AnatomyChemicals and DrugsPhenomena and ProcessesInformation Science
KallikreinsTissue KallikreinsKininogensKininsKallikrein-Kinin SystemPlasma KallikreinSubmandibular GlandPrekallikreinReceptor, Bradykinin B2EsterasesBradykininSerine EndopeptidasesAmino Acid SequenceSubstrate SpecificityMolecular Sequence DataEndopeptidasesProstate-Specific AntigenMolecular WeightTumor Markers, BiologicalKinetics
Serine proteasesKLK1TissueComponents of the kallikrein-kininKLK5RecombinantPeptidasesProteinPlasmaBiomarkersKininsHereditary AngioedemaInhibitorSubfamilyKLK11ProteaseGeneELISAHumanAntigenEnzymeAbstractBiopsyCleavesAprotininSubstrateEvidence suggestsRoleExpressionBloodFunctionsAbnormalityHypertensiveActivityTherapeutic
Serine proteases7
  • Kallikreins are a subgroup of serine proteases, enzymes capable of cleaving peptide bonds in proteins. (wikipedia.org)
  • In humans, plasma kallikrein (encoded by KLKB1 gene) has no known paralogue, while tissue kallikrein-related peptidases (KLKs) encode a family of fifteen closely related serine proteases. (wikipedia.org)
  • The venom of solenodons and some shrews like the northern short-tailed shrew consist of multiple copies of kallikrein 1 (KLK1) serine proteases. (wikipedia.org)
  • Human kallikreins are serine proteases that comprise a recently identified large and closely related 15-member family. (rcsb.org)
  • Tissue kallikrein KLK1 and the kallikrein-related peptidases KLK2-15 are a subfamily of serine proteases that have defined or proposed roles in a range of central nervous system (CNS) and non-CNS pathologies. (fsu.edu)
  • Kallikrein-14 belongs to the kallikrein subgroup of serine proteases, which have diverse physiologic functions in many tissues. (rockland.com)
  • The serine proteases kallikrein 5 (KLK5) and kallikrein 7 (KLK7) control enzymatic processing of cathelicidin precursor in the skin and regulate the eventual function of the final forms of these peptides. (irosacea.org)
KLK14
  • Similar to KLKB1, three tissue kallikreins KLK1, KLK2 and KLK12 also participate in regulation of blood pressure via the activation of bradykinin. (wikipedia.org)
  • The pegylated KLK1 provided in the present invention has the advantages of significantly-extended life period, significantly-reduced immunogenicity and a stable and uniform structure, can be used for improving activities of the pegylated tissue kallikrein to a higher extent, and particularly, has more significant biological activities in the aspect of treating cerebral apoplexy and diabetic nephropathy. (onacademic.com)
  • Kallikrein-14 may activate or inactivate the proteinase-activated receptors F2R, F2RL1 and F2RL3 and other kallikreins including KLK1, KLK3, KLK5 and KLK11. (rockland.com)
  • METHODS AND RESULTS: Here, we demonstrate that tissue kallikrein knockout mice (KLK1-/-) show impaired muscle neovascularization in response to hindlimb ischemia. (ox.ac.uk)
Tissue15
  • Distinct from plasma kallikrein, tissue kallikreins (KLKs) are expressed throughout the human body and perform various physiological roles. (wikipedia.org)
  • This article is a review of exciting, recently generated genetic, biochemical and clinical data from studies that have examined the importance of the tissue kallikrein-kinin system in protection from hypertension, vascular remodeling and renal fibrosis. (nature.com)
  • 1993) A kallikrein-like enzyme in human vascular tissue. (nature.com)
  • Human tissue kallikrein (human K1) is the best functionally characterized member of this family, and is known to play an important role in blood pressure regulation. (rcsb.org)
  • Kallikreins (tissue and plasma kallikrein) are a subgroup of the serine protease family. (wikidoc.org)
  • Borgono, C.A., and Diamandis, E.P. "The emerging roles of human tissue kallikreins in cancer" Nature Reviews Cancer 4: 876-90, 2004. (wikidoc.org)
  • Diamandis, E.P., and Yousef, G.M. "Human Tissue Kallikreins: A Family of New Cancer Biomarkers" Clinical Chemistry 48: 1198-1205, 2002. (wikidoc.org)
  • The tissue kallikrein has a sequence shown in SEQ ID No. 1 or SEQ ID No. 2, the tissue kallikrein can be natural or recombinant, polyethylene glycol is polyethylene glycol with a molecular weight of 20-40kDa, and is coupled on an N-terminal primary amine of the tissue kallikrein. (onacademic.com)
  • 1. The liver is the main organ clearing both plasma and tissue kallikreins from the circulation. (unifesp.br)
