Cleavage of the SARS-CoV-2 S2 spike protein required for viral entry into cells can be accomplished by proteases TMPRSS2 located on the cell membrane, or by cathepsins (primarily cathepsin L) in endolysosomes. (wikipedia.org)
Cathepsins are a class of globular lysosomal proteases playing a vital role in mammalian cellular turnover. (mobitec.com)
In dermal fibroblasts, chronic exposure to non-cytotoxic doses of UVA caused pronounced inactivation of the lysosomal cysteine-proteases cathepsin B and L, effects not observed in primary keratinocytes and occurring only to a minor extent in primary melanocytes. (nih.gov)
For invasion, untreated microglia primarily used cysteine proteases, but IL4-treated cells used a wider range of enzymes (cysteine proteases, cathepsin S and K, heparanase, and matrix metalloproteases). (biomedcentral.com)
Cathepsins K and V are members of the cysteine family of proteases and represent two of the most potent elastases yet identified in humans. (gatech.edu)
Protease8
The protein is a cysteine cathepsin, a lysosomal cysteine protease that plays a major role in intracellular protein catabolism. (wikipedia.org)
Although Cathepsin L is usually characterized as a lysosomal protease, it can be secreted, resulting in pathological inflammation. (wikipedia.org)
Although the mechanism of this therapy is not known with certainty, low pH was shown to increase the release of active cathepsin B, an important matrix remodeling protease. (aacrjournals.org)
Neuronal lysosomal impairment caused by Calpain over activation leads to the release of the lysosomal protease Cathepsin S that in sCJD mainly localises in axons, although massive Cathepsin S overexpression is detected in microglial cells. (nih.gov)
Cathepsin K is the lysosomal cysteine protease involved in bone remodeling and resorption. (mobitec.com)
Recently, we have identified the thiol-dependent cysteine-protease cathepsin B as a novel UVA-target undergoing photo-oxidative inactivation upstream of autophagic-lysosomal dysfunction in fibroblasts. (nih.gov)
A ubiquitously-expressed cysteine protease that plays an enzymatic role in POST-TRANSLATIONAL PROTEIN PROCESSING of proteins within SECRETORY GRANULES . (bvsalud.org)
Proteinases2
The major, if not exclusive, intestinal proteinases of this aphid are of the cysteine type. (nih.gov)
The AgCatL protein shows high sequence similarity with mammalian and some arthropod cathepsin L-like proteinases, but can be reliably distinguished from the secreted (digestive) proteinases identified in other arthropods. (nih.gov)
Proteolytic2
However, at higher concentrations of the enzyme, testicans switch from being cathepsin L inhibitors to cathepsin RO5126766 (CH5126766) L substrates (104) and nidogen-1 is prone to proteolytic degradation by cathepsin S (105). (cancerhappens.com)
Sickle cell disease promotes sex-dependent pathological bone loss through enhanced cathepsin proteolytic activity in mice. (nih.gov)
Protein3
Cathepsin L1 is a protein that in humans is encoded by the CTSL1 gene. (wikipedia.org)
Cathepsin L1 is a member of the Peptidase C1 (cathepsin) MEROPS family, which plays an important role in diverse processes including normal lysosome mediated protein turnover, antigen and proprotein processing, and apoptosis. (wikipedia.org)
The protein encoded by this gene is a lysosomal cysteine proteinase that plays a major role in intracellular protein catabolism. (nih.gov)
20211
Drugs 2021, 19,4 ofcysteine residues within the WAP domain and 12 cysteine residues in the C-terminal area. (cathepsin-s.com)
Proteinase1
A cDNA has been cloned from a gut library and codes for the cysteine proteinase AgCatL, a cathepsin L-like cysteine proteinase. (nih.gov)
Degradation1
The beams were incubated up to 6 months and incubation media were used to analyze solubilized telopeptide (ICTP and CTX) fragments as indicators of MMP- and cathepsin K-mediated degradation after 1, 3 and 6 months of incubation. (elsevierpure.com)
Dentin1
It has been hypothesized that cysteinecathepsins (CTs) along with matrix metalloproteases (MMPs) may work in conjunction in the proteolysis of mature dentin matrix. (elsevierpure.com)
Endothelial cells3
Cathepsins K and V are powerful elastases elevated in endothelial cells by tumor necrosis factor-α (TNFα) stimulation and disturbed blood flow both of which contribute to inflammation-mediated arterial remodeling. (degruyter.com)
In conclusion, NF-κB and AP-1 activation were necessary to activate cathepsin K expression in endothelial cells, highlighting integration of biochemical and biomechanical stimuli to control cathepsins K and V, powerful elastases implicated for arterial remodeling due to chronic inflammation and disturbed blood flow. (degruyter.com)
Due to the compelling histological similarities between vasculopathy in sickle cell disease and atherosclerosis, we tested the hypothesis that the unique inflammatory milieu, in conjunction with the biomechanical vascular environment of sickle cell disease upregulates cathepsin K and V activity in large artery endothelial cells, ultimately leading to arterial remodeling and stroke. (gatech.edu)
Inhibitor3
Truncated monomeric cystatin F is a potent inhibitor of cathepsins C and H (84), the latter known as major progranzyme convertases that direct the cytotoxicity of NK cells and cytotoxic T lymphocytes (CTL) (85). (cancerhappens.com)
Cathepsin X is not inhibited by cystatin F, however, since cathepsin L RO5126766 (CH5126766) is needed to activate procathepsin X, it is tempting to speculate that cystatin F, as a cathepsin L inhibitor, indirectly controls cathepsin X dependent adhesion, and the maturation of dendritic cells (86). (cancerhappens.com)
