• 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)
  • We conclude that UCN-01, at clinically relevant concentrations, exerts an anti-neovascularization effect by blocking two important steps in vessel formation: (1) the response of cancer cells to hypoxia, and (2) endothelial cell proliferation. (karger.com)
  • Cisplatin is an alkylating agent that inhibits DNA synthesis and, thus, cell proliferation by causing DNA cross-links and denaturation of the double helix. (medscape.com)
  • Vinblastine inhibits microtubule formation, which disrupts formation of the mitotic spindle, causing cell proliferation to arrest at metaphase. (medscape.com)
  • Protein tyrosine kinase inhibitors inhibit both proliferation and chemotaxis of vascular smooth muscle cells. (researchmap.jp)
  • Bidirectional regulation of smooth muscle cell proliferation by IFN gamma. (researchmap.jp)
  • Protein kinase C-mediated inhibition of vascular smooth muscle cell proliferation : The isoform that may mediate G1/S inhibition. (researchmap.jp)
  • NTRK gene fusions are genomic alterations that result in constitutively-activated chimeric TRK fusion proteins, which act as an oncogenic driver, promoting cell proliferation and survival in tumor cell lines. (worldpharmanews.com)
  • Previous studies have demonstrated that glycolysis inhibitors reduce the proliferation of non‑small cell lung cancer (NSCLC) cells by interfering with the aerobic glycolytic pathway. (spandidos-publications.com)
  • These drugs, called GGTIs, inhibit proliferation of various human cancer cells and inhibit tumor growth in animal model systems. (uclahealth.org)
  • Protein transport between the nuclear and the cytoplasmic compartment is a key factor for cell viability and proliferation. (massgeneral.org)
  • This work not only defines the role of the ARTS gene in the underlying mechanism of mammalian tumor cell resistance to programmed cell death, but also links this gene to another hallmark of cancer, stem and progenitor cell proliferation," said Marion Zatz, who oversees cell death grants, including Steller's, at the NIH's National Institute of General Medical Sciences. (scienceblog.com)
  • Menin mutations lead to increased Hedgehog signaling and cell proliferation. (medindia.net)
  • The GAS1 protein promotes Hedgehog signaling, and thus by inhibiting Gas1 expression, menin and PRMT5 effectively dial down the pathway's tendency towards cell proliferation. (medindia.net)
  • What's more, treating a mouse model of human MEN1 syndrome with a Hedgehog pathway inhibitor called Erivedge (FDA-approved in 2012 for metastatic or locally advanced basal cell carcinoma) reduced proliferation of tumor cells and blood insulin levels. (medindia.net)
  • Enzastaurin apparently inhibits tumor growth via multiple mechanisms: suppression of tumor cell proliferation, induction of tumor cell apoptosis and inhibition of tumor-induced angiogenesis. (lclabs.com)
  • Enzastaurin had a synergistic inhibitory effect with the EGFR inhibitor gefitinib on the proliferation of parental and gefitinib-resistant (GR) cancer cells. (lclabs.com)
  • They inhibit CELL DIFFERENTIATION and induce CELL PROLIFERATION by modulating different CELL CYCLE regulators. (bvsalud.org)
  • It interferes with DNA synthesis by blocking methylation of deoxyuridylic acid and inhibiting thymidylate synthetase and, subsequently, cell proliferation. (medscape.com)
  • Here, we show that primitive (CD34(+)CD38(-)) CML cells, in contrast to corresponding normal cells, express a functional interleukin-1 (IL-1) receptor complex and respond with NF-κB activation and marked proliferation in response to IL-1. (lu.se)
  • its inhibition could disrupt stemness properties, but translation inhibitors are limited clinically due to toxicity. (nih.gov)
  • The end result is inhibition of DNA, ribonucleic acid (RNA), and protein synthesis. (medscape.com)
  • Protein kinase C-mediated inhibition of cyclin A expression in human vascular endothelial cells. (researchmap.jp)
  • Scientific Methods: In vitro growth inhibition assays were completed with AHCC alone and in combination with PLD in panel of human cancer cell lines and findings confirmed in vivo in an ovarian cancer xenograft mouse model. (researchgate.net)
  • However, in recent years, there has been increasing evidence that metformin exerts its anticancer effects through the inhibition of oxidative phosphorylation (OXPHOS) of tumor cell mitochondria, and metabolic pathways based on metformin targeting have only recently become the focus of intensive research. (spandidos-publications.com)
  • This inhibition of the Hh signaling pathway helps to slow down the spread of cancer cells and may help shrink tumors. (rxlist.com)
  • Bacitrac99 is the most pure form of bacitracin available, and should be used for the most sensitive applications and on the most sensitive cell lines since any impurities that might cause inhibition of resistant cell lines have been removed. (goldbio.com)
  • All impurities that might cause inhibition of resistant cell lines have been removed. (goldbio.com)
  • Reversible inhibitors produce different types of inhibition depending on whether they bind to the enzyme, the enzyme-substrate complex, or both. (wikipedia.org)
  • Kim JM, Noh EM, Kwon KB, et al: Curcumin suppresses the TPA-induced invasion through inhibition of PKCα-dependent MMP-expression in MCF-7 human breast cancer cells. (spandidos-publications.com)
  • Considering the destructive potential of the complement system, it is no surprise that nearly half of the system's proteins are involved in its inhibition. (lu.se)
  • Among the many protease inhibitors in plasma, tissue factor pathway inhibitor (TFPI) and antithrombin are the ones that are most specifically involved in inhibition of coagulation factors. (medscape.com)
  • The presence of protein Z, a vitamin K-dependent plasma protein, increases its inhibition of factor Xa over 1000-fold. (medscape.com)
  • Argos is a secreted protein that is an inhibitor of the epidermal growth factor receptor (EGFR) pathway in Drosophila melanogaster. (wikipedia.org)
  • Argos inhibits the EGFR pathway by sequestering the EGFR ligand Spitz. (wikipedia.org)
