Genomes and Genes
Summary: An enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.
- Sharma A, Radha Kishan K. Serine protease inhibitor mediated peptide bond re-synthesis in diverse protein molecules. FEBS Lett. 2011;585:3465-70 pubmed publisher..We also investigate the plausible mechanism of such a reaction and demonstrate through biochemical studies and X-ray crystallography that proximity of reacting termini is essential for the feasibility of this reaction. ..
- De Bank P, Kendall D, Alexander S. A spectrophotometric assay for fatty acid amide hydrolase suitable for high-throughput screening. Biochem Pharmacol. 2005;69:1187-93 pubmed..This assay system was also adapted for use in microtiter plates and its ability to detect a known inhibitor of FAAH demonstrated, highlighting its potential for use in high-throughput screening. ..
- Crichlow G, Lubetsky J, Leng L, Bucala R, Lolis E. Structural and kinetic analyses of macrophage migration inhibitory factor active site interactions. Biochemistry. 2009;48:132-9 pubmed publisher..We also find that the commonly used protease inhibitor, phenylmethylsulfonyl fluoride (PMSF), forms a covalent complex with MIF and inhibits the tautomerase activity...
- Jewell C, Ackermann C, Payne N, Fate G, Voorman R, Williams F. Specificity of procaine and ester hydrolysis by human, minipig, and rat skin and liver. Drug Metab Dispos. 2007;35:2015-22 pubmed..Rat skin and liver esterase activity was inhibited additionally by phenylmethylsulfonyl fluoride and the arylesterase inhibitor mercuric chloride, indicating a different esterase profile...
- Gaudin P, Berthier S, Barro C, Zaoui P, Morel F. Proteolytic potential of human neutrophil membranes. Eur J Cell Biol. 1997;72:345-51 pubmed..of phorbol 12-myristate 13-acetate (PMA), in a dose-dependent manner, and was partially sensitive to phenylmethylsulfonyl fluoride treatment. The effect was abolished by the addition of 1 M KCl or 0.05% Brij 35 extraction...
- Li F, Yang L, Lv X, Liu D, Xia H, Chen S. Purification and characterization of a novel extracellular alkaline protease from Cellulomonas bogoriensis. Protein Expr Purif. 2016;121:125-32 pubmed publisher..Irreversible inhibition of the enzyme activity by phenylmethylsulfonyl fluoride and tosyl-l-phenylalanine chloromethyl ketone demonstrated that the purified enzyme is a chymotrypsin ..
- Yuan L, Jian W, Zhang D, Aubry A, Arnold M. Application of a stabilizer cocktail of N-ethylmaleimide and phenylmethanesulfonyl fluoride to concurrently stabilize the disulfide and ester containing compounds in a plasma LC-MS/MS assay. J Pharm Biomed Anal. 2014;88:552-61 pubmed publisher..The validated method was successfully applied to sample analysis in Phase I clinical studies. ..
- Lu J, Xu H, Chen F, Huang Y, Lu N. Standardization and quality control for the determination of alpha-glucosidase in seminal plasma. Arch Androl. 2006;52:447-53 pubmed..001). An additional 6 samples of seminal plasma with or without phenylmethylsulfonyl fluoride (PMSF), obtained at 3000 g for 15 min centrifugation, were frozen for 20 days, and each of 6 samples ..
- Oz M, Jaligam V, Galadari S, Petroianu G, Shuba Y, Shippenberg T. The endogenous cannabinoid, anandamide, inhibits dopamine transporter function by a receptor-independent mechanism. J Neurochem. 2010;112:1454-64 pubmed publisher..The amidohydrolase inhibitor, phenylmethylsulfonyl fluoride (0.2 mM), failed to alter the AEA-evoked inhibition of ASP(+) accumulation...
- Fujiyama N, Miura M, Satoh S, Inoue K, Kagaya H, Saito M, et al. Influence of carboxylesterase 2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Xenobiotica. 2009;39:407-14 pubmed publisher..In conclusion, the study demonstrated that while CES1 and/or CES2 are involved in the hydrolysis of MMF to MPA, CES2 allelic variants appeared to make only a minor contribution to inter-personal differences in MPA pharmacokinetics. ..
