abatacept   

GtoPdb Ligand ID: 6891

Synonyms: BMS-188667 | CTLA4-IgG4m | Orencia® | RG-1046 | RG-2077
abatacept is an approved drug (FDA (2005), EMA (2005))
Compound class: Antibody
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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Peptide Sequence
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.