• In this work, we have tested the human canonical members of the RNase family using a spot-culture growth inhibition assay based mycobacteria-infected macrophage model for evaluating their anti-tubercular properties. (frontiersin.org)
  • The present study was designed to examine the underlying mechanism(s) by which CKS-17 down-regulates the TNF-alpha mRNA expression using a human acute monocytic leukemia cell line THP-1 stimulated with the superantigen staphylococcal enterotoxin E. A cyclooxygenase inhibitor indomethacin does not reverse the inhibition of TNF-alpha mRNA expression by CKS-17, suggesting that prostaglandins are not responsible for the suppressive action of CKS-17. (duke.edu)
  • Taken together, these results suggest that the synthetic retroviral peptide CKS-17 down-regulates TNF-alpha mRNA expression through inhibition of transcriptional activation of the TNF-alpha gene, which requires de novo synthesis of a transcriptional repressor protein(s). (duke.edu)
  • The organizing team coordinated with various contract research organizations (CROs) and collaborating institutions to synthesize and test 878 compounds for biological activity against proteases (Nsp5, Nsp3, TMPRSS2), nucleocapsid N, RdRP (only the Nsp12 domain), and (alpha) spike protein S. Overall, 27 compounds with weak inhibition/binding were experimentally identified by binding-, cleavage-, and/or viral suppression assays and are presented here. (bvsalud.org)
  • We determined NAI 50% inhibitory concentrations (IC 50 s) of isolates using fluorometric-based NA inhibition assays ( 5 ) and evaluated their NA activity (V max [maximum velocity of substrate conversion]) by performing enzyme kinetics experiments ( 6 ). (cdc.gov)
  • Among Difopein supplier the examined kinase inhibitors, PP1, PP2 as well as the Lck inhibitor exhibited solid inhibition of PTK6 (Desk I). The IC50 beliefs for PP1, PP2 as well as the Lck inhibitor had been 230.0, 50.0 and 60.0 nM, respectively (Desk II). (scienceexhibitions.org)
  • Inhibition from the catalytic activity of purified PTK6 by chosen kinase inhibitors IC50 (nM)akinase assay. (scienceexhibitions.org)
  • Some of the extracts were showed remarkable inhibition percentage (60-80%) against PTP1B by p NPP assay. (icbb.com.np)
  • Recombinant OATP1B1-, OATP2B1-, and OATP1B3-mediated fluvastatin transport was inhibited to 97, 70, and 62% by gemfibrozil (200 μM), respectively, whereas only a small inhibitory effect by gemfibrozil (200 μM) on fluvastatin uptake into primary human hepatocytes was observed (27% inhibition). (aspetjournals.org)
  • Protein S also interacts with TFPIα and serves as TFPIα-cofactor in factor Xa (FXa) inhibition. (lu.se)
  • FV-Short and protein S function as synergistic TFPIα-cofactors in inhibition of FXa. (lu.se)
  • The synergistic TFPIα cofactor activity between FV-Short variants and protein S was analyzed by FXa-inhibition. (lu.se)
  • Crystal structures of Eis in complexes with three of the inhibitors showed that the inhibitors were bound in the aminoglycoside binding site of Eis, consistent with the competitive mode of inhibition, as established by kinetics measurements. (cdc.gov)
  • When tested in Mtb cultures, two inhibitors (47 and 55) completely abolished resistance to KAN of the highly KAN-resistant strain Mtb mc(2) 6230 K204, likely due to Eis inhibition as a major mechanism. (cdc.gov)
  • Neuraminidase inhibitors (NAIs) are recommended for the control of severe influenza A and B infections ( 1 ). (cdc.gov)
  • All tested isolates were susceptible to 4 neuraminidase inhibitors (oseltamivir, zanamivir, peramivir and laninamivir). (who.int)
  • Our TMPRSS2-drug structures are made public to guide the design of more potent and specific inhibitors. (rsc.org)
  • One of them, the protease TMPRSS2, is required to activate the viral spike protein (S). Even though two inhibitors, camostat and nafamostat, are known to inhibit TMPRSS2 and block cell entry of SARS-CoV-2, finding further potent therapeutic options is still an important task. (bvsalud.org)
  • PD 0325901 is a potent MKK1 (MEK1) and MKK2 (MEK2) inhibitor. (sigmaaldrich.com)
  • So, the research is focused on identification of the potent plants extracts that exhibit inhibitory activity against PTP1B enzyme. (icbb.com.np)