- Burster T, Beck A, Poeschel S, Øren A, Baechle D, Reich M, et al. Interferon-gamma regulates cathepsin G activity in microglia-derived lysosomes and controls the proteolytic processing of myelin basic protein in vitro. Immunology. 2007;121:82-93 pubmed..Thus, the cytokine environment modulates lysosomal proteases in microglia by a selective down-regulation of CatG, leading to decreased MBP-processing by microglia-derived lysosomal proteases in vitro. ..
- Wiley J, Dewey M, Jefferson R, Winckler R, Bridgen D, Willoughby K, et al. Influence of phenylmethylsulfonyl fluoride on anandamide brain levels and pharmacological effects. Life Sci. 2000;67:1573-83 pubmed..These results further suggest that metabolite contribution to anandamide's effects, if any, would occur primarily at later times. ..
- McGrath M, Mirzadegan T, Schmidt B. Crystal structure of phenylmethanesulfonyl fluoride-treated human chymase at 1.9 A. Biochemistry. 1997;36:14318-24 pubmed..Moreover, the cationic nature of S1' provides a structural basis for human chymase's poor catalytic efficiency when angiotensin II is the substrate. ..
- Dawkins R, Keller S, Sewell W. Pharmacology of acetylcholine-mediated cell signaling in the lateral line organ following efferent stimulation. J Neurophysiol. 2005;93:2541-51 pubmed..The effect of apamin was not enhanced by co-administration of phenylmethylsulfonyl fluoride, a proteolysis inhibitor...
- Jiang X, Chen L, Xu J, Yang Q. Molecular mechanism analysis of Gloydius shedaoensis venom gloshedobin interaction with inhibitors by homology modeling. Int J Biol Macromol. 2011;48:129-33 pubmed publisher..The analysis indicated that the strongest inhibitor, PMSF, was via a covalent bond with the catalytic Ser195, while other inhibitors showing weaker inhibitory activity were via hydrogen bond with Ser195 or non-catalytic residues. ..
- Aguilar B, Amissah F, Duverna R, Lamango N. Polyisoprenylation potentiates the inhibition of polyisoprenylated methylated protein methyl esterase and the cell degenerative effects of sulfonyl fluorides. Curr Cancer Drug Targets. 2011;11:752-62 pubmed..Its susceptibility to the nonspecific serine hydrolase inhibitor, phenylmethylsulfonyl fluoride (PMSF) paved the way for its use as a prototypical compound to design and synthesize a series of ..
- Sawada T, Hashimoto S, Tohma S, Nishioka Y, Nagai T, Sato T, et al. Inhibition of L-leucine methyl ester mediated killing of THP-1, a human monocytic cell line, by a new anti-inflammatory drug, T614. Immunopharmacology. 2000;49:285-94 pubmed..Based on the similarity of T614 and PMSF, we suggest that, besides their roles as COX-2 inhibitors, T614 and other mNSAIDs may act as lysosomal protease inhibitors. ..
- Silva Jardim I, Horta M, Ramalho Pinto F. The Leishmania chagasi proteasome: role in promastigotes growth and amastigotes survival within murine macrophages. Acta Trop. 2004;91:121-30 pubmed..These results demonstrate that intact parasite proteasome function is required for replication of L. chagasi and for amastigotes survival inside the vertebrate host cell. ..
- Li A, Xie C, Zhang J, Zhang J, Li D. Cloning, expression, and characterization of serine protease from thermophilic fungus Thermoascus aurantiacus var. levisporus. J Microbiol. 2011;49:121-9 pubmed publisher..The protease activity was found to be inhibited by PMSF, but not by DTT or EDTA. The enzyme has broad substrate specificity such as gelatin, casein and pure milk, and exhibiting highest activity towards casein. ..
- Singhal S, Singhal J, Cheng J, Pikuła S, Sharma R, Zimniak P, et al. Purification and functional reconstitution of intact ral-binding Gtpase activating protein, RLIP76, in artificial liposomes. Acta Biochim Pol. 2001;48:551-62 pubmed
- Sethi B, Nanda P, Sahoo S. Characterization of biotechnologically relevant extracellular lipase produced by Aspergillus terreus NCFT 4269.10. Braz J Microbiol. 2016;47:143-9 pubmed publisher..b>Phenylmethylsulfonyl fluoride (1mM) and the reducing, Î²-mercaptoethanol significantly inhibited lipase activity...
