Amino acid chloromethyl ketones. Medical search

Inhibitors of SERINE ENDOPEPTIDASES and sulfhydryl group-containing enzymes. They act as alkylating agents and are known to interfere in the translation process.

An inhibitor of SERINE ENDOPEPTIDASES. Acts as an alkylating agent and is known to interfere with the translation process.

An inhibitor of Serine Endopeptidases. Acts as alkylating agent and is known to interfere with the translation process.

A substance that is an irritant to the eyes and respiratory tract and may be carcinogenic.

Compounds which inhibit or antagonize biosynthesis or actions of proteases (ENDOPEPTIDASES).

Exogenous or endogenous compounds which inhibit SERINE ENDOPEPTIDASES.

The metabolic substances ACETONE; 3-HYDROXYBUTYRIC ACID; and acetoacetic acid (ACETOACETATES). They are produced in the liver and kidney during FATTY ACIDS oxidation and used as a source of energy by the heart, muscle and brain.

A di-isopropyl-fluorophosphate which is an irreversible cholinesterase inhibitor used to investigate the NERVOUS SYSTEM.

Organic compounds that generally contain an amino (-NH2) and a carboxyl (-COOH) group. Twenty alpha-amino acids are the subunits which are polymerized to form proteins.

Chemical compounds derived from acids by the elimination of a molecule of water.

Hydrolases that specifically cleave the peptide bonds found in PROTEINS and PEPTIDES. Examples of sub-subclasses for this group include EXOPEPTIDASES and ENDOPEPTIDASES.

A very strong halogenated derivative of acetic acid. It is used in acid catalyzed reactions, especially those where an ester is cleaved in peptide synthesis.

Compounds that contain a 1-dimethylaminonaphthalene-5-sulfonyl group.

Derivatives of acetic acid with one or more fluorines attached. They are almost odorless, difficult to detect chemically, and very stable. The acid itself, as well as the derivatives that are broken down in the body to the acid, are highly toxic substances, behaving as convulsant poisons with a delayed action. (From Miall's Dictionary of Chemistry, 5th ed)

Any member of the group of ENDOPEPTIDASES containing at the active site a serine residue involved in catalysis.

The rate dynamics in chemical or physical systems.

The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.

An enzyme that catalyzes the release of a N-terminal pyroglutamyl group from a polypeptide provided the next residue is not proline. It is inhibited by thiol-blocking reagents and occurs in mammalian tissues, microorganisms, and plants. (From Enzyme Nomenclature, 1992) EC 3.4.19.3.

A protease of broad specificity, obtained from dried pancreas. Molecular weight is approximately 25,000. The enzyme breaks down elastin, the specific protein of elastic fibers, and digests other proteins such as fibrin, hemoglobin, and albumin. EC 3.4.21.36.

The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.

A subclass of PEPTIDE HYDROLASES that catalyze the internal cleavage of PEPTIDES or PROTEINS.

An organic mercurial used as a sulfhydryl reagent.

A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.

The sum of the weight of all the atoms in a molecule.

The parts of a macromolecule that directly participate in its specific combination with another molecule.

A serine endopeptidase secreted by the pancreas as its zymogen, CHYMOTRYPSINOGEN and carried in the pancreatic juice to the duodenum where it is activated by TRYPSIN. It selectively cleaves aromatic amino acids on the carboxyl side.

Serine proteinase inhibitors which inhibit trypsin. They may be endogenous or exogenous compounds.

ENDOPEPTIDASES which have a cysteine involved in the catalytic process. This group of enzymes is inactivated by CYSTEINE PROTEINASE INHIBITORS such as CYSTATINS and SULFHYDRYL REAGENTS.

Electrophoresis in which a polyacrylamide gel is used as the diffusion medium.

A genus of microorganisms of the order SPIROCHAETALES, many of which are pathogenic and parasitic for man and animals.

The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH = log 1/2[1/(H+)], where (H+) is the hydrogen ion concentration in gram equivalents per liter of solution. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)

Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.

The naturally occurring or experimentally induced replacement of one or more AMINO ACIDS in a protein with another. If a functionally equivalent amino acid is substituted, the protein may retain wild-type activity. Substitution may also diminish, enhance, or eliminate protein function. Experimentally induced substitution is often used to study enzyme activities and binding site properties.

A group of acylated oligopeptides produced by Actinomycetes that function as protease inhibitors. They have been known to inhibit to varying degrees trypsin, plasmin, KALLIKREINS, papain and the cathepsins.

An enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.

Physiologically inactive substances that can be converted to active enzymes.

Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.

The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.

An enzyme formed from PROTHROMBIN that converts FIBRINOGEN to FIBRIN.

A species of gram-negative, anaerobic, rod-shaped bacteria originally classified within the BACTEROIDES genus. This bacterium produces a cell-bound, oxygen-sensitive collagenase and is isolated from the human mouth.

The process of cleaving a chemical compound by the addition of a molecule of water.

The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.

A serine endopeptidase that is formed from TRYPSINOGEN in the pancreas. It is converted into its active form by ENTEROPEPTIDASE in the small intestine. It catalyzes hydrolysis of the carboxyl group of either arginine or lysine. EC 3.4.21.4.

Analogs of those substrates or compounds which bind naturally at the active sites of proteins, enzymes, antibodies, steroids, or physiological receptors. These analogs form a stable covalent bond at the binding site, thereby acting as inhibitors of the proteins or steroids.

Established cell cultures that have the potential to propagate indefinitely.

Exogenous and endogenous compounds which inhibit CYSTEINE ENDOPEPTIDASES.

A thiol-containing non-essential amino acid that is oxidized to form CYSTINE.

Peptides composed of between two and twelve amino acids.

Antibiotic substance isolated from streptomycin-producing strains of Streptomyces griseus. It acts by inhibiting elongation during protein synthesis.

A genus of gram-negative, anaerobic, rod-shaped bacteria. Its organisms are normal inhabitants of the oral, respiratory, intestinal, and urogenital cavities of humans, animals, and insects. Some species may be pathogenic.

Ubiquitous, inducible, nuclear transcriptional activator that binds to enhancer elements in many different cell types and is activated by pathogenic stimuli. The NF-kappa B complex is a heterodimer composed of two DNA-binding subunits: NF-kappa B1 and relA.

Amino acids that are not synthesized by the human body in amounts sufficient to carry out physiological functions. They are obtained from dietary foodstuffs.

Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.

An industrial solvent which causes nervous system degeneration. MBK is an acronym often used to refer to it.

Cellular proteins and protein complexes that transport amino acids across biological membranes.

Salts and derivatives of acetoacetic acid.

The arrangement of two or more amino acid or base sequences from an organism or organisms in such a way as to align areas of the sequences sharing common properties. The degree of relatedness or homology between the sequences is predicted computationally or statistically based on weights assigned to the elements aligned between the sequences. This in turn can serve as a potential indicator of the genetic relatedness between the organisms.

BUTYRIC ACID substituted in the beta or 3 position. It is one of the ketone bodies produced in the liver.

Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.

Agents that emit light after excitation by light. The wave length of the emitted light is usually longer than that of the incident light. Fluorochromes are substances that cause fluorescence in other substances, i.e., dyes used to mark or label other compounds with fluorescent tags.

The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.

Commonly observed structural components of proteins formed by simple combinations of adjacent secondary structures. A commonly observed structure may be composed of a CONSERVED SEQUENCE which can be represented by a CONSENSUS SEQUENCE.

Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.

The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).

A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.

Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.