  • Enzymatic assays were performed using the recombinant form of this protein wich displayed potent inhibitory activity against the cysteine proteinases of S. levis larvae. (usp.br)
  • A structure-activity relationship study of 38 compounds in this structural family yielded highly potent (IC(50) 1M) Eis inhibitors, which did not inhibit other acetyltransferases. (cdc.gov)
  • We discovered that an antipsychotic drug, haloperidol (HPD, 1), was a potent Eis inhibitor with IC(50) = 0.39 0.08 M. We determined the crystal structure of the Eis-haloperidol (1) complex, which guided synthesis of 34 analogues. (cdc.gov)
  • A broad range of reactivities was observed when 13 purified rat cytochrome P450 isozymes were tested for epitope relatedness in a noncompetitive enzyme-linked immunosorbent assay or on immunoblots. (nih.gov)
  • The purified recombinant CHIKV nsP1 has been used for the development of a rapid and sensitive non-radioactive enzyme linked immunosorbent assay (ELISA) to identify the inhibitors of CHIKV nsP1. (tenoeverlab.com)
  • Receptor interacting protein 1 kinase (RIPK1) is a key mediator of not only a process of regulated necrosis, termed necroptosis, but also promotion of caspase-8-dependent apoptosis and pro-inflammatory gene expression 13 . (nature.com)
  • TRIM13-induced NSCLC cell apoptosis was attenuated by a caspase-3 inhibitor Ac-DEVD-CHO, suggesting that TRIM13 induced cell apoptosis partially through a caspase-3-dependent pathway. (cancerindex.org)
  • Carbon nanotube s induce apoptosis resistance through FLICE-inhibitory protein. (cdc.gov)
  • DNA microarray and Western blot analyses of key apoptosis-regulatory proteins in the transformed cells revealed FLICE-inhibitory protein (FLIP) as an important target of regulation by SWCNT. (cdc.gov)
  • Paclitaxel triggers anti-mitotic actions by impeding the cell cycle in the late Everolimus mTOR inhibitor stages of mitosis, backing microtubule formation, and eventually inducing apoptosis. (gp120-inhibitors.com)
  • Furthermore, 5c and 5h were tested for their effects on cell cycle and apoptosis induction capability in HepG2 cell lines by DNA-flow cytometry analysis and annexin V-FITC apoptosis assay, respectively. (dntb.gov.ua)
  • This Human Neuronal apoptosis inhibitory protein (NAIP) ELISA Kit employs a two-site sandwich ELISA to quantitate NAIP in samples. (abbkine.com)
  • Human Neuronal apoptosis inhibitory protein (NAIP) ELISA Kit has high sensitivity and excellent specificity for detection of Human NAIP. (abbkine.com)
  • Neuronal apoptosis inhibitory protein encoded by NAIP contains regions of homology to two baculovirus inhibitor of apoptosis proteins, and it is able to suppress apoptosis induced by various signals. (abbkine.com)
  • The hydroxyl- and superoxide-radical-eliminating ability of water-soluble biosubstances was examined by ESR combined with the spin-trapping method, indicating a median inhibitory dose, ID h 50 (m M ) and id h 50 (mg/mL) for the hydroxyl radical, and ID s 50 (m M ) and id s 50 (mg/mL) for the superoxide radical. (go.jp)
  • In vitro assays confirm that both drugs inhibit the human protein TMPRSS2, a SARS-Cov-2 spike protein activator. (rsc.org)
  • This model is backed by our in vitro experiments and consistent with previous virus cell entry assays. (rsc.org)
  • A trypsin inhibitor assay reveals that Ara h 3 allergen protein has trypsin inhibitory activity. (usda.gov)
  • At the protein level, it is demonstrated that peanut allergen Ara h 3 also has trypsin inhibitory activity. (usda.gov)
  • The results were confirmed using caspase specific inhibitors and caspase activity assays. (cdc.gov)
  • It has been shown that altering any of the proline residues reduces the inhibitory activity to zero. (wikipedia.org)
  • It has also been shown that the compound inhibits Mitochondrial permeability transition pore (MPTP) by inhibiting the activity of the pore regulator, cyclophilin D (CyP-D). CyP-D is a peptidyl-prolyl cis-trans isomerase or protein that causes a proline residue in a peptide to switch from its trans isomer to its cis isomer. (wikipedia.org)
  • The inhibitory effect of CKS-17 is, however, significantly blocked by a protein synthesis inhibitor cycloheximide, indicating that CKS-17 requires de novo protein synthesis to induce the suppressive activity. (duke.edu)