- Jones D, Cummings J, Langdon S, MacLellan A, Higgins T, Rozengurt E, et al. Metabolism of the broad-spectrum neuropeptide growth factor antagonist: [D-Arg1, D-Phe5, D-Trp7,9, Leu11]-substance P. Br J Cancer. 1996;73:715-20 pubmed..These results provide some of the first structure-activity information on the factors that determine which neuropeptides these compounds inhibit and on the relative potency of that inhibition. ..
- Negrel J, Javelle F, Morandi D. Detection of a plant enzyme exhibiting chlorogenate-dependant caffeoyltransferase activity in methanolic extracts of arbuscular mycorrhizal tomato roots. Plant Physiol Biochem. 2013;66:77-83 pubmed publisher..Surprisingly this caffeoyltransferase activity could also be detected in hydro-alcoholic extracts of G. intraradices-colonised roots of leek, sorghum or barrel medic. ..
- Hammami A, Hamdi M, Abdelhedi O, Jridi M, Nasri M, Bayoudh A. Surfactant- and oxidant-stable alkaline proteases from Bacillus invictae: Characterization and potential applications in chitin extraction and as a detergent additive. Int J Biol Macromol. 2017;96:272-281 pubmed publisher..0 to 11.0. At least six clear caseinolytic protease bands were observed in a zymogram. Phenylmethylsulfonyl fluoride (PMSF), a serine-protease inhibitor, was found to inhibit completely the protease activity...
- D Ávila Levy C, Volotão A, Araújo F, De Jesus J, Motta M, Vermelho A, et al. Bodo sp., a free-living flagellate, expresses divergent proteolytic activities from the closely related parasitic trypanosomatids. J Eukaryot Microbiol. 2009;56:454-8 pubmed publisher..All these enzymes belong to the serine peptidase class, based on inhibition by aprotinin and phenylmethylsulfonyl fluoride. This is the first biochemical characterization of peptidases in a free-living Bodo sp...
- Alizadeh Khiavi K, Ali Khan Z. Biochemical nature and cellular origin of amyloid enhancing factor (AEF) as determined by anti-AEF antibody. Br J Exp Pathol. 1988;69:605-19 pubmed..The role of lysosomal proteases and anti-AEF antibody which has been successfully generated for the first time is discussed with reference to the origin of AEF and its presumed biological function in amyloidogenesis. ..
- Zhou W, Scott S, Shelton S, Crutcher K. Cathepsin D-mediated proteolysis of apolipoprotein E: possible role in Alzheimer's disease. Neuroscience. 2006;143:689-701 pubmed..These results suggest that aspartic proteases, catD in particular, may be involved in proteolysis of apoE and perhaps contribute to the generation of apoE fragments previously implicated in AD pathology. ..
- Sessa W, Kaw S, Hecker M, Vane J. The biosynthesis of endothelin-1 by human polymorphonuclear leukocytes. Biochem Biophys Res Commun. 1991;174:613-8 pubmed..These findings indicate that human PMNs contain and/or release neutral proteases, which can both rapidly produce and degrade ET-1, an observation which may have important (patho)physiologic implications. ..
- Marshall J, Kupchak P, Zhu W, Yantha J, Vrees T, Furesz S, et al. Processing of serum proteins underlies the mass spectral fingerprinting of myocardial infarction. J Proteome Res. 2003;2:361-72 pubmed..Time course and inhibitor studies demonstrated that the peptide patterns in the serum reflect the balance of disease-specific-protease and aminopeptidase activity ex vivo. ..
- Fasia L, Karava V, Siafaka Kapadai A. Uptake and metabolism of [3H]anandamide by rabbit platelets. Lack of transporter?. Eur J Biochem. 2003;270:3498-506 pubmed..In conclusion, anandamide is rapidly taken up by rabbit platelets and metabolized mainly into water-soluble metabolites. Interestingly, the present study also suggests the absence of a transporter for anandamide in these cells. ..