Activation of stress-activated protein kinase/c-Jun NH2-terminal kinase and p38 kinase in calphostin C-induced apoptosis requires caspase-3-like proteases but is dispensable for cell death. (1/1161)

Apoptosis was induced in human glioma cell lines by exposure to 100 nM calphostin C, a specific inhibitor of protein kinase C. Calphostin C-induced apoptosis was associated with synchronous down-regulation of Bcl-2 and Bcl-xL as well as activation of caspase-3 but not caspase-1. The exposure to calphostin C led to activation of stress-activated protein kinase/c-Jun NH2-terminal kinase (SAPK/JNK) and p38 kinase and concurrent inhibition of extracellular signal-regulated kinase (ERK). Upstream of ERK, Shc was shown to be activated, but its downstream Raf1 and ERK were inhibited. The pretreatment with acetyl-Tyr-Val-Ala-Asp-aldehyde, a relatively selective inhibitor of caspase-3, or benzyloxycarbonyl-Val-Ala-Asp-fluoromethylketone (z-VAD.fmk), a broad spectrum caspase inhibitor, similarly inhibited calphostin C-induced activation of SAPK/JNK and p38 kinase as well as apoptotic nuclear damages (chromatin condensation and DNA fragmentation) and cell shrinkage, suggesting that caspase-3 functions upstream of SAPK/JNK and p38 kinase, but did not block calphostin C-induced surface blebbing and cell death. On the other hand, the inhibition of SAPK/JNK by transfection of dominant negative SAPK/JNK and that of p38 kinase by SB203580 induced similar effects on the calphostin C-induced apoptotic phenotypes and cell death as did z-VAD.fmk and acetyl-Tyr-Val-Ala-Asp-aldehyde, but the calphostin C-induced PARP cleavage was not changed, suggesting that SAPK/JNK and p38 kinase are involved in the DNA fragmentation pathway downstream of caspase-3. The present findings suggest, therefore, that the activation of SAPK/JNK and p38 kinase is dispensable for calphostin C-mediated and z-VAD.fmk-resistant cell death. (+info)

Role of hypoxia-induced Bax translocation and cytochrome c release in reoxygenation injury. (2/1161)

We investigated mechanisms of cell death during hypoxia/reoxygenation of cultured kidney cells. During glucose-free hypoxia, cell ATP levels declined steeply resulting in the translocation of Bax from cytosol to mitochondria. Concurrently, there was cytochrome c release and caspase activation. Cells that leaked cytochrome c underwent apoptosis after reoxygenation. ATP depletion induced by a mitochondrial uncoupler resulted in similar alterations even in the presence of oxygen. Moreover, inclusion of glucose during hypoxia prevented protein translocations and reoxygenation injury by maintaining intracellular ATP. Thus, ATP depletion, rather than hypoxia per se, was the cause of protein translocations. Overexpression of Bcl-2 prevented cytochrome c release and reoxygenation injury without ameliorating ATP depletion or Bax translocation. On the other hand, caspase inhibitors did not prevent protein translocations, but inhibited apoptosis during reoxygenation. Nevertheless, they could not confer long-term viability, since mitochondria had been damaged. Omission of glucose during reoxygenation resulted in continued failure of ATP production, and cell death with necrotic morphology. In contrast, cells expressing Bcl-2 had functional mitochondria and remained viable during reoxygenation even without glucose. Therefore, Bax translocation during hypoxia is a molecular trigger for cell death during reoxygenation. If ATP is available during reoxygenation, apoptosis develops; otherwise, death occurs by necrosis. By preserving mitochondrial integrity, BCL-2 prevents both forms of cell death and ensures cell viability. (+info)

Anti-apoptotic role of telomerase in pheochromocytoma cells. (3/1161)

Telomerase is a protein-RNA enzyme complex that adds a six-base DNA sequence (TTAGGG) to the ends of chromosomes and thereby prevents their shortening. Reduced telomerase activity is associated with cell differentiation and accelerated cellular senescence, whereas increased telomerase activity is associated with cell transformation and immortalization. Because many types of cancer have been associated with reduced apoptosis, whereas cell differentiation and senescence have been associated with increased apoptosis, we tested the hypothesis that telomerase activity is mechanistically involved in the regulation of apoptosis. Levels of telomerase activity in cultured pheochromocytoma cells decreased prior to cell death in cells undergoing apoptosis. Treatment of cells with the oligodeoxynucleotide TTAGGG or with 3,3'-diethyloxadicarbocyanine, agents that inhibit telomerase activity in a concentration-dependent manner, significantly enhanced mitochondrial dysfunction and apoptosis induced by staurosporine, Fe2+ (an oxidative insult), and amyloid beta-peptide (a cytotoxic peptide linked to neuronal apoptosis in Alzheimer's disease). Overexpression of Bcl-2 and the caspase inhibitor zVAD-fmk protected cells against apoptosis in the presence of telomerase inhibitors, suggesting a site of action of telomerase prior to caspase activation and mitochondrial dysfunction. Telomerase activity decreased in cells during the process of nerve growth factor-induced differentiation, and such differentiated cells exhibited increased sensitivity to apoptosis. Our data establish a role for telomerase in suppressing apoptotic signaling cascades and suggest a mechanism whereby telomerase may suppress cellular senescence and promote tumor formation. (+info)

Monocytic cell necrosis is mediated by potassium depletion and caspase-like proteases. (4/1161)

Apoptosis is a physiological cell death that culminates in mitochondrial permeability transition and the activation of caspases, a family of cysteine proteases. Necrosis, in contrast, is a pathological cell death characterized by swelling of the cytoplasm and mitochondria and rapid plasma membrane disruption. Necrotic cell death has long been opposed to apoptosis, but it now appears that both pathways involve mitochondrial permeability transition, raising the question of what mediates necrotic cell death. In this study, we investigated mechanisms that promote necrosis induced by various stimuli (Clostridium difficile toxins, Staphylococcus aureus alpha toxin, ouabain, nigericin) in THP-1 cells, a human monocytic cell line, and in monocytes. All stimuli induced typical features of necrosis and triggered protease-mediated release of interleukin-1beta (IL-1beta) and CD14 in both cell types. K+ depletion was actively implicated in necrosis because substituting K+ for Na+ in the extracellular medium prevented morphological features of necrosis and IL-1beta release. N-benzyloxycarbonyl-Val-Ala-Asp-fluoromethyl ketone, a broad-spectrum caspase inhibitor, prevented morphological features of necrosis, plasma membrane destruction, loss of mitochondrial membrane potential, IL-1beta release, and CD14 shedding induced by all stimuli. Thus, in monocytic cells, necrosis is a cell death pathway mediated by passive K+ efflux and activation of caspase-like proteases. (+info)

Identification of megalin/gp330 as a receptor for lipoprotein(a) in vitro. (5/1161)

Lipoprotein(a) [Lp(a)] is an atherogenic lipoprotein of unknown physiological function. The mechanism of Lp(a) atherogenicity as well as its catabolic pathways are only incompletely understood at present. In this report, we show that the low density lipoprotein receptor (LDLR) gene family member megalin/glycoprotein (gp) 330 is capable of binding and mediating the cellular uptake and degradation of Lp(a) in vitro. A mouse embryonic yolk sac cell line with native expression of megalin/gp330 but genetically deficient in LDLR-related protein (LRP) and a control cell line carrying a double knockout for both LRP and megalin/gp330 were compared with regard to their ability to bind, internalize, and degrade dioctadecyltetramethylindocarbocyanine perchlorate (DiI)-fluorescence-labeled Lp(a) as well as equimolar amounts of 125I-labeled Lp(a) and LDL. Uptake and degradation of radiolabeled Lp(a) by the megalin/gp330-expressing cells were, on average, 2-fold higher than that of control cells. This difference could be completely abolished by addition of the receptor-associated protein, an inhibitor of ligand binding to megalin/gp330. Mutual suppression of the uptake of 125I-Lp(a) and of 125I-LDL by both unlabeled Lp(a) and LDL suggested that Lp(a) uptake is mediated at least partially by apolipoprotein B100. Binding and uptake of DiI-Lp(a) resulted in strong signals on megalin/gp330-expressing cells versus background only on control cells. In addition, we show that purified megalin/gp330, immobilized on a sensor chip, directly binds Lp(a) in a Ca2+-dependent manner with an affinity similar to that for LDL. We conclude that megalin/gp330 binds Lp(a) in vitro and is capable of mediating its cellular uptake and degradation. (+info)

Caspase-dependent activation of calpain during drug-induced apoptosis. (6/1161)

We have previously demonstrated that calpain is responsible for the cleavage of Bax, a proapoptotic protein, during drug-induced apoptosis of HL-60 cells (Wood, D. E., Thomas, A., Devi, L. A., Berman, Y., Beavis, R. C., Reed, J. C., and Newcomb, E. W. (1998) Oncogene 17, 1069-1078). Here we show the sequential activation of caspases and calpain during drug-induced apoptosis of HL-60 cells. Time course experiments using the topoisomerase I inhibitor 9-amino-20(S)-camptothecin revealed that cleavage of caspase-3 substrates poly(ADP-ribose) polymerase (PARP) and the retinoblastoma protein as well as DNA fragmentation occurred several hours before calpain activation and Bax cleavage. Pretreatment with the calpain inhibitor calpeptin blocked calpain activation and Bax cleavage but did not inhibit PARP cleavage, DNA fragmentation, or 9-amino-20(S)-camptothecin-induced morphological changes and cell death. Pretreatment with the pan-caspase inhibitor benzyloxycarbonyl-Val-Ala-Asp-fluoromethylketone (Z-VAD-fmk) inhibited PARP cleavage, DNA fragmentation, calpain activation, and Bax cleavage and increased cell survival by 40%. Interestingly, Z-VAD-fmk-treated cells died in a caspase- and calpain-independent manner that appeared morphologically distinct from apoptosis. Our results suggest that excessive or uncontrolled calpain activity may play a role downstream of and distinct from caspases in the degradation phase of apoptosis. (+info)