  • However, the mitochondrial oxidative phosphorylation (OXPHOS) pathway in tumor cells has also been implicated in lung cancer metabolism. (spandidos-publications.com)
  • In the 1920s, Otto Heinrich Warburg discovered that cancer cells, unlike normal cells, use the glycolytic pathway to obtain energy for growth even in the presence of oxygen, which is a phenomenon known as 'aerobic glycolysis' or the Warburg effect ( 9 ), and aerobic glycolysis is a common metabolic phenotype in NSCLC ( 11 ). (spandidos-publications.com)
  • It has been reported that lung cancer cells exhibit upregulated expression of all key glycolytic enzymes [hexokinase 2 (HK2), phosphofructokinase and pyruvate kinase (PK)] ( 13 ), suggesting that the essential enzymes of the aerobic glycolytic pathway have a critical role in the development of lung carcinoma. (spandidos-publications.com)
  • Genetic studies using fission yeast and Drosophila established that Rheb plays critical roles in both cell growth and cell cycle progression at the G1/S boundary and that this function of Rheb is mediated by its ability to activate the TOR/S6K signaling pathway. (uclahealth.org)
  • Likewise, WIKI4 also effectively inhibits the Wnt/β-catenin pathway-dependent growth of DLD1 (by 67% in 10 days;1μM). (fishersci.com)
  • We make a connection between apoptosis, stem cells and cancer that has not been made in this way before: this pathway is critically important in stem cell death and in reducing tumor risk," Steller says. (scienceblog.com)
  • It also suggests that the premature silencing of the Sept4/ARTS pathway at the stem cell level may herald cancer to come. (scienceblog.com)
  • How Do Antineoplastic Hedgehog Pathway Inhibitors Work? (rxlist.com)
  • Hh pathway inhibitors are drugs designed to selectively inhibit abnormal signaling in the Hh pathway that plays an essential role in cell growth and differentiation in the developing embryo. (rxlist.com)
  • In postembryonic life, the Hh pathway promotes cellular development and division in several cell types, both by direct cellular activation and secondary activation of multiple pathways of tissue generation, including angiogenesis (new blood vessel formation) and tissue growth. (rxlist.com)
  • The Hh pathway inhibitors bind to and inhibit Smoothened, a transmembrane protein involved in Hh signal transduction. (rxlist.com)
  • Hh pathway inhibitors are administered orally once daily with or without food. (rxlist.com)
  • Our results indicate that oscillatory behavior in the ERK pathway alters homeostatic gene regulation patterns and that the cellular response to perturbation may manifest differently in oscillating vs nonoscillating cells. (cdc.gov)
  • Scientists have identified that pancreatic cancer cells growth and spread are fueled by an unusual metabolic pathway that someday might be blocked with targeted drugs to control the deadly cancer. (medindia.net)
  • The protein kinase Cβ-selective inhibitor, enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. (lclabs.com)
  • Enzastaurin induces apoptosis in multiple myeloma (MM) cell lines by inhibiting signaling through the AKT pathway, which is caspase-independent. (lclabs.com)
  • Enzastaurin (LY317615), a protein kinase Cβ inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines. (lclabs.com)
  • For example, enzymes in a metabolic pathway may be inhibited by molecules produced later in the pathway, thus curtailing the production of molecules that are no longer needed. (wikipedia.org)
  • Zhang S, Li Z, Wu X, Huang Q, Shen HM and Ong CN: Methyl-3-indolylacetate inhibits cancer cell invasion by targeting the MEK1/2-ERK1/2 signaling pathway. (spandidos-publications.com)
  • Hedgehog ligand-expressing cancerous epithelial cells that are activated by the hedgehog signaling pathway may cause growth-promotion. (medscape.com)
  • Vismodegib is a Hedgehog (Hh) pathway inhibitor. (medscape.com)
  • We present a rate equation model for the TGF-b pathway in endothelial cells together with novel measurements. (lu.se)
  • Protein kinase C inhibitor enzastaurin induces in vitro and in vivo antitumor activity in Waldenström macroglobulinemia. (lclabs.com)
  • Chronic myeloid leukemia (CML) is currently treated with tyrosine kinase inhibitors, but these do not effectively eliminate the CML stem cells. (lu.se)
  • Outside the cell, it binds the EGFR-activator Spitz, preventing it from binding and activating EGFR. (wikipedia.org)
  • The menin-PRMT5 complex binds to the promoter of the Gas1 gene, where PRMT5 (an enzyme that adds methyl groups to histone proteins) functions as an epigenetic inhibitor, tamping down gene transcription. (medindia.net)
  • An enzyme inhibitor is a molecule that binds to an enzyme and blocks its activity . (wikipedia.org)
  • [7] A special case of protein enzyme inhibitors are zymogens that contain an autoinhibitory N-terminal peptide that binds to the active site of enzyme that intramolecularly blocks its activity as a protective mechanism against uncontrolled catalysis. (wikipedia.org)
  • The binding site of inhibitors on enzymes is most commonly the same site that binds the substrate of the enzyme. (wikipedia.org)
  • In active state binds to a variety of effector proteins to regulate cellular responses, such as secretory processes, phagocytose of apoptotic cells and epithelial cell polarization. (lu.se)
  • 3 Key Laboratory of Cell Differentiation and Apoptosis of the Chinese Ministry of Education, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, China. (nih.gov)
  • Mesenchymal stem cells (MSCs) show trilineage differentiation because these cells differentiate into osteocytes, chondrocytes and adipocytes. (nature.com)
  • The Ras-superfamily G-proteins play critical roles in cell growth and differentiation. (uclahealth.org)
  • Histone Deacetylase (HDAC) inhibitors induce cancer cell cycle arrest, differentiation and cell death, reduce angiogenesis and modulate immune response. (pharmiweb.com)
  • Inhibitor of differentiation proteins are negative regulators of BASIC HELIX-LOOP-HELIX TRANSCRIPTION FACTORS. (bvsalud.org)
  • Histone Deacetylase (HDAC) inhibitors increases the acetylation of lysine residues on histone proteins by inhibiting the activity of HDAC enzymes. (pharmiweb.com)