- Yang X, Pu F, Chen C, Ren J, Qu X. An enzyme-responsive nanocontainer as an intelligent signal-amplification platform for a multiple proteases assay. Chem Commun (Camb). 2012;48:11133-5 pubmed publisher..Based on selective pore-opening in the presence of protease, we have developed a novel signal amplification assay for multiple proteases detection and their inhibition using protein-capped mesoporous scaffolding as the substrate. ..
- Hanzon J, Smirnoff P, Applebaum S, Mattoo A, Birk Y. Thiol-activated serine proteinases from nymphal hemolymph of the African migratory locust, Locusta migratoria migratorioides. Arch Biochem Biophys. 2003;410:83-8 pubmed..The locust trypsins LmHP-1 and LmHP-2 constitute a new category of serine proteases wherein the active site of the enzyme is exposed by thiol activation without cleavage of peptide bonds. ..
- Levine L. Amplification of arachidonic acid metabolism in rat liver cells (the C-9 cell-line) by tosyl-L-phenylalanine chloromethyl ketone and phenylmethyl-sulfonyl fluoride. Prostaglandins. 1995;50:89-101 pubmed..While phenylmethyl-sulfonyl fluoride's amplification of PGI2 production by cells treated with TPA was blocked by prior incubation with TPA for 20 h, a similar block of amplification in EGF-treated cells was not observed. ..
- Castillo Yáñez F, Pacheco Aguilar R, García Carreño F, Navarrete del Toro M. Isolation and characterization of trypsin from pyloric caeca of Monterey sardine Sardinops sagax caerulea. Comp Biochem Physiol B Biochem Mol Biol. 2005;140:91-8 pubmed..General characteristics of the Monterey sardine trypsin resemble those of trypsins from other fish, especially trypsins from the anchovy Engraulis japonica and Engraulis encrasicholus and the sardine Sardinops melanostica. ..
- Cha W, Park S, Kim S, Choi D. Biochemical and enzymatic properties of a fibrinolytic enzyme from Pleurotus eryngii cultivated under solid-state conditions using corn cob. Bioresour Technol. 2010;101:6475-81 pubmed publisher..18 mM and 53.5 U/ml, respectively. The enzyme was completely inhibited by 1.0 mM phenylmethylsulfonyl fluoride (PMSF). The N-terminal sequence was A-M-D-S-Q-T-D-A-S-Y-G-LA-N-D...
- Goller S, Schoisswohl D, Baron M, Parriche M, Kubicek C. Role of endoproteolytic dibasic proprotein processing in maturation of secretory proteins in Trichoderma reesei. Appl Environ Microbiol. 1998;64:3202-8 pubmed..These data point to the existence of different endoproteolytic proprotein processing enzymes in T. reesei and demonstrate that dibasic processing is obligatory for the secretion of the proproteins containing this target. ..
- Ross R, Gibson T, Brockie H, Leslie M, Pashmi G, Craib S, et al. Structure-activity relationship for the endogenous cannabinoid, anandamide, and certain of its analogues at vanilloid receptors in transfected cells and vas deferens. Br J Pharmacol. 2001;132:631-40 pubmed..In the mouse vas deferens, which seems to express vanilloid and CB(1) receptors, both receptor types appear to contribute to anandamide-induced inhibition of evoked contractions. ..
- De Vendittis E, Ursby T, Rullo R, Gogliettino M, Masullo M, Bocchini V. Phenylmethanesulfonyl fluoride inactivates an archaeal superoxide dismutase by chemical modification of a specific tyrosine residue. Cloning, sequencing and expression of the gene coding for Sulfolobus solfataricus superoxide dismutase. Eur J Biochem. 2001;268:1794-801 pubmed..The covalent modification caused by PhCH2SO2F reinforced the heat stability of SsSOD. These results show that Tyr41 plays an important role in the enzyme activity and the maintenance of the structural architecture of SsSOD. ..
- Khosravi J, Diamandi A, Bodani U, Khaja N, Krishna R. Pitfalls of immunoassay and sample for IGF-I: comparison of different assay methodologies using various fresh and stored serum samples. Clin Biochem. 2005;38:659-66 pubmed..In such cases, underestimation of the in vivo levels by the intact assays would occur, but the findings of low IGF-I levels may be indicative of questionable sample quality. ..