Essential role of caspase-3 in apoptosis of mouse beta-cells transfected with human Fas. (7/1161)

Several recent studies have indicated that the Fas-Fas ligand system may be critical for pancreatic beta-cell destruction in type 1 diabetes. Although the fundamental roles of caspases in the mammalian apoptotic machinery have been elucidated, it is not known which caspase or caspases play a major role in Fas-mediated apoptosis of beta-cells. In this study, we transfected human Fas cDNA into a mouse beta-cell line (betaTC1) and established a beta-cell clone expressing human Fas. This clone, designated hFas/betaTC1, underwent apoptosis when exposed to anti-Fas, showing hallmarks of apoptosis (chromatin condensation, nucleolar disintegration, internucleosomal DNA fragmentation, and annexin V staining), indicating that the mouse beta-cell line has the intact machinery of Fas-mediated apoptosis. The cross-linking of Fas by anti-Fas resulted in the elevation of caspase-3-like, but not caspase-1-like, protease activity 2-12 h after the addition of the anti-Fas. A caspase-3 inhibitor, Z-Asp-Glu-Val-Asp-fluoromethyl ketone, attenuated the Fas-mediated beta-cell apoptosis, while a caspase-1 inhibitor, acetyl-Tyr-Val-Ala-Asp-chloromethylketone, failed to suppress the apoptosis. Thus the Fas-induced death signal apparently bypassed caspase-1 in the cells. Furthermore, an antisense caspase-3 construct blocked caspase-3 activation and substantially suppressed Fas-triggered apoptosis of hFas/betaTC1 cells. These observations suggest the essential role of caspase-3 in Fas-mediated apoptosis of the beta-cell line. (+info)

The release of cytochrome c from mitochondria during apoptosis of NGF-deprived sympathetic neurons is a reversible event. (8/1161)

During apoptosis induced by various stimuli, cytochrome c is released from mitochondria into the cytosol where it participates in caspase activation. This process has been proposed to be an irreversible consequence of mitochondrial permeability transition pore opening, which leads to mitochondrial swelling and rupture of the outer mitochondrial membrane. Here we present data demonstrating that NGF-deprived sympathetic neurons protected from apoptosis by caspase inhibitors possess mitochondria which, though depleted of cytochrome c and reduced in size, remained structurally intact as viewed by electron microscopy. After re-exposure of neurons to NGF, mitochondria recovered their normal size and their cytochrome c content, by a process requiring de novo protein synthesis. Altogether, these data suggest that depletion of cytochrome c from mitochondria is a controlled process compatible with function recovery. The ability of sympathetic neurons to recover fully from trophic factor deprivation provided irreversible caspase inhibitors have been present during the insult period, has therapeutical implications for a number of acute neuropathologies. (+info)

It is a popular method of producing β-amino acids from α-amino acids. Aside from the acid chloride substrate, three reagents ... Not taking diazomethane in excess results in HCl reacting with the diazoketone to form chloromethyl ketone and N2. Mild ... Acid anhydrides can be used in place of acid chloride. The reaction yields a 1:1 mixture of the homologated acid and the ... The preparation of the beta-amino acid from phenylalanine illustrates the Arndt-Eistert synthesis carried out with the Newman- ...

https://en.wikipedia.org/wiki/Arndt–Eistert_reaction

The phenylalanine moiety is bound to the enzyme because of specificity for aromatic amino acid residues at the active site (as ... Tosyl phenylalanyl chloromethyl ketone (TPCK) is a protease inhibitor. Its structural formula is 1-chloro-3-tosylamido-4-phenyl ... The chloromethyl group reacts with the active site cysteine to form a covalent bond with the loss of the chlorine. TPCK is ...

https://en.wikipedia.org/wiki/Tosyl_phenylalanyl_chloromethyl_ketone

a cytosolic domain of 21 amino acids length inside the cell which is involved in the signaling function of TF. ... 2b8o: Crystal Structure of Glu-Gly-Arg-Chloromethyl Ketone-Factor VIIa/Soluble Tissue Factor Complex ... Guo W, Wang H, Zhao W, Zhu J, Ju B, Wang X (January 2001). "Effect of all-trans retinoic acid and arsenic trioxide on tissue ...

https://en.wikipedia.org/wiki/Tissue_factor

TAILS is also compatible with Stable isotope labeling by amino acids in cell culture (SILAC). COFRADIC was the earliest ... Zymogen/enzyme discrimination using peptide chloromethyl ketones J. Biol. Chem., 264 (13) 7536-7545 (1989). Kidd D., Liu Y., ... Standard peptides synthesized from amino acids labeled with stable isotope atoms serve as internal standards for serial ... enzymatic activity profiling in complex proteomes Amino Acids, 30 (4) 333-350 (2006). Greenbaum D.C., Baruch A., Grainger M., ...

https://en.wikipedia.org/wiki/Degradomics

... cuts peptide chains mainly at the carboxyl side of the amino acids lysine or arginine. It is used for numerous ... The activity of trypsin is not affected by the enzyme inhibitor tosyl phenylalanyl chloromethyl ketone, TPCK, which deactivates ... This means that trypsin predominantly cleaves proteins at the carboxyl side (or "C-terminal side") of the amino acids lysine ... The peptide products are then further hydrolyzed into amino acids via other proteases, rendering them available for absorption ...

https://en.wikipedia.org/wiki/Trypsin

... ester Phosphonothioic acid, methyl-, S-(2-(bis(1-methylethyl)amino)ethyl) O-ethyl ester Phosphonothioic acid, methyl-, O-(4- ... chloromethyl) ketone Bitoscanate Boron trichloride Boron trifluoride Boron trifluoride compound with dimethyl ether (1:1) ... Chlormequat chloride Chloroacetic acid 2-chloroethanol Chloroethyl chloroformate Chloroform Chloromethyl ether Chloromethyl ... 4-amino- Pyridine, 4-nitro-, 1-oxide Pyriminil Ricin Salcomine Sarin Selenious acid Semicarbazide hydrochloride Silane, (4- ...

https://en.wikipedia.org/wiki/EPA_list_of_extremely_hazardous_substances

... diazomethane methylene group is inserted into the carbon-chlorine bond of an acid chloride to generate an α-chloromethyl ketone ... Organic Syntheses provides the example of t-BOC protected (S)-phenylalanine (2-amino-3-phenylpropanoic acid) being reacted ... 3-amino-4-phenylbutanoic acid. Mechanistically, the α-diazoketone undergoes a Wolff rearrangement to form a ketene in a 1,2- ... a methylene unit is inserted into the carboxyl-carbon bond of carboxylic acid to form the next acid in the homologous series. ...

https://en.wikipedia.org/wiki/Insertion_reaction

The mechanism requires zinc and acetic acid as catalysts. It will proceed at room temperature. Because α-amino-ketones self- ... The 5-methyl group can be variously oxidized to chloromethyl, aldehyde, or carboxylic acid functionality by the use of ... The method involves the reaction of an α-amino-ketone (1) and a compound containing an electron-withdrawing group (e.g. an ... and tertiary-butyl groups can be removed by treatment with trifluoroacetic acid, or boiling aqueous acetic acid. R1 and R3 (as ...

https://en.wikipedia.org/wiki/Knorr_pyrrole_synthesis

... chloromethyl ketone formation (4) with hydrochloric acid, organic reduction of chlorine to methylketone (5), ketone ... Has been used to convert β-amino esters from α-amino esters through an ynolate intermediate. Seyferth-Gilbert homologation in ... pyruvic acid is removed from a linear aliphatic carboxylic acid yielding a new acid with 2 carbon atoms less. The original ... Arndt-Eistert reaction is a series of chemical reactions designed to convert a carboxylic acid to a higher carboxylic acid ...

https://en.wikipedia.org/wiki/Homologation_reaction

... and trypsin with amino acid and peptide thioesters: development of new sensitive substrates". Biochemistry. 20 (25): 7196-206. ... "Synthesis of tripeptide chloromethyl ketones and examination of their inhibitory effects on plasmin and plasma kallikrein". ...

