Page last updated: 2024-12-10

cathepsin g

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Description

Cathepsin G: A serine protease found in the azurophil granules of NEUTROPHILS. It has an enzyme specificity similar to that of chymotrypsin C. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4381936
SCHEMBL ID10305897
MeSH IDM0528193

Synonyms (3)

Synonym
cathepsin g
4-[[(2s)-1-[[(2s)-1-[(2s)-2-[[(2s)-1-(4-nitroanilino)-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-oxobutanoic acid
SCHEMBL10305897

Research Excerpts

Overview

Cathepsin G (CatG) is a pro-inflammatory neutrophil serine protease. It is important for host defense, and has been implicated in several inflammatory disorders. CathepsIn G (CTSG) can increase the permeability of vascular endothelial cells.

ExcerptReferenceRelevance
"Cathepsin G (CatG) is a pro-inflammatory neutrophil serine protease that is important for host defense, and has been implicated in several inflammatory disorders. "( Homogeneous, Synthetic, Non-Saccharide Glycosaminoglycan Mimetics as Potent Inhibitors of Human Cathepsin G.
Afosah, DK; Al-Horani, RA; Desai, UR; Diagne, SR; Fayyad, RM; Langmia, EK; Merrell, S; Puliafico, VR, 2023
)
2.57
"Cathepsin G (CTSG) is a bactericidal serine protease stored in the neutrophil azurophilic granules."( The N125S polymorphism in the cathepsin G gene (rs45567233) is associated with susceptibility to osteomyelitis in a Spanish population.
Álvarez, V; Asensi, V; Carton, JA; Fierer, J; Meana, Á; Montes, AH; Ocaña, MG; Pérez-Is, L; Valle-Garay, E, 2019
)
1.52
"Cathepsin G (CTSG) is a neutrophil serine protease of the chymotrypsin C family known to degrade extracellular matrix components and to have regulatory functions in inflammatory disorders."( Absence of the neutrophil serine protease cathepsin G decreases neutrophil granulocyte infiltration but does not change the severity of acute pancreatitis.
Aghdassi, AA; John, DS; Krüger, B; Lerch, MM; Mayerle, J; Sendler, M; Storck, C; van den Brandt, C; Weiss, FU, 2019
)
1.5
"Cathepsin G is a neutrophil-derived protease that can activate IL-36γ."( Downregulation of interleukin 36γ and its cleaver cathepsin G following treatment with narrow-band ultraviolet B phototherapy in psoriasis vulgaris.
AlOrbani, AM; Amer, MA; El Desouky, ED; El-Kalioby, M; El-Komy, MHM; Nouredin Mohammed, F; Rashed, LA; Saadi, DG; Said, ER, 2022
)
1.7
"Cathepsin G (CTSG) is a member of the serine proteases family and can increase the permeability of vascular endothelial cells and the chemotaxis of inflammatory cells."( The role and mechanism of cathepsin G in dermatomyositis.
Gao, S; Li, Q; Luo, H; Yang, H; Zhang, H; Zhu, H, 2017
)
1.48
"Cathepsin G is a serine protease with a broad range of catalytic activities, including production of angiotensin II, degradation of extracellular matrix and cell-cell junctions, modulation of chemotactic responses, and induction of apoptosis. "( Cathepsin G deficiency decreases complexity of atherosclerotic lesions in apolipoprotein E-deficient mice.
Karunakaran, D; Leenen, FH; Milne, RW; Rafatian, N; Rayner, KJ; Whitman, SC, 2013
)
3.28
"Cathepsin G (CatG) is a neutral proteinase originating from human neutrophils. "( Inhibitors of cathepsin G: a patent review (2005 to present).
Kosikowska, P; Lesner, A, 2013
)
2.19
"Cathepsin G (CatG) is a serine protease that mediates angiotensin I to angiotensin II (Ang-II) conversion and is highly expressed in human abdominal aortic aneurysms (AAAs). "( Cathepsin G deficiency reduces periaortic calcium chloride injury-induced abdominal aortic aneurysms in mice.
Kovanen, PT; Lesner, A; Libby, P; Liu, J; Ozaki, K; Shi, GP; Sukhova, GK; Wang, J, 2015
)
3.3