- Samra Z, Shabir S, Rahmat Z, Zaman M, Nazir A, Dar N, et al. Synthesis of cholesterol-conjugated magnetic nanoparticles for purification of human paraoxonase 1. Appl Biochem Biotechnol. 2010;162:671-86 pubmed publisher..Mg(+2), Mn(+2), glycerol, (NH(4))(2)SO(4), PEG 6000, Triton X-100, and phenylmethylsulfonyl fluoride did not show any effect on activity...
- Song F, Yan Y, Zhao X, Dou D, Zhang C, Xie K. Phenylmethylsulfonyl fluoride protects against the degradation of neurofilaments in tri-ortho-cresyl phosphate (TOCP) induced delayed neuropathy. Toxicology. 2009;262:258-64 pubmed publisher..of TOCP administration on NF content and NF degradation when OPIDN is blocked by pretreatment with phenylmethylsulfonyl fluoride (PMSF)...
- Gaur R, Sangwan A, Sangwan N, Ghosh M, Kumar S. Comparative study of esterases in deltamethrin and diazinon resistant Rhipicephalus microplus and Hyalomma anatolicum ticks collected from the Trans-Gangetic plains of India. Exp Appl Acarol. 2017;73:115-127 pubmed publisher..Inhibition studies with eserine sulfate, p-chloromercuribenzoate, copper sulphate and phenylmethylsulfonyl fluoride revealed a marked variation in band intensity between susceptible and resistant ticks, with the latter ..
- Huszar G, Celik Ozenci C, Cayli S, Kovacs T, Vigue L, Kovanci E. Semen characteristics after overnight shipping: preservation of sperm concentrations, HspA2 ratios, CK activity, cytoplasmic retention, chromatin maturity, DNA integrity, and sperm shape. J Androl. 2004;25:593-604 pubmed..Home collection of semen should enhance study participation, and semen assessment in centralized laboratories will address concerns regarding interlaboratory variations and quality control. ..
- Hoover C, Ng C, Felton J. Correlation of haemagglutination activity with trypsin-like protease activity of Porphyromonas gingivalis. Arch Oral Biol. 1992;37:515-20 pubmed..These results suggest that the proteolytic site of the trypsin-like protease participates in haemagglutination activity of P. gingivalis. ..
- McPherson P, Young I, McEneny J. A dual role for lecithin:cholesterol acyltransferase (EC 188.8.131.52) in lipoprotein oxidation. Free Radic Biol Med. 2007;43:1484-93 pubmed..Thus, we have demonstrated that the high-density lipoprotein-associated enzyme LCAT may have a significant role to play in lipoprotein modification and hence atherogenesis. ..
- Souza A, Gerlach R, Line S. Inhibition of human gelatinases by metals released from dental amalgam. Biomaterials. 2001;22:2025-30 pubmed..These findings suggest that the activity of oral tissue MMPs may be modulated by metal ions released from dental amalgam. ..
- Tasteyre A, Barc M, Karjalainen T, Bourlioux P, Collignon A. Inhibition of in vitro cell adherence of Clostridium difficile by Saccharomyces boulardii. Microb Pathog. 2002;32:219-25 pubmed..These results suggest that the yeast could inhibit adherence of C. difficile to cells thanks to its proteolytic activity but also through steric hindrance. ..
- Fowler C, Borjesson M, Tiger G. Differences in the pharmacological properties of rat and chicken brain fatty acid amidohydrolase. Br J Pharmacol. 2000;131:498-504 pubmed..Chicken FAAH was less sensitive to indomethacin than its rodent counterpart, but the inhibition was also competitive (K(i)). It is concluded that chicken FAAH activity has different pharmacological properties to its rodent counterpart. ..
- Kostellow A, Ma G, Morrill G. The first product of phospholipid N-methylation, phosphatidylmonomethylethanolamine, is a lipid mediator for progesterone action at the amphibian oocyte plasma membrane. Steroids. 2001;66:849-56 pubmed
- Wojtczak M, Ciereszko A. Improvement of electrophoretic detection of antitrypsin activity in fish blood and seminal plasma. Electrophoresis. 2005;26:514-6 pubmed..We report a modification of this method based on inhibition of esterases in samples by phenylmethylsulfonyl fluoride (PMSF)...