Target General Infomation
Target ID
T15000
Former ID
TTDC00259
Target Name
Cytotoxic T-lymphocyte protein 4
Gene Name
CTLA4
Synonyms
CD152; CTLA-4; Cytotoxic T-lymphocyte-associated antigen 4; CTLA4
Target Type
Successful
Disease Autoimmune diabetes [ICD10: E08-E13]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Late-stage melanoma; Prostate cancer [ICD9:172, 185; ICD10: C43, C61]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Function
Possibly involved in T-cell activation. Binds to B7-1 (CD80) and B7-2 (CD86).
BioChemical Class
Immunoglobulin
Target Validation
T15000
UniProt ID
Sequence
MACLGFQRHKAQLNLATRTWPCTLLFFLLFIPVFCKAMHVAQPAVVLASSRGIASFVCEY
ASPGKATEVRVTVLRQADSQVTEVCAATYMMGNELTFLDDSICTGTSSGNQVNLTIQGLR
AMDTGLYICKVELMYPPPYYLGIGNGTQIYVIDPEPCPDSDFLLWILAAVSSGLFFYSFL
LTAVSLSKMLKKRSPLTTGVYVKMPPTEPECEKQFQPYFIPIN
Drugs and Mode of Action
Drug(s) Ipilimumab Drug Info Approved Late-stage melanoma; Prostate cancer [531351], [531783], [541945]
Tremelimumab Drug Info Phase 3 Solid tumours [525318], [543152]
Inhibitor Alpha-D-Mannose Drug Info [551393]
Fucose Drug Info [551393]
Modulator Concatameric CTLA4Ig Drug Info [543700]
CTLA-4-XTEN Drug Info [543700]
Tremelimumab Drug Info [543700]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Cell adhesion molecules (CAMs)
T cell receptor signaling pathway
Autoimmune thyroid disease
Rheumatoid arthritis
Pathway Interaction Database Calcineurin-regulated NFAT-dependent transcription in lymphocytes
Reactome CTLA4 inhibitory signaling
WikiPathways Vitamin D Receptor Pathway
T-Cell Receptor and Co-stimulatory Signaling
Allograft Rejection
Costimulation by the CD28 family
References
Ref 525318ClinicalTrials.gov (NCT02551159) Phase III Open Label First Line Therapy Study of MEDI 4736 With or Without Tremelimumab Versus Standard of Care (SOC) in SCCHN.
Ref 531351Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
Ref 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
Ref 541945(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: 6888).
Ref 543152(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: 8462).
Ref 531351Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
Ref 536574Therapeutic applications of aptamers. Expert Opin Investig Drugs. 2008 Jan;17(1):43-60.
Ref 543700(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: 2743).
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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