  • The substrate is cell-permeable and serves as the basis for the HDAC Cellular Activity Assay Kit (Prod. (enzolifesciences.com)
  • secretase inhibitor to the membrane would confer inhibitory activity upon it by bringing it to the right compartment. (healthnewstrack.com)
  • COX activity was assayed by prostaglandin (PG)E2 production following 30 min incubation with 5 mM arachidonic acid. (ersjournals.com)
  • Inhibitory activity was established in SARS-CoV-2 viral load systems. (bvsalud.org)
  • Inhibitory activity of A1AT was established in a SARS-CoV-2 viral load system. (bvsalud.org)
  • The amide group certainly plays a significant function in the inhibitory activity of the inhibitors. (idplink.net)
  • The results showed that here was no inhibitory effect of the sugarcane protein leaf extract on the cysteine proteinase activity of the insect larvae. (usp.br)
  • With an ATP regeneration assay we prove that the inhibitory part is indeed due to a decrease in activity because of high allocrite load in the transporter. (unibas.ch)
  • The inhibitory antibodies were then used to assess the role of cytochrome P450h in microsomal benzphetamine N-demethylation, since this isozyme exhibits high catalytic activity for this substrate. (nih.gov)
  • Thus, despite the high level of expression of cytochrome P450h in microsomes from adult male rats and the high catalytic activity of the purified protein for benzphetamine, this isozyme contributes only a small portion of the metabolism of this substrate in microsomes. (nih.gov)
  • Conclusion: The preAR2 region is demonstrated to be crucial for the synergistic TFPIα-cofactor activity between FV-Short and protein S and for the assembly of a trimolecular FXa-inhibitory complex comprising FV-Short, protein S, and TFPIα. (lu.se)
  • The cyclin-dependent kinase (CDK) inhibitors p21 and p16 inhibit the activity of CDKs, such as CDK4. (medscape.com)
  • Among the mAbs, there were significant differences in ability to extract BoNT/B subtypes and inhibitory effect on BoNT catalytic activity. (cdc.gov)
  • Our enzymatic assay demonstrated the IC50 beliefs for JH1C4 are 31.95 nM, 6.60 M, 27.31 nM, and 2.18 M, respectively. (idplink.net)
  • Acknowledgments We give thanks to Jaroslaw Maciejewski from Cleveland Medical clinic for presenting us to PNH as well as for useful conversations, and Shaomeng Wang from School of Michigan for offering equipment to carry out enzymatic and hemolysis assays. (idplink.net)
  • We thank Liu Liu also, Bruce Palfey, and Mou-Chi Cheng for useful discussions over the enzymatic assay. (idplink.net)
  • Endopep-MS currently uses an antibody-affinity concentration/purification step before the enzymatic reaction with the substrate, and the choice of antibody is critical for the success of this assay [ 5 ]. (cdc.gov)
  • The protein induction of autophagy was analyzed by RT-qPCR, western blot, immunofluorescence, and electron microscopy. (frontiersin.org)
  • Treatment effects were assessed using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay, western blot, cell viability, and cell cycle progression. (nih.gov)
  • In the present study, chikungunya virus (CHIKV) nsP1 MTase and GT reactions were confirmed by an indirect non-radioactive colorimetric assay and western blot assay using an antibody specific for the m 7 G cap, respectively. (tenoeverlab.com)
  • Our data provide proof-of principle of a new approach for directing small molecule inhibitors to disease causing RAFT targets in cellular membranes. (healthnewstrack.com)
  • In this work, we report the results of an open science community effort, the "Billion molecules against COVID-19 challenge", to identify small-molecule inhibitors against SARS-CoV-2 or relevant human receptors. (bvsalud.org)
  • A survey of various species by immunoblot analysis with several antibodies revealed little if any epitope relatedness among microsomal proteins from rats, mice, rabbits, hamsters, squirrel monkeys, guinea pigs, or humans. (nih.gov)
  • All of the antibodies were screened as potential inhibitors of cytochrome P450h-mediated testosterone hydroxylation in a reconstituted system. (nih.gov)
  • These inhibitory antibodies gave similar results when benzphetamine N-demethylation was evaluated in the reconstituted system. (nih.gov)