https://en.wikipedia.org/wiki/Plasma_kallikrein

... iodoacetic acid, EDTA or by other serine protease inhibitors like Nα-Tosyl-Lys Chloromethyl Ketone (TLCK) and Nα-Tosyl-Phe ... the enzyme digests proteins preferentially after hydrophobic amino acids (aliphatic, aromatic and other hydrophobic amino acids ... N-alpha-tosyl-L-lysyl-chloromethyl-ketone (TLCK), or N-alpha-Tosyl-l-phenylalanine Chloromethyl Ketone (TPCK), although ... Jany KD, Lederer G, Mayer B (1986). "Amino acid sequence of proteinase K from the mold Tritirachium album Limber". FEBS Lett. ...

https://en.wikipedia.org/wiki/Proteinase_K

... tosylphenylalanyl chloromethyl ketone MeSH D12.125.067.500 - aspartic acid MeSH D12.125.067.500.150 - d-aspartic acid MeSH ... 2-amino-5-phosphonovalerate MeSH D12.125.072.050 - amino acids, aromatic MeSH D12.125.072.050.342 - dextrothyroxine MeSH ... 2-aminoadipic acid MeSH D12.125.119.170 - aspartic acid MeSH D12.125.119.170.150 - d-aspartic acid MeSH D12.125.119.170.275 - ... aspartic acid MeSH D12.125.427.300 - glutamic acid MeSH D12.125.481.100 - allylglycine MeSH D12.125.481.700 - n-substituted ...

https://en.wikipedia.org/wiki/List_of_MeSH_codes_(D12.125)

It is formed in the metabolism of amino acids[which?] and is found in the bloodstream of humans and other primates at ... Transition metal complexes of aldehydes and ketones includess several complexes of formaldehyde. 1,3-Dioxetane DMDM hydantoin ... the product is the chloromethyl compound, as described in the Blanc chloromethylation. If the arene is electron-rich, as in ... The binding of formaldehyde loosens the skeletal structure of albumin and causes exposure of aromatic ring amino acids in the ...

https://en.wikipedia.org/wiki/Formaldehyde

ADDA (amino acid). *Adenophostin. *Adipamide. *Adipic acid dihydrazide. *Advantame. *Agelasimine. *Ageliferin. *Aleuritic acid ... Chloromethyl chloroformate. *Chlorophenol red. *(2-Chlorophenyl)thiourea. *3-Chloropropyl octyl sulfoxide. *Chloroxuron ...

https://en.wikipedia.org/wiki/Category:Organic_compound_stubs

Other unsaturated functional groups-alkynes, imines, ketones, and aldehydes. An example is the hydrosilation of phenylacetylene ... Synthesis and Structure of a Base-Stabilized C-Phosphino-Si-Amino Silyne. Angewandte Chemie International Edition, 49: 6585- ... chloromethyl)silane, trichloro(dichlorophenyl)silane, trichloroethylsilane, and phenyltrichlorosilane. Although proportionately ... reaction for the synthesis of this compound class is by heating hexaalkyldisiloxanes R3SiOSiR3 with concentrated sulfuric acid ...

https://en.wikipedia.org/wiki/Organosilicon

Amino Acid Chloromethyl Ketones / pharmacology * Amino Acid Chloromethyl Ketones / therapeutic use* * Animals ... Treatment with fluoromethyl ketone-derivatized pseudopeptides rescued mice from lethal infection. The optimal pseudopeptide ...

https://pubmed.ncbi.nlm.nih.gov/9705954/

Amino Acid Chloromethyl Ketones / pharmacology * Animals * Antineoplastic Combined Chemotherapy Protocols / therapeutic use* ... Comparable effects were achieved in human and canine OS cells using the HDAC inhibitor suberoylanilide hydroxamic acid (SAHA/ ...

https://pubmed.ncbi.nlm.nih.gov/22957032/?dopt=Abstract

0 (Amino Acid Chloromethyl Ketones); 0 (Benzamidines); 0 (Caspase Inhibitors); 0 (Macrolides); 0 (Reactive Oxygen Species); 0 ( ... Clorometilcetonas de Amino cidos/farmacologia. Benzamidinas/qu mica. Inibidores de Caspase/farmacologia. Caspases/metabolismo. ... In addition, sclerotia production, cell membrane permeability and oxalic acid content significantly decreased. On detached ... N-(2-butanoyloxyethyl)-4-(chloromethyl)-3-nitrobenzamide (NBCN) is a nitroaromatic bioreducible compound with cytotoxic effects ...

http://bases.bireme.br/cgi-bin/wxislind.exe/iah/online/?IsisScript=iah/iah.xis&nextAction=lnk&base=MEDLINE&lang=p&format=detailed.pft&indexSearch=EX&exprSearch=D02.078.100

benzyloxycarbonyl-valyl-aspartic acid fluoromethyl ketone: a dipeptide caspase inhibitor with potent in vivo antiapoptotic ... Amino Acids, Peptides, and Proteins*Amino Acids: 10808*Amino Acid Chloromethyl Ketones*benzyloxycarbonyl-valyl-aspartic acid ... benzyloxycarbonyl-valyl-aspartic acid fluoromethyl ketone. Subscribe to New Research on benzyloxycarbonyl-valyl-aspartic acid ... EP1013; MX1013; N-benzyloxycabonyl-Val Asp-fluoromethyl ketone; Z-VD-FMK; zVD-FMK ...

http://www.curehunter.com/public/keywordSummaryC484771-benzyloxycarbonyl-valyl-aspartic-acid-fluoromethyl-ketone.do

Amino Acid Chloromethyl Ketones. Papers overview. Semantic Scholar uses AI to extract papers important to this topic. ... methoxysuccinyl-alanyl-alanyl-alanyl-prolyl-valine chloromethyl ketone. Known as: MeOSuc-AAAPV-CH2Cl, methoxysuccinyl-Ala-Ala- ...

https://www.semanticscholar.org/topic/methoxysuccinyl-alanyl-alanyl-alanyl-prolyl-valine/11765212

Commonly used amino acid and peptide abbreviations and their meanings ... Chloromethyl ketone. CMV Cytomegalovirus. CNP C-type Natriuretic Peptide. Cpa. Cyclopropylalanine. Cpg. Cyclpentylglycine. ... Azido Amino Acids. • Beta-Amino Acids. • Beta-Homo Amino Acids. • BOC-Amino Acids. - Boc-D-Amino Acids. - Boc-L-Amino Acids. • ... Fmoc-Amino Acid Wang Resins. • Fmoc-Amino Acids. - Fmoc-D-Amino Acids. - Fmoc-L-Amino Acids. - Fmoc-Amino Acid OPfp. • Glyco- ...

https://www.peptide.com/abbreviations-their-meanings-i-231.html

Silver, J., Laursen, R.A.: Inactivation of aminoacyl-tRNA synthetases by amino acid chloromethyl ketones. Biochim. Biophys. ... Papas, T.S., Mehler, A.H.: Analysis of the amino acid binding in the proline transfer ribonucleic acid synthetase of ... The enzymatic synthesis of 5-amino-1-ribosyl-4-imidazole carboxylic acid 5′-phosphate from 5-amino-1-ribosylimidazole 5′- ... Enzymatic formation of dihydrofolic acid from dihydropteroic acid and of tetrahydropteroyl-polyglutamic acid compounds from ...

https://link.springer.com/chapter/10.1007%2F978-3-642-66856-2_2

Amino Acid Chloromethyl Ketones/pharmacology. *Caspase Inhibitors. *Cysteine Proteinase Inhibitors/pharmacology. *Humans ...

https://openi.nlm.nih.gov/detailedresult.php?img=PMC2195712_JEM980433.f3b&req=4

The deduced amino acid sequence for the E1 alpha subunit of the patients cell was normal. An 11-bp deletion was identified in ... Heat-inactivation, diisopropylfluorophosphate, PMSF, and N-benzyloxycarbonylglycylleucylphenylalanyl-chloromethyl ketone ... The HLA-DQB1*0301 chain shares an identical seven amino acid sequence with DQB1*0302, *0602, and *0603 chains in the third ... indicated that apo B67 was a truncated species of apo B that contained approximately the amino-terminal 3,000-3,100 amino acids ...