"Cathepsin G is a serine peptidase whose physiological role is mainly associated with an early immune response, anti-microbial activity as well as platelet activation or hydrolysis of coagulation factors. "( Determination of cathepsin G in endometrial tissue using a surface plasmon resonance imaging biosensor with tailored phosphonic inhibitor.
Burchacka, E; Gorodkiewicz, E; Grzywa, R; Laudański, P; Lesner, A; Sieńczyk, M; Łukaszewski, Z, 2014
)
2.18
"Cathepsin G is an enzyme with dual chymotrypsin and trypsin-like specificity. "( New potent cathepsin G phosphonate inhibitors.
Legowska, A; Lesner, A; Oleksyszyn, J; Pietrusewicz, E; Rolka, K; Sieńczyk, M; Wysocka, M, 2008
)
2.18
"Cathepsin G is a serine protease secreted by activated neutrophils that play a role in the inflammatory response. "( Cathepsin G, a neutrophil protease, induces compact cell-cell adhesion in MCF-7 human breast cancer cells.
Hagiwara, T; Kigoshi, H; Kudo, T; Takino, T; Yamazaki, M; Yui, S, 2009
)
3.24
"As cathepsin G is a serpin involved both in inflammation and coagulation activation, this confirms and expands the concept of a marked dysregulation of both inflammatory and hemostatic balances occurring after CABG."( Proteomic analysis of plasma from patients undergoing coronary artery bypass grafting reveals a protease/antiprotease imbalance in favor of the serpin alpha1-antichymotrypsin.
Alamanni, F; Banfi, C; Barcella, S; Brioschi, M; Centenaro, C; Loardi, C; Mussoni, L; Parolari, A; Tremoli, E, 2010
)
0.87
"Cathepsin G is a major secreted serine peptidase of neutrophils and mast cells. "( How immune peptidases change specificity: cathepsin G gained tryptic function but lost efficiency during primate evolution.
Caughey, GH; Craik, CS; Makarova, A; Ray, M; Raymond, WW; Trivedi, NN, 2010
)
2.07
"Cathepsin G (Cat-G) is a neutrophil serine-protease found in the colonic lumen of ulcerative colitis (UC) patients. "( Intracolonic infusion of fecal supernatants from ulcerative colitis patients triggers altered permeability and inflammation in mice: role of cathepsin G and protease-activated receptor-4.
Annahazi, A; Bézirard, V; Bueno, L; Cartier, C; Dabek, M; Ferrier, L; Leveque, M; Polizzi, A; Roka, R; Theodorou, V; Wittmann, T, 2011
)
2.01
"Cathepsin G (CG) is a serine protease secreted from activated neutrophils."( Cathepsin G induces cell aggregation of human breast cancer MCF-7 cells via a 2-step mechanism: catalytic site-independent binding to the cell surface and enzymatic activity-dependent induction of the cell aggregation.
Ichisugi, T; Mizoguchi, S; Morimoto-Kamata, R; Yui, S, 2012
)
2.54
"Cathepsin G is a neutrophil-derived serine protease that contributes to tissue damage at sites of inflammation. "( Neutrophil cathepsin G promotes detachment-induced cardiomyocyte apoptosis via a protease-activated receptor-independent mechanism.
Alcott, SG; Andrade-Gordon, P; Derian, C; Elouardighi, H; Kinnally, K; Pak, E; Sabri, A; Steinberg, SF, 2003
)
2.15
"Cathepsin G (CatG) is a serine protease found in the azurophilic granules of monocytes that is known to have antimicrobial properties, but its role in Mycobacterium tuberculosis infection is unknown. "( The down-regulation of cathepsin G in THP-1 monocytes after infection with Mycobacterium tuberculosis is associated with increased intracellular survival of bacilli.
Rivera-Marrero, CA; Roman, J; Shafer, WM; Stewart, J, 2004
)
2.08
"Cathepsin G is a hematopoietic serine protease stored in the azurophil granules of neutrophil granulocytes. "( The proximal promoter of the human cathepsin G gene conferring myeloid-specific expression includes C/EBP, c-myb and PU.1 binding sites.
Garwicz, D; Gullberg, U; Lennartsson, A; Lindmark, A, 2005
)
2.05
