Target Information

Target General Infomation
Target ID
T86057
Former ID
TTDC00243
Target Name
Solute carrier family 22 member 12
Gene Name
SLC22A12
Synonyms
Organic anion transporter 4-like protein; RST; Renal-specific transporter; Urate anion exchanger 1; SLC22A12
Target Type
Clinical Trial
Disease Gout [ICD9: 274.00274.1274.8274.9; ICD10: M10]
Hyperuricaemia [ICD9: 274, 274.00274.1274.8274.9, 790.6; ICD10: E79.0, M10]
Function
Required for efficient urate re-absorption in the kidney. Regulates blood urate levels. Mediates saturable urate uptake by facilitating the exchange of urate against organic anions.
BioChemical Class
Major facilitator superfamily
Target Validation
T86057
UniProt ID
Q96S37
Sequence
MAFSELLDLVGGLGRFQVLQTMALMVSIMWLCTQSMLENFSAAVPSHRCWAPLLDNSTAQ
ASILGSLSPEALLAISIPPGPNQRPHQCRRFRQPQWQLLDPNATATSWSEADTEPCVDGW
VYDRSIFTSTIVAKWNLVCDSHALKPMAQSIYLAGILVGAAACGPASDRFGRRLVLTWSY
LQMAVMGTAAAFAPAFPVYCLFRFLLAFAVAGVMMNTGTLLMEWTAARARPLVMTLNSLG
FSFGHGLTAAVAYGVRDWTLLQLVVSVPFFLCFLYSWWLAESARWLLTTGRLDWGLQELW
RVAAINGKGAVQDTLTPEVLLSAMREELSMGQPPASLGTLLRMPGLRFRTCISTLCWFAF
GFTFFGLALDLQALGSNIFLLQMFIGVVDIPAKMGALLLLSHLGRRPTLAASLLLAGLCI
LANTLVPHEMGALRSALAVLGLGGVGAAFTCITIYSSELFPTVLRMTAVGLGQMAARGGA
ILGPLVRLLGVHGPWLPLLVYGTVPVLSGLAALLLPETQSLPLPDTIQDVQNQAVKKATH
GTLGNSVLKSTQF
Drugs and Mode of Action
Drug(s) Lesinurad Drug Info Approved Hyperuricaemia [523730], [542652]
RDEA-684 Drug Info Phase 2 Gout [524409]
RDEA3170 Drug Info Phase 2 Hyperuricaemia [524664]
URC102 Drug Info Phase 2 Gout [524997]
Modulator Lesinurad Drug Info [543360]
RDEA3170 Drug Info [544332]
Inhibitor MORIN Drug Info [528700]
RDEA-684 Drug Info [543360]
URC102 Drug Info [550551]
Pathways
WikiPathways Transport of glucose and other sugars, bile salts and organic acids, metal ions and amine compounds
References
Ref 523730ClinicalTrials.gov (NCT01493531) Combining Lesinurad With Allopurinol in Inadequate Responders. U.S. National Institutes of Health.
Ref 524409ClinicalTrials.gov (NCT01927198) RDEA3170 Monotherapy in Subjects With Gout. U.S. National Institutes of Health.
Ref 524664ClinicalTrials.gov (NCT02078219) Phase II Dose Finding Study of RDEA3170 Versus Placebo in Japanese Patients With Gout or Asymptomatic Hyperuricemia. U.S. National Institutes of Health.
Ref 524997ClinicalTrials.gov (NCT02290210) Phase 2 Study of URC102 to Assess the Efficacy and Safety in Gout Patients. U.S. National Institutes of Health.
Ref 542652(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7673).
Ref 528700Drug Metab Dispos. 2007 Jun;35(6):981-6. Epub 2007 Feb 26.Morin (3,5,7,2',4'-pentahydroxyflavone) exhibits potent inhibitory actions on urate transport by the human urate anion transporter (hURAT1) expressed in human embryonic kidney cells.
Ref 543360(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1031).
Ref 544332The pathophysiology of hyperuricaemia and its possible relationship to cardiovascular disease, morbidity and mortality. BMC Nephrol. 2013; 14: 164.
Ref 550551Clinical pipeline report, company report or official report of Chugai Pharmaceutical (2013).

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