  • Antiphospholipid (APL) antibodies are group of antibodies directed against epitopes on plasma proteins that are uncovered by binding of these proteins to anionic phospholipids on plasma membranes. (medscape.com)
  • To confirm the role of the Gly407Ser mutation, we expressed the recombinant wild-type and Gly407Ser mutant proteins (obtained by PCR-mediated mutagenesis) in 293T cells ( 7 ) and found that Gly407Ser also increased oseltamivir, zanamivir, and peramivir IC 50 levels by 4.16-, 10.07- and 16.36-fold, respectively ( Table ). (cdc.gov)
  • cells were washed inside a buffer consisting of 20 mM Tris/HCl, pH 7.5, supplemented with protease inhibitors (1 mM phenylmethylsulfonyl fluoride, 0.1 mM for 10 min. (bioskinrevive.com)
  • Briefly, bacterial cells were softly suspended in phosphate-buffered saline (PBS), pH 7.4, supplemented with 0.1% (w/v) Triton X-100 and protease inhibitors. (bioskinrevive.com)
  • The remaining pelleted cell body (comprising the inner membrane) was suspended in the same volume of PBS with protease inhibitors, then disrupted by sonication. (bioskinrevive.com)
  • Abstract Synthesis of new anticancer candidates with protein kinases inhibitory potency is a major goal of pharmaceutical science and synthetic research. (dntb.gov.ua)
  • The addition of C 7 /3-phth (100 μM) had no significant effect on the inhibitory potency of SCH-202676. (aspetjournals.org)
  • Multiple steps standard sandwich ELISA assay with a working time of 3-5 hours. (abbkine.com)
  • The developed ELISA nsP1 assay measures this m 7 GMP-nsP1 complex by utilizing anti-m 7 G cap monoclonal antibody. (tenoeverlab.com)
  • Additionally, using the developed ELISA nsP1 assay, the inhibitory effects of sinefungin, aurintricarboxylic acid (ATA) and ribavirin were determined and the IC 50 values were estimated to be 2.69 μM, 5.72 μM and 1.18 mM, respectively. (tenoeverlab.com)
  • Because a bigger quantity of biotinylated protein are required within this assay, recombinant individual aspect D portrayed from Sf9 insect cells was found NMDA-IN-1 in the BLI tests. (idplink.net)
  • demonstrated in vivo TE with TNP-470 which is a covalent inhibitor against methionine aminopeptidase-2 6 . (nature.com)
  • Through Markov modeling, we describe the binding process of both drugs and a metabolic product of camostat (GBPA) to TMPRSS2, reaching a Michaelis complex (MC) state, which precedes the formation of a long-lived covalent inhibitory state. (rsc.org)
  • In this study, treatment of EMT6 mouse mammary tumor cells with hypoxia or the chemical stress agents brefeldin A (BFA) or okadaic acid (OA) causes the development of resistance to the topoisomerase II inhibitor etoposide. (aspetjournals.org)
  • Furthermore, they imply that coadministration of agents that inhibit NF-κB may enhance the efficacy of topoisomerase II inhibitors in clinical cancer chemotherapy. (aspetjournals.org)
  • Effect of safranal on the response of cancer cells to topoisomerase I inhibitors: Does sequence matter? (uaeu.ac.ae)
  • The mechanism of physiological stress-induced drug resistance may involve the activation of stress-responsive proteins and transcription factors. (aspetjournals.org)
  • Pretreatment with the proteasome inhibitor carbobenzyoxyl-leucinyl-leucinyl-leucinal inhibits stress-induced NF-κB activation and reverses BFA-induced drug resistance. (aspetjournals.org)
  • Although topotecan (TPT), a topoisomerase1 inhibitor, is a first- and second-line drug for lung and colon cancers, the development of drug resistance and toxicity still remain as a major obstacle to chemotherapeutic success. (uaeu.ac.ae)
  • Our objectives are to investigate the synergistic effects of GSK-3β in combination with autophagy inhibitors to evade GSK-3β drug resistance. (mdpi.com)
  • Hence, it is anticipated that PP1, PP2 as well as the Lck inhibitor inhibit PTK6. (scienceexhibitions.org)
  • Although PP1 and PP2 are even more selective for SFKs compared to the prior era of PTK inhibitors (including herbimycin A and genistein), they are able to inhibit off-target kinases (including C-terminal Src kinase, ephrin type-A receptor 2, platelet-derived development aspect receptor, fibroblast development aspect receptor 1, p21 turned on kinase, receptor-interacting proteins 2, p38 and casein kinase 1) with enough strength (24C27). (scienceexhibitions.org)