  • Changes of gene expression by lysophosphatidylcholine in vascular endothelial cells, 12 upregulated distinct genes including 5 cell growth-related, 3 thrombosis-related. (researchmap.jp)
  • Oxidized low density lipoprotein induces apoptosis in cultured human umbilicalvein endothelial cells by common and unique mechanisms. (researchmap.jp)
  • Enzastaurin enhances the antiangiogenic effects of radiation by radiosensitizing human endothelial cells in pancreatic cancer xenografts. (lclabs.com)
  • Enzastaurin, an inhibitor of PKCβ, enhances antiangiogenic effects and cytotoxicity of radiation against endothelial cells. (lclabs.com)
  • Endothelial cells are the primary site of plasma TFPI synthesis. (medscape.com)
  • [ 4 ] Most circulating TFPI is bound to lipoproteins, but on the surface of endothelial cells, a second pool of TFPI is bound to heparan sulfates. (medscape.com)
  • endothelial cells. (lu.se)
  • The SERPINA1 gene provides instructions for making a protein called alpha-1 antitrypsin, which is a type of serine protease inhibitor (serpin). (medlineplus.gov)
  • Coagulation factors XIa and Xa are inhibited by ZPI, an Mr 72,000 serine protease inhibitor. (medscape.com)
  • Cerulenin, an inhibitor of protein acylation, selectively attenuates nutrient stimulation of insulin release: a study in rat pancreatic islets. (diabetesjournals.org)
  • In bax − / − bak − / − cells, introduction of Bak mutants selectively targeted to either mitochondria or the ER can induce apoptosis. (rupress.org)
  • Dabrafenib inhibits some mutated forms of BRAF kinases with in vitro IC50 values of 0.65, 0.5, and 1.84 nM for BRAF V600E, BRAF V600K, and BRAF V600D enzymes, respectively. (medscape.com)
  • Serpins help control several types of chemical reactions by blocking (inhibiting) the activity of certain enzymes. (medlineplus.gov)
  • Alpha-1 antitrypsin also inhibits other enzymes, including a powerful enzyme called neutrophil elastase that is released from white blood cells to fight infection. (medlineplus.gov)
  • Enzymes are proteins that speed up chemical reactions necessary for life , in which substrate molecules are converted into products . (wikipedia.org)
  • [2] Enzyme inhibitors also control essential enzymes such as proteases or nucleases that, if left unchecked, may damage a cell. (wikipedia.org)
  • Many poisons produced by animals or plants are enzyme inhibitors that block the activity of crucial enzymes in prey or predators . (wikipedia.org)
  • Small molecule inhibitors include essential primary metabolites that inhibit upstream enzymes that produce those metabolites. (wikipedia.org)
  • PARP enzymes are drug targets: Drugs that inhibit PARP activity are already in use today in treatment of certain forms of cancer. (lu.se)
  • Stanford scientists have found a mouse gene that transports this substance, pyrophosphate, into and out of cells. (stanford.edu)
  • The ank gene that the team found produces a protein that spans the membrane surrounding cells. (stanford.edu)
  • Kingsley and his colleagues believe that if there is a defect in the ank gene, the shuttle transporter stops working and pyrophosphate accumulates inside cells. (stanford.edu)
  • His group is the first to pinpoint the ank gene, identify the protein encoded by it and construct a model explaining how the ank protein may be involved in arthritis. (stanford.edu)
  • Cloning and characterization of a novel human gene encoding a zinc finger protein with 25 finger. (researchmap.jp)
  • Protein tyrosines and protein kinase C are required for gene expression of monocyte chemoattractant protein-1 in human monocytes. (researchmap.jp)
  • Many SERPINA1 gene variants change single protein building blocks (amino acids) in alpha-1 antitrypsin, which can alter the protein's structure. (medlineplus.gov)
  • Still other gene variants prevent the production of any alpha-1 antitrypsin protein. (medlineplus.gov)
  • The protein encoded by this gene is an unusual orphan receptor that contains a putative ligand-binding domain but lacks a conventional DNA-binding domain. (cancerindex.org)
  • What does this gene/protein do? (cancerindex.org)
  • What pathways are this gene/protein implicaed in? (cancerindex.org)
  • The protein encoded by this gene is one of at least two lipid transfer proteins found in human plasma. (nih.gov)
  • Research associate Maria Garcia-Fernandez, Hermann Steller, head of the Strang Laboratory of Apoptosis and Cancer Biology, and their colleagues explored the activity of a gene called Sept4, which encodes a protein, ARTS, that increases programmed cell death, or apoptosis, by antagonizing other proteins that prevent cell death. (scienceblog.com)
  • The identification of the ARTS gene and its role in cancer cell death provides a potential target for new therapeutic approaches. (scienceblog.com)
  • Histone deacetylase (HDAC) inhibitors are important epigenetic mechanisms that regulate gene expression and transcription. (pharmiweb.com)
  • These high purity reagents are useful in gene selection, diagnostics and other laboratory applications without harming your selected cells or microorganisms. (goldbio.com)
  • We investigated the clinical significance of E2F1 gene expression in relation to its target genes, thymidylate synthase ( TS ) and Survivin , in case of non-small-cell lung cancer (NSCLC). (aacrjournals.org)
  • Significantly, Hua's team found that menin mutant proteins associated with MEN1 cancer in patients were impaired in their ability to interact with PRMT5, and thus, in adding the methyl chemical group to the Gas1 promoter gene. (medindia.net)
  • Western blot analysis and real-time PCR showed that celastrol dose-dependently suppressed TNF-α-induced MMP-9 gene expression at both the mRNA and protein levels in MDA-MB-231 cells. (spandidos-publications.com)
  • Specifically, the WNT5A gene was hypermethylated at the promotor region in the diabetic cells and its protein was markedly repressed. (medscape.com)
  • The hemagglutinin (HA) gene codes for one of the two surface glycoproteins and is central to species speci city because it is responsible for virus attachment and fusion with host cells. (cdc.gov)
