Details of the BTS

General Information of Binding Target of SBP (BTS) (ID: ST00088)
BTS Name
Plasma kallikrein
Synonyms
EC 3.4.21.34; Fletcher factor; Kininogenin; Plasma prekallikrein; PKK
BTS Type
Protein
Family
Peptidase S1 family;
Plasma kallikrein subfamily
Gene Name
KLKB1
Organism
Homo sapiens (Human)
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.
UniProt ID
P03952
UniProt Entry
KLKB1_HUMAN
PFam
PF00024 ; PF00089
Gene ID
3818
Sequence
MILFKQATYFISLFATVSCGCLTQLYENAFFRGGDVASMYTPNAQYCQMRCTFHPRCLLF
SFLPASSINDMEKRFGCFLKDSVTGTLPKVHRTGAVSGHSLKQCGHQISACHRDIYKGVD
MRGVNFNVSKVSSVEECQKRCTNNIRCQFFSYATQTFHKAEYRNNCLLKYSPGGTPTAIK
VLSNVESGFSLKPCALSEIGCHMNIFQHLAFSDVDVARVLTPDAFVCRTICTYHPNCLFF
TFYTNVWKIESQRNVCLLKTSESGTPSSSTPQENTISGYSLLTCKRTLPEPCHSKIYPGV
DFGGEELNVTFVKGVNVCQETCTKMIRCQFFTYSLLPEDCKEEKCKCFLRLSMDGSPTRI
AYGTQGSSGYSLRLCNTGDNSVCTTKTSTRIVGGTNSSWGEWPWQVSLQVKLTAQRHLCG
GSLIGHQWVLTAAHCFDGLPLQDVWRIYSGILNLSDITKDTPFSQIKEIIIHQNYKVSEG
NHDIALIKLQAPLNYTEFQKPICLPSKGDTSTIYTNCWVTGWGFSKEKGEIQNILQKVNI
PLVTNEECQKRYQDYKITQRMVCAGYKEGGKDACKGDSGGPLVCKHNGMWRLVGITSWGE
GCARREQPGVYTKVAEYMDWILEKTQSSDGKAQMQSPA
Sequence Length
638
Synthetic Binding Protein (SBP) Targeting This BTS
SBP Name Highest Status Mechanism Affinity Application Details Ref
Bicyclic peptide anti-PKK PK100 Research Inhibitor N.A. Hereditary angioedema [ICD-11: 4A00.14]
SBP Info
 		[1]
Bicyclic peptide anti-PKK PK115 Research Inhibitor N.A. Hereditary angioedema [ICD-11: 4A00.14]
SBP Info
 		[1]
Bicyclic peptide anti-PKK PK128 Research Inhibitor N.A. Hereditary angioedema [ICD-11: 4A00.14]
SBP Info
 		[1]
Bicyclic peptide anti-PKK PK15 Research Inhibitor N.A. Hereditary angioedema [ICD-11: 4A00.14]
SBP Info
 		[1]
Kunitz domain anti-PKK EPI-K503 Research Inhibitor Kd: 0.04 nM Research tool
SBP Info
 		[2]
Kunitz domain anti-PKK/FXIa KALI-DY Research Inhibitor Kd: 0.015 nM Tools as inhibitors of human plasma kallikrein
SBP Info
 		[3]
Kunitz domain Ecallantide Marketed Inhibitor Kd: 0.044 nM Hereditary angioedema [ICD-11: 4A00.14]
SBP Info
 		[4], [5]
References
1 Bicyclic peptides with optimized ring size inhibit human plasma kallikrein and its orthologues while sparing paralogous proteases. ChemMedChem. 2012 Jul;7(7):1173-6.
2 Iterative optimization of high-affinity protease inhibitors using phage display. 2. Plasma kallikrein and thrombin. Biochemistry. 1996 Jun 18;35(24):8058-67.
3 Potent and selective Kunitz domain inhibitors of plasma kallikrein designed by phage display. J Biol Chem. 1995 Oct 27;270(43):25411-7.
4 In vitro-engineered non-antibody protein therapeutics. Protein Cell. 2018 Jan;9(1):3-14.
5 KEGG DRUG Database. Ecallantide