  • Advanced bladder cancer (BC) (local invasive and/or metastatic) is not curable even with cytotoxic chemotherapy, immune checkpoint inhibitors, and targeted treatment. (mdpi.com)
  • Immune checkpoint inhibitors used in treatment of advanced cancers are emerging as one of the important causes for worsening or de novo presentation of MG often associated with myositis and myocarditis and may carry grave prognosis. (medscape.com)
  • Tripartite Motif Containing 13 (TRIM13), a member of TRIM proteins, is deleted in multiple tumor types, especially in B-cell chronic lymphocytic leukemia and multiple myeloma. (cancerindex.org)
  • Scholars@Duke publication: Transcriptional down-regulation of tumor necrosis factor-alpha gene expression by a synthetic peptide homologous to retroviral envelope protein. (duke.edu)
  • Receptor-interacting protein kinase 1 (RIPK1) is a key component of the tumor necrosis factor (TNF) receptor signaling complex that regulates both pro- and anti-apoptotic signaling. (mdpi.com)
  • Proteins tyrosine kinase (PTK)6, also called breasts tumor kinase, is a non-receptor tyrosine kinase. (scienceexhibitions.org)
  • [ 1 ] His prediction was subsequently supported by the cloning of the retinoblastoma tumor suppressor gene ( RB1 ) and by functional studies of the retinoblastoma protein, Rb. (medscape.com)
  • Like Rb protein, many of the proteins encoded by tumor suppressor genes act at specific points in the cell cycle. (medscape.com)
  • Another important class of tumor suppressor genes involved in cell cycle control and in the generation of human cancers is the cyclin-dependent kinase (CDK) inhibitors. (medscape.com)
  • It has been found that altering the 6 and 9 positions in the cyclic peptide ring disables the inhibitory effect on the pore by the drug. (wikipedia.org)
  • We have previously shown that a synthetic peptide (CKS-17) homologous to retroviral envelope protein suppresses the accumulation of superantigen staphylococcal enterotoxin-induced TNF-alpha mRNA in human PBMC and in highly purified human monocytes. (duke.edu)
  • Highly sensitive and convenient alternative to radiolabeled, acetylated histones or peptide/HPLC methods for the assay of histone deacetylases. (enzolifesciences.com)
  • Concentrations as low as 100 nM of the anchored inhibitor were sufficient to completely block appearance of amyloid peptide. (healthnewstrack.com)
  • We performed this study to identify and characterise the inhibitory potential of the latarcin peptide (Ltc 1, SMWSGMWRRKLKKLRNALKKKLKGE) against dengue virus replication in infected cells. (biomedcentral.com)
  • The Ltc 1 peptide showed a significantly inhibitory effect against the dengue protease NS2B-NS3pro at 37°C, a physiological human temperature, (IC 50 , 12.68 ± 3.2 μM), and greater inhibitory effect was observed at 40°C, a temperature similar to a high fever (IC 50 , 6.58 ± 4.1 μM). (biomedcentral.com)
  • The Ltc 1 peptide exhibited significant inhibitory effects against dengue NS2B-NS3pro and virus replication in the infected cells. (biomedcentral.com)
  • This method can detect all seven known BoNT serotypes and involves incubating BoNT with a peptide substrate that mimics each toxin's natural in vivo neuronal protein target. (cdc.gov)
  • This report demonstrates that CETSA can not only quantitatively evaluate the drug-TE in mouse peripheral blood, but also confirm TE in animal tissues exemplified by using the receptor interacting protein 1 kinase (RIPK1) lead compound we have developed. (nature.com)
  • Desk I. PTK6 inhibitory actions of proteins kinase inhibitors screened from a targeted kinase inhibitor. (scienceexhibitions.org)
  • Thiazolidinones 5c and 5h were further evaluated to be kinase inhibitors against EGFR showing effective inhibitory impact. (dntb.gov.ua)
  • Moreover, molecular docking studies by the Moe 2015 program showed better binding patterns for 5c and 5hwith the active site of the EGFR protein kinase [PDB code 1M17]. (dntb.gov.ua)
  • We developed a high-throughput yeast-based assay to screen for chemical inhibitors of Ca(2+)/calmodulin-dependent kinase pathways. (duke.edu)
  • The relative selectivity of COX inhibitors has not been studied in human airway cells. (ersjournals.com)