https://www.jci.org/87/5

stable isotope labeling by amino acids in cell culture. phosphoPSM. phosphopeptide-spectrum match. TPCK. L-1-tosylamido-2- ... phenylethyl chloromethyl ketone. LC-MS/MS. liquid chromatography-tandem mass spectrometry. IAP. immunoaffinity purification. E2 ... In order to label cells with stable isotopic amino acids, MCF7-CTRL and MCF7-TamR cells were propagated in RPMI 1640 SILAC ... 2002) Stable isotope labeling by amino acids in cell culture, SILAC, as a simple and accurate approach to expression proteomics ...

https://www.mcponline.org/content/14/11/2887?ijkey=973e438b526b32f00a34f065048ec97f4f3b232d&keytype2=tf_ipsecsha

Sequence analysis of the complete genomes of the MA virus revealed a total of 16 amino acid substitutions. These mutations ... mutations in PB2 contribute to the phenotype differences and emphasize the importance of monitoring the identified amino acid ... 6 sialic acid receptors (avian and human receptors), raising concern whether these viruses possess pandemic potential. To ... and fresh medium supplemented with 1 μg/mL tosyl phenylalanyl chloromethyl ketone (TPCK) and trypsin (Sigma, St. Louis, MO, USA ...

https://www.nature.com/articles/s41598-019-56122-6?error=cookies_not_supported&code=9e03dd71-1114-4aee-b736-4d7adfa26188

Trypsin is a serine protease that cleaves peptides on C-terminal end of lysine and arginine amino acid residues. The pH optimum ... Trypsin is inhibited by serine protease inhibitors including TLCK (N-p-tosyl-L-lysine chloromethyl ketone), PMSF ( ... Isovaleryl-Val-Val-AHMHA-Ala-AHMHA where AHMHA= (3S, 4S)-4-amino-3-hydroxy-6-methyl-heptanoic acid Specificity: A potent ... Carboxypeptidase B specifically hydrolyses basic amino acids including lysine, arginine and histidine from the C-terminal end ...

https://www.thomassci.com/nav/cat1/enzymesinhibitors/manufacturer/gbiosciences/0

Incorporation of unusual amino acids. *Cyclic and phosphorylated peptides. *Peptide libraries. *Chloromethyl Ketone peptides ... The peptides range from di-peptides to peptides having more than 60 Amino Acid residues. ...

http://www.usvindia.com/custom-peptide-synthesis.php

Post-translational isomerization of l-amino acids to d-amino acids is a subtle modification, not detectable by standard… (More) ... phenylalanyl-phenylalanyl-arginine chloromethyl ketone. Known as: FFRCK, Phe-Phe-Arg-CK, L-Phenylalaninamide, D-phenylalanyl-N ... Characterization of D-amino-acid-containing excitatory conotoxins and redefinition of the I-conotoxin superfamily. ... 1. To determine whether differential release of products of arachidonic acid metabolism, via the cyclo-oxygenase pathway… (More ...

https://www.semanticscholar.org/topic/phenylalanyl-phenylalanyl-arginine-chloromethyl/3886432

The disclosed invention provides tetrapeptides with the amino acid sequence proline-glutamine-glutamate-X (P-Q-E-X), where X ... D-val-phe-lys chloromethyl ketone dihydrochloride, 1,3-di-(N-carboxybenzoyl-L-leucyl-L-leucyl)amino acetone, o-phenanthroline, ... less than 20 amino acid residues in length, less than 15 amino acid residues in length, or less than 10 amino acid residues in ... less than 100 amino acid residues in length, less than 50 amino acid residues in length, less than 45 amino acid residues in ...

https://www.freepatentsonline.com/y2009/0142280.html

https://en.wikipedia.org/wiki/Tosyl_phenylalanyl_chloromethyl_ketone

https://en.wikipedia.org/wiki/Arndt%E2%80%93Eistert_reaction

Amino Acid Chloromethyl Ketones. 1. + +. 235. Melatonin. 1. + +. 236. Sialoglycoproteins. 1. + +. 237. Heparin, Low-Molecular- ... 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid. 1. + +. ...

https://lookfordiagnosis.com/results.php?symptoms=Cerebral+Hemorrhage%2C+Traumatic%3B%20Brain%20Hemorrhage%2C%20Cerebral%2C%20Traumatic%3B%20Cerebral%20Hematoma%2C%20Traumatic%3B%20Intracerebral%20Hemorrhage%2C%20Traumatic&lang=1&parent=%2F&mode=F&therapy_ap=1

Amino Acid Chloromethyl Ketones; Animals; Antibodies; Apoptosis; Caspases; Cell Line; Cyclic AMP Response Element-Binding ...

https://escholarship.umassmed.edu/oapubs/716/

N-alpha-p-tosyl-L-lysyl-chloromethyl-ketone and other amino acid analogs and trypsin-chimotrypsin inhibitors. ... N-alpha-p-tosyl-L-lysyl-chloromethyl-ketone and trypsin-chimotrypsin inhibitors. ... N-alpha-p-tosyl-L-lysyl-chloromethyl-ketone and trypsin-chimotrypsin inhibitors. ... N-alpha-p-tosyl-L-lysyl-chloromethyl-ketone and trypsin-chimotrypsin inhibitors. ...

https://www.google.ch/patents/US20050147572

Trypsin is a serine protease that cleaves peptides on C-terminal end of lysine and arginine amino acid residues. The pH optimum ... Trypsin is inhibited by serine protease inhibitors including TLCK (N-p-tosyl-L-lysine chloromethyl ketone), PMSF ( ... Trypsin is a serine protease that cleaves peptides on C-terminal end of lysine and arginine amino acid residues. The pH optimum ...

https://www.gbiosciences.com/Trypsin_Human_Recombinant

... in the presence of 0.5 μg of tosylsulfonyl phenylalanyl chloromethyl ketone (TPCK)-treated trypsin (Sigma Chemical Co., St. ... amino acids from NA sequences. Amino acids shown in boldface type are from TR sequences. Amino acids in lowercase type are due ... Numbers above amino acid sequences represent amino acid positions (indicated by ↓) of the WT NA peptide. ... Although the 6 amino acids (aa) in the CT of NA are extremely conserved among the influenza A viruses (7), little is known ...

https://jvi.asm.org/content/78/10/5258?ijkey=7a46196eebd4cfb9a8f1bd416a9d379431545562&keytype2=tf_ipsecsha

MeSH-minor] Amino Acid Chloromethyl Ketones / pharmacology. Animals. Apoptosis / drug effects. Cell Line, Tumor. Cell ... Chemical-registry-number] 0 / Amino Acid Chloromethyl Ketones; 0 / Intracellular Signaling Peptides and Proteins; 0 / ... Nucleic Acid, Nucleoside, or Nucleotide. A1.4.1.2.1.6. Organophosphorus Compound. A1.4.1.2.1.7. Amino Acid, Peptide, or Protein ... A2.1.5.3.2. Amino Acid Sequence. A2.1.5.3.3. Carbohydrate Sequence. A2.1.5.4. Geographic Area. A2.2. Finding. A2.2.1. ...

http://www.bmlsearch.com/?kwr=mouse+gastric+adenocarcinoma+drug+therapy+2000:2010%5Bpubdate%5D&cxts=100&stmp=b1

Amino Acid Chloromethyl Ketones, Animals, Apoptosis, Caspase 3, Caspase 6, Caspases, Cell Extracts, Cysteine Proteinase ... Amino Acid Chloromethyl Ketones,Animals,Apoptosis,Caspase 3,Caspase 6,Caspases,Cell Extracts,Cysteine Proteinase Inhibitors, ...

https://lup.lub.lu.se/search/publication/5b8f99f5-08ae-4701-a87c-1b45581f2ba5

Amino Acids [D12.125]. *Amino Acid Chloromethyl Ketones [D12.125.065]. *Tosylphenylalanyl Chloromethyl Ketone [D12.125.065.930] ... "Tosylphenylalanyl Chloromethyl Ketone" by people in this website by year, and whether "Tosylphenylalanyl Chloromethyl Ketone" ... "Tosylphenylalanyl Chloromethyl Ketone" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, ... Below are the most recent publications written about "Tosylphenylalanyl Chloromethyl Ketone" by people in Profiles. ...

https://profiles.uchicago.edu/profiles/display/20341

... resulting in an amino acid polymorphism at position 126 [20]. The amino acid polymorphisms will be discussed below. ... Inhibition of proteinase K by methoxysuccinyl-Ala-Ala-Pro-Ala-chloromethyl ketone. An X-ray study at 2.2-Å resolution. J Biol ... Amino acid sequence alignment. Multiple sequence alignment was performed using the CLUSTALW program [46] with the gap open and ... The amino acid numbering used throughout this paper corresponds to that of 1IC6. Substrate-binding site residues in the S2, S1 ...