  • Bradykinin, an effector molecule of the kallikrein system, is known to stimulate tissue plasminogen activator production. (le.ac.uk)
  • Paradoxically, however, tissue plasminogen activator protein levels were augmented with increasing kallikrein mRNA silencing. (le.ac.uk)
  • Critical role of tissue kallikrein in vessel formation and maturation: implications for therapeutic revascularization. (ox.ac.uk)
  • OBJECTIVE: Human Tissue Kallikrein (hKLK1) overexpression promotes an enduring neovascularization of ischemic tissue, yet the cellular mechanisms of hKLK1-induced arteriogenesis remain unknown. (ox.ac.uk)
  • CONCLUSIONS: These results demonstrate the fundamental role of endogenous Tissue Kallikrein in vascular repair and provide novel information on the cellular and molecular mechanisms responsible for the robust arterialization induced by hKLK1 overexpression. (ox.ac.uk)
  • Researchers suggest that this lack (deficiency) of functional plasma kallikrein protein does not generally cause any symptoms because another process called the extrinsic coagulation pathway (also known as the tissue factor pathway) can compensate for the impaired intrinsic coagulation pathway. (medlineplus.gov)
Components of the kallikrein-kinin1
  • Treatment of cells with siRNA resulted in a dose-dependent decrease in kallikrein mRNA levels, which impacted on other components of the kallikrein-kinin system, dose-dependently reducing bradykinin B2 receptor mRNA expression. (le.ac.uk)
KLK51
  • Stratum corneum tryptic enzyme kallikrein 5 (KLK5) is a serine protease that is involved in the cell renewal and maintenance of the skin barrier function. (irosacea.org)
Recombinant1
Peptidases1
  • The Role of Kallikrein-Related Peptidases in Atopic Dermatitis. (bvsalud.org)
Protein4
  • Kallikrein-14 is a protein that in humans is encoded by the KLK14 gene. (rockland.com)
  • Results: Western blotting demonstrated that mesangial cells produced a kallikrein protein, which was of a different molecular weight to urinary kallikrein from rats of the same species. (le.ac.uk)
  • Kallikrein suppression resulted in significant increases in fibronectin and transforming growth factor-[beta] protein levels in culture supernatants over control levels. (le.ac.uk)
  • This protein, when converted to an active form called plasma kallikrein in the blood, is involved in the early stages of blood clotting . (medlineplus.gov)
Plasma21
  • The KLKB1 gene encoding plasma kallikrein is located on chromosome 4q34-35. (wikipedia.org)
  • Plasma kallikrein liberates kinins (bradykinin and kallidin) from the kininogens, peptides responsible for the regulation of blood pressure and activation of inflammation. (wikipedia.org)
  • 1. Urinary prostaglandins (PG), kallikrein and plasma renin activity (PRA) were measured in 35 patients with essential hypertension and 22 normotensive controls before and 15 min after frusemide (40 mg intravenously). (portlandpress.com)
  • Preclinical evidence implicates the activity of plasma kallikrein in diabetic retinopathy, which is a leading cause of visual loss in patients suffering from diabetes mellitus. (nih.gov)
  • Employing a technology based on phage-display combined with chemical cyclization, we have identified highly selective bicyclic peptide inhibitors with nano- and picomolar potencies toward plasma kallikrein. (nih.gov)
  • A competitive ELISA for quantitative measurement of Canine KalliKrein 1 in samples from blood, plasma, serum, cell culture supernatant and other biological fluids. (gentaur.pl)
  • Prekallikrein is the precursor of plasma kallikrein. (wikidoc.org)
  • Hepatocytes are responsible for the internalization of rat plasma kallikrein (RPK) and the clearance of plasma kallikrein by the liver is Ca2+-independent. (unifesp.br)
  • The hepatic clearance of the alpha(2)-macroglobulin-plasma kallikrein complex is less efficient than the clearance of the free enzyme. (unifesp.br)
  • A coagulation disorder characterized by the partial or complete absence of plasma-type kallikrein activity in the blood. (nih.gov)
  • Role of Factor XIa and Plasma Kallikrein in Arterial and Venous Thrombosis. (nih.gov)
  • We propose that blocking the B2R and inhibiting plasma kallikrein activity might have an ameliorating effect on early disease caused by COVID-19 and might prevent acute respiratory distress syndrome (ARDS). (ru.nl)
  • Evaluation of the kallikrein-kinine system activity in blood plasma is of importance due to participation of the components of this system in regulation of blood plasma proteolysis. (msk.ru)