  • To achieve this goal, maintaining compound concentrations in vivo is a key factor because reversible compounds leave the target protein when the concentration is less than the binding affinity between the compound and the target through the sample preparation processes. (nature.com)
  • The protein concentration was measured using a Pierce BCA Protein Assay kit (Thermo Scientific, Rockford, IL, USA). (bioskinrevive.com)
  • Combinations of concentrations of butyrophenones or control EPI (chlorpromazine) along with ciprofloxacin (CIP) were utilized in checkerboard assays to determine their minimum inhibitory concentration (MIC) and fractional inhibitory concentration (FIC). (confex.com)
  • Intact cell assays of acetylcholine-mediated phosphoinositide hydrolysis in the absence or presence of SCH-202676 revealed a mixed competitive/noncompetitive mode of interaction that was dependent on the concentration of SCH-202676. (aspetjournals.org)
  • Transmembrane serine protease 2 (TMPRSS2) is regarded as one of the main proteases implicated in the coronavirus S protein priming, an important step for binding of the S protein to the angiotensin-converting enzyme 2 (ACE2) receptor before cell entry. (bvsalud.org)
  • The transmembrane semaphorin Sema4D/CD100, an inhibitor of axonal growth, is expressed on oligodendrocytes and upregulated after CNS lesion. (ox.ac.uk)
  • Transmembrane protein 16A (TMEM16A) channels are recently discovered membrane proteins that functions as a calcium activated chloride channel (CaCC). (elsevierpure.com)
  • Histone deacetylases from all known classes have been successfully assayed with the FLUOR DE LYS ® Substrate. (enzolifesciences.com)
  • Sufficient for 100-1000 assays of HDACs or sirtuins (50 µl reaction volume, 50-500 µM (substrate). (enzolifesciences.com)
  • secretase is internalized from the cell membrane into intracellular compartments (endosomes) where it cleaves its substrate, Amyloid Precursor Protein (APP). (healthnewstrack.com)
  • Development of Eis inhibitors as KAN adjuvant therapeutics is an attractive path to forestall and overcome KAN resistance. (cdc.gov)
  • In conclusion, putative peanut trypsin inhibitors have been isolated and reveal high similiarity at the nucleotide and amino acid level to peanut allergen Ara h 3 and Ara h 4. (usda.gov)
  • Assays using protein extracts of transgenic plants were performed to address a putative inhibitory effect of Chagasin onto the cysteine proteinases of S. levis . (usp.br)
  • Structural modeling revealed that A1AT docked to an extracellular domain of TMPRSS2 in a conformation that is suitable for catalysis, resembling similar serine protease inhibitor complexes. (bvsalud.org)
  • The p16INK4A protein is a cell-cycle inhibitor that acts by inhibiting activated cyclin D:CDK4/6 complexes, which play a crucial role in the control of the cell cycle by phosphorylating Rb protein. (medscape.com)
  • As other coronaviruses, 6-9 SARS-CoV-2 exploits host proteins to initiate cell-entry, in particular TMPRSS2 and ACE2, two membrane-bound proteins expressed in the upper and lower respiratory tract. (rsc.org)
  • Semaphorins are a family of secreted and membrane-bound proteins, known to regulate axonal pathfinding. (ox.ac.uk)
  • Studies have been done using the Calcium retention capacity (CRC) assay on mouse liver mitochondria in order to measure antamanide's effect on the permeability transition pore. (wikipedia.org)
  • Rosiglitazone, a PPAR γ agonist, could increase PON2 expression in A10 cells, while the PPAR γ inhibitor prevented the effect of fisetin on PON2. (hindawi.com)
  • The growth inhibitory effect of the proposed combination given in different sequences was assessed using the colony formation assay. (uaeu.ac.ae)
  • The comet assay, cell cycle distribution, Annexin-V staining, and expression of proteins involved in DNA damage/repair were utilized to understand the mechanism underlying the effect of the combination. (uaeu.ac.ae)
  • In the presence of the Shh ligand, PTCH eliminates its inhibitory effect on SMO, which will promote activation of GLI1, its translocation to the nucleus, and thereby stimulation of transcription of its target genes such as GLI1, BCL-2, MYCN, BMI1, CCND2, PTCH1 and HHIP. (scholars.direct)
