abatacept
有货
产品名称 | abatacept |
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CAS编号和信息 | rp173355 |
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Target ID | 2744 | ||||||||||||||||||||||||
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名称 | CD80 | ||||||||||||||||||||||||
缩写名 | SHP2 | ||||||||||||||||||||||||
家族 | Other immune checkpoint proteins | ||||||||||||||||||||||||
别名 | KCa2.1 | ||||||||||||||||||||||||
基因和蛋白信息 |
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RefSeq Protein | NP_005182 (Hs) , NP_033985 (Mm) , NP_037058 (Rn) | ||||||||||||||||||||||||
RefSeq Nucleotide | NM_005191 (Hs) , NM_009855 (Mm) , NM_012926 (Rn) | ||||||||||||||||||||||||
Entrez Gene | 941 (Hs) , 12519 (Mm) , 25408 (Rn) | ||||||||||||||||||||||||
UniProtKB | P33681 (Hs) , Q00609 (Mm) | ||||||||||||||||||||||||
Ensembl Gene | ENSG00000121594 (Hs) , ENSMUSG00000075122 (Mm) , ENSRNOG00000001527 (Rn) | ||||||||||||||||||||||||
OMIM | 112203 (Hs) | ||||||||||||||||||||||||
Protein GI | 4885123 (Hs) , 112983684 (Mm) , 29789034 (Rn) | ||||||||||||||||||||||||
DrugBank Target | P33681 (Hs) | ||||||||||||||||||||||||
CATH/Gene3D | 2.60.40.10 (N/A) | ||||||||||||||||||||||||
ChEMBL Target | CHEMBL2364157 (Hs) |
Target ID | 2745 | ||||||||||||||||||||||||
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名称 | CD86 | ||||||||||||||||||||||||
缩写名 | SHP2 | ||||||||||||||||||||||||
家族 | Other immune checkpoint proteins | ||||||||||||||||||||||||
别名 | KCa2.1 | ||||||||||||||||||||||||
基因和蛋白信息 |
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RefSeq Protein | NP_787058 (Hs) , NP_062261 (Mm) , NP_064466 (Rn) | ||||||||||||||||||||||||
RefSeq Nucleotide | NM_175862 (Hs) , NM_019388 (Mm) , NM_020081 (Rn) | ||||||||||||||||||||||||
Entrez Gene | 942 (Hs) , 12524 (Mm) , 56822 (Rn) | ||||||||||||||||||||||||
UniProtKB | P42081 (Hs) , P42082 (Mm) | ||||||||||||||||||||||||
Ensembl Gene | ENSG00000114013 (Hs) , ENSMUSG00000022901 (Mm) , ENSRNOG00000038835 (Rn) | ||||||||||||||||||||||||
OMIM | 601020 (Hs) | ||||||||||||||||||||||||
Protein GI | 332634934 (Hs) , 161484599 (Mm) , 11464989 (Rn) | ||||||||||||||||||||||||
DrugBank Target | P42081 (Hs) | ||||||||||||||||||||||||
CATH/Gene3D | 2.60.40.10 (N/A) | ||||||||||||||||||||||||
ChEMBL Target | CHEMBL2364156 (Hs) |
Ligand ID | 6891 |
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名称 | abatacept |
别名 | RG-1046 |
类别 | Peptide |
学名 | 4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide |
生物活性评价 |
In a cell based CD80/86 inhibition assay abatacept inhibits IL-2 release with an IC50 of 22.6 nM |
评价 |
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) |
配体家族 | Immune checkpoint modulators |
单字母多肽序列 | MGVLLTQRTLLSLVLALLFPSMASMAMHVAQPAVVLASSRGIASFVCEYASPGKATEVRVTVLRQADSQVTEVCAATYMMGNELTFLDDSICTGTSSGNQVNLTIQGLRAMDTGLYICKVELMYPPPYYLGIGNGTQIYVIDPEPCPDSDQEPKSSDKTHTSPPSPAPELLGGSSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK |
三字母多肽序列 | |
翻译后修饰 | |
化学修饰 | 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. |
1. Linsley PS, Brady W, Urnes M, Grosmaire LS, Damle NK, Ledbetter JA. (1991) CTLA-4 is a second receptor for the B cell activation antigen B7.. J Exp Med, 174 (3): (561-9). [PMID:1714933] |
2. Ludvigsson J. (2016) Therapies to Preserve β-Cell Function in Type 1 Diabetes.. Drugs, 76 (2): (169-85). [PMID:26645223] |
3. Davis IC, Randell J, Davis SN. (2015) Immunotherapies currently in development for the treatment of type 1 diabetes.. Expert Opin Investig Drugs, 24 (10): (1331-41). [PMID:26364507] |
4. Douthwaite J, Moisan J, Privezentzev C, Soskic B, Sabbah S, Cohen S, Collinson A, England E, Huntington C, Kemp B et al.. (2017) A CD80-Biased CTLA4-Ig Fusion Protein with Superior In Vivo Efficacy by Simultaneous Engineering of Affinity, Selectivity, Stability, and FcRn Binding.. J Immunol, 198 (1): (528-537). [PMID:27881707] |