Target Information

Target General Infomation
Target ID
T87939
Former ID
TTDI02261
Target Name
mRNA of Plasma kallikrein
Gene Name
KLKB1
Synonyms
Fletcher factor (mRNA); KLKB1 (mRNA); Kininogenin (mRNA); Plasma kallikrein (mRNA); Plasma kallikrein light chain (mRNA); Plasma prekallikrein (mRNA); KLKB1
Target Type
Clinical Trial
Disease Amyloid polyneuropathy [ICD code not available]
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 play a role in the renin-angiotensin system by converting prorenin into renin.
BioChemical Class
Target of antisense drug
UniProt ID
P03952
EC Number
EC 3.4.21.34
Sequence
MILFKQATYFISLFATVSCGCLTQLYENAFFRGGDVASMYTPNAQYCQMRCTFHPRCLLF
SFLPASSINDMEKRFGCFLKDSVTGTLPKVHRTGAVSGHSLKQCGHQISACHRDIYKGVD
MRGVNFNVSKVSSVEECQKRCTNNIRCQFFSYATQTFHKAEYRNNCLLKYSPGGTPTAIK
VLSNVESGFSLKPCALSEIGCHMNIFQHLAFSDVDVARVLTPDAFVCRTICTYHPNCLFF
TFYTNVWKIESQRNVCLLKTSESGTPSSSTPQENTISGYSLLTCKRTLPEPCHSKIYPGV
DFGGEELNVTFVKGVNVCQETCTKMIRCQFFTYSLLPEDCKEEKCKCFLRLSMDGSPTRI
AYGTQGSSGYSLRLCNTGDNSVCTTKTSTRIVGGTNSSWGEWPWQVSLQVKLTAQRHLCG
GSLIGHQWVLTAAHCFDGLPLQDVWRIYSGILNLSDITKDTPFSQIKEIIIHQNYKVSEG
NHDIALIKLQAPLNYTEFQKPICLPSKGDTSTIYTNCWVTGWGFSKEKGEIQNILQKVNI
PLVTNEECQKRYQDYKITQRMVCAGYKEGGKDACKGDSGGPLVCKHNGMWRLVGITSWGE
GCARREQPGVYTKVAEYMDWILEKTQSSDGKAQMQSPA
Drugs and Mode of Action
Drug(s) ISIS-PKK Drug Info Phase 3 Amyloid polyneuropathy [549250]
Inhibitor compound 11 Drug Info [527967]
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 549250Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034193)
Ref 527967Small molecule inhibitors of plasma kallikrein. Bioorg Med Chem Lett. 2006 Apr 1;16(7):2034-6. Epub 2006 Jan 18.
Ref 551948Clinical pipeline report, company report or official report of ISIS Pharmaceuticals.

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