• Matrix metalloproteinases ( MMPs ) and tissue inhibitor of metalloproteinases (TIMPs) play a vital role in the pathogenesis of multiple myeloma (MM), especially for tumor invasion and osteolytic osteopathy. (bvsalud.org)
  • By breaking down extracellular matrix (ECM) components and releasing the proteins composing the ECM and growth factors , as well as their receptors, MMPs affect tissue integrity and promote cancer cell invasion and metastasis . (bvsalud.org)
  • 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)
  • however, in the corneal stroma, excessive infiltration of monocytes/macrophages is considered to be unfavorable because they secrete matrix metalloproteinases (MMPs) and other proteins undesirable for tissue healing. (medscape.com)
  • Matrix metalloproteinases (MMPs) are a group of structurally related endopeptidases that require a metal cofactor. (medscape.com)
  • 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)
  • One particular CMT (CMT-5, pyrazole analogue), which is neither antimicrobial nor capable of binding metal cations, did not inhibit the MMPs. (nih.gov)
  • The major pathologic manifestations of rheumatoid arthritis (RA) and osteoarthritis (OA) are joint inflammation and articular cartilage resorption by proinflammatory cytokine-stimulated matrix metalloproteinases (MMPs) and aggrecanases. (aspetjournals.org)
  • Therefore, besides its anti-inflammatory activity, this agent may also be effective in blocking cartilage matrix resorption by MMPs by impairing AP-1 and NF-κB binding activities. (aspetjournals.org)
  • Thus, TWHF extract contains novel inhibitors of MMP expression that may be of therapeutic potential in arthritis and other conditions associated with increased MMPs. (aspetjournals.org)
  • A large number of cytokines, extracellular matrix (ECM), and matrix metalloproteinases (MMPs) are synthesized and secreted by synthetic VSMCs during the progression of AS [ 7 , 8 ]. (hindawi.com)
  • Several studies have shown that miRNAs play multiple roles in the phenotypic transformation, migration, and proliferation of VSMCs by inhibiting ERK1/2 activation [ 11 , 12 ], partly by regulating the tissue inhibitor of metalloproteinases (TIMPs)-MMPs and p21-cyclins interactions [ 13 - 18 ]. (hindawi.com)
  • 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)
  • The underlying mechanisms of matrix destruction in TB remain poorly understood but consideration of the lung extracellular matrix predicts that matrix metalloproteinases (MMPs) will play a central role, owing to their unique ability to degrade fibrillar collagens and other matrix components. (ersjournals.com)
  • Since we proposed the concept of a matrix degrading phenotype in TB a decade ago, diverse data implicating MMPs as key mediators in TB pathology have accumulated. (ersjournals.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)
  • CMTs may inhibit MMPs by binding to the key metal ions or by regulating MMP transcription. (chemdiv.com)
  • 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)
  • Matrix metalloproteinases (MMPs) play an important role in cancer progression by degrading extracellular matrix components, promoting tumor cell migration, and thus enhancing tumor metastasis. (suny.edu)
  • Several generations of anticancer drug were designed to inhibit the proteolytic functions of MMPs, but these drugs failed in clinic trails due to lack of selectivity. (suny.edu)
  • The most notorious endogenous metalloproteinases are tissue inhibitors of metalloproteinases (TIMPs). (wikipedia.org)
  • miR-128-5p targets the tissue inhibitor of metalloproteinases (TIMPs), silent information regulator 2 (SIRT2), peroxisome proliferator-activated receptor (PPAR), and p21 genes, which are linked to the behaviours of VSMCs. (hindawi.com)
  • In vivo, tissue inhibitors of metalloproteinases (TIMPs) inhibit collagenase activity. (medscape.com)
  • VSMCs were transfected with the miR-128-5p mimic and inhibitor, and the migration, phenotypic modulation, and proliferation of VSMCs were investigated. (hindawi.com)
  • AA and the extracellular regulated protein kinase 1/2 (ERK1/2) blocker U0126 markedly inhibited migration, elevated smooth muscle 22 α (SM22 α ) expression, repressed VSMC proliferation, elevated miR-466f-3p and miR-425-3p expression, and suppressed miR-27a-5p and miR-128-5p expression in ox-LDL-induced VSMCs. (hindawi.com)
