• Diabetes mellitus in rats is characterized by excessive activity of several matrix metalloproteinases (MMPs), notably collagenase(s) and gelatinase(s), in skin, gingiva, and other tissues. (nih.gov)
  • TCs have potential utility in management of diabetic complications mediated by excessive activity of MMPs. (nih.gov)
  • Matrix metalloproteinases (MMPs) are a large family of mostly secreted, extracellularly acting proteolytic enzymes. (nature.com)
  • Matrix metalloproteinases (MMPs) are extracellularly acting enzymes that have long been known to have deleterious roles in brain injury and disease. (nature.com)
  • BACKGROUND: Changes in myocardial matrix metalloproteinases (MMPs) and the inhibitors of MMPs (TIMPs) have been demonstrated in congestive heart failure (CHF). (duke.edu)
  • Elastolytic enzymes such as matrix metalloproteinases (MMPs) may be directly responsible for elastin degradation in anetoderma. (medscape.com)
  • For example, matrix metalloproteinases (MMPs), such as MMP-2 and −9, have been shown to be typical NF-κB target proteins that are responsible for extracellular matrix breakdown and cell invasion ( 7 ). (spandidos-publications.com)
  • In the present study, we utilize a broad-spectrum MMP inhibitor, Marimastat, along with a previously described oropharyngeal aspiration model of MWCNT administration to investigate the role of MMPs in MWCNT-derived serum peptide generation and endothelial bioactivity. (cdc.gov)
  • Batimastat (BB-94) is a potent and synthetic inhibitor of a broad spectrum of matrix metalloproteinases (MMPs), including interstitial collagenase (IC50 = 3 nM), stromelysin (IC50 = 20 nM), Mr 72,000 type IV collagenase (IC50 = 4 nM), Mr 92,000 type IV collagenase (IC50 = 4 nM), and matrilysin (IC50 = 6 nM). (adooq.com)
  • GM 6001 is a potent, reversible broad spectrum inhibitor of zinc-containing proteases, including matrix metalloproteinases (MMPs). (adooq.com)
  • TAPI-2 is an inhibitor of TACE, ADAMs, ACE secretase, and other MMPs (metalloproteinases). (adooq.com)
  • UK 356618 is a selective and potent inhibitor of MMP-3 that shows selectivity over a range of MMPs. (adooq.com)
  • These groups include: serine proteinases, cysteine (thiol) proteinases, aspartic proteinases, and matrix metalloproteinases (MMPs). (stratech.co.uk)
  • The balance of metalloproteinases (MMPs) and their tissue inhibitors (TIMPs) is crucial for the manifestation and progression of periodontal diseases and is one of the promising areas of scientific research in terms of developing methods for selective inhibition of MMPs. (spr-journal.ru)
  • Remodeling of atrial extracellular matrix (ECM) in atrial fibrillation (AF) involves changes in the expression of matrix metalloproteinases (MMPs) and tissue inhibitors of MMPs (TIMPs). (unboundmedicine.com)
  • Together with the survey of several MMPs transcripts and the level of transforming growth factor-beta1 (TGF-beta1), we proposed that the increased activity of gelatinase (i.e. (unboundmedicine.com)
  • Matrix metalloproteases (MMPs) are a family of zinc-dependent endopeptidases that collectively have the capacity to degrade virtually every component of the extracellular matrix (ECM). (chemdiv.com)
  • Due to the important roles that MMPs play in cancer, a number of matrix metalloproteinase inhibitors (MMPIs) have been investigated. (chemdiv.com)
  • Small-molecules inhibitors such as CGS 27023A also target MMPs. (chemdiv.com)
  • This approach can be established using radiolabeled MMP inhibitors (MMPIs) as tracers for the detection of activated MMPs by means of PET. (amsterdamumc.org)
  • The pathology of ankylosing spondylitis (AS) suggests that certain cytokines and matrix metalloproteinases (MMPs) might provide useful markers of disease activity. (bath.ac.uk)
