Target Information

Target General Infomation
Target ID
T76024
Former ID
TTDC00085
Target Name
C1 esterase
Gene Name
C1S
Synonyms
C1 esterase; C1-esterase; C1S
Target Type
Successful
Disease Hereditary angioedema [ICD9: 277.6; ICD10: D84.1]
Stroke [ICD9: 434.91, 437.6, 453, 671.5, 671.9; ICD10: I61-I63, I80-I82]
Function
C1s b chain is a serine protease that combineswith c1q and c1s to form c1, the first component of the classical pathway of the complement system. C1r activates c1s so that it can, in turn, activate c2 and c4.
BioChemical Class
Peptidase
Target Validation
T76024
UniProt ID
P09871
EC Number
EC 3.4.21.42
Sequence
MWCIVLFSLLAWVYAEPTMYGEILSPNYPQAYPSEVEKSWDIEVPEGYGIHLYFTHLDIE
LSENCAYDSVQIISGDTEEGRLCGQRSSNNPHSPIVEEFQVPYNKLQVIFKSDFSNEERF
TGFAAYYVATDINECTDFVDVPCSHFCNNFIGGYFCSCPPEYFLHDDMKNCGVNCSGDVF
TALIGEIASPNYPKPYPENSRCEYQIRLEKGFQVVVTLRREDFDVEAADSAGNCLDSLVF
VAGDRQFGPYCGHGFPGPLNIETKSNALDIIFQTDLTGQKKGWKLRYHGDPMPCPKEDTP
NSVWEPAKAKYVFRDVVQITCLDGFEVVEGRVGATSFYSTCQSNGKWSNSKLKCQPVDCG
IPESIENGKVEDPESTLFGSVIRYTCEEPYYYMENGGGGEYHCAGNGSWVNEVLGPELPK
CVPVCGVPREPFEEKQRIIGGSDADIKNFPWQVFFDNPWAGGALINEYWVLTAAHVVEGN
REPTMYVGSTSVQTSRLAKSKMLTPEHVFIHPGWKLLEVPEGRTNFDNDIALVRLKDPVK
MGPTVSPICLPGTSSDYNLMDGDLGLISGWGRTEKRDRAVRLKAARLPVAPLRKCKEVKV
EKPTADAEAYVFTPNMICAGGEKGMDSCKGDSGGAFAVQDPNDKTKFYAAGLVSWGPQCG
TYGLYTRVKNYVDWIMKTMQENSTPRED
Drugs and Mode of Action
Drug(s) Cinryze Drug Info Approved Hereditary angioedema [537022]
TS01 Drug Info Phase 1 Stroke [549430]
Modulator Cinryze Drug Info [529941]
TS01 Drug Info [1572591]
Inhibitor compound 28 Drug Info [528015]
Fucose Drug Info [551393]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Complement and coagulation cascades
Pertussis
Staphylococcus aureus infection
Systemic lupus erythematosus
NetPath Pathway TGF_beta_Receptor Signaling Pathway
WikiPathways Complement and Coagulation Cascades
Complement Activation, Classical Pathway
Human Complement System
Complement cascade
References
Ref 537022Emerging drug candidates of dipeptidyl peptidase IV (DPP IV) inhibitor class for the treatment of Type 2 Diabetes. Curr Drug Targets. 2009 Jan;10(1):71-87.
Ref 549430Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037017)
Ref
Ref 528015A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s. Bioorg Med Chem Lett. 2006 Apr 15;16(8):2200-4. Epub 2006 Feb 3.
Ref 5299412008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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