  • The inhibitor increased p21, p27, and SM22ɑ expression and repressed the migration, phenotypic transformation, and proliferation of VSMCs. (hindawi.com)
  • Our research showed that the migration, phenotypic transformation, and proliferation of ox-LDL-induced VSMCs were repressed by AA through inhibiting miR-128-5p by targeting the p21 gene, which may provide an effective option for the treatment of atherosclerosis. (hindawi.com)
  • In conclusion, the present study indicated that propofol inhibited the proliferation and invasion, but enhanced the apoptosis of GC cells by regulating the circ‑PVT1/miR‑195‑5p/ETS1 axis. (spandidos-publications.com)
  • In GC, Yang et al ( 7 ) reported that propofol suppressed the proliferation of SGC-7901 and MGC-803 cells by promoting inhibitor of growth 3 ( 7 ). (spandidos-publications.com)
  • Peng and Zhang ( 8 ) indicated that propofol inhibited proliferation, but induced apoptosis of SGC-7901 cells by regulating matrix metalloproteinase (MMP)2 ( 8 ). (spandidos-publications.com)
  • Substances that inhibit or prevent the proliferation of NEOPLASMS. (lookformedical.com)
  • We demonstrate that UCN-01, at concentrations lower than those necessary to inhibit cancer cell growth, inhibit proliferation of human endothelial cells in vitro. (karger.com)
  • Among cancer of LDL and inhibit SMC and EC proliferation, poten- patients, there was a delayed cancer onset for those who tially reducing the risk of arteriosclerosis. (gotomydoctor.com)
  • Retinoids inhibit the proliferation of several types of tumour cells, and are used for patients with several malignant tumours. (johnshopkins.edu)
  • Combined with in-vitro proliferation assays using CRISPR-Cas9/RNAi and patient survival analysis, MEK inhibitors PD19830 and BRD-K12244279, pilocarpine, and tremorine were discovered as potential new drug options for treating breast cancer. (cdc.gov)
  • 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)
  • In vitro , a concentration-dependent anti-invasive action of either FAAH inhibitor was demonstrated, accompanied with upregulation of tissue inhibitor of matrix metalloproteinases-1 (TIMP-1). (oncotarget.com)
  • In this study, we used the OrganoPlate to develop a humanized 3D in vitro inflammation-on-a-chip model to recapitulate neutrophil transmigration across the endothelium and subsequent migration through the extracellular matrix (ECM). (nature.com)
  • During an inflammatory response, neutrophils move from the blood to the site of inflammation by transmigrating across the endothelial barrier and through the basement membrane (BM) of the surrounding extracellular matrix (ECM). (nature.com)
  • KYQG exhibited the therapeutic effects on oral ulcers probably by inhibiting inflammation, regulating immunological response, and suppressing oxidative stress through a complex multi-pathways network. (biomedcentral.com)
  • The mechanisms leading to IF/TA in the transplanted kidney include inflammation, activation of renal fibroblasts, and deposition of extracellular matrix proteins. (biomedcentral.com)
  • In addition to reducing inflammation, EPA & DHA also inhibit platelet aggregation (lowering the risk of blood clots). (phoenixhelix.com)
  • 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)
  • Compounds that inhibit the function or proteolytic action of the PROTEASOME. (lookformedical.com)
  • A possible mechanism of action for TFPI-2 protein the TFPI-2 gene manifestation product is definitely inhibition of the actions of several proteolytic enzymes along with a subsequent reduced amount of their harming effects over the extracellular matrix. (cell-signaling-pathways.com)
  • Proteolytic enzymes secreted by tumor cells get excited about the degradation from the extracellular matrix that is the key stage of tumor invasion or metastasis. (cell-signaling-pathways.com)
  • There are also cartilage-derived angiogenesis inhibitors. (wikipedia.org)
  • Batimastat is an anticancer drug that belongs to the family of drugs called angiogenesis inhibitors. (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)