  • Serum levels of some cytokines and MMPs have been found to be elevated in active disease, but there is a general lack of information about biomarker profiles in AS and how these are related to disease activity and function. (bath.ac.uk)
  • The purpose of this study was to investigate whether clinical measures of disease activity and function in AS are associated with particular profiles of circulating cytokines and MMPs. (bath.ac.uk)
  • Measurement of 30 cytokines, five MMPs and four tissue inhibitors of metalloproteinases was carried out using Luminex® technology on a well-characterised population of AS patients (n = 157). (bath.ac.uk)
  • The aim of the study was to explore whether the serum level of interleukin 6 (IL-6) is correlated with matrix metalloproteinases (MMPs) and tissue inhibitors of metalloproteinases (TIMPs), and with clinical markers of the disease activity in rheumatoid arthritis (RA). (termedia.pl)
  • We conclude that analysis of the serum IL-6, MMPs and TIMPs levels may be useful in the assessment of the RA activity. (termedia.pl)
  • This gene encodes a member of the peptidase M10 family of matrix metalloproteinases (MMPs). (cancerindex.org)
  • Matrix metalloproteinases (MMPs) have been considered to be associated with tumor progression or poor prognosis. (cancerindex.org)
  • TIMP-2 (tissue inhibitor of metalloproteinases 2) is one of several TIMPs that form complexes with matrix metalloproteinases (MMPs) and inhibit their proteolytic activity. (rndsystems.com)
  • Aims Matrix metalloproteinases (MMPs) play a significant function in wound recovery: they are able to degrade all the different parts of the extracellular matrix. (researchensemble.com)
  • This process occurs as a result of the proteolytic enzymes resident in the extracellular matrix (ECM), mainly matrix metalloproteinases (MMPs) and elastase ( Figure 1 ). (dovepress.com)
  • Ours results suggest an effect of fluoride on the activity of MMPs 2 and 9 at the initial period of alveolar repair which could be associated to the process of blood clot remission and delay in bone repair. (bvsalud.org)
  • Further studies are needed to establish the relationship between the initial process of resorption of the blood clot, and the involvement of MMPs 2 and 9 and its regulators/tissue inhibitors. (bvsalud.org)
  • Some molecules are involved in several stages of the process of alveolar repair, for example matrix metalloproteinases (MMPs) 2 , among others. (bvsalud.org)
  • MMPs are an important family of metal-dependent endopeptidases and represent the major class of enzymes responsible for the degradation or resorption of all components of the extra-cellular matrix (ECM) 38 . (bvsalud.org)
  • Known elastolytic enzyme inhibitors include serine proteinase inhibitors (serpins) and tissue inhibitors of metalloproteinase (TIMPs). (medscape.com)
  • The HX repeats of some matrixins bind tissue inhibitor of metalloproteinases (TIMPs). (embl.de)
  • It is suggested that the hemopexin domain facilitates binding to a variety of molecules and proteins, for example the HX repeats of some matrixins bind tissue inhibitor of metallopeptidases (TIMPs). (embl.de)
  • Structural features of the reprolysin atrolysin C and tissue inhibitors of metalloproteinases (TIMPs) interaction. (ox.ac.uk)
  • The tissue inhibitors of metalloproteinases (TIMPs) are effective inhibitors of matrix metalloproteinases which share some structural similarity with the SVMPs. (ox.ac.uk)
  • The aim of this study was to evaluate the effect of different concentrations of triethylene glycol dimethacrylate (TEGDMA) on the inhibition of matrix metalloproteinase 2 (MMP-2). (springer.com)
  • Mouse gingival explants were cultured overnight in DMEM and the expression of secreted enzymes was analyzed by gelatin zymography in buffers containing 5 mM CaCl 2 (Tris-CaCl 2 ) in 50 mM Tris-HCl buffer with the addition of TEGDMA at different concentrations (0.62%, 1.25%, 2.5%, or 5.0% (v/v)). The gelatinolytic proteinase present in the conditioned media was characterized as matrix metalloproteinase by means of specific chemical inhibition. (springer.com)
