Target Information

Target General Infomation
Target ID
T60724
Former ID
TTDNC00461
Target Name
Sclerostin
Gene Name
SOST
Synonyms
SOST
Target Type
Clinical Trial
Disease Metabolic bone disease [ICD10: E50-E64, E70-E90]
Osteopenia [ICD9: 733.9; ICD10: M85.8]
Osteoporosis [ICD9: 733.0, V07.4; ICD10: M80-M81, Z79.890]
Postmenopausal osteoporosis [ICD9: 733; ICD10: M80-M81]
Function
Negative regulator of bone growth that acts through inhibition of Wnt signaling and bone formation.
BioChemical Class
Sclerostin (SOST)
UniProt ID
Q9BQB4
Sequence
MQLPLALCLVCLLVHTAFRVVEGQGWQAFKNDATEIIPELGEYPEPPPELENNKTMNRAE
NGGRPPHHPFETKDVSEYSCRELHFTRYVTDGPCRSAKPVTELVCSGQCGPARLLPNAIG
RGKWWRPSGPDFRCIPDRYRAQRVQLLCPGGEAPRARKVRLVASCKCKRLTRFHNQSELK
DFGTEAARPQKGRKPRPRARSAKANQAELENAY
Drugs and Mode of Action
Drug(s) Romosozumab Drug Info Phase 3 Postmenopausal osteoporosis [523960], [542966]
BPS-804 Drug Info Phase 2 Metabolic bone disease [524231]
LY2541546 Drug Info Phase 2 Osteoporosis [523075]
AMG 167 Drug Info Phase 1 Osteopenia [523001]
Modulator AMG 167 Drug Info [544316]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Wnt signaling pathway
NetPath Pathway TWEAK Signaling Pathway
Reactome TCF dependent signaling in response to WNT
Negative regulation of TCF-dependent signaling by WNT ligand antagonists
References
Ref 523001ClinicalTrials.gov (NCT01101048) An Ascending Multiple Dose Study Evaluating AMG 167 in Healthy Men and Postmenopausal Women With Low Bone Mineral Density. U.S. National Institutes of Health.
Ref 523075ClinicalTrials.gov (NCT01144377) A Study of LY2541546 in Women With Low Bone Mineral Density. U.S. National Institutes of Health.
Ref 523960ClinicalTrials.gov (NCT01631214) Study to Determine the Efficacy and Safety of Romosozumab in the Treatment of Postmenopausal Women With Osteoporosis. U.S. National Institutes of Health.
Ref 524231ClinicalTrials.gov (NCT01806610) Study of Safety and Tolerability of BPS804 in Patients With Late-stage Chronic Kidney Disease. U.S. National Institutes of Health.
Ref 542966(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: 8092).
Ref 531711Rat-specific decreases in platelet count caused by a humanized monoclonal antibody against sclerostin. Toxicol Sci. 2012 Feb;125(2):586-94.
Ref 532609Romosozumab in postmenopausal women with low bone mineral density. N Engl J Med. 2014 Jan 30;370(5):412-20.
Ref 544316Osteoporosis - a current view of pharmacological prevention and treatment. Drug Des Devel Ther. 2013; 7: 435-448.
Ref 550150WO patent application no. 2010,1001,79, Self-forming gel system for sustained drug delivery.

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