  • Chelators targeting matrix metalloproteinases library contains 9,300 compounds. (chemdiv.com)
  • Methods: Beas-2B human bronchial epithelial cells were treated with HDE in the absence or presence of signaling pathway inhibitors, and EGFR and ERK1/2 phosphorylation were then assessed by immunoblotting. (cdc.gov)
  • Losartan has protective effect on aortic wall of rats with aortic dissection, and the mechanism may be through inhibiting transforming growth factor-beta 1 pathway, which activates downstream phosphoinositide 3-kinase/protein kinase B pathway related proteins, and then inhibits the expansion and progression of aortic dissection. (ijpsonline.com)
  • Existing studies have shown that there is crossover between Renin-Angiotensin-Aldosterone (RAAS) signaling pathway and TGF-β pathway, but little is known about whether ARB drug losartan can block Angiotensin-II (Ang-II) signaling pathway, inhibit the activation of Transforming Growth Factor- Beta (TGF-β) pathway, and regulate vascular remodeling. (ijpsonline.com)
  • LIPUS promotes the extracellular matrix synthesis of degenerative human nucleus pulposus cells through activation of FAK/PI3K/Akt pathway. (qigonginstitute.org)
  • Across three different murine models of human prostate and breast cancer, KBU2046 inhibits metastasis, decreases bone destruction, and prolongs survival at nanomolar blood concentrations after oral administration. (nature.com)
  • This study addressed the impact of two FAAH inhibitors (arachidonoyl serotonin [AA-5HT], URB597) on A549 lung cancer cell metastasis and invasion. (oncotarget.com)
  • TFPI-2 is able to inhibit the growth invasion and metastasis of glioma (8) lung malignancy (9) prostate malignancy (10) laryngeal malignancy (11) and pancreatic malignancy (12). (cell-signaling-pathways.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)
  • 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)
  • 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)
  • 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)
  • WAY 170523 has been reported to be a selective and potent inhibitor of MMP-13. (adooq.com)
  • The present invention provides methods and compositions of prophylaxis for, or for treating, chronic obstructive pulmonary disease (COPD), cancer, arthritis, skin damage, or atherosclerotic plaque rupture in a subject in need thereof, which comprise i) a statin or ii) selective serotonin reuptake inhibitor (SSRI). (justia.com)
  • Additionally, these drugs, both non-selective inhibitors and selective cyclooxygenase-2 inhibitors, are frequently associated with side effects, impairing patients' compliance to their use 6 . (bvsalud.org)
  • 1] R. Roy, J. Yang, and M. A. Moses, "Matrix metalloproteinases as novel biomarkers and potential therapeutic targets in human cancer," J. Clin. (chemdiv.com)
  • 2] J. Cathcart, A. Pulkoski-Gross, and J. Cao, "Targeting matrix metalloproteinases in cancer: Bringing new life to old ideas," Genes and Diseases, vol. 2, no. 1. (chemdiv.com)
  • Evidence suggests that cannabis has the potential of inhibiting the growth of and even killing cancer cells and can help patients manage symptoms associated with cancer treatments. (qualifyingconditions.com)
  • THC and CBD have been shown to inhibit the progression of cancers located in the breast, lung, prostate, and colon in animal models, suggesting that the cannabinoids may also be effective at mediating cancer cell death in human subjects35,53,63,74. (qualifyingconditions.com)
  • In 2016, the same team of researchers found CBDA to effectively inhibit the migration of breast cancer cells and was able to identify the effect to be associated with the cannabinoid's downregulation of the proto-oncogene c-fos and the enzyme cyclooxygenase-294. (qualifyingconditions.com)
  • UCN-01, a protein kinase C (PKC) inhibitor, induces growth arrest and apoptosis in cancer cells and was recently introduced in a phase I clinical trial. (karger.com)
  • Based on this gene expression signature, the VEGFR inhibitor ZM-306416 was discovered as a new drug for treating breast cancer. (cdc.gov)
  • It was identified that propofol inhibited the viability and invasion, but promoted apoptosis of HGC‑27 and AGS cells in a dose‑dependent manner. (spandidos-publications.com)
