abatacept   Click here for help

GtoPdb Ligand ID: 6891

Synonyms: BMS-188667 | CTLA4-IgG4m | Orencia® | RG-1046 | RG-2077
Approved drug Immunopharmacology Ligand
abatacept is an approved drug (FDA (2005), EMA (2005))
Compound class: Peptide or derivative
Comment: Abatacept is a recombinant protein fusing the extracellular domain of human cytotoxic T-lymphocyte-associated antigen 4 (CTLA-4) to the modified Fc (hinge, CH2, and CH3 domains) portion of human immunoglobulin G1 (IgG1) [3]. In essence, abatacept is a CTLA-4 mimetic, that enhances CTLA-4's inhibitory signal to T cells, thereby down-modulating T cell mediated inflammation.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species

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View more information in the IUPHAR Pharmacology Education Project: abatacept

Peptide Sequence Click here for help
MGVLLTQRTLLSLVLALLFPSMASMAMHVAQPAVVLASSRGIASFVCEYASPGKATEVRVTVLRQADSQVTEVCAATYMM
GNELTFLDDSICTGTSSGNQVNLTIQGLRAMDTGLYICKVELMYPPPYYLGIGNGTQIYVIDPEPCPDSDQEPKSSDKTH
TSPPSPAPELLGGSSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVS
VLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESN
GQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
Chemical Modification
The drug is a dimeric protein, consisting of two identical subunits linked by a disulphide bridge (between Cys146 on each subunit). The sequence shown above is for a single monomer. Intra-subunit disulphide bridges form between cysteines 47-118, 74-92, 197-217 and 303-401. There are glycosylation sites at Asn102, Asn134 and Asn233. This additional structural information is taken from the INN record for the drug.