"Cathepsin g is a neutrophil- and mast cell-derived protease, which can convert angiotensin I to angiotensin II and thereby activate the TGF-beta pathway, resulting in myocyte necrosis, hypertrophy, and increased fibrosis."( Mast cell-derived cathepsin g: a possible role in the adverse remodeling of the failing human heart.
Assad-Kottner, C; Jahanyar, J; Koerner, MM; Loebe, M; Noon, GP; Torre-Amione, G; Youker, KA, 2007
)
1.39
"Cathepsin G is a very potent platelet agonist and degranulator, comparable to maximal thrombin, which alters platelet surface glycoprotein expression for enhanced neutrophil binding and effective platelet aggregation. "( Human neutrophil cathepsin G is a potent platelet activator.
Barnard, MR; Benoit, SE; LaRosa, CA; Michelson, AD; Rodino, LJ; Rohrer, MJ, 1994
)
2.07
"Cathepsin G is a neutral serine protease of the granzyme B family which is found in human PMN, cells known to be important in the defense of the periodontium against periodontal bacteria. "( Identification of CG-1, a natural peptide antibiotic derived from human neutrophil cathepsin G.
Cho, Y; Harwig, SS; Lehrer, RI; Miyasaki, KT; Qu, XD, 1995
)
1.96
"Cathepsin G is a neutrophil-derived protease that has been shown to inhibit the effects of thrombin on some cells expressing thrombin receptors while acting as an agonist on others. "( Proteolysis of the human platelet and endothelial cell thrombin receptor by neutrophil-derived cathepsin G.
Abrams, C; Belmonte, E; Blanchard, N; Brass, LF; Cerletti, C; Hoxie, JA; Molino, M; Tarver, AP, 1995
)
1.95
"Cathepsin G is a serine, chymotrypsin-like protease released by activated polymorphonuclear leukocytes (PMN) that may act as a platelet agonist. "( Effects of leukocyte-derived cathepsin G on platelet membrane glycoprotein Ib-IX and IIb-IIIa complexes: a comparison with thrombin.
Cerletti, C; de Gaetano, G; Di Lallo, M; Martelli, N; Molino, M, 1993
)
2.02
"Cathepsin G is a serine protease located in the azurophil granules of neutrophils. "( Cathepsin G binds to human lymphocytes.
Aoki, Y; Yamazaki, T, 1997
)
3.18
"Cathepsin G is a serine protease located in the azurophil granules of neutrophils. "( Cathepsin G enhances human natural killer cytotoxicity.
Aoki, Y; Yamazaki, T, 1998
)
3.19
"Cathepsin G is a neutral serine proteinase that exists primarily in azurophilic granules of neutrophils, but also as a proteolytically active membrane-bound form. "( Augmented inflammatory responses and altered wound healing in cathepsin G-deficient mice.
Abbott, RE; Corral, CJ; Ley, TJ; Lin, X; MacIvor, DM; Mustoe, TA, 1998
)
1.98
"Cathepsin G is a neutral serine protease that is highly expressed at the promyelocyte stage of myeloid development. "( Normal neutrophil function in cathepsin G-deficient mice.
Abraham, SN; Belaaouaj, A; Ley, TJ; MacIvor, DM; Pham, CT; Shapiro, SD, 1999
)
2.03
"Cathepsin G is a neutrophil granule derived antimicrobial chymotrypsin-like enzyme. "( The neutrophil granule protein cathepsin G activates murine T lymphocytes and upregulates antigen-specific IG production in mice.
Chertov, O; Murphy, WJ; Oppenheim, JJ; Tani, K; Wang, JM, 2001
)
2.04
"The cathepsin G is a glycoprotein, while the elastase molecule lacks carbohydrate components."( Isolation and some physical and chemical properties of elastase and cathepsin G from dog neutrophils.
Andreeva, YV; Berlov, MN; Kokryakov, VN; Lodygin, PA, 2001
)
1.03
"Cathepsin G is a neutral serine protease that is found in the azurophil granules of neutrophils and monocytes. "( Developmental regulation of the human cathepsin G gene in myelomonocytic cells.
Burnett, D; Campbell, EJ; Connolly, NL; Hanson, RD; Ley, TJ; Senior, RM, 1990
)
1.99
"Cathepsin G is a 26,000-Da serine protease that is found in the azurophil granules of neutrophils and monocytes. "( Genomic organization and chromosomal localization of the human cathepsin G gene.
Hanson, RD; Hohn, PA; Ley, TJ; Popescu, NC; Salvesen, G, 1989
)
1.96

