Ontology highlight
ABSTRACT:
SUBMITTER: Tan PK
PROVIDER: S-EPMC5054527 | biostudies-literature | 2016 Oct
REPOSITORIES: biostudies-literature
Scientific reports 20161007
Gout is caused by elevated serum urate levels, which can be treated using inhibitors of the uric acid transporter, URAT1. We exploited affinity differences between the human and rat transporters to map inhibitor binding sites in URAT1. Human-rat transporter chimeras revealed that human URAT1 serine-35, phenylalanine-365 and isoleucine-481 are necessary and sufficient to provide up to a 100-fold increase in affinity for inhibitors. Moreover, serine-35 and phenylalanine-365 are important for high- ...[more]