  • Plasma kallikrein structure reveals apple domain disc rotated conformation compared to factor XI. (nottingham.ac.uk)
  • Data presentations included new data from the Phase 2 trial highlighting rapid suppression of plasma kallikrein activity after KVD900 administration and its relationship with symptomatic relief. (pharmaceuticaldaily.com)
  • These data from our phase 2 trial in on-demand use for HAE attacks show that oral KVD900 is quickly absorbed, leading to rapid, near-complete suppression of plasma kallikrein activity, a key mediator of HAE attacks," said Andrew Crockett, Chief Executive Officer of KalVista. (pharmaceuticaldaily.com)
  • We believe that this rapid absorption followed by rapid suppression of plasma kallikrein activity is the basis for the early symptom relief we observed in the trial. (pharmaceuticaldaily.com)
  • KalVista has developed a proprietary portfolio of novel, small molecule plasma kallikrein inhibitors initially targeting hereditary angioedema (HAE) and diabetic macular edema (DME). (pharmaceuticaldaily.com)
  • In DME, an intravitreally administered plasma kallikrein inhibitor, called KVD001, has completed a Phase 2 clinical trial. (pharmaceuticaldaily.com)
  • Plasma kallikrein plays a role in a process called the intrinsic coagulation pathway (also called the contact activation pathway). (medlineplus.gov)
  • The KLKB1 gene mutations that cause prekallikrein deficiency reduce or eliminate functional plasma kallikrein, which likely impairs the intrinsic coagulation pathway. (medlineplus.gov)
Biomarkers3
  • While the function of the majority of the kallikreins remains to be elucidated, two members are useful biomarkers for prostate cancer and several others are potentially useful biomarkers for breast cancer, Alzheimer's, and Parkinson's disease. (rcsb.org)
  • Growing evidence suggests that many kallikreins are implicated in carcinogenesis and some have potential as novel cancer and other disease biomarkers. (rockland.com)
  • We will utilize multiple different approaches to discover and evaluate novel noninvasive diagnostic and prognostic biomarkers, including measurements of four kallikrein markers and microseminoprotein- beta (MSP) in blood adjusted with the interaction from GWAS-based genetic variation in certain biomarker-encoding gene loci to further improve the specificity in our previously reported detection of lethal PCa-forms at very early, curable stages. (lu.se)
Kinins1
Hereditary Angioedema1
  • Ecallantide, lanadelumab, and berotralstat are FDA-approved drugs that inhibit kallikrein and can be used for managing Hereditary Angioedema. (wikipedia.org)
Inhibitor1
  • 1. The acute effects of the kallikrein inhibitor aprotinin (498 ki.u./min), and the kininase II inhibitor SQ 14 225 (250 μg), given intravenously during saralasin-induced angiotensin blockade, were studied in conscious sham-operated rats and rats with benign and malignant two-kidney, one-clip Goldblatt hypertension during dietary sodium restriction. (portlandpress.com)
Subfamily2
  • This gene is one of the fifteen kallikrein subfamily members located in a cluster on chromosome 19. (rockland.com)
  • Kallikrein 11 (KLK11) is also known as Hippostasin, Serine protease 20, Trypsin-like protease, PRSS20, TLSP, which belongs to the peptidase S1 family and Kallikrein subfamily. (biovisi.com)
KLK111
  • Kallikrein 11 /KLK11 is a possible multifunctional protease and efficiently cleaves 'bz-Phe-Arg-4-methylcoumaryl-7-amide', a kallikrein substrate, and weakly cleaves other substrates for kallikrein and trypsin. (biovisi.com)
Protease2
  • It is also capable of generating plasmin from plasminogen: Kallikrein is homologous to factor XI and consists of four apple domains and one serine protease domain. (wikipedia.org)
  • Inhibition of Human Kallikrein 5 Protease by Triterpenoids from Natural Sources. (irosacea.org)
Gene3
  • hk3, human kallikrein gene 3) and human glandular kallikrein (hK2) are used as tumor markers for prostate cancer. (wikipedia.org)
  • Kallikrein-14 gene is identified in the kallikrein gene cluster on chromosome 19q13.4. (rockland.com)
  • Kallikrein gene 'knock-down' by small interfering RNA transfection induces a profibriotic phenotype in rat mesangial cells. (le.ac.uk)
ELISA1
  • The Human Kallikrein 3 ELISA ki can be used to identify samples from the human species. (elisakit.cc)
