Target Information
Target General Infomation | |||||
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Target ID |
T82739
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Former ID |
TTDC00013
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Target Name |
Plasma kallikrein
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Gene Name |
KLKB1
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Synonyms |
Fletcher factor; KLK3; Kininogenin; Plasma kallikrein heavy chain; Plasma kallikrein light chain; Plasma prekallikrein; KLKB1
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Target Type |
Successful
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Disease | Retinal venous occlusion [ICD10: H34.8] | ||||
Function |
The enzyme cleaves Lys-Arg and Arg-Ser bonds. It activates, in a reciprocal reaction, factor XII after its binding to a negatively charged surface. It also releases bradykinin from HMW kininogen and may also playa role in the renin-angiotensin system by converting prorenin into renin.
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BioChemical Class |
Peptidase
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Target Validation |
T82739
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UniProt ID | |||||
EC Number |
EC 3.4.21.34
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Sequence |
MILFKQATYFISLFATVSCGCLTQLYENAFFRGGDVASMYTPNAQYCQMRCTFHPRCLLF
SFLPASSINDMEKRFGCFLKDSVTGTLPKVHRTGAVSGHSLKQCGHQISACHRDIYKGVD MRGVNFNVSKVSSVEECQKRCTNNIRCQFFSYATQTFHKAEYRNNCLLKYSPGGTPTAIK VLSNVESGFSLKPCALSEIGCHMNIFQHLAFSDVDVARVLTPDAFVCRTICTYHPNCLFF TFYTNVWKIESQRNVCLLKTSESGTPSSSTPQENTISGYSLLTCKRTLPEPCHSKIYPGV DFGGEELNVTFVKGVNVCQETCTKMIRCQFFTYSLLPEDCKEEKCKCFLRLSMDGSPTRI AYGTQGSSGYSLRLCNTGDNSVCTTKTSTRIVGGTNSSWGEWPWQVSLQVKLTAQRHLCG GSLIGHQWVLTAAHCFDGLPLQDVWRIYSGILNLSDITKDTPFSQIKEIIIHQNYKVSEG NHDIALIKLQAPLNYTEFQKPICLPSKGDTSTIYTNCWVTGWGFSKEKGEIQNILQKVNI PLVTNEECQKRYQDYKITQRMVCAGYKEGGKDACKGDSGGPLVCKHNGMWRLVGITSWGE GCARREQPGVYTKVAEYMDWILEKTQSSDGKAQMQSPA |
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Drugs and Mode of Action | |||||
Inhibitor | (3,4-dichlorophenyl)(1H-pyrazol-1-yl)methanone | Drug Info | [529037] | ||
(3-nitro-1H-pyrazol-1-yl)(p-tolyl)methanone | Drug Info | [529037] | |||
(3-nitro-1H-pyrazol-1-yl)(phenyl)methanone | Drug Info | [529037] | |||
(4-bromo-1H-pyrazol-1-yl)(p-tolyl)methanone | Drug Info | [529037] | |||
1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide | Drug Info | [529037] | |||
D-Pro-Phe-Arg chloromethyl ketone | Drug Info | [529454] | |||
Ecallantide | Drug Info | [536771] | |||
ZK-810388 | Drug Info | [528872] | |||
ZK-814048 | Drug Info | [528872] | |||
Pathways | |||||
KEGG Pathway | Complement and coagulation cascades | ||||
NetPath Pathway | AndrogenReceptor Signaling Pathway | ||||
PANTHER Pathway | Blood coagulation | ||||
PathWhiz Pathway | Coagulation | ||||
Reactome | Intrinsic Pathway of Fibrin Clot Formation | ||||
Activation of Matrix Metalloproteinases | |||||
WikiPathways | Complement and Coagulation Cascades | ||||
Human Complement System | |||||
Blood Clotting Cascade | |||||
Formation of Fibrin Clot (Clotting Cascade) | |||||
References | |||||
Ref 528872 | J Med Chem. 2007 Jun 28;50(13):2967-80. Epub 2007 May 31.Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors. | ||||
Ref 529037 | J Med Chem. 2007 Oct 4;50(20):4928-38. Epub 2007 Sep 12.N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase. |
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