Effects

Cithepsin G has in primates both chymase and tryptase activity. Studies on its enzymatic properties have been limited by a lack of sensitive synthetic substrates. Anti-cathepsIn G antibodies have been detected by using three different methods.

ExcerptReferenceRelevance
"Cathepsin G has in primates both chymase and tryptase activity."( Mast Cell and Basophil Granule Proteases -
Akula, S; Fu, Z; Hellman, L; Wernersson, S, 2022
)
1.44
"Anti-cathepsin G antibodies have been detected by using three different methods. "( Methods of detection of anti-cathepsin G autoantibodies in human.
Halbwachs-Mecarelli, L; Lesavre, P; Nusbaum, P, 1993
)
1.09
"Cathepsin G has both trypsin- and chymotrypsin-like activity, but studies on its enzymatic properties have been limited by a lack of sensitive synthetic substrates. "( New, sensitive fluorogenic substrates for human cathepsin G based on the sequence of serpin-reactive site loops.
Brillard-Bourdet, M; Gauthier, F; Juliano, L; Juliano, MA; Moreau, T; Réhault, S, 1999
)
2

Actions

ExcerptReferenceRelevance
"Cathepsin G promotes E-cadherin/catenin complex formation and Rap1 activation in MCF-7 cells, which reportedly regulates E-cadherin-based cell-cell junctions."( Cathepsin G, a neutrophil protease, induces compact cell-cell adhesion in MCF-7 human breast cancer cells.
Hagiwara, T; Kigoshi, H; Kudo, T; Takino, T; Yamazaki, M; Yui, S, 2009
)
2.52

Treatment

Pretreatment with cathepsin G did not affect responses to ADP or a low concentration of platelet-activating factor. The function of the fibrinogen receptor, GPIIb/IIIa was unchanged. Treatment with diisopropyl fluorophosphate reduced its bactericidal activity against Capnocytophaga spp.

ExcerptReferenceRelevance
"Pretreatment with cathepsin G did not affect responses to ADP or a low concentration of platelet-activating factor in the presence of fibrinogen, indicating that receptors for these agonists were unaffected and that the function of the fibrinogen receptor, GPIIb/IIIa was unchanged."( Effects of cathepsin G pretreatment of platelets on their subsequent responses to aggregating agents.
Kinlough-Rathbone, RL; Packham, MA; Perry, DW; Rand, ML, 1999
)
1.02
"Pretreatment with cathepsin G markedly increased susceptibility of macrophages but not CD4(+) T cells to acute HIV-1 infection."( Cathepsin G, a neutrophil-derived serine protease, increases susceptibility of macrophages to acute human immunodeficiency virus type 1 infection.
Fauci, AS; Moriuchi, H; Moriuchi, M, 2000
)
2.07
"Treatment of cathepsin G with diisopropyl fluorophosphate significantly reduced its bactericidal activity against Capnocytophaga spp."( In vitro killing of Actinobacillus actinomycetemcomitans and Capnocytophaga spp. by human neutrophil cathepsin G and elastase.
Bodeau, AL; Miyasaki, KT, 1991
)
0.85