https://rd.springer.com/article/10.1186/1472-6807-7-33

The NF-κB inhibitors pyrrolidine dithiocarbamate andN α-p-tosyl-l-lysine chloromethyl ketone abrogated LPS- and interferon-γ- ... This correlated with an increased mRNA expression for iNOS and the cationic amino acid transporter CAT-2B (analyzed by reverse ... Factor-κB Mediates Simultaneous Induction of Inducible Nitric-Oxide Synthase and Up-Regulation of the Cationic Amino Acid ... Factor-κB Mediates Simultaneous Induction of Inducible Nitric-Oxide Synthase and Up-Regulation of the Cationic Amino Acid ...

http://molpharm.aspetjournals.org/content/58/6/1294

Draw a structural formula for each of the following ketones. a. Isopropyl propyl ketone b. Chloromethyl methyl .... General, ... Two proteins with the same amino acid composition do not have to have the same primary structure. Explain why.. Organic And ... 18-45 Give the expected organic product formed when phenylacetic acid, C6H5CH2COOH, is treated with each of the.... ...

https://www.bartleby.com/solution-answer/chapter-33-problem-36pe-college-physics-1st-edition/9781938168000/verify-the-quantum-numbers-given-for-the-proton-and-neutron-in-table-332-by-adding-the-quantum/0c361a42-7df0-11e9-8385-02ee952b546e

... pantothenic acid derivatives, and tanning actives; and a dermatologically acceptable carrier. The composition can also comprise ... ursolic acid, and plant extract compounds; at least one acute skin care active selected from the group consisting of ... L-lysine chloromethyl ketone, N-acetyl- beta -D-mannosamine, oxaloacetic acid, finasteride, arginase inhibitor, N- ... 3-amino-2,3-dihydro benzoic acid, 6-fluoro-2,5-diamino hexanoic acid, (S)-2-amino-4-amino oxy-butyric acid, triarylmethane ...

https://www.google.ch/patents/WO2005110353A1?cl=en

Assignment of tryptic peptides and alignment of amino acid sequences were based on published data (24). The amino acid sequence ... l-phenylamine chloromethyl ketone-treated trypsin (Worthington Biochemical, Freehold, NJ), and the tryptic peptides were ... and the resulting phenylthiohydantoin amino acids were identified using an on-line ABI model 120A PTH amino acid analyzer. ... The reciprocal hydrophobic amino acids of SCR3 of H were Phe56, Trp57, Leu6, and Ala10. The surface structures of the putative ...

https://www.jimmunol.org/content/163/8/4590?ijkey=9e894aeee0ecc6e7592a9c1b8c5ad414c65016ab&keytype2=tf_ipsecsha

Ami-noacyl compounds may be stabilized as tRNA-esters or enzyme thioesters (pantetheine-mediated peptide synthesis), while CoA-derivatives of amino acids have not been observed. (springer.com)
1. An isolated peptide, wherein the amino acid sequence of the peptide consists of proline-glutamine-glutamate-X (P-Q-E-X), wherein X is lysine (K) or isoleucine (I). (freepatentsonline.com)
3. The peptide of claim 1, wherein the peptide has a non-peptide bond between adjacent amino acid residues. (freepatentsonline.com)
4. The peptide of claim 1, wherein the peptide has an amino acid residue in the D-enantiomeric form. (freepatentsonline.com)
5. The peptide of claim 1, wherein the amino acid sequence consists of SEQ ID NO:14. (freepatentsonline.com)
Such a cleavage is essential for viral infectivity because in the acidic pH of the endosome it exposes a membrane fusion peptide at the amino terminus of the HA2 subunit required for membrane fusion ( 26 ). (asm.org)
Further, the chloromethyl ketone derivatized peptide MeO-Suc-Ala-Ala-Pro-Leu-CMK, known to specifically inhibit the schistosome elastase, prevented IgE cleavage. (dundee.ac.uk)
Trypsin consists of a single chain polypeptide of 223 amino acid residues, produced by the removal of the N-terminal hexapeptide from trypsinogen which is cleaved at the Lys - lle peptide bond. (sigmaaldrich.com)
Specificity for chymotrypsin-like enzymes is determined by the amino acid targeting peptide, the FAM-Leu-CMK probe inhibits chymotrypsin C. (bio-rad-antibodies.com)
Stability improvement of natural food colors: Impact of amino acid and peptide addition on anthocyanin stability in model beverages. (umassmed.edu)
Identification of the Reactive Histidine of Cucumisin, a Plant Serine Protease: Modification with Peptidyl Chloromethyl Ketone Derivative of Peptide Substrate. (nii.ac.jp)

Depending on the structure of the prodomain and their function, caspases are typically divided into 3 major groups (Figure 1 A). The caspases with large prodomains are referred to as inflammatory caspases (group I) and initiator of apoptosis caspases (group II), while caspases with a short prodomain of 20-30 amino acids are named effector caspases (group III). (jci.org)

Biosynthesis of peptides requires (1) carboxyl group activation , and (2) specific addition of acceptor amino (imino) group. (springer.com)
Trypsin is a serine protease that cleaves peptides on C-terminal end of lysine and arginine amino acid residues. (thomassci.com)
The peptides range from di-peptides to peptides having more than 60 Amino Acid residues. (usvindia.com)
Trypsin is a serine protease enzyme (EC number of 3.4.21.4), which hydrolyses esters of basic amino acids such as lysine and arginine in the peptides. (pharmiweb.com)
Tryptase will cleave peptides on the C-terminal side of lysine and arginine amino acid residues with more strict specificity than trypsin. (sigmaaldrich.com)
Cleavage of peptides is performed using trifluoroacetic acid (TFA), hydrogen fluoride (HF), or other appropriate methods. (mobitec.com)

The NF-κB inhibitors pyrrolidine dithiocarbamate and N α - p -tosyl- l -lysine chloromethyl ketone abrogated LPS- and interferon-γ-induced increase of nitrite accumulation and l -[ 3 H]arginine uptake as well as up-regulation of iNOS and CAT-2B mRNA. (aspetjournals.org)
Peptidyl chloromethylketones are substrate‐mimicking, mechanism‐based inhibitors of rhomboid protease. (embopress.org)
FLISP inhibitors are cell-permeable and non-cytotoxic fluorochrome-labeled analogs of the first serine protease inhibitor, tosyl-phenlalanylchloromethyl ketone (TPCK), labeled with carboxyfluorescein (FAM) which fluoresces green. (bio-rad-antibodies.com)
6. The anticoagulant of claim 1 wherein the active site serine region of said factor Xa or polypeptide fragment thereof, is inactivated with an inhibitor selected from the group consisting of chloromethyl ketones, fluorophosphates, sulfonylfluoride inhibitors, and antibodies or fragments thereof which interact with the active site of factor Xa without blocking the factor Va binding activity. (patentgenius.com)

NA, a type II transmembrane glycoprotein, possesses an enzyme activity that removes sialic acid from host cell glycocongugates as well as newly synthesized viral proteins. (asm.org)
Twenty alpha-amino acids are the subunits which are polymerized to form proteins. (umassmed.edu)
PLAAC: a web and command-line application to identify proteins with prion-like amino acid composition. (umassmed.edu)
A sequence of about forty amino-acid residues found in epidermal growth factor (EGF) has been shown [( PUBMED:2288911 ), ( PUBMED:6334307 ), ( PUBMED:3534958 ), ( PUBMED:6607417 ), ( PUBMED:3282918 )] to be present in a large number of membrane-bound and extracellular, mostly animal, proteins. (embl-heidelberg.de)
The acyl-enzyme is next resolved by nucleophilic attack by the amino groups within cell wall cross-bridges or pilin proteins, thereby covalently attaching the polypeptides to the cell wall or the next pilin subunit. (aspetjournals.org)

The phenylalanine moiety is bound to the enzyme because of specificity for aromatic amino acid residues at the active site (as in chymotrypsin, in which it binds to the Histidine-57 residue in the active site). (wikipedia.org)
Amino acid residues within the pro-region mediate their membrane association, and play a role in the transport of the proenzyme to lysosomes. (embl.de)

Treatment with fluoromethyl ketone-derivatized pseudopeptides rescued mice from lethal infection. (nih.gov)