  • The neuraminidase (NA) gene encodes the other surface protein of the virus. (cdc.gov)
  • Trametinib is a reversible inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2 activation, and of MEK1 and MEK2 kinase activity. (medscape.com)
  • Y-27632A, CAS 331752-47-7, is a cell-permeable, reversible, inhibitor of Rho kinases (K i = 140 nM for p160ROCK). (sigmaaldrich.com)
  • A highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinase (Ki = 140 nM for p160 ROCK (ROCK-I). Also inhibits ROCK-II with almost equal potency. (sigmaaldrich.com)
  • A highly potent, cell-permeable, reversible, and selective inhibitor of Rho-associated protein kinases (K i = 140 nM for p160 ROCK ). (sigmaaldrich.com)
  • By contrast, reversible inhibitors bind non-covalently and may spontaneously leave the enzyme, allowing the enzyme to resume its function. (wikipedia.org)
  • Compartmentalized secretory leukocyte protease inhibitor expression and hormone responses along the reproductive tract of postmenopausal women. (springer.com)
  • The present manuscript from the laboratory of Prof. Münch, University Medical Center, Ulm, demonstrates that alpha 1 antitrypsin, a protease inhibitor produced in the human body during inflammation, blocks TMPRSS2 and SARS-CoV-2 infection. (dpz.eu)
  • Another potentially important regulator of the coagulation system, the protein Z/protein Z-dependent protease inhibitor (ZPI) system, is also emerging. (medscape.com)
  • 8 Astrocytes interact with blood vessels, pericytes, and epithelial cells to organize CNS flow and modulate the blood-brain barrier (BBB). (news-medical.net)
  • however, Gper1 and PR levels are reduced in both stromal and epithelial cells in a time-specific manner. (springer.com)
  • The abnormal wound healing is due to impaired limbal epithelial stem cells, and the new research, published online July 18 in Diabetologia , involved isolation of those cells from 30 donor eyes of humans with and 23 without diabetes. (medscape.com)
  • However, treatment with various approaches, including exogenous WNT5A methylation inhibitors and a nanoconjugate that inhibits WNT5A suppression, improved corneal epithelial wound healing as well as expression of the limbic epithelial stem cells. (medscape.com)
  • Overall, Wnt-5a is a new corneal epithelial wound healing stimulator that can be targeted to improve wound healing and stem cells in the diabetic cornea," write Ruchi Shah, PhD, of the Board of Governors Regenerative Medicine Institute, Cedars-Sinai Medical Center, Los Angeles, California, and colleagues. (medscape.com)
  • The present study analyzed the effect of adenovirus on bacterial adherence to human respiratory tract epithelial cells. (lu.se)
  • Anticytotoxic T-lymphocyte-associated protein 4 (CTLA-4) is a humanized antibody that overcomes CTLA-4-mediated T-cell suppression to enhance the immune response against tumors. (medscape.com)
  • p53's ability to inhibit tumors can be considered as a specific outcome of its stress-responsive effects. (nature.com)
  • Among immune cells, Foxp3 + regulatory T cells (Treg cells) are potent inhibitors of cancer immunity, and their presence within solid tumors is generally associated with a poor prognosis. (mdpi.com)
  • By identifying a mechanism that regulates programmed cell death in precursor cells for blood, or hematopoietic stem cells, the work is the first to connect the death of such cells to a later susceptibility to tumors in mice. (scienceblog.com)
  • Individuals with MEN1 are at a substantially increased risk of developing neuroendocrine tumors, including cancer of the pancreatic islet cells that secrete insulin. (medindia.net)
  • They found that inhibiting proteins in the Hedgehog network using drugs reduces growth of tumors in an animal model of human MEN1 syndrome. (medindia.net)
  • On the contrary, treatment with the protein synthesis inhibitors cycloheximide, anisomycin, or puromycin as well as prolonged exposure to the RNA synthesis inhibitor actinomycin D mimicked the biochemical modulating effects of 6AN on cisplatin action. (aspetjournals.org)
  • The investigators moved on to think about evaluating the therapeutic potential of pharmacologically inhibiting Cx32, using 2-aminoethoxy-dipenyl-borate (2APB), a compound previously shown to transiently inhibit Cx32 gap junctions in vitro, and which they confirmed was specific to the Cx32 gap junction protein. (genengnews.com)
  • Transcriptional Control of Regulatory T Cells in Cancer: Toward Therapeutic Targeting? (mdpi.com)
  • Therapeutic approaches that target the metabolism of tumor cells have been a popular research topic in recent years. (spandidos-publications.com)
  • Our investigations are ongoing in biomarkers of resistance and potential new targets for therapeutic intervention in colorectal cancer, melanoma and Merkel cell carcinoma. (massgeneral.org)
  • Chung TW, Moon SK, Chang YC, et al: Novel and therapeutic effect of caffeic acid and caffeic acid phenyl ester on hepato-carcinoma cells: complete regression of hepatoma growth and metastasis by dual mechanism. (spandidos-publications.com)
  • In vivo administration of IL1RAP antibodies in mice transplanted with chronic and blast phase CML cells resulted in therapeutic effects mediated by murine effector cells. (lu.se)
  • The term "oncotarget" encompasses all molecules, pathways, cellular functions, cell types, and even tissues that can be viewed as targets relevant to cancer as well as other diseases. (oncotarget.com)
  • The Incucyte ® Live-Cell Analysis System delivers flexible kinetic quantification of biological phenotypes to monitor growth, motility, morphology, and cellular function. (news-medical.net)
  • Understanding the cellular and molecular mechanisms that define cancer and how these mechanisms differ from normal cells is crucial for developing new innovative therapies," says Bentires-Alj. (unibas.ch)
  • Furthermore, cerulenin abolished augmentation of both Ca2+-stimulated and Ca2+-independent insulin release by 10 micromol/l palmitate, which causes palmitoylation of cellular proteins. (diabetesjournals.org)