  • CL-82198 is a selective inhibitor of human collagenase-3, also known as matrix metalloproteinase-13 (MMP-13), producing 89% inhibition at 10 mg/ml. (adooq.com)
  • TIMP-1 and TIMP-3 may play differential roles in the inhibition of gelatinase activity in vivo. (unboundmedicine.com)
  • Matrix metalloproteinase (MMP) inhibition has been proposed as a novel pharmacological approach for ICH treatment. (unav.edu)
  • pCellular activation of latent matrix metalloproteinase-2 (proMMP-2) requires formation of a cell membrane-associated activation complex that involves specific binding between the hemopexin domain of proMMP-2 (PEX) and the C-terminal domain of tissue inhibitor of matrix metalloproteinases-2 (C-TIMP-2). (amrita.edu)
  • The two clones showed an increased expression of MMP-2 protein and enhanced enzyme activity. (eurekamag.com)
  • In addition, nuclear factor (NF)‑κB and matrix metalloproteinase (MMP) expression was examined by western blotting, and MMP‑2/‑9 activities were determined by gelatin zymography. (spandidos-publications.com)
  • This study evaluated the in situ activity and expression of gelatinases (MMP-2 and MMP-9) and their relationship with TIMP-1 or TIMP-3 in atria undergoing rapid atrial pacing for the induction of AF (4 weeks' pacing followed by 2 weeks of maintained AF) in pigs. (unboundmedicine.com)
  • In contrast, EGFR ligand-induced CD44 expression was reduced by EGFR inhibitors, AG1478 and lapatinib, respectively. (iiarjournals.org)
  • Interestingly, we observed that EGFR ligand-induced CD44 and matrix metalloproteinase-9 (MMP-9) expression was reduced by silibinin treatment in a dose-dependent manner. (iiarjournals.org)
  • Expression of Matrix Metalloproteinases in Intraductal Papillary Mucinous Neoplasm of the Pancreas. (cancerindex.org)
  • A Disintegrin and Metalloproteases (ADAM), originally named metalloproteinases disintegrin cystein-rich (MDC), are membrane-anchored cell surface proteins containing both disintegrin and metalloproteinase domains. (frontiersin.org)
  • A critical step in this process is degradation of the basement membrane, which contains extracellular matrix (ECM) proteins and functions as a barrier to surrounding tissues. (aacrjournals.org)
  • Bacterial and fungal proteases are particularly important to the global carbon and nitrogen cycles in the recycling of proteins, and such activity tends to be regulated by nutritional signals in these organisms. (stratech.co.uk)
  • The net impact of nutritional regulation of protease activity among the thousands of species present in soil can be observed at the overall microbial community level as proteins are broken down in response to carbon, nitrogen, or sulfur limitation. (stratech.co.uk)
  • An Illustration of the Laminin-111 complex depicting the domain organization Laminins are high-molecular weight (~400 to ~900 kDa) proteins of the extracellular matrix. (pearltrees.com)
  • Proteins in this family are involved in the breakdown of extracellular matrix in normal physiological processes, such as embryonic development, reproduction, and tissue remodeling, as well as in disease processes, such as arthritis and metastasis. (cancerindex.org)
  • Atrolysin C is a P-I snake venom metalloproteinase (SVMP) from Crotalus atrox venom, which efficiently degrades capillary basement membranes, extracellular matrix, and cell surface proteins to produce hemorrhage. (ox.ac.uk)
  • Gusman H, Santana RB, Zehnder M (2002) Matrix metalloproteinase levels and gelatinolytic activity in clinically healthy and inflamed human dental pulps. (springer.com)
