Nucleotide dissociation inhibitorGuanosineConstantsProteinsEnzyme inhibitorReceptorInhibitsSubstrateGTPaseVitroProteaseRab5IrreversibleEnzymesInteractionInduceComplementBindMetabolismCompoundInteractionsComplexesReactionMoleculesIncorporationHepaticActivationReactionsConcentrationActivityCellsDiseaseAcuteRateSimilarCalculated the associationTargetProcessResultsCapacitySmallResearch
Nucleotide dissociation inhibitor1
- The researchers used the algorithm to identify split sites on a number of proteins, including tyrosine kinase Lyn, guanosine nucleotide dissociation inhibitor, and guanine exchange factor. (genengnews.com)
Guanosine1
- In molecular biology, the Guanosine dissociation inhibitors (GDIs) constitute a family of small GTPases that serve a regulatory role in vesicular membrane traffic. (wikipedia.org)
Constants4
- Medicinal enzyme inhibitors often have low dissociation constants , meaning that only a minute amount of the inhibitor is required to inhibit the enzyme. (wikipedia.org)
- The association rate constants for the binding of recombinant human cystatin C to papain, ficin, actinidin and recombinant rat cathepsin B were 1.1 x 10(7), 7.0 x 10(6), 2.4 x 10(6) and 1.4 x 10(6) M-1.s-1, whereas the corresponding dissociation rate constants were 1.3 x 10(-7), 9.2 x 10(-6), 4.6 x 10(-2) and 3.5 x 10(-4) s-1. (lu.se)
- Rate constants and dissociation constants for these reactions fall within the normal range for protease-protease inhibitor interactions. (eurekamag.com)
- The average dissociation constants K(s) were 3.4 and 20.2 μM for MB-COMT and S-COMT, respectively. (lu.se)
Proteins7
- Enzyme inhibitors are a chemically diverse set of substances that range in size from organic small molecules to macromolecular proteins . (wikipedia.org)
- In addition to small molecules, some proteins act as enzyme inhibitors. (wikipedia.org)
- [6] Another class of inhibitor proteins is the ribonuclease inhibitors , which bind to ribonucleases in one of the tightest known protein-protein interactions . (wikipedia.org)
- 1997) Association of the Rho family small GTP-binding proteins with Rho GDP dissociation inhibitor (Rho GDI) in Saccharomyces cerevisiae. (yeastgenome.org)
- GDP dissociation inhibitors are proteins that regulate the GDP-GTP exchange reaction of members of the rab family, small GTP-binding proteins of the ras superfamily, that are involved in vesicular trafficking of molecules between cellular organelles. (thermofisher.com)
- GDIs slow the rate of dissociation of GDP from rab proteins and release GDP from membrane-bound rabs. (thermofisher.com)
- We have purified and characterized several GDP/GTP exchange proteins (GDP dissociation stimulator (GDS) and GDP dissociation inhibitor (GDI)) and GTPase activating Proteins (GAP) for small G proteins. (nii.ac.jp)
Enzyme inhibitor4
- An enzyme inhibitor is a molecule that binds to an enzyme and blocks its activity . (wikipedia.org)
- enzyme (E) accelerates conversion of substrates (S) to products (P). Bottom: by binding to the enzyme, inhibitor (I) blocks binding of substrate. (wikipedia.org)
- An enzyme inhibitor stops ("inhibits") this process, either by binding to the enzyme's active site (thus preventing the substrate itself from binding) or by binding to another site on the enzyme such that the enzyme's catalysis of the reaction is blocked. (wikipedia.org)
- A low concentration of the enzyme inhibitor reduces the risk for liver and kidney damage and other adverse drug reactions in humans. (wikipedia.org)
Receptor2
- 4C, D). We conclude that the dissociation on the agonist receptor complex prevented subsequent antagonist binding for the receptor. (achrinhibitor.com)
- Complex relationships between rates of receptor binding and dissociation appear to strongly influence the durations of action of those DPP-4 inhibitors with comparatively shorter half-lives. (nih.gov)
Inhibits3
- The aim of the present study was to determine whether BAY11‑7082, an inhibitor of the NF‑κB pathway, inhibits the expressions of tissue factor (TF) and plasminogen activator inhibitor‑1 (PAI‑1) in AECⅡ in response to TNF‑α. (spandidos-publications.com)
- Inhibits bacterial growth, possibly by blocking dissociation of peptidyl tRNA from ribosomes, causing RNA-dependent protein synthesis to arrest. (medscape.com)