  • RNA viruses may escape acquired humoral and cellular immune responses by mutations in protective antigenic epitopes (e.g., avian influenza viruses), while accessory nonstructural proteins or multifunctional structural proteins interfere with the interferon system (e.g. (imperial.ac.uk)
  • Cycloheximide can be used to study cellular processes and inhibit yeast growth. (goldbio.com)
  • The purpose of this study was to determine the ontogeny of cellular changes in the expression of estrogen receptors (ERα, ERβ), G protein-coupled estrogen receptor 1 (GPER1), and progesterone receptors (PRs) in endometriosis using a mouse model. (springer.com)
  • Studies of the Infection Biology Unit revealed that SARS-CoV-2 uses the cellular protease for activation of its spike protein. (dpz.eu)
  • After ingestion of melanoma-derived exosomes during incubation, mouse embryonic fibroblasts cells emerged cellular invasiveness with the presentation of a marked increase in miR-21 expression. (dovepress.com)
  • In the present study, we reported that celastrol potentiated tumor necrosis factor-α (TNF-α)-induced apoptosis, affected activation of caspase-8, caspase-3 and PARP cleavage, and inhibited the expression of anti-apoptotic proteins such as cellular inhibitor of apoptosis protein 1 and 2 (cIAP1 and cIAP2), cellular FLICE-inhibitory protein (FLIP), and B-cell lymphoma 2 (Bcl-2). (spandidos-publications.com)
  • Although older chemotherapeutic drugs are often toxic to normal cells, advances in genetics and cellular and molecular biology have led to development of more selective drugs. (msdmanuals.com)
  • Tamanoi's laboratory has developed anti-cancer drugs against Ras proteins aimed at inhibiting their posttranslational modification and membrane association. (uclahealth.org)
  • While it has been suggested that Amphotericin B interacts with ergosterol of the fungal cell membrane leading to an altered cell membrane permeability and death, more recent studies show that the mechanism behind amphotericin B's fungicidal activity is more complex. (goldbio.com)
  • Monocarboxylate transporters (MCTs) are cell membrane proteins transporting lactate, pyruvate, and ketone bodies across the plasma membrane. (bvsalud.org)
  • This leads to initiation of cascade of enzymatic cleavages and formation of crucial enzymatic complexes (C3 and C5 convertases), release of pro-inflammatory anaphylatoxins (C5a, C3a) that attract white blood cells and finally formation of membrane attack complex (MAC, pore in a membrane). (lu.se)
  • For chemotherapy drugs, one of the best characterized resistance mechanisms is overexpression of MDR1 , a cell membrane transporter that causes efflux of certain drugs (eg, vinca alkaloids, taxanes, anthracyclines). (msdmanuals.com)
  • Tamanoi and his researchers were the first to show that these nanoparticles can deliver anticancer drugs and inhibit tumor growth in vitro and in vivo. (uclahealth.org)
  • The Argos domain has features in common with the three finger toxin fold that is found in a number of proteins including TGF beta receptors and the urokinase (uPA) receptor. (wikipedia.org)
  • The protein has been shown to interact with retinoid and thyroid hormone receptors, inhibiting their ligand-dependent transcriptional activation. (cancerindex.org)
  • The major role of the NA is to release new progeny virions from an infected cell by enzymatically cleaving sialic acid receptors, which aids virus spread to uninfected cells within an infected host. (cdc.gov)
  • Medicinal enzyme inhibitors often have low dissociation constants , meaning that only a minute amount of the inhibitor is required to inhibit the enzyme. (wikipedia.org)
  • Most inhibitors act on complement convertases through increased dissociation of these enzymatic complexes (acceleration of decay) or through promoting enzymatic cleavage of activated complement factors C3b or C4b by a serine proteinase factor I (FI). (lu.se)
  • Regulated by guanine nucleotide exchange factors (GEFS) which promote the exchange of bound GDP for free GTP, GTPase activating proteins (gaps) which increase the GTP hydrolysis activity, and GDP dissociation inhibitors which inhibit the dissociation of the nucleotide from the GTPase. (lu.se)
  • Three are neuraminidase inhibitor antiviral drugs: oseltamivir (available as a generic version or under the trade name Tamiflu®) for oral administration, zanamivir (trade name Relenza®) for oral inhalation using an inhaler device, and peramivir (trade name Rapivab®) for intravenous administration. (cdc.gov)
  • There is another class of FDA-approved antiviral drugs, M2 inhibitors amantadine and rimantadine, also called the adamantanes, that in the past were active against flu A viruses (but not flu B viruses). (cdc.gov)
  • The enzymatic activity of NA is inhibited by one class of antiviral drugs that are FDA-approved for treatment of in uenza (i.e. (cdc.gov)
  • Hox genes modulate the properties of hematopoietic stem cells (HSCs) and reacquired Hox expression in progenitors contributes to leukemogenesis. (nih.gov)
  • First identified in embryonic stem cells, SEs mediate pluripotent state maintenance by promoting the expression of pluripotent identity genes, including Oct4 , Sox2 , Nanog and Klf4 . (nature.com)
  • Studies were undertaken to determine whether extracellular signal regulated kinase (ERK) oscillations regulate a unique subset of genes in human keratinocytes and subsequently whether the p38 stress response inhibits ERK oscillations. (cdc.gov)
  • Once activated, p53 coordinates multiple downstream pathways, thereby maintaining the homeostasis of the host cell or organism (if the stress is mild, transient, and repairable) or eliminating damaged cells (if the stress is acute, prolonged, and difficult to resist). (nature.com)
  • In this review, we summarize the current knowledge on the different intracellular pathways involved in the programming of Treg cell homeostasis and functions in cancer. (mdpi.com)
  • Lee SO, Jeong YJ, Yu MH, et al: Wogonin suppresses TNF-alpha-induced MMP-9 expression by blocking the NF-kappaB activation via MAPK signaling pathways in human aortic smooth muscle cells. (spandidos-publications.com)