  • The processing mechanism and gelatinolytic activity of the membrane-type matrix metalloproteinase 1 (MT-MMP-1) were examined by expressing in COS-1 cells a deletion mutant of MT-MMP-1 lacking the transmembrane domain (ΔMT1) and its site-directed mutant with a furin-resistant sequence in the propeptide domain (mutant ΔMT1). (elsevierpure.com)
  • ΔMT1, but not mutant ΔMT1, was processed to an active form and exhibited gelatinolytic activity as seen using gelatin zymography. (elsevierpure.com)
  • A human breast carcinoma cell line (MDA-MB-231 cells) also secreted MT-MMP-1 into culture media, which was purified in a complex form with TIMP-2 and showed gelatinolytic activity as seen using zymography. (elsevierpure.com)
  • After incubation within a buffer to activate the enzyme, the gel can be stained with Coomassie Blue (Sigma, Saint Quentin Fallavier, France): protein with gelatinolytic activity are hence discovered as unstained rings. (researchensemble.com)
  • Bode W, Maskos K (2003) Structural basis of the matrix metalloproteinases and their physiological inhibitors, the tissue inhibitors of metalloproteinases. (springer.com)
  • Similarly, bioactive peptides, which are specific protein fragments that are thought to have physiological health benefits, are good candidates for cosmeceutical components that provide enzyme-modulating activity. (dovepress.com)
  • A profile consisting of high levels of MMP-8, MMP-9, hepatocyte growth factor and CXCL8 is associated with increased disease activity in AS. (bath.ac.uk)
  • This proteolytic activity is also required for further metastasis. (chemdiv.com)
  • In this work, we evaluated the inhibitory profile of TIMP-1, TIMP-2, and the N-terminal domain of TIMP-3 (N-TIMP-3) on the proteolytic activity of atrolysin C and analyzed the structural requirements and molecular basis of inhibitor-enzyme interaction using molecular modeling. (ox.ac.uk)
  • WAY 170523 has been reported to be a selective and potent inhibitor of MMP-13. (adooq.com)
  • While TIMP-1 and TIMP-2 had no inhibitory activity upon atrolysin C, the N-terminal domain of TIMP-3 (N-TIMP-3) was a potent inhibitor with a K(i) value of approximately 150nM. (ox.ac.uk)
  • In this study, we tested the feasibility of inhibiting activation of proMMP-2 by exogenous inhibitors, which block the binding between PEX and TIMP-2. (amrita.edu)
  • The recombinant C-TIMP-2 and synthetic peptides from C-TIMP-2 were used as inhibitors for proMMP-2 activation. (amrita.edu)
  • To investigate matrix metalloproteinase-2 (MMP-2) and tissue inhibitor of metalloproteinase-2 (TIMP-2) expressions in the cultured rat mesangial cells (MsC) transfected with Smad 7 vector and to elucidate the mechanism of Smad 7 in blocking tissue fibrosis. (eurekamag.com)
  • The inhibitory activities of glycosylated TIMP-1 and TIMP-3, but not TIMP-2, in AF tissues were markedly elevated and also localized in the atrial interstitium. (unboundmedicine.com)
  • TIMP-1 was found to be mostly colocalized with gelatinase activity over the AF tissues, implying the coexistence of gelatinase activity and TIMP-1, but TIMP-3 appeared only partially colocalized and discontinued the gelatinase activity surrounding the cardiomyocytes. (unboundmedicine.com)
  • ΔMT1 isolated in a complex form with tissue inhibitor of metalloproteinases 2 (TIMP-2) from the stable transfectants demonstrated the NH 2 -terminal sequence of Ala 113 -Ile-Gln-Gly-Leu, indicating cleavage at one amino acid down-stream from the furin recognition sequence. (elsevierpure.com)
  • ΔMT1 isolated in a complex form with tissue inhibitor of metalloproteinases 2 (TIMP-2) from the stable transfectants demonstrated the NH2-terminal sequence of Ala113-Ile-Gln-Gly-Leu, indicating cleavage at one amino acid down-stream from the furin recognition sequence. (elsevierpure.com)
  • Specific, high affinity binding of tissue inhibitor of metalloproteinases-4 (TIMP-4) to the COOH-terminal hemopexin-like domain of human gelatinase A. TIMP-4 binds progelatinase A and the COOH-terminal domain in a similar manner to TIMP-2. (embl.de)