Toxicity

ExcerptReferenceRelevance
"We have recently demonstrated that polymorphonuclear neutrophils were toxic to hepatocytes through a protease-mediated mechanism."( Decreased toxicity of polymorphonuclear neutrophils toward hepatocytes isolated from rats with acute inflammatory reaction.
Dhumeaux, D; Mallat, A; Mavier, P; Preaux, AM; Rosenbaum, J, 1990
)
0.28

Pharmacokinetics

ExcerptReferenceRelevance
" A population pharmacokinetic (PPK) model was developed to characterize brensocatib exposure, determine potential relationships between brensocatib exposure and efficacy and safety measures, and inform dose selection in clinical studies."( Pharmacokinetic/Pharmacodynamic Evaluation of the Dipeptidyl Peptidase 1 Inhibitor Brensocatib for Non-cystic Fibrosis Bronchiectasis.
Chalmers, JD; Fernandez, C; Mange, KC; Rubino, CM; Teper, A; Usansky, H; Zou, J, 2022
)
0.72
" A total of 1284 steady-state brensocatib concentrations from 225 individuals were included in the PPK data set; 241 patients with NCFBE from the phase II study were included in the pharmacodynamic (PD) population for the PK/PD analyses."( Pharmacokinetic/Pharmacodynamic Evaluation of the Dipeptidyl Peptidase 1 Inhibitor Brensocatib for Non-cystic Fibrosis Bronchiectasis.
Chalmers, JD; Fernandez, C; Mange, KC; Rubino, CM; Teper, A; Usansky, H; Zou, J, 2022
)
0.72

Bioavailability

ExcerptReferenceRelevance
" This, together with the fact that it has a good bioavailability and a very low anticoagulant activity, suggests that it might be an adjuvant of MPI-based therapy of cystic fibrosis."( Heparin accelerates the inhibition of cathepsin G by mucus proteinase inhibitor: potent effect of O-butyrylated heparin.
Bieth, JG; Duranton, J; Ermolieff, J; Petitou, M, 1998
)
0.57
" Compound 6h was orally bioavailable in rats (F=39%), and orally efficacious in a hamster model of inflammation."( Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.
Almond, HR; Cantwell, AM; Corcoran, TW; Damiano, BP; de Garavilla, L; Di Cera, E; Greco, MN; Hall, J; Hawkins, MJ; Maryanoff, BE; Minor, LK; Powell, ET; Savvides, SN; Wang, Y, 2007
)
0.34
" In this review, we describe the physicochemical functions of these proteases, toward a goal of better delineating their role in human diseases and identifying new therapeutic strategies based on the modulation of their bioavailability and activity."( Neutrophil elastase, proteinase 3, and cathepsin G as therapeutic targets in human diseases.
Gauthier, F; Horwitz, MS; Jenne, DE; Korkmaz, B, 2010
)
0.63

Dosage Studied

ExcerptRelevanceReference
" Only a few drugs, when dosed therapeutically, achieved synovial fluid concentrations sufficient to inhibit the activities of both proteinases."( The inhibitory effects of antirheumatic drugs on the activity of human leukocyte elastase and cathepsin G.
Kalbhen, DA; Steinmeyer, J, 1996
)
0.51
"Angiotensin I-converting enzyme (ACE/kininase II) inhibitors potentiated guinea pig ileum's isotonic contractions to bradykinin (BK) and its analogues, shifting the BK dose-response curve to the left."( Potentiation of the effects of bradykinin on its receptor in the isolated guinea pig ileum.
Erdös, EG; Igić, R; Minshall, RD; Nedumgottil, SJ; Rabito, SF, 2000
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,120)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990167 (14.91)18.7374
1990's440 (39.29)18.2507
2000's262 (23.39)29.6817
2010's192 (17.14)24.3611
2020's59 (5.27)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 42.50

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index42.50 (24.57)
Research Supply Index7.05 (2.92)
Research Growth Index4.73 (4.65)
Search Engine Demand Index66.94 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (42.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (0.88%)5.53%
Reviews53 (4.65%)6.00%
Case Studies5 (0.44%)4.05%
Observational4 (0.35%)0.25%
Other1,068 (93.68%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]