  • C4b-binding protein (C4BP) is the major soluble inhibitor of the classical and lectin pathways whereas factor H (FH) inhibits the alternative route. (lu.se)
  • Their experiments demonstrated that treating mice with a small molecule inhibitor that specifically target the hepatic gap junction protein connexion 32 (Cx32) provides significant protection against liver damage and death resulting from subsequent or simultaneous challenge with known hepatotoxic drugs such as acetaminophen. (genengnews.com)
  • [3] [2] Small molecule enzyme inhibitors also include secondary metabolites , which are not essential to the organism that produces them, but provide the organism with an evolutionary advantage, in that they can be used to repel predators or competing organisms or immobilize prey. (wikipedia.org)
  • Interferon gamma suppresses PDGF production from THP-1 cells and blood monocyte-derived macrophages. (researchmap.jp)
  • It is expressed by hepatocytes, the principal cell source, and by monocyte/macrophages (4). (rndsystems.com)
  • It enhances entry of cationic inhibitors into macrophages (6). (rndsystems.com)
  • It may increase tumor infiltration by lymphocytes, dendritic cells, and macrophages. (medscape.com)
  • Significant differences were found in DNA methylation between the cells of those two groups. (medscape.com)
  • Targeted therapies focus on binding to specific molecules that are important for cancer cell survival and growth. (cancercare.org)
  • ARTS interferes with molecules called inhibitor of apoptosis proteins (IAPs), which prevent cells from killing themselves. (scienceblog.com)
  • Many drug molecules are enzyme inhibitors that inhibit an aberrant human enzyme or an enzyme critical for the survival of a pathogen such as a virus , bacterium or parasite . (wikipedia.org)
  • Enzyme inhibitors are a chemically diverse set of substances that range in size from organic small molecules to macromolecular proteins . (wikipedia.org)
  • In addition to small molecules, some proteins act as enzyme inhibitors. (wikipedia.org)
  • Studies have shown that miR-21 can promote invasion of melanoma cells. (dovepress.com)
  • 10 High expression of miR-21 in melanoma cells inhibits mRNA expression of crucial tumor suppressor proteins such as the tissue inhibitor of metalloproteinases 3 (TIMP3). (dovepress.com)
  • Signal transduction of PDGF-induced chemotaxis of vascular smooth muscle cells. (researchmap.jp)
  • Dr. Fuyu Tamanoi's research focuses on signal transduction involving the Ras-superfamily G-proteins, anti-cancer drugs and nanoparticle-based delivery of anticancer drugs. (uclahealth.org)
  • Mathematical modeling of signal transduction networks has previously been used to map out thermodynamical using rate equations is increasingly attracting attention as a properties of protein-folding models (6,7). (lu.se)
  • Also acts as a potent inhibitor of agonist-induced Ca 2+ sensitization of myosin phosphorylation and smooth muscle contractions (IC 50 = 700 nM for phenylephrine-induced contractions in aortic strips). (sigmaaldrich.com)
  • Also acts as a potent inhibitor of agonist-induced Ca 2+ sensitization of myosin phosphorylation and smooth muscle contraction. (sigmaaldrich.com)
  • Ritonavir is a potent inhibitor of CYP3A4- and CYP2D6- mediated drug metabolism. (who.int)
  • Kinase proteins send signals to the cell's control center to help tumor cells grow. (cancercare.org)
  • Certain metabolic alterations, also referred to as metabolic reprogramming, are commonly observed in tumor cells and are proposed to be hallmarks of cancer ( 8 ). (spandidos-publications.com)
  • Given the vast differences in metabolism between healthy and tumor cells, there is hope that selective targeting of tumor metabolism may be achieved while limiting toxicity to healthy tissue. (spandidos-publications.com)
  • So tumor cells-derived exosomes. (dovepress.com)
  • In summary, these data demonstrate that SVC112 suppresses CSC-related proteins, enhances the effects of radiation, and blocks growth of HNSCC PDXs by inhibiting CSCs. (nih.gov)
  • The present study was undertaken to examine the mechanistic basis for the recent observation that the pyridine nucleotide derivative 6-aminonicotinamide (6AN, NSC 21206) enhances the accumulation and resulting cytotoxicity of cisplatin in a variety of tumor cell lines. (aspetjournals.org)
  • Prevents apoptosis and enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency. (sigmaaldrich.com)
  • Nutrients such as glucose stimulate insulin release from pancreatic beta-cells through both ATP-sensitive K+ channel-independent and -dependent mechanisms, which are most likely interrelated. (diabetesjournals.org)
  • In isolated rat pancreatic islets, cerulenin inhibited the glucose augmentation of Ca2+-stimulated insulin release evoked by a depolarizing concentration of K+ in the presence of diazoxide and Ca2+-independent insulin release triggered by a combination of forskolin and phorbol ester under stringent Ca2+-free conditions. (diabetesjournals.org)
  • Following 48 h exposure, we found significant decreases in the levels of KRAS, RHOA, RAC1, and CDC42 ranging within 20-66% after NSL-YHJ-2-27 (5 μM) treatment in all four cell lines tested, A549, NCI-H1299, MDA-MB-231, and MDA-MB-468. (oncotarget.com)
  • Moreover, after PCAIs treatment, migration, and invasion of A549 cells were inhibited by 72 and 70%, respectively while the levels of vinculin and fascin dropped by 33 and 43%, respectively. (oncotarget.com)
  • When A549 lung cancer cells or K562 leukemia cells were treated with 62.5 μM 6AN for 21 h and then pulse-labeled with [ 35 S]methionine for 1 h, increased labeling of five polypeptides, one of which corresponded to a M r ∼78,000 glucose-regulated protein (GRP78), was observed. (aspetjournals.org)
  • The most common chemotherapeutic agent used in superficial basal cell carcinoma is topical 5-fluorouracil. (medscape.com)
  • This agent is indicated for treatment of adults with metastatic basal cell carcinoma or with locally advanced basal cell carcinoma that has recurred following surgery, or those who are not candidates for surgery or radiation. (medscape.com)
  • It is not approved by the US Food and Drug Administration for treating basal cell carcinoma. (medscape.com)