  • This study was designed to determine the effects of the long non-coding RNA (lncRNA) plasmacytoma variant translocation 1 ( PVT1 ) on vascular smooth muscle cell (VSMC) apoptosis and extracellular matrix (ECM) disruption in a murine abdominal aortic aneurysm (AAA) model. (molcells.org)
  • Of note, the effects of Ang II in facilitating cell apoptosis, increasing matrix metalloproteinase (MMP)-2 and MMP-9, reducing tissue inhibitor of MMP (TIMP)-1, and promoting switching from the contractile to synthetic phenotype in cultured VSMCs were enhanced by overexpression of PVT1 but attenuated by knockdown of PVT1 . (molcells.org)
  • A prior research indicated that TFPI-2 gene appearance inhibits the development of choriocarcinoma by inducing choriocarcinoma cell apoptosis (13). (cell-signaling-pathways.com)
  • Surprisingly, low-dose RAs enhanced the activity of tissue-type plasminogen activator (tPA), and activated pro-matrix metalloproteinases (proMMP2 and proMMP9). (johnshopkins.edu)
  • In vitro photophysical and biological studies show high intrinsic ability to inhibit the activity of urokinase plasminogen activator (uPA) and matrix metalloproteinase-9 (MMP-9). (ua.pt)
  • P-selectin, soluble endothelial protein C receptor, soluble thrombomodulin, plasminogen activator inhibitor 1, ADAMTS-13, von Willebrand factor, tissue factor, soluble intercellular adhesion molecule 1, and vascular cell adhesion molecule 1 were more elevated in LF patients than in controls. (cdc.gov)
  • Endothelial protein C receptor, thrombomodulin, intercellular adhesion molecule 1, plasminogen activator inhibitor 1, D-dimer, and hepatocyte growth factor were higher in fatal than nonfatal LF cases. (cdc.gov)
  • Early inhibitors targeting MMP activity were designed to bind within the catalytic domain of these proteases. (chemdiv.com)
  • Inhibition of neutrophil proteases inhibited neutrophil transmigration on geltrex mix, but not collagen I. These findings highlight the important role of the ECM in determining cell phenotype and response to inhibitors. (nature.com)
  • Epithelial cells adjacent to the area of the defect flatten, lose their hemidesmosome attachments, and migrate on transient focal contact zones that are formed between cytoplasmic actin filaments and extracellular matrix proteins. (medscape.com)
  • 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)
  • KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all the hallmarks of classical chaperone inhibitors, including toxicity. (nature.com)
  • chromatographic separation of collagenase from collagenase inhibitor and subsequent activation of the collagenase with trypsin yielded the active species in stimulated but not in unstimulated cells. (wustl.edu)
  • Interferon‐γ (IFN‐γ), a known resorption inhibitor, blocked the increment in collagenase production caused by all agents tested. (wustl.edu)
  • University of Wisconsin solution inhibits the class II collagenase within crude Clostridium histolyticum collagenase. (ox.ac.uk)
  • In athymic nude mice FAAH inhibitors were shown to elicit a dose-dependent antimetastatic action yielding a 67% and 62% inhibition of metastatic lung nodules following repeated administration of 15 mg/kg AA-5HT and 5 mg/kg URB597, respectively. (oncotarget.com)
  • The results of the present study indicate that TFPI-2 manifestation was inhibited in the gastric tumor and peritumoral cells suggesting the inhibition of TFPI-2 manifestation may decrease the stability of the extracellular matrix. (cell-signaling-pathways.com)
  • this ERK phosphorylation was inhibited by AG1478, indicating EGFR involvement, and by the MEK inhibitor U0126 (10 mM). (cdc.gov)
  • The fundamental mechanism of interstitial fibrosis is the imbalance of extracellular matrix metabolism and abnormal accumulation via interaction of various inflammatory cytokines. (biomedcentral.com)
  • By coupling efficient chemical synthesis routes to multiple upfront in parallel phenotypic screens, we identify that KBU2046 inhibits cell motility and cell invasion in vitro. (nature.com)
  • Because they inhibit cell migration, they have antiangiogenic effects. (wikipedia.org)