Tosylphenylalanyl Chloromethyl Ketone" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (uchicago.edu)
This graph shows the total number of publications written about "Tosylphenylalanyl Chloromethyl Ketone" by people in this website by year, and whether "Tosylphenylalanyl Chloromethyl Ketone" was a major or minor topic of these publications. (uchicago.edu)
Below are the most recent publications written about "Tosylphenylalanyl Chloromethyl Ketone" by people in Profiles. (uchicago.edu)

Tosyl phenylalanyl chloromethyl ketone (TPCK) is a protease inhibitor. (wikipedia.org)
yl chloromethyl ketone (TPCK) reduces the chymotrypsin activity which is usually present in trypsin. (sigmaaldrich.com)
There are many manufacturers producing immobilized trypsin like Thermo Fischer Scientific who manufactures immobilized trypsin, treated with L-1-tosylamido-2-phenylethyl chloromethyl ketone (TPCK) to inhibit chymotrypsin activity without altering the activity of trypsin, in order to prevent contamination. (pharmiweb.com)

The HA protein, a type I transmembrane protein, is responsible for binding to the cell surface sialic acid (the receptor), eliciting neutralizing antibodies, and mediating virus entry into the cell by fusion of the viral membrane with the endosomal membrane ( 46 ). (asm.org)

The preparation of the beta-amino acid from phenylalanine illustrates the Arndt-Eistert synthesis carried out with the Newman-Beal modification, which involves the inclusion of triethylamine in the diazomethane solution. (wikipedia.org)
This in vitro assay employs the green fluorescent label carboxyfluorescein (FAM), which is linked to a 6 carbon spacer, phenylalanine, and a chloromethyl ketone (CMK) reactive group, forming the fluorescent inhibitor probe, FAM-Spacer-Phe-CMK. (immunochemistry.com)
The 6 carbon hexanoic spacer is designed to reduce steric hindrance of the single amino acid phenylalanine target. (immunochemistry.com)
The method comprises oral administration of ascorbic acid, a source of biologically available calcium, a precursor or stimulant of epinephrine or nor-epinephrine selected from tyrosine and phenylalanine, and an anti-inflammatory substance selected from anti-inflammatory sugars, amino sugars and biocompatible acid addition salts thereof, and anti-inflammatory amino acids. (patents.com)
Tyrosine-1073 was mutated to a phenylalanine and a glycine, amino acids that cannot be phosphorylated, and to the other commonly phosphorylated hydroxyamino acids, serine and threonine. (ubc.ca)

The HLA-DQB1*0301 chain shares an identical seven amino acid sequence with DQB1*0302, *0602, and *0603 chains in the third hypervariable region of the HLA-DQ molecule. (jci.org)
Sequence analysis of the complete genomes of the MA virus revealed a total of 16 amino acid substitutions. (nature.com)
The disclosed invention provides tetrapeptides with the amino acid sequence proline-glutamine-glutamate-X (P-Q-E-X), where X can be either lysine (K) or isoleucine (I). These tetrapeptides inhibit ultraviolet light (UV)-induced expression of the pro-inflammatory cytokine interleukin-6 (IL-6) by skin epithelial cells and fibroblasts. (freepatentsonline.com)
The fact that some albumins are ineffective indicates that minor differences in amino acid sequence may be critical. (aspetjournals.org)
The sequence of amino acids is cross-linked by 6 disulfide bridges. (sigmaaldrich.com)
It has orthologs in several other apicomplexans, and its predicted amino acid sequence shows a high degree of conservation among several B. bovis isolates from North and South America. (biomedcentral.com)
Clans, in turn, are subdivided in families, according to their amino acid sequence similarities. (biomedcentral.com)
These four amino acids are present in three separate, well conserved regions of the primary sequence that correspond to the mature protease, which are known as the eukaryotic thiol (cysteine) proteases cysteine, histidine, and asparagine active site regions. (biomedcentral.com)
Amino Acid Sequence and Some Properties of Phytolacain R, a Cysteine Protease from Full-Growth Fruits of Pokeweed, Phytolacca americana. (nii.ac.jp)

An accumulation of amino acid substitutions in HA was observed in viruses derived from the late epidemic waves. (biomedcentral.com)

deren Derivate" [A process for the conversion of carboxylic acids into their higher homologs or their derivatives]. (wikipedia.org)
Trypsin will also hydrolyze ester and amide linkages of synthetic derivatives of amino acids such as: benzoyl L-arginine ethyl ester (BAEE), p-toluenesulfonyl- L-arginine methyl ester (TAME), tosyl-L-arginine methyl ester, N-α-benzoyl-L-arginine p-nitroanilide (BAPNA), L-lysyl-p-nitroanilide, and benzoyl-L-tyrosine ethyl ester (BTEE). (creativebiomart.net)
Trypsin can also act to cleave ester and amide linkages of synthetic derivatives of amino acids. (sigmaaldrich.com)
D,L-, L- and D-phenyl alanine derivatives of formula (I) defined in claim 1 in which R.sub.1 is an amidino-, guanidino-, oxamidino-, aminomethyl- or amino group have been discovered which effectively prevent blood coagulation or thrombosis. (patents.com)

Trypsin is soluble in 1 mM hydrochloric acid (pH approximately 3). (sigmaaldrich.com)
CRL-1746) in the presence of tosyl phenylalanyl chloromethyl ketone-treated trypsin. (cdc.gov)

Aside from the acid chloride substrate, three reagents are required: diazomethane, water, and a metal catalyst. (wikipedia.org)

Abiko, Y.: Pantothenic acid and coenzyme A: Phosphopantothenoyl-cysteine synthetase from rat liver. (springer.com)
The chloromethyl group reacts with the active site cysteine to form a covalent bond with the loss of the chlorine. (wikipedia.org)
Hydrolysis involves usually a catalytic triad consisting of the thiol group of the cysteine, the imidazolium ring of a histidine, and a third residue, usually asparagine or aspartic acid, to orientate and activate the imidazolium ring. (embl.de)
In only one family of cysteine peptidases, is the role of the general base assigned to a residue other than a histidine: in peptidases from family C89 (acid ceramidase) an arginine is the general base. (embl.de)
C': cysteine, involved in disulphide bond 'x': any amino acid. (embl-heidelberg.de)

Two distinct H9N2 poultry lineages, G1-like (A/quail/Hong Kong/G1/97) and Y280-like (A/Duck/Hong Kong/Y280/1997) viruses, are usually associated with binding affinity for both α 2,3 and α 2,6 sialic acid receptors (avian and human receptors), raising concern whether these viruses possess pandemic potential. (nature.com)
It has been shown previously that NA is not required for virus replication or budding except in the final step of releasing the virus particles from the cell surface sialic acid receptor as well as preventing aggregation among the progeny virus particles ( 29 ). (asm.org)

They are available with either a chloromethyl ketone (CMK) or diphenyl 1-(N-peptidylamino) alkanephosphonate (DAP) reactive group containing compound. (bio-rad-antibodies.com)

Here, we found that a single amino acid substitution of Asp-to-Gly at position 222 in the HA protein of the A (H1N1) virus occurred after two passage propagation in the allantoic cavities of chicken embryonated eggs, and this single residue variation dramatically increased the viral replication ability in MDCK cells and pathogenicity in BALB/c mice. (biomedcentral.com)
The results indicated that amino acid substitution at residue 144 significantly affected neutralization activity, acting as an escape mutation. (biomedcentral.com)

Our findings elucidate the specific mutations in PB2 contribute to the phenotype differences and emphasize the importance of monitoring the identified amino acid substitutions due to their potential threat to human health. (nature.com)
To investigate whether these NGSs are associated with re-emergence of H3N2 within the subtype, we tested the effect of amino acid substitutions on neutralizing activity by using the antisera raised against H3N2 strains with or without additional NGSs. (biomedcentral.com)

A substitution of Asp-to-Gly at position 222 in the HA protein was prone to occur under positive selection pressures, and this single amino acid mutation could dramatically increase the virus replication ability in vitro and pathogenicity in vivo . (biomedcentral.com)

These results show that although the sequences of NA CT and TMD per se are not absolutely essential for the virus life cycle, specific amino acid sequences play a critical role in providing structural stability, enzyme activity, and lipid raft association of NA. (asm.org)