  • We want to understand enzymatic mechanisms and improve the fit of PARP inhibitors to their enzymatic pockets. (lu.se)
  • Since anti-pathogen inhibitors generally target only one enzyme, such drugs are highly specific and generally produce few side effects in humans, provided that no analogous enzyme is found in humans. (wikipedia.org)
  • A low concentration of the enzyme inhibitor reduces the risk for liver and kidney damage and other adverse drug reactions in humans. (wikipedia.org)
  • In addition to the HA and NA, the RNA transcription and replication complex (PB2, PB1, PA, NP) also have species-speci c determinants that impact e cient replication in humans and other mammals, particularly polymerase basic protein 2 (PB2). (cdc.gov)
  • The toxicity data of protein kinase inhibitors in humans is also well established [5]. (who.int)
  • Lenalidomide (Revlimid) helps the bone marrow produce healthy blood cells while killing abnormal cells. (cancercare.org)
  • Abnormal alpha-1 antitrypsin proteins, including those produced from the Z allele, may bind together to form a large molecule, or polymer, that cannot leave the liver. (medlineplus.gov)
  • Scope includes mutations and abnormal protein expression. (cancerindex.org)
  • We report that, in addition to direct inhibitory effects on endothelial cell growth, UCN-01 abrogates hypoxia-mediated transactivation of HIF-1-responsive promoters in a prostate cancer cell line. (karger.com)
  • Unlike other coagulation protease inhibitors, TFPI has inhibitory sites for factor Xa and for the factor VIIa/tissue factor (TF) complex, and it cannot inhibit the factor VIIa/TF complex without being bound to factor Xa. (medscape.com)
  • We used the autologous uterine tissue transfer mouse model and studied the mRNA and protein expression of ERα, ERβ, GPER1, and PR in ectopic lesions at 2, 4, and 8 weeks of induction of endometriosis. (springer.com)
  • Expression of the G protein-coupled estrogen receptor (GPER) in endometriosis: a tissue microarray study. (springer.com)
  • MiR-21 promoted invasion of fibroblasts by down-regulation of tissue inhibitor of metalloproteinase 3 (TIMP3) expression and increasing of matrix metalloprotein (MMP) expression in fibroblast cells via melanoma-derived exosomes in a time-dependent manner. (dovepress.com)
  • Woessner JF Jr: Matrix metalloproteinases and their inhibitors in connective tissue remodeling. (spandidos-publications.com)
  • Several of these inhibitors circulate in blood whereas others are expressed on virtually all cells of the body to protect self-tissue from complement attack. (lu.se)
  • During the experimental setup, it is recommended to add the linear DNA template in the last step to allow GamS to bind and inhibit RecBCD exonuclease before RecBCD has a chance to act on the DNA. (neb.com)
  • Enzyme inhibitors may bind reversibly or irreversibly. (wikipedia.org)
  • [6] Another class of inhibitor proteins is the ribonuclease inhibitors , which bind to ribonucleases in one of the tightest known protein-protein interactions . (wikipedia.org)
  • The virus-infected cells were harvested at various times after infection and analyzed for the ability to bind strains of Haemophilus influenzae and Streptococcus pneumoniae. (lu.se)
  • Enzastaurin inhibits tumours sensitive and resistant to anti-EGFR drugs. (lclabs.com)
  • Polyisoprenylated cysteinyl amide inhibitors (PCAIs) are agents that mimic the essential posttranslational modifications of G-proteins. (oncotarget.com)
  • My research revolves around ADP-ribosyltransferases, which cleave NAD+ to link ADP-ribose to their target proteins. (lu.se)
  • This flags these target proteins for specific activities in our cells. (lu.se)
  • Because protein acylation might be a sequel of cytosolic long-chain acyl-CoA accumulation, we examined if this reaction is engaged in nutrient stimulation of insulin release, using cerulenin, an inhibitor of protein acylation. (diabetesjournals.org)
  • Cerulenin also inhibited augmentation of insulin release by alpha-ketoisocaproate, a mitochondrial fuel. (diabetesjournals.org)
  • In contrast, cerulenin did not attenuate insulin release elicited by nonnutrient secretagogues, such as a depolarizing concentration of K+, activators of protein kinases A and C, and mastoparan. (diabetesjournals.org)
  • In conclusion, cerulenin inhibits nutrient augmentation of insulin release with a high selectivity. (diabetesjournals.org)
  • It inhibits both insulin receptor autophosphorylation and undesirable calcification (7, 8). (rndsystems.com)
  • Yu HY, Kim KS, Moon HI, Kim KM, Lee YC and Lee JH: JNP3, a new compound, suppresses PMA-induced tumor cell invasion via NF-κB down regulation in MCF-7 breast cancer cells. (spandidos-publications.com)
  • Novel selective inhibitors of nuclear export (SINE) have achieved outstanding preclinical results and are currently in Phase I trials. (massgeneral.org)
  • They thus postulated that liver-specific gap junction inhibitors might act to protect the liver if they could be co-formulated with hepatotoxic drugs. (genengnews.com)
  • Chemotherapy drugs, given intravenously (through a needle into a vein) or in pill form, can kill cancer cells. (cancercare.org)
  • We hope to create inhibitors also for their activities, with the aim of creating new anti-infective drugs. (lu.se)
  • Cytotoxic drugs damage DNA and kill many normal cells as well as cancer cells. (msdmanuals.com)
  • In contrast, other drugs (eg, DNA cross-linkers, also known as alkylating agents) have a linear dose-response relationship, killing more cancer cells at higher doses. (msdmanuals.com)
  • Single drugs may cure selected cancers (eg, choriocarcinoma, hairy cell leukemia). (msdmanuals.com)
  • Cycloheximide is a protein synthesis inhibitor in eukaryotic cells. (goldbio.com)
  • and 2) simultaneous treatment of cells with 6AN and cycloheximide prevented the increase in GRP78 but not the sensitizing effect of 6AN. (aspetjournals.org)
  • Small G-proteins, monomeric GTPases, or the RAS (Rat sarcoma) superfamily are a large family of small guanine nucleotide-binding proteins with molecular weights ranging from 20 to 30 kDa [ 1 , 2 ]. (oncotarget.com)