  • Here, we show that in primary human femoral head osteoarthritic and normal bovine chondrocytes, TWHF partially or completely inhibited mRNA and protein expression of tumor necrosis factor-α, interleukin (IL)-1, and IL-17-inducible MMP-3 and MMP-13. (aspetjournals.org)
  • Instead, TWHF partially inhibited DNA binding capacity of cytokine-stimulated activating protein-1 (AP-1) and nuclear factor-κB (NF-κB) transcription factors. (aspetjournals.org)
  • 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)
  • Trouw L., Nilsson S., Goncalvez I., Landberg G. and Blom A. M. (2005) C4b-binding protein binds to necrotic cells and DNA, which limits DNA release and inhibits complement activation. (lu.se)
  • This difference provides the principle basis for identification of inhibitors targeting the hemopexin domain with high selectivity and specificity. (suny.edu)
  • However, plasma IL-1β and IL-6 concentrations at 90 min after endotoxin treatment were unaffected by GM-6001 following lethal endotoxin challenge, confirming the in vivo specificity of this matrix metalloproteinase inhibitor for TNFα processing. (elsevierpure.com)
  • Drug discovery and development of MMP inhibitors "The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances" (PDF). (wikipedia.org)
  • The mechanism whereby Mtb targets the lung apices is unknown, but once it reaches the lung interstititum, breakdown of the extracellular matrix must occur for the pathogen to disseminate via the airways. (ersjournals.com)
  • Additionally, the effects of transfection with circ‑PVT1 small interfering RNA (si‑circ‑PVT1) on HGC‑27 and AGS cells could be reversed by treatment with miR‑195‑5p inhibitor. (spandidos-publications.com)
  • Low Intensity Pulsed Ultrasound Promotes the Extracellular Matrix Synthesis of Degenerative Human Nucleus Pulposus Cells through FAK/PI3K/AktPathway. (qigonginstitute.org)
  • LIPUS has been used successfully for bone fracture healing and been proved to be effective instimulatingextracellular matrix metabolismin animal intervertebraldisc cells.However, whether LIPUS also exerts an anabolic effect on degenerative human nucleus pulposuscells and the possible molecular mechanism is yet unclear. (qigonginstitute.org)
  • All-trans retinoic acid (ATRA) and 13-cis retinoic acid (13-cisRA) (10 -6 and 10 -7 M) inhibited the growth of the cells, but low-dose ATRA and 13-cisRA (10 -8 M) marginally affected the growth of the cells. (johnshopkins.edu)
  • GM-6001 also inhibited the release of soluble TNF receptor (p75) from peripheral blood mononuclear cells stimulated with endotoxin and/or TNFα. (elsevierpure.com)
  • LC-MS analyses revealed increased levels of FAAH substrates (AEA, 2-AG, OEA, PEA) in cells incubated with either FAAH inhibitor. (oncotarget.com)
  • Metalloproteinases are secreted as proenzymes by neutrophils infiltrating the wound, injured epithelial cells, and keratocytes. (medscape.com)
  • 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)
  • The recombinant C-TIMP-2 and synthetic peptides from C-TIMP-2 were used as inhibitors for proMMP-2 activation. (amrita.edu)
  • Inhibitor experiments point toward a role of CB 2 and transient receptor potential vanilloid 1 in conferring anti-invasive effects of FAAH inhibitors and FAAH siRNA. (oncotarget.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)
  • Meanwhile, miR‑195‑5p inhibitor reversed the si‑circ‑PVT1‑induced low expression of ETS1. (spandidos-publications.com)
  • The LY294002 group was stimulated by LIPUS and treated with LY294002 simultaneously.The expression of aggrecan, collagen-II, Sox9, tissue inhibitor of metalloproteinase-1and matrix metalloproteinase-3were evaluated by ELISA, western blot orRT-PCR. (qigonginstitute.org)
  • LIPUS significantly upregulated expression of aggrecan, collagen-II, Sox9 and tissue inhibitor of metalloproteinase-1 compared to control group, but inhibited secretion ofmatrix metalloproteinase-3. (qigonginstitute.org)
  • Recently, Roflumilast, a phosphodiesterase type 4 (PDE-4) inhibitor was approved as a new therapeutic for COPD exacerbations with sales progressively growing since release (Fabbri et al. (justia.com)
  • The introduction of calcineurin inhibitor (CNI) therapy - first cyclosporine (CsA) in the 1980s and later tacrolimus - was initially hampered by early dosing regimens that led to a wide variety of side effects. (biomedcentral.com)