  • The binding properties of the newly described tissue inhibitor of metalloproteinases-4 (TIMP-4) to progelatinase A and to the COOH-terminal hemopexin-like domain (C domain) of the enzyme were examined. (embl.de)
  • Amplite™ Universal Fluorimetric Protease Activity Assay Kit is an ideal choice to perform routine protease isolation assays or for identifying the presence of contaminating proteases in protein samples. (stratech.co.uk)
  • Blom A. M. , Kask L. and B. Dahlbäck (2001) Structural requirements for the complement regulatory activities of C4b-binding protein. (lu.se)
  • Kask L., Hillarp A., Ramesh B., Dahlbäck B., and Blom A. M. (2002) Structural requirements for the intra-cellular subunit polymerization of the complement inhibitor C4b-binding protein. (lu.se)
  • Sjöberg A., Trouw L., McGrath F., Hack E. C. and Blom A. M. (2006) Regulation of complement activation by C-reactive protein: targeting of the inhibitory activity of C4b-binding protein. (lu.se)
  • Second, changes in cytokine activity were related to changes in plasma MMP levels. (duke.edu)
  • TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors. (adooq.com)
  • Using an in vitro spectrophotometric technique, the Zn(++) reactivity of several CMTs was assessed and found to be positively related to the potency of these compounds as MMP inhibitors. (nih.gov)
  • MMI270B is a matrix metalloproteinase inhibitor (MMPI) with in vitro and in vivo activity. (eur.nl)
  • Several botanical extracts showing anti-aging properties of cosmeceutical interest possess anti-elastase and/or anti-collagenase activities in vitro. (dovepress.com)
  • 2002 and supplemented with EDTA-free proteinase inhibitor cocktail/1?μM pepstatin (Roche Diagnostics Mannheim Germany). (biosemiotics2013.org)
  • Pulmonary delivery of the broad-spectrum matrix metalloproteinase inhibitor marimastat diminishes multiwalled carbon nanotube -induced circulating bioactivity without reducing pulmonary inflammation. (cdc.gov)
  • Marimastat acted as a broad-spectrum matrix metalloproteinase inhibitor. (adooq.com)
  • T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes. (adooq.com)
  • MMP3 inhibitor 1 is a potent and highly selective MMP-3 inhibitor with an IC50 of 1 nM. (adooq.com)
  • ARP 100 is a selective inhibitor of matrix metalloproteinases 2 (MMP-2) with IC50 value of 12 nM. (adooq.com)
  • ARP 101, selective inhibitor of MMP-2 that displays ~ 600-fold selectivity over MMP-1 (IC50 values are 0.81 and 486 nM respectively). (adooq.com)
  • Compound 4 is also worth of note for its high potency as hBChE inhibitor (IC50 = 7 nM) and for the three order of magnitude selectivity versus hAChE. (ibecbarcelona.eu)
  • Early inhibitors targeting MMP activity were designed to bind within the catalytic domain of these proteases. (chemdiv.com)
  • In vivo, using rats made diabetic with streptozotocin (STZ), oral administration of various TCs led to decreased weight loss and substantial reductions in the activity of both skin collagenase and skin gelatinase (primarily MMP-9, 92 kDa) without affecting blood glucose. (nih.gov)
  • SB-3CT is an effective and selective gelatinase inhibitor with Ki of 13.9 nM and 600 nM for MMP-2 and MMP-9. (adooq.com)
  • In AF atria, in situ gelatinase activity was mainly localized in the interstitium of atrial myocardium, and was significantly larger than that of sinus rhythm control (i.e., sham control). (unboundmedicine.com)
  • The significant increase of MMP-9 in its pro-form and mRNA level, but not MMP-2, was shown to be responsible for the increased gelatinase activity in atria with AF. (unboundmedicine.com)
  • LTP-associated MMP proteolysis is probably then terminated by an increase in the activity of endogenous inhibitors called tissue inhibitors of metalloproteinases. (nature.com)
