Inhibitors: A Patent Review (2012 - 2015)

Expert Opinion on Therapeutic Patents, 2016
Human urate transporter 1 (URAT1, encoded by SLC22A12) has been identified as a key urate transporter expressed at the apical membrane of renal proximal tubule cells for regulating urate homeostasis. Therefore, URAT1 is an attractive target for the development of new uricosurics against hyperuricemia.
Ying Pan, Ling-Dong Kong
exaly   +3 more sources

URAT1 and GLUT9 mutations in Spanish patients with renal hypouricemia

Clinica Chimica Acta, 2018
Renal hypouricemia (RHUC), a rare inherited disorder characterized by impaired uric acid (UA) reabsorption in the proximal tubule, is caused by mutations in SLC22A12 or SLC2A9. Most mutations have been identified in Japanese patients, and only a few have been detected in Europeans.We report clinical, biochemical and genetics findings of fourteen ...
Felix Claverie-Martin, Jorge Trujillo-Suarez, Hilaria Gonzalez-Acosta, Cristina Aparicio, Maria L. Justa Roldan, Blanka Stiburkova, Kimiyoshi Ichida, Maria A. Martín-Gomez, Maria Herrero Goñi, Marta Carrasco Hidalgo-Barquero, Victoria Iñigo, Ricardo Enriquez, Elizabeth Cordoba-Lanus, Victor M. Garcia-Nieto   +13 more
openaire   +2 more sources

Recurrent URAT1 Gene Mutations and Prevalence of Renal Hypouricemia in Japanese

Pediatric Nephrology, 2005
Recent identification of the urate transporter in the kidney (URAT1, encoded by SLC22A12) led to the molecular elucidation of idiopathic renal hypouricemia, which is a predisposition toward exercise-induce acute renal failure. One Japanese patient with renal hypouricemia demonstrated compound heterozygous mutations of the URAT1 gene (Q297X and IVS2+1G ...
Satoko Tsuchida
exaly   +3 more sources

Loss of Urat1 exacerbates APAP-induced liver injury in mice

Toxicology
Acetaminophen (APAP) overdose stands as the paramount contributor to drug-elicited liver damage in clinical settings. Despite this, the intricate interplay between uric acid (UA) levels, its metabolism-linked regulatory genes, and their effects on APAP metabolism and hepatic functions remains elusive.
Kunlu Zhao, Shuaishuai Zhang, Jinhong Tian, Siyan Wu, Yongjun Chen, Zhenkun Wu, Jiacheng Liang, Huicong Wu, Jianxin Pang, Ting Wu   +9 more
openaire   +2 more sources

SAT0521 Lesinurad, an Inhibitor of the Uric Acid Transporter URAT1 and A Potential Therapy for Gout, Requires URAT1 Phenylalanine 365 for High Affinity Inhibition

Annals of the Rheumatic Diseases, 2014
Background In most patients, gout is caused by inefficient excretion of uric acid, resulting in hyperuricemia and the formation of crystal deposits of uric acid. The renal uric acid transporter URAT1 (SLC22A12) is important for regulating serum uric acid levels.
P.K. Tan, D. Hyndman, J.N. Miner
openaire   +1 more source

Discovery of Novel Benzomorpholine Derivatives as Potent URAT1 Inhibitors With Hypouricemic Effects

Bioorganic and Medicinal Chemistry Letters
Urate transporter 1 (URAT1) is a clinically validated therapeutic target for hyperuricemia and gout. To obtain structurally novel URAT1 inhibitors, a series of benzomorpholine derivatives were designed by adopting a pharmacophore guided molecular hybridization strategy.
Zhiyan Xiao, Xuechen Li, Xianxin Hou
exaly   +3 more sources