KLKB1
Synonyms
EC 3.4.21, Kallikrein B1, Kallikrein B, Plasma (Fletcher Factor) 1, Kininogenin, KLK3, PKK, Plasma Kallikrein, EC 3.4.21.34, PKKD, PPK, Fletcher factor, Plasma prekallikrein, KLKB1, EC:3.4.21.34
Description
KLKB1 (Plasma kallikrein) 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.
KO Status
RenMab: Antibody Discovery
Drug Information
Launched drugs: 3
Drugs in clinical trials: 6
Latest Research Phase: Approved
Drug Name
Code
Phase
Company
Indications
Clinical Trials
Lanadelumab
SHP-643, DX-2930, TAK-743, 2372V1TKXK (UNII code), X124-G01
Approved
Dyax Pharma
Coronavirus Disease 2019 (COVID-19), Angioedemas, Hereditary, Angioedema
Berotralstat
BCX-7353
Approved
Biocryst Pharmaceuticals
Angioedemas, Hereditary
Ecallantide
DX-88, EPI-KAL2, FOV-2302, CB-500929
Approved
Dyax Pharma
Macular Edema, Blood Loss, Surgical, Angioedemas, Hereditary, Retinal Vein Occlusion, Angioedema
KVD-900
KVD-900
Phase 2 Clinical
Kalvista Pharmaceuticals
Angioedemas, Hereditary
THR-149
TG-758, THR-149
Phase 2 Clinical
Bicycle Therapeutics, Thrombogenics Inc
Diabetic macular oedema, Diabetic Retinopathy, Diabetes Mellitus
KVD-824
KVD-824
Phase 2 Clinical
Vantia
Diabetic macular oedema, Hereditary Angioedema Types I and II, Angioedemas, Hereditary
KVD-001
KVD-001
Phase 2 Clinical
Vantia
Diabetic macular oedema
MDPK-67b
DM-107, MDPK-67, MDPK-67b
Phase 1 Clinical
Med Discovery
Neutropenia, Netherton Syndrome, Prostatic Neoplasms, Dermatitis, Atopic
ATN-249
ATN-249
Phase 1 Clinical
Attune Pharmaceuticals
Angioedemas, Hereditary
NTLA-2002
NTLA-2002
Preclinical
Intellia Therapeutics Inc
Angioedemas, Hereditary
References
Title
Authors
Source
Complete sequencing and characterization of 21,243 full-length human cDNAs
Ota T., Suzuki Y., Nishikawa T., Otsuki T., Sugiyama T., Irie R., Wakamatsu A., Hayashi K., Sato H., Nagai K., Kimura K., Makita H., Sekine M., Obayashi M., Nishi T., Shibahara T., Tanaka T., Ishii S., Sugano S.,
Nat. Genet. 36:40-45(2004)
Generation and annotation of the DNA sequences of human chromosomes 2 and 4
Hillier L.W., Graves T.A., Fulton R.S., Fulton L.A., Pepin K.H., Minx P., Wagner-McPherson C., Layman D., Wylie K., Sekhon M., Becker M.C., Fewell G.A., Delehaunty K.D., Miner T.L., Nash W.E., Kremitzki C., Oddy L., Du H., Wilson R.K.,
Nature 434:724-731(2005)
The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC)
The MGC Project Team,
Genome Res. 14:2121-2127(2004)
Location of the disulfide bonds in human plasma prekallikrein: the presence of four novel apple domains in the amino-terminal portion of the molecule
McMullen B.A., Fujikawa K., Davie E.W.,
Biochemistry 30:2050-2056(1991)
Inactivation of human plasma kallikrein and factor XIa by protein C inhibitor
Meijers J.C., Kanters D.H., Vlooswijk R.A., van Erp H.E., Hessing M., Bouma B.N.,
Biochemistry 27:4231-4237(1988)
Identification and quantification of N-linked glycoproteins using hydrazide chemistry, stable isotope labeling and mass spectrometry
Zhang H., Li X.-J., Martin D.B., Aebersold R.,
Nat. Biotechnol. 21:660-666(2003)
Human plasma N-glycoproteome analysis by immunoaffinity subtraction, hydrazide chemistry, and mass spectrometry
Liu T., Qian W.-J., Gritsenko M.A., Camp D.G. II, Monroe M.E., Moore R.J., Smith R.D.,
J. Proteome Res. 4:2070-2080(2005)
Glycoproteomics analysis of human liver tissue by combination of multiple enzyme digestion and hydrazide chemistry
Chen R., Jiang X., Sun D., Han G., Wang F., Ye M., Wang L., Zou H.,
J. Proteome Res. 8:651-661(2009)
Severe prekallikrein (Fletcher factor) deficiency due to a compound heterozygosis (383Trp stop codon and Cys529Tyr)
Lombardi A.M., Sartori M.T., Cabrio L., Fadin M., Zanon E., Girolami A.,
Thromb. Haemost. 90:1040-1045(2003)
A new type of plasma prekallikrein deficiency associated with homozygosity for Gly104Arg and Asn124Ser in apple domain 2 of the heavy-chain region
Katsuda I., Maruyama F., Ezaki K., Sawamura T., Ichihara Y.,
Eur. J. Haematol. 79:59-68(2007)