Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T15000
|
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| Former ID |
TTDC00259
|
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| Target Name |
Cytotoxic T-lymphocyte protein 4
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| Gene Name |
CTLA4
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| Synonyms |
CD152; CTLA-4; Cytotoxic T-lymphocyte-associated antigen 4; CTLA4
|
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| Target Type |
Successful
|
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| 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).
|
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| BioChemical Class |
Immunoglobulin
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| Target Validation |
T15000
|
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| UniProt ID | |||||
| Sequence |
MACLGFQRHKAQLNLATRTWPCTLLFFLLFIPVFCKAMHVAQPAVVLASSRGIASFVCEY
ASPGKATEVRVTVLRQADSQVTEVCAATYMMGNELTFLDDSICTGTSSGNQVNLTIQGLR AMDTGLYICKVELMYPPPYYLGIGNGTQIYVIDPEPCPDSDFLLWILAAVSSGLFFYSFL LTAVSLSKMLKKRSPLTTGVYVKMPPTEPECEKQFQPYFIPIN |
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| Drugs and Mode of Action | |||||
| Drug(s) | Ipilimumab | Drug Info | Approved | Late-stage melanoma; Prostate cancer | [1], [2], [3] |
| Tremelimumab | Drug Info | Phase 3 | Solid tumours | [4], [5] | |
| Inhibitor | Alpha-D-Mannose | Drug Info | [6] | ||
| Fucose | Drug Info | [6] | |||
| Modulator | Concatameric CTLA4Ig | Drug Info | [7] | ||
| CTLA-4-XTEN | Drug Info | [7] | |||
| Tremelimumab | Drug Info | [7] | |||
| 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 1 | Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5. | ||||
| REF 2 | 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4. | ||||
| REF 3 | (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 4 | ClinicalTrials.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 5 | (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 6 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
| REF 7 | (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). | ||||
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