  • More recently, they have focused their attention on a novel family of the Ras-superfamily G-proteins called Rheb. (uclahealth.org)
  • It is a major plasma protein and a member of the cystatin superfamily of protease inhibitors (2, 3). (rndsystems.com)
  • Cell Rep. 2021 Apr 20;35(3):109017. (dpz.eu)
  • SVC112 had greater antiproliferative effects on HNSCC cells compared with the FDA-approved translation inhibitor omacetaxine mepesuccinate (HHT). (nih.gov)
  • however, direct antiproliferative effects against malignant cells and modulation of host immune response may be important. (medscape.com)
  • It is hypothesized that PCAIs work as anticancer agents by disrupting polyisoprenylation-dependent functional interactions of the G-Proteins. (oncotarget.com)
  • Astrocytes are a heterogeneous population of cells with distinguishing functional and morphological characteristics and are specialized to their different brain regions and locations. (news-medical.net)
  • This article discusses how a combination of live-cell analysis methods deliver the required flexibility to allow these highly dynamic astrocytic models to be characterized, via quantification of their growth, motility, morphology, and functional analysis. (news-medical.net)
  • Some microorganisms either produce a functional mimic of a complement regulatory protein or hijack host's regulatory proteins. (lu.se)
  • A deficiency of antithrombin increases the risk of thrombosis, revealing its importance as a functional inhibitor of the blood coagulation proteases. (medscape.com)
  • The hormone estrogen acts as a signaling molecule in cells by binding to its cognate receptor, the estrogen receptor, thereby inducing a range of biological effects. (unibas.ch)
  • The researchers found the human version of the protein using the mouse ank protein as a guide. (stanford.edu)
  • Human Neonatal and adult vascular smooth muscle cells in culture. (researchmap.jp)
  • Mitogenic activity of interferon gamma on growth-arrested human vascular smooth muscle cells. (researchmap.jp)
  • Stem cells have an enormous amount of potential to increase the health, and overall living standards of the human species in general. (scienceblog.com)
  • Bromate inhibited ERK oscillations in human keratinocytes and JB6 cells and induced an increase in phospho-p38 and a decrease in phospho-MED1 protein levels. (cdc.gov)
  • Kolkova Z, Noskova V, Ehinger A, Hansson S, Casslén B. G protein-coupled estrogen receptor 1 (GPER, GPR 30) in normal human endometrium and early pregnancy decidua. (springer.com)
  • Further, the study shows that the spike-protein is robustly expressed at the temperature in human airways. (dpz.eu)
  • Laporte et al, The SARS-CoV-2 and other human coronavirus spike proteins are fine-tuned towards temperature and proteases of the human airways. (dpz.eu)
  • In addition, celastrol significantly reduced the invasion of MDA-MB-231 human breast cancer cells after TNF-α stimulation. (spandidos-publications.com)
  • Park SK, Hwang YS, Park KK, Park HJ, Seo JY and Chung WY: Kalopanaxsaponin A inhibits PMA-induced invasion by reducing matrix metalloproteinase-9 via PI3K/Akt- and PKCdelta-mediated signaling in MCF-7 human breast cancer cells. (spandidos-publications.com)
  • They are present in factor VIII inhibitors, which are IgG antibodies against factor VIII, occur in hemophilia A (alloantibodies). (medscape.com)
  • IL1RAP antibodies that inhibit IL-1 signaling could block these effects. (lu.se)
  • This has increased demand for histone deacetylase (HDAC) inhibitors that inhibit the actions of HDAC enzyme. (pharmiweb.com)
  • We also offer solutions for automation, site-directed mutagenesis, as well as your favorite restriction enzyme, ligase or competent cell products. (neb.com)
  • Unlike many cancer-associated proteins, menin is neither an enzyme nor a signaling receptor. (medindia.net)
  • enzyme (E) accelerates conversion of substrates (S) to products (P). Bottom: by binding to the enzyme, inhibitor (I) blocks binding of substrate. (wikipedia.org)
  • An enzyme inhibitor stops ("inhibits") this process, either by binding to the enzyme's active site (thus preventing the substrate itself from binding) or by binding to another site on the enzyme such that the enzyme's catalysis of the reaction is blocked. (wikipedia.org)
  • Irreversible inhibitors form a chemical bond with the enzyme such that the enzyme is inhibited until the chemical bond is broken. (wikipedia.org)
  • Enzyme inhibitors play an important role in all cells, since they are generally specific to one enzyme each and serve to control that enzyme's activity. (wikipedia.org)
  • This involves both farnesylation (catalyzed by protein farnesyltransferase) and geranylgeranylation (catalyzed by protein geranylgeranyltransferase-I). Small molecular inhibitors of protein geranylgeranyltransferase-I were identified from a library of compounds generated by phosphine catalysis of allenoate compounds. (uclahealth.org)
  • In general, our Molecular Grade Hygromycin B (which is still ≥92 % pure and less expensive) will not adversely affect your cells and is suitable for most experiments. (goldbio.com)
  • 1 It has been found that exosomes can mediate local and systemic cell communication with transmitting signals from one cell to another on the molecular level. (dovepress.com)
  • 2 , 3 Tumor cell-derived exosomes carry particular molecular components originated from donor cells to mediate tumorigenesis and drive tumor progression by regulating tumor microenvironment. (dovepress.com)
  • Although many related studies have been performed, differences in cell lines, experimental conditions and downstream mechanisms have generally resulted in contradictory findings. (nature.com)
  • Although the conventional activities of p53 such as cell cycle arrest, senescence, and apoptosis are well accepted as the major checkpoints in stress responses, accumulating evidence implicates the importance of other tumor suppression mechanisms. (nature.com)
  • To date, various mechanisms have been suggested to explain the powerful tumor-suppressive effect of p53, including the induction of cell cycle arrest, senescence, and apoptosis. (nature.com)