  • Its inhibitory effect on thyroid hormone production has led to concerns that exposure even to low levels of perchlorate in the environment might affect vulnerable groups, such as pregnant women with inadequate iodine intake and infants for whom thyroid hormone levels must be maintained adequately for normal brain development. (cdc.gov)
  • Botulism is caused by botulinum neurotoxins (BoNTs), extremely toxic proteins which can induce respiratory failure leading to long-term intensive care or death. (cdc.gov)
  • The DNA repair protein methylguanine-DNA methyl transferase (MGMT) confers resistance to temozolomide. (nih.gov)
  • In this study, cultured human temozolomide resistance GB (43RG) cells were introduced to the MGMT inhibitor O 6 -benzylguanine combined with temozolomide and either LY2835219 (CDK 4/6 inhibitor) or LY2157299 (TGF-βRI inhibitor) seeking to overcome GB treatment resistance. (nih.gov)
  • haloperidol, droperidol and spiperone, as NorA efflux pump inhibitors that reverse ciprofloxacin resistance in S. aureus 1199B. (confex.com)
  • Overexpression of the enhanced intracellular survival (Eis) protein by Mtb confers resistance to the second-line antibiotic kanamycin (KAN). Eis is an acetyltransferase that acetylates KAN, inactivating its antimicrobial function. (cdc.gov)
  • Cyclopamine, an inhibitor of the SMO oncogenic protein, and GLI1 siRNA were used as inhibitory agents of the Shh pathway in the two cell lines. (scholars.direct)
  • Peanut trypsin inhibitors play an important role in the plant defense mechanism against insects. (usda.gov)
  • Alphavirus non-structural protein, nsP1 has a distinct molecular mechanism of capping the viral RNAs than the conventional capping mechanism of host. (tenoeverlab.com)
  • Unsurprisingly temozolomide-resistant tumors tend to possess elevated MGMT protein levels or lack inhibitory MGMT promotor methylation. (nih.gov)
  • In the cell lines studied, cyclopamine showed a high inhibitory growth of subcutaneous tumors in the D283 Med and DAOY lines. (scholars.direct)
  • The cellular thermal shift assay (CETSA) has recently been reported to monitor the binding of ligand to its target protein in cells and tissue samples. (nature.com)
  • Within the RNaseA superfamily there is a group of highly cationic proteins secreted by innate immune cells with anti-infective and immune-regulatory properties. (frontiersin.org)
  • A number of COX inhibitors in cultured human airway cells were compared which exclusively express either COX 1 (primary degree cultured human airway smooth muscle (HASM) cells) or COX 2 (A549 pulmonary epithelial cell-line) as measured by Western blotting. (ersjournals.com)
  • HASM cells 92.2+/-12.1 ng PGE2 x mg-1 protein, A549 cells 87.7+/-24.4 ng PGE2 mg-1 protein. (ersjournals.com)
  • In conclusion the present study has shown that cyclo-oxygenase inhibitors have a range of selectivities for cyclo-oxygenase 1 and cyclo-oxygenase 2 in intact human airway cells. (ersjournals.com)
  • This study establishes the groundwork for the development of a combinatorial pharmacologic approach by using either LY2385219 or LY2157299 inhibitor plus O 6 -Benzylguanine to augment temozolomide response in temozolomide-resistant GB cells. (nih.gov)
  • SARS-CoV-2, the cause of the COVID-19 pandemic, exploits host cell proteins for viral entry into human lung cells. (bvsalud.org)
  • SAF enhanced the growth inhibitory effects of TPT particularly when it was added to the cells prior to TPT. (uaeu.ac.ae)
  • For the in vivo assay, for each cell line, each experimental group consisted of 6 mice injected subcutaneously with control cells on the right flank, and cells treated with cyclopamine or GLI1 siRNA on the left flank. (scholars.direct)
  • The Eis inhibitors generally did not exhibit cytotoxicity against mammalian cells. (cdc.gov)
  • The protein encoded by this gene belongs to the pyridine nucleotide-disulfide oxidoreductase family, and is a member of the thioredoxin (Trx) system. (cancerindex.org)
  • What does this gene/protein do? (cancerindex.org)
  • What pathways are this gene/protein implicaed in? (cancerindex.org)
  • Preparation of antiserum to TmpC The gene, encoding the entire TmpC protein, was amplified by PCR from your chromosomal DNA of ATCC 35405 using the primers His-tmpC-F and His-tmpC-R, to which restriction enzyme acknowledgement sites had been appended (Table 1). (bioskinrevive.com)
