Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| 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 | |||||
| Drug(s) | Ecallantide | Drug Info | Approved | Retinal venous occlusion | [1], [2] |
| Inhibitor | (3,4-dichlorophenyl)(1H-pyrazol-1-yl)methanone | Drug Info | [3] | ||
| (3-nitro-1H-pyrazol-1-yl)(p-tolyl)methanone | Drug Info | [3] | |||
| (3-nitro-1H-pyrazol-1-yl)(phenyl)methanone | Drug Info | [3] | |||
| (4-bromo-1H-pyrazol-1-yl)(p-tolyl)methanone | Drug Info | [3] | |||
| 1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide | Drug Info | [3] | |||
| D-Pro-Phe-Arg chloromethyl ketone | Drug Info | [4] | |||
| Ecallantide | Drug Info | [5] | |||
| ZK-810388 | Drug Info | [6] | |||
| ZK-814048 | Drug Info | [6] | |||
| 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 1 | ClinicalTrials.gov (NCT00969293) Study to Assess the Safety and Tolerability of a Single Administration of FOV2302 (Ecallantide) in Patients With Macular Edema Associated With Central Retinal Vein Occlusion. U.S. National Institutes of Health. | ||||
| REF 2 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6955). | ||||
| REF 3 | 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. | ||||
| REF 4 | J Med Chem. 2008 Jun 12;51(11):3077-80. Epub 2008 May 7.Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors. | ||||
| REF 5 | Ecallantide (DX-88), a plasma kallikrein inhibitor for the treatment of hereditary angioedema and the prevention of blood loss in on-pump cardiothoracic surgery. Expert Opin Biol Ther. 2008 Aug;8(8):1187-99. | ||||
| REF 6 | 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. | ||||
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