Human4
  • Aliquot 0.1ml per well of the 1000pg/ml, 500pg/ml, 250pg/ml, 125pg/ml, 62.5pg/ml, 31.2pg/ml, 15.6pg/ml human Kallikrein 14 standard solutions into the precoated 96-well plate. (rockland.com)
  • It is recommended that each human Kallikrein 14 standard solution and each sample be measured in duplicate. (rockland.com)
  • Validation and characterization of human kallikrein 11 as a serum marker for diagnosis of ovarian carcinoma. (uw.edu)
  • Measurements of urokinase receptor fractions and human glandular kallikrein 2 in serum improves discrimination of men with prostate cancer from men with no evidence of malignant disease. (ox.ac.uk)
Antigen1
  • Improving the Specificity of Screening for Lethal Prostate Cancer Using Prostate-specific Antigen and a Panel of Kallikrein Markers: A Nested Case-Control Study. (lu.se)
Enzyme2
  • 1990) A kallikrein-like enzyme in blood vessels of one-kidney, one clip hypertensive rats. (nature.com)
  • 1994) A kallikrein-like enzyme in the aorta of normotensive and hypertensive rats. (nature.com)
Abstract1
  • abstract = "30 asthenozoospermic subfertile men were treated parenterally for 3 months with kallikrein. (tau.ac.il)
Biopsy2
  • A Four-kallikrein Panel Predicts High-grade Cancer on Biopsy: Independent Validation in a Community Cohort. (lu.se)
  • Predicting High-Grade Cancer at Ten-Core Prostate Biopsy Using Four Kallikrein Markers Measured in Blood in the ProtecT Study. (lu.se)
Cleaves1
  • Prekallikrein is cleaved by factor XII to form kallikrein, which then cleaves factor XII first to alpha-factor XIIa and then to beta-factor XIIa. (nih.gov)
Aprotinin1
  • Prekallikrein Kinin-kallikrein system Kinin Aprotinin List of cutaneous conditions Raspi G (September 1996). (wikipedia.org)
Substrate2
  • Using D-Pro-Phe-Arg-pNA as a substrate, a procedure for simultaneous estimation of four patterns of the kallikrein-kinine system activity was developed: I. maintenance of contact phase, 2. (msk.ru)
  • Dotsenko V.L., Iarovaia G.A., Neshkova E.A. (1989) The use of a tripeptide chromogenic substrate for simultaneous determination of 4 indices of kallikrein-kinin system. (msk.ru)
Evidence suggests1
  • Background: Emerging evidence suggests that kallikrein exerts renoprotective effects independent of its haemodynamic actions. (le.ac.uk)
Role2
  • These properties of the liver are affected by pathological situations, particularly the acute-phase response to inflammation, in which the kallikrein-kinin system plays a major role. (unifesp.br)
  • The aim of the current investigation was to delineate the role of kallikrein in the regulation of fibrosis, by 'knocking down' its expression using specific small interfering RNAs (siRNA). (le.ac.uk)
Expression1
  • Kallikrein Expression and Cathelicidin Processing Are Independently Controlled in Keratinocytes by Calcium, Vitamin D(3), and Retinoic Acid. (irosacea.org)
Blood3
  • Kallikreins are responsible for the coordination of various physiological functions including blood pressure, semen liquefaction and skin desquamation. (wikipedia.org)
  • 4. Our demonstration that two agents with known opposite actions on the kallikrein-kinin system produced predictable and opposite effects on blood pressure may indicate that this system is involved in the homeostatic regulation of blood pressure. (portlandpress.com)
  • The kallikreins include both regulatory- and degradative-type proteases, impacting a variety of physiological processes including regulation of blood pressure, neuronal health, and the inflammatory response. (rcsb.org)
Functions1
  • As some kallikreins are able to catalyse the activation of other kallikreins, several cascades involving these proteases have been implicated in the regulation of homeostatic functions. (wikipedia.org)
Abnormality1
  • 3. These findings support the view that there is an abnormality of renal vasodilator systems (PGE 2 and kallikrein) in essential hypertension. (portlandpress.com)
Hypertensive1
  • 2. PGE 2 and kallikrein excretion rates were lower in hypertensive subjects, and failed to rise to the same extent after frusemide. (portlandpress.com)
Activity1
  • activity of kallikrein (0.104 un/ml), 4. (msk.ru)
Therapeutic1
  • Although the findings of this study indicate that PF-04886847 possesses limited anti-thrombotic and anti-inflammatory effects, PF-04886847 may have therapeutic potential in other kallikrein-kinin mediated diseases. (healthyconnectionsinc.com)