Microfluidic Platform for Microparticle Fabrication and Release of a Cathepsin Inhibitor. (nih.gov)
Pathological1
Cathepsin L and other cysteinecathepsins tend to be secreted by macrophages and other tissue-invading immune cells when causing pathological inflammation. (wikipedia.org)
indicate the 12 conserved cysteine residues located inside the Crustins, which includes the WAP line. (cathepsin-s.com)
Triangles indicate the 12 conserved cysteine residues found inside the Crustins, which includes the WAP domain.The deduced amino acid sequences of Al-crus three and Al-crus 7 were compared together with the deduced amino acid sequences of Al-crus and Al-crus sequence was Crustin these of other close Crustins (Figure 1). (cathepsin-s.com)
Amongst the 12 conserved cysteine residues, there have been three amino acids in between the very first two cysteine residues (Cys1 ys2 ), a sequence of 16 or 17 amino acids amongst Cys4 ys5 , plus a sequence of 82 residues between Cys6 ys7 (Figure 1). (cathepsin-s.com)
It is synthesized as an inactive disulfide-linked dimer that has to lose RO5126766 (CH5126766) 15 amino acid residues at the N-terminus (presumably cleaved by cathepsin V) to be converted to the active monomer. (cancerhappens.com)
Macrophages2
Especially tumor-associated myeloid cells, such as tumor-associated macrophages and myeloid-derived suppressor cells, which are known for their tumor promoting and immunosuppressive functions, constitute the major source of excessive cysteine cathepsin activity in cancer. (cancerhappens.com)
Redundant cathepsins are involved in generating peptides for MHC II presentation (25).by infected macrophages (34).Cathepsin B regulates IL-12 secretion from DC and from macrophages in infected mice (35).Cathepsin L negatively regulates B lymphocyte production in bone marrow and restricts numbers of peripheral B lymphocytes (65).is an exception in that it is the only cystatin that targets cathepsins inside endosomes and lysosomes (83). (cancerhappens.com)
Enzymatic1
In order to determine if UVA-induced lysosomal impairment requires single or dual inactivation of cathepsin B and/or L, we used a genetic approach (siRNA) to selectively downregulate enzymatic activity of these target cathepsins. (nih.gov)
Biomechanical2
However, mechanisms behind endothelial cell integration of biochemical and biomechanical cues to regulate cathepsin production are not known. (degruyter.com)
JNK/c-jun were still phosphorylated, but cathepsin K mRNA levels were significantly reduced to almost null indicating separate biomechanical regulation of cathepsin K by shear stress separate from biochemical stimulation. (degruyter.com)
Arterial1
Comparative analysis of arterial compliance in mice genetically null for cathepsins K, L, or S. (nih.gov)
Therapeutic3
Since they are enriched in the tumor microenvironment, cysteinecathepsins represent exciting targets for development of new diagnostic and therapeutic moieties. (cancerhappens.com)
The Role of Cathepsins in Tumor Diagnosis and as Targets for Therapeutic Intervention Numerous studies established a prominent link between cysteinecathepsins and tumor progression. (cancerhappens.com)
Alterations in Ca 2+ homeostasis and activation of Calpain-Cathepsin axis already occur at pre-clinical stages of the disease as detected in a humanized sCJD mouse model.Altogether our work indicates that unbalanced Calpain-Cathepsin activation is a relevant contributor to the pathogenesis of sCJD at multiple molecular levels and a potential target for therapeutic intervention. (nih.gov)
Enzyme1
The SensoLyte® Rh110 Cathepsin K Assay Kit provides a convenient assay for high throughput screening of enzyme inhibitors or for continuous assay of enzyme activity utilizing a fluorogenic peptide. (mobitec.com)
Gene1
Upregulation of cathepsin L gene under mild cold conditions in young Japanese male adults. (nih.gov)
Cloning1
Cloning, genomic organization, and chromosomal localization of human cathepsin L". J Biol Chem. (wikipedia.org)
Cells1
The other, and most intensively studied, type II cystatin, (testican and its homologs ?2 ad ?3) with yet unknown functions, possessing inhibitory activity toward cathepsin L. (1 and 2), produced by mesenchymal cells, are necessary constituents of basement membranes since they link laminins and type IV collagens non-covalently (102), and have been shown to inhibit cathepsin K (103). (cancerhappens.com)
Human2
The proform was activated by Recombinant Human Cathepsin L (Catalog # 952-CY ) and further purified. (rndsystems.com)
UVA causes dual inactivation of cathepsin B and L underlying lysosomal dysfunction in human dermal fibroblasts. (nih.gov)
Role1
Furthermore, the role of Cathepsins has been well established in other cardiovascular remodeling diseases, such as atherosclerosis. (gatech.edu)
Range1
In this study, we examined UVA effects on a wider range of cathepsins and explored the occurrence of UVA-induced cathepsin inactivation in other cultured skin cell types. (nih.gov)
Activation1
TNFα upregulated cathepsin K via JNK/c-jun activation, but vasoprotective shear stress inhibited TNFα-stimulated cathepsin K expression. (degruyter.com)
Term1
Tests other irreversible wide spectrum inhibitors increased RO5126766 (CH5126766) concerns regarding feasible unwanted effects of long-term systemic ablation of cysteinecathepsins stimulating design of particular and reversible inhibitors (109). (cancerhappens.com)
Shown1
CTSL1 has been shown to interact with Cystatin A. Cathepsin L has been reported in many organisms including fish, birds, mammals, and sponges. (wikipedia.org)
Development1
Accordingly, cathepsins received considerable attention as healing targets, leading to development of many little molecular inhibitors. (cancerhappens.com)