  • The serum compositional changes after MWCNT exposure have been identified as a surge of fragmented endogenous peptides, likely derived from matrix metalloproteinase (MMP) activity. (cdc.gov)
  • Doxycycline Hydrochloride is a synthetic tetracycline derivative with similar antimicrobial activity. (adooq.com)
  • TY - JOUR T1 - Upregulation of matrix metalloproteinase-9 and tissue inhibitors of metalloproteinases in rapid atrial pacing-induced atrial fibrillation. (unboundmedicine.com)
  • In general, 10 mg/ml eucalyptol was more effective than 1 mg/ml and, at both doses, we observed an upregulation of SOD activity when compared to the CS group (p (greenmedinfo.com)
  • Clinical and serum variables, colonic inflammation (histologic grading), and measurement of myeloperoxidase (MPO) activity, malondialdehyde (MDA) and prostaglandin E 2 (PGE 2 ) concentrations, ingesta volatile fatty acid (VFA) content, and arterial blood flow in the RDC were evaluated for a 21-day period in horses administered phenylbutazone (8.8 mg/kg, PO, q 24 h) or a control substance. (avma.org)
  • Our aim was to determine whether serum concentrations of TGFβ1 are a good biomarker of disease activity in children with LS. (biomedcentral.com)
  • Serum TGFβ1 concentration levels were measured by enzyme linked immunosorbent assay (ELISA), analyzed and correlated with disease subtypes and disease activity. (biomedcentral.com)
  • Serum concentration of TGFβ1 were elevated in patients with all subtypes of LS irrespective of clinical disease activity. (biomedcentral.com)
  • Our study objectives were to determine the peripheral blood levels of TGFβ1 in children with LS and to determine the relationship of serum levels to disease activity. (biomedcentral.com)
  • Objective -To establish an in vivo method for matrix metalloproteinase (MMP)-2 and MMP-9 induction in horses via IV administration of lipopolysaccharide (LPS) and to evaluate the ability of doxycycline, oxytetracycline, flunixin meglumine, and pentoxifylline to inhibit equine MMP-2 and MMP-9 production. (avma.org)
  • The noninvasive imaging of MMP activity in vivo could have a high impact in basic research as well as in clinical applications. (amsterdamumc.org)
  • Alternatively, they may act indirectly by modulating other inflammatory events, such as proteolytic activation of latent cytokines, which, in turn, may regulate the activity of other undiscovered elastolytic enzymes. (medscape.com)
  • PEX blocks MMP-2 activity on the chick chorioallantoic membrane where it disrupts angiogenesis and tumor growth. (embl.de)
  • The relationship between biomarker levels and measures of disease activity (Bath ankylosing spondylitis disease activity index (BASDAI)), function (Bath ankylosing spondylitis functional index) and global health (Bath ankylosing spondylitis global health) was investigated. (bath.ac.uk)
  • A number of tetracyclines (TCs), both antimicrobial compounds as well as chemically modified non-antimicrobial TC analogues (CMTs) are known to possess potent inhibitory activity against these enzymes. (nih.gov)
  • Chelators targeting matrix metalloproteinases library contains 9,300 compounds. (chemdiv.com)
  • All compounds exhibited a good activity, and eight of them (5-8, 10, 14, 15 and 20) shared comparable low micromolar inhibitory potency versus Aβ40 aggregation and human acetylcholinesterase (AChE), while inhibiting human butyrylcholinesterase (BChE) even at submicromolar concentration. (ibecbarcelona.eu)
  • Although TGFβ1 may play an important role in the pathogenesis of local skin fibrosis, circulating blood levels of molecules known to act locally may not be useful biomarkers of disease activity. (biomedcentral.com)
  • The catalytic domain, which is responsible for enzyme activity, contains the highly conserved Zn 2+ binding region. (chemdiv.com)