Comparable effects were achieved in human and canine OS cells using the HDAC inhibitor suberoylanilide hydroxamic acid (SAHA/Vorinostat) and the DNA methylation inhibitor Zebularine (Zeb), with significantly more pronounced cytotoxicity in cells whose molecular phenotypes were indicative of aggressive biological behavior. (nih.gov)
In a preferred embodiment, Factor Xa, a serine esterase that forms a complex with Factor Va, Ca++, and phospholipid to catalyze prothrombin activation, is first inactivated with an active site inhibitor, such as dansyl-glu- gly-arg-chloromethyl ketone, to form inactivated factor Xa. (patentgenius.com)
7. The anticoagulant of claim 6 wherein the inhibitor is selected from the group consisting of dansyl-glu-gly-arg-chloromethyl ketone, para-amidinophenylmethyl sulfonyl fluoride, and diisopropyl fluorophosphate and all unbound inhibitor isremoved from the inactivated factor Xa. (patentgenius.com)

Among the influenza A viruses, both the cytoplasmic tail (CT) and transmembrane domain (TMD) amino acid sequences of NA are highly conserved, yet their function(s) in virus biology remains unknown. (asm.org)

Amino Acids" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (umassmed.edu)

naphthyl, 5-(dimethylamino)-naphthyl, or quinolyl, wherein lower alkyl denotes alkyl of 1-4 carbon atoms, or pharmaceutically acceptable salts thereof with mineral or organic acids. (patents.com)

Full List of ' 2-fluoro-4-methyl-1-nitro- 2-nitro-5-fluoro toluene 4-amino-2-fluorobenzoic acid 4-chloro-2-fluorobenzoic acid 3- 2 ' Manufacturers& 2-fluoro-4-methyl-1-nitro- 2-nitro-5-fluoro toluene 4-amino-2-fluorobenzoic acid 4-chloro-2-fluorobenzoic acid 3- 2 Suppliers in European Global & USA Asian. (twfta.com)

To investigate the role of amino acid sequences of the CT and TMD on the virus life cycle, we systematically mutagenized the entire CT and TMD of NA by converting two to five contiguous amino acids to alanine. (asm.org)

Characterization of D-amino-acid-containing excitatory conotoxins and redefinition of the I-conotoxin superfamily. (semanticscholar.org)

Synthesis of tripeptide chloromethyl ketones and examination of their inhibitory effects on plasmin and plasma kallikrein. (nii.ac.jp)
The yeast transcription factor Gcn4 is regulated by amino acid starvation at the levels of both protein synthesis and stability. (asm.org)
In addition, Gcn4 is degraded extremely rapidly but is stabilized under conditions of amino acid limitation or partial inhibition of protein synthesis ( 21 , 26 ). (asm.org)

In addition, exogenous application of SA or its analogs, such as 2,6-dichloroisonicotinic acid (INA) and benzo(1,2,3)thiadiazole-7-carbothioic acid S-methyl ester has been shown to induce SAR ( 17 , 18 ). (pnas.org)

The reaction yields a 1:1 mixture of the homologated acid and the corresponding methyl ester. (wikipedia.org)

This graph shows the total number of publications written about "Amino Acids" by people in this website by year, and whether "Amino Acids" was a major or minor topic of these publications. (umassmed.edu)

Brown, G.M.: The metabolism of pantothenic acid. (springer.com)

Amino acid polymorphisms in cuticle-degrading enzymes were discussed with respect to functional effects and host preference. (springer.com)

amino-4-methoxy- 2 , 5-Dimethyl Benzoxazole Benzenamine , 3-fluoro-2-nitro- 1 , 12-Dodecanediol (R)-2-chloro-1-phenylethanol 2-Amino-4-Hydroxy-6-Phenylpyrimidine 5-Amino-2-Fluorobenzoic acid Z-Glu-OMe 4-(2-Methoxyethyl)Phenol Tryptophan , 5-hydroxy- Benzenepropanoic acid , .alpha. (twfta.com)

Organic compounds that generally contain an amino (-NH2) and a carboxyl (-COOH) group. (umassmed.edu)

Bratcher, S.C., Hsu, R.T.: Separation of active enzyme components from the fatty acid synthetase of chicken liver. (springer.com)

The rearrangement leaves untouched the stereochemistry at the carbon alpha to the acid chloride. (wikipedia.org)

Vayarin contains Lipirinen, a proprietary composition containing phosphatidylserine-omega 3, EPA (Eicosapentaenoic acid) enriched. (drugbank.ca)

Anatomy2

Organisms5

Chemicals and Drugs43

Analytical, Diagnostic and Therapeutic Techniques and Equipment4

Phenomena and Processes15

Information Science3

Activation of stress-activated protein kinase/c-Jun NH2-terminal kinase and p38 kinase in calphostin C-induced apoptosis requires caspase-3-like proteases but is dispensable for cell death. (1/1161)

Role of hypoxia-induced Bax translocation and cytochrome c release in reoxygenation injury. (2/1161)

Anti-apoptotic role of telomerase in pheochromocytoma cells. (3/1161)

Monocytic cell necrosis is mediated by potassium depletion and caspase-like proteases. (4/1161)

Identification of megalin/gp330 as a receptor for lipoprotein(a) in vitro. (5/1161)

Caspase-dependent activation of calpain during drug-induced apoptosis. (6/1161)

Essential role of caspase-3 in apoptosis of mouse beta-cells transfected with human Fas. (7/1161)

The release of cytochrome c from mitochondria during apoptosis of NGF-deprived sympathetic neurons is a reversible event. (8/1161)

Amino Acid Chloromethyl Ketones

Tosyllysine Chloromethyl Ketone

Tosylphenylalanyl Chloromethyl Ketone

Ketones

Bis(Chloromethyl) Ether

Protease Inhibitors

Serine Proteinase Inhibitors

Ketone Bodies

Isoflurophate

Amino Acids

Anhydrides

Peptide Hydrolases

Trifluoroacetic Acid

Dansyl Compounds

Fluoroacetates

Serine Endopeptidases

Kinetics

Amino Acid Sequence

Pyroglutamyl-Peptidase I

Pancreatic Elastase

Sequence Homology, Amino Acid

Endopeptidases

p-Chloromercuribenzoic Acid

Substrate Specificity

Molecular Weight

Binding Sites

Chymotrypsin

Tosyl Compounds

Trypsin Inhibitors

Cysteine Endopeptidases

Electrophoresis, Polyacrylamide Gel

Treponema

Hydrogen-Ion Concentration

Molecular Sequence Data

Amino Acid Substitution

Leupeptins

Phenylmethylsulfonyl Fluoride

Enzyme Precursors

Peptide Fragments

Structure-Activity Relationship

Thrombin

Porphyromonas gingivalis

Hydrolysis

Cloning, Molecular

Trypsin

Affinity Labels

Cell Line

Cysteine Proteinase Inhibitors

Cysteine

Oligopeptides

Cycloheximide

Bacteroides

NF-kappa B

Protein Precursors

Amino Acids, Essential

Cattle

Methyl n-Butyl Ketone

Amino Acid Transport Systems

Acetoacetates

Sequence Alignment

3-Hydroxybutyric Acid

Enzyme Activation

Fluorescent Dyes

Base Sequence

Amino Acid Motifs

Cells, Cultured

Protein Conformation

Escherichia coli

Mutation

Activation of stress-activated protein kinase/c-Jun NH2-terminal kinase and p38 kinase in calphostin C-induced apoptosis requires caspase-3-like proteases but is dispensable for cell death. (1/1161)

Role of hypoxia-induced Bax translocation and cytochrome c release in reoxygenation injury. (2/1161)

Anti-apoptotic role of telomerase in pheochromocytoma cells. (3/1161)

Monocytic cell necrosis is mediated by potassium depletion and caspase-like proteases. (4/1161)

Identification of megalin/gp330 as a receptor for lipoprotein(a) in vitro. (5/1161)

Caspase-dependent activation of calpain during drug-induced apoptosis. (6/1161)

Essential role of caspase-3 in apoptosis of mouse beta-cells transfected with human Fas. (7/1161)

The release of cytochrome c from mitochondria during apoptosis of NGF-deprived sympathetic neurons is a reversible event. (8/1161)

Z-VAD(OMe)-FMK (General Caspase Inhibitor) - Antibodies & Reagents Flow Cytometry Reagents, Recombinant Proteins, PCR Reagents

benzyloxycarbonyl-valyl-aspartic acid fluoromethyl ketone Summary Report | CureHunter

Plus it

$Gentaur Molecular :Biovis \ Z VEID FMK1 mg \ 1146-1$ Gentaur Molecular :Biovis \ Z VEID FMK1 mg \ 1146-1

$Gentaur Molecular :Biovis \ Z ATAD FMK5 mg \ 1152-5$ Gentaur Molecular :Biovis \ Z ATAD FMK5 mg \ 1152-5

Z-VAD-FMK | カスパーゼ阻害剤&活性剤