  • This gene was isolated from Trypanosoma cruzi and its biochemical characterization revealed that the gene product is a strong cysteine proteinase inhibitor. (usp.br)
  • For example, the TP53 gene, located on chromosome 17, encodes a 53-kd nuclear protein that functions as a cell cycle checkpoint. (medscape.com)
  • All tested compounds were modestly metabolically stable in human liver microsomes, exhibiting 30-60% metabolism over the course of the assay. (cdc.gov)
  • The initial velocity decreased at enzyme concentrations higher than 0.13 mg protein per 2.0 ml of incubation mixture. (who.int)
  • Double-labeling experiments with different markers of oligodendrocyte lineage such as olig1, olig2, platelet-derived growth factor receptor alpha, and proteolipid protein showed that Sema4D was expressed selectively by oligodendrocytes and myelin. (ox.ac.uk)
  • Small molecule GSK-3β inhibitors and GSK-3β knockdown using siRNA promote the expression of autophagy-related proteins. (mdpi.com)
  • 10-13 TMPRSS2 contains an extracellular trypsin-like serine-protease domain that can proteolytically activate the spike (S) protein on the surface of SARS-CoV-2 viral particles 14 ( Fig. 1 ). (rsc.org)
  • METHODS: We developed a cell-based assay to identify TMPRSS2 inhibitors. (bvsalud.org)
  • This study evaluated the safety and efficacy of switching HIV-infected patients with stable viral suppression on nonnucleoside reverse transcriptase inhibitor/nucleoside reverse transcriptase inhibitor (NNRTI/NRTI) therapy to lopinavir/ritonavir (LPV/r) monotherapy. (researchgate.net)
  • The host cell furin and the viral NS2B-NS3 serine protease NS2B-NS3pro cleave the viral polyprotein at different positions to release viral structural and non-structural proteins [ 6 - 9 ]. (biomedcentral.com)
  • Participating teams used a wide variety of computational methods to screen a minimum of 1 billion virtual molecules against 6 protein targets. (bvsalud.org)
  • Components and methods Chemical substances PP1, PP2 and these Lck inhibitor had been bought from Calbiochem (EMD Millipore, Billerica, MA, USA). (scienceexhibitions.org)
  • In vivo , BoNT cleaves proteins necessary for nerve signal transmission. (cdc.gov)
  • The obtained results are depicted two-dimensionally, taking id h 50 (mg/mL) as the abscissa and id s 50 (mg/mL) as the ordinate in the ROS inhibitory diagram. (go.jp)
  • The results showed an inhibitory response. (wikipedia.org)
  • The results of luciferase reporter assay revealed that miR-338-3p and G6PC2 were the potential targets of has_circ_0046060. (hindawi.com)
  • These results led us to introduce into the sugarcane genome a new cysteine proteinase inhibitor called Chagasin. (usp.br)
  • All together these results show that butyrophenones are inhibitors of the NorA efflux pump , and its derivatives have potential for treating ciprofloxacin resistant S. aureus infections in combination therapy. (confex.com)
  • Overexpression of Protein tyrosine phosphatase 1B (PTP1B) enzyme is responsible for type 2 diabetes and obesity. (icbb.com.np)
  • Nuclear run-on transcription assays further reveal that CKS-17 suppresses the TNF-alpha mRNA transcription rate. (duke.edu)
  • Electrostatic Energetics of Bacillus subtilis Ribonuclease P Protein Determined by Nuclear Magnetic Resonance-Based Histidine pKa Measurements. (duke.edu)
  • Even though conditional ablation of Mtmr2 in motorneurons in mice did not reveal signs of axonal damage or neuronopathy, a cell autonomous part of Mtmr2 paid down excitatory synapse density and function and it had been suggested that the MTMR2/PSD95 complex contributes to the maintenance of excitatory synapses by suppressing exorbitant endosome formation and harmful Conjugating enzyme inhibitor endosomal traffic to lysosomes. (gp120-inhibitors.com)
  • JH3 and JH1 were contained in the Novartis patent.19 Aspect D extracted from normal human serum bought from Supplement Technology was found in the assay. (idplink.net)
  • The cellular thermal shift assay (CETSA) is expected to facilitate direct measurement of intracellular TE at all stages of drug development. (nature.com)
  • We observed the proteins internalization within macrophages and their capacity to eradicate the intracellular mycobacterial infection at a low micro-molar range. (frontiersin.org)