Target Information

Target General Infomation
Target ID
T25726
Former ID
TTDI02084
Target Name
Glypican-3
Gene Name
GPC3
Synonyms
GTR22; Intestinal protein OCI5; MXR7; Secreted glypican3; GPC3
Target Type
Clinical Trial
Disease Hepatocellular carcinoma [ICD9: 155; ICD10: C22.0]
Function
Cell surface proteoglycan that bears heparan sulfate. Inhibits the dipeptidyl peptidase activity of DPP4. May be involved in the suppression/modulation of growth in the predominantly mesodermal tissues and organs. May play a role in the modulation of IGF2 interactions with its receptor and thereby modulate its function. May regulate growth and tumor predisposition.
BioChemical Class
Glypican
UniProt ID
P51654
Sequence
MAGTVRTACLVVAMLLSLDFPGQAQPPPPPPDATCHQVRSFFQRLQPGLKWVPETPVPGS
DLQVCLPKGPTCCSRKMEEKYQLTARLNMEQLLQSASMELKFLIIQNAAVFQEAFEIVVR
HAKNYTNAMFKNNYPSLTPQAFEFVGEFFTDVSLYILGSDINVDDMVNELFDSLFPVIYT
QLMNPGLPDSALDINECLRGARRDLKVFGNFPKLIMTQVSKSLQVTRIFLQALNLGIEVI
NTTDHLKFSKDCGRMLTRMWYCSYCQGLMMVKPCGGYCNVVMQGCMAGVVEIDKYWREYI
LSLEELVNGMYRIYDMENVLLGLFSTIHDSIQYVQKNAGKLTTTIGKLCAHSQQRQYRSA
YYPEDLFIDKKVLKVAHVEHEETLSSRRRELIQKLKSFISFYSALPGYICSHSPVAENDT
LCWNGQELVERYSQKAARNGMKNQFNLHELKMKGPEPVVSQIIDKLKHINQLLRTMSMPK
GRVLDKNLDEEGFESGDCGDDEDECIGGSGDGMIKVKNQLRFLAELAYDLDVDDAPGNSQ
QATPKDNEISTFHNLGNVHSPLKLLTSMAISVVCFFFLVH
Drugs and Mode of Action
Drug(s) GPC-3298306 Drug Info Phase 2 Hepatocellular carcinoma [533301]
RG7686 Drug Info Phase 2 Hepatocellular carcinoma [523754], [543113]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Proteoglycans in cancer
NetPath Pathway IL2 Signaling Pathway
Pathway Interaction Database Glypican pathway
Glypican 3 network
Reactome A tetrasaccharide linker sequence is required for GAG synthesis
HS-GAG degradation
Retinoid metabolism and transport
WikiPathways Visual phototransduction
References
Ref 523754ClinicalTrials.gov (NCT01507168) A Study of RO5137382 (GC33) in Patients With Advanced or Metastatic Hepatocellular Carcinoma. U.S. National Institutes of Health.
Ref 533301Glypican-3 is a biomarker and a therapeutic target of hepatocellular carcinoma. Hepatobiliary Pancreat Dis Int. 2015 Aug;14(4):361-6.
Ref 543113(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: 8406).
Ref 529782Usefulness of a novel oncofetal antigen, glypican-3, for diagnosis and immunotherapy of hepatocellular carcinoma. Nihon Rinsho Meneki Gakkai Kaishi. 2008 Oct;31(5):383-91.
Ref 532207First-in-man phase I study of GC33, a novel recombinant humanized antibody against glypican-3, in patients with advanced hepatocellular carcinoma. Clin Cancer Res. 2013 Feb 15;19(4):920-8.

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