  • Batimastat is an anticancer drug that belongs to the family of drugs called angiogenesis inhibitors. (adooq.com)
  • Disruption of angiogenesis by PEX, a noncatalytic metalloproteinase fragment with integrin binding activity. (embl.de)
  • Finally, fibrinolytic effects of MMP-10 and rivaroxaban were evaluated by thromboelastometry and thrombin-activatable fibrinolysis inhibitor (TAFI) activation assays. (unav.edu)
  • The enzyme is involved in wound healing, and studies in mice suggest that it regulates the activity of defensins in intestinal mucosa. (cancerindex.org)
  • The prototype of ADAM with sheddase activity is exemplified in ADAM17. (frontiersin.org)
  • BH3 mimetics with high affinity for BCL-XL (BCL-XLi) reduce metabolic activity and induce mitochondrial apoptosis in senescent PA cells at nano-molar concentrations. (ibecbarcelona.eu)
  • Blom A. M. , Mörgelin M., Öyen M., Jarvet J. and Fries E. (1999) Structural characterization of inter-a-inhibitor - evidence for an extended shape. (lu.se)
  • In the current study, the anti‑invasive activities and associated signaling pathways of celastrol were determined in ovarian cancer cells. (spandidos-publications.com)
  • Epithelial-mesenchymal transition (EMT) is a key cellular process in which immotile epithelial cells transform into mesenchymal cells through cell polarity loss, cell-cell junction disassembly, and extracellular matrix (ECM) alteration. (bmbreports.org)
  • Moreover, at 0.1-10 μM it also exhibited neuroprotective activity against tau toxicity induced by okadoic acid in human neuroblastoma SH-SY5Y cells, that was comparable to that of estradiol and PD38. (ibecbarcelona.eu)
  • Pertoft H. and Fries E. (1995) Inter-a-inhibitor is required for the formation of the hyaluronan-containing coat on fibroblasts and mesothelial cells. (lu.se)
  • To this end, selective and potent MMP-13 inhibitors based on a N,N′-bis(benzyl)pyrimidine-4,6-dicarboxamide core have been synthesized and successfully radiolabeled with carbon-11, fluorine-18, and gallium-68. (amsterdamumc.org)
  • CTS-1027 is a potent MMP inhibitor that protects Against TNFα- and α-Fas-Induced liver Injury. (adooq.com)
  • Pitolisant hydrochloride Type I collagenolytic activity assay Enzymes were incubated with 0.25?μg/ml type I collagen from bovine skin (Millipore) with or without inhibitors/APMA as indicated in a total volume of Pitolisant hydrochloride 40?μl with 25?μM ZnCl2 and 1?mM CaCl2 in the presence of the proteinase inhibitor cocktail and pepstatin at 24? (biosemiotics2013.org)
  • A fragment of MMP-2, which comprises the C-terminal hemopexin-like domain, termed PEX, prevents this enzyme binding to alphavbeta3 and blocks cell surface collagenolytic activity. (embl.de)
  • The activity can be a destructive change, abolishing a protein's function or digesting it to its principal components. (stratech.co.uk)
  • Sjöberg A., Önnerfjord, P., Mörgelin, M., Heinegård, D. and Blom A. M. (2005) Extracellular matrix and inflammation: fibromodulin activates the classical pathway of complement by directly binding C1q. (lu.se)
  • It inhibited lung cancer cell invasion and down-regulated matrix metalloproteinase-7 (MMP-7), which promoted lung cancer cell invasion. (aacrjournals.org)
  • LDH activity This assay (Roche Diagnostics) was performed in 96-well plates (Nunc). (biosemiotics2013.org)
  • These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. (guidetopharmacology.org)
  • Reversal of this process involves targeting oxidation and the aforementioned proteolytic enzymes, now recognized as valuable pharmacological targets for active ingredients in cosmeceuticals and other dermatological products to modulate their action, either directly (inhibitors) or indirectly (down-regulators). (dovepress.com)
  • Plasma was harvested and analyzed for MMP-2 and MMP-9 activities via zymography. (avma.org)