- C4b-binding protein (C4BP) is the major soluble inhibitor of the classical and lectin pathways whereas factor H (FH) inhibits the alternative route. (lu.se)
Substrate4
- Binding site shown in blue checkerboard, substrate as black rectangle, and inhibitor as green rounded rectangle. (wikipedia.org)
- Reversible inhibitors produce different types of inhibition depending on whether they bind to the enzyme, the enzyme-substrate complex, or both. (wikipedia.org)
- The binding site of inhibitors on enzymes is most commonly the same site that binds the substrate of the enzyme. (wikipedia.org)
- The use of tight-binding inhibitors such as entacapone enabled the estimation of actual enzyme concentrations and, thereby, comparison of velocity parameters, substrate selectivity, and regioselectivity of the methylation of both enzyme forms. (lu.se)
GTPase1
- Prevents the dissociation of GDP from a GTPase, thereby preventing GTP from binding. (ntu.edu.sg)
Vitro1
- IC50 value: 1.9 nM [1] ;Target: ALK;In vitro: The dissociation constant (KD) value of CH5424802 for ALK in an ATP-competitive manner is 2.4 nM. (chemspider.com)
Protease2
- Examples include methotrexate (used in chemotherapy and in treating rheumatic arthritis ) and the protease inhibitors used to treat HIV/AIDS . (wikipedia.org)
- C.hivin.1r and C.hivin.1s react with C.hivin.1-inhibitor to form complexes which contain 1 mol of C.hivin.1-inhibitor per mol of protease monomer. (eurekamag.com)
Rab52
- The mechanism of REP-1-mediated membrane association of Rab5 is similar to that mediated by Rab GDP dissociation inhibitor (GDI). (wikipedia.org)
- Recognition and stabilization of geranylgeranylated human Rab5 by the GDP Dissociation Inhibitor (GDI). (mpg.de)
Irreversible1
- Irreversible inhibitors form a chemical bond with the enzyme such that the enzyme is inhibited until the chemical bond is broken. (wikipedia.org)
Enzymes4
- [2] Enzyme inhibitors also control essential enzymes such as proteases or nucleases that, if left unchecked, may damage a cell. (wikipedia.org)
- Many poisons produced by animals or plants are enzyme inhibitors that block the activity of crucial enzymes in prey or predators . (wikipedia.org)
- Small molecule inhibitors include essential primary metabolites that inhibit upstream enzymes that produce those metabolites. (wikipedia.org)
- P450 isoform-specific inhibitors, monoclonal antibodies directed against P450 isoforms, and recombinantly expressed human P450 enzymes were used to define the P450 isoform profile of PHX 4-monohydroxylations. (aspetjournals.org)
Interaction2
- This behaviour indicates that the contribution of the N-terminal segment of the two inhibitors to the interaction mechanism varies with the target proteinase as a result of structural differences in the active-site region of the enzyme. (lu.se)
- The C.hivin.1r-(C.hivin.1-inhibitor) reaction is inhibited by extremes of ionic strength and has a more marked temperature-dependence than the C.hivin.1s-(C.hivin.1-inhibitor) interaction. (eurekamag.com)
Induce1
- No DPP-4 inhibitor has been shown to inhibit or to induce hepatic CYP-mediated drug metabolism. (nih.gov)
Complement3
- The interactions of the 2 classical serine proteases of the complement [C] system with their natural inhibitor, C.hivin.1[activated C1]-inhibitor, were studied. (eurekamag.com)
- Several of these inhibitors circulate in blood whereas others are expressed on virtually all cells of the body to protect self-tissue from complement attack. (lu.se)
- Most inhibitors act on complement convertases through increased dissociation of these enzymatic complexes (acceleration of decay) or through promoting enzymatic cleavage of activated complement factors C3b or C4b by a serine proteinase factor I (FI). (lu.se)
Bind2
- Enzyme inhibitors may bind reversibly or irreversibly. (wikipedia.org)
- By contrast, reversible inhibitors bind non-covalently and may spontaneously leave the enzyme, allowing the enzyme to resume its function. (wikipedia.org)
Metabolism2
- DPP-4 inhibitor metabolism is widely variable, with reported terminal half-lives ranging from approximately 3 to more than 200 hours. (nih.gov)
- Studying an enzyme's kinetics in this way can reveal the catalytic mechanism of this enzyme, its role in metabolism , how its activity is controlled, and how a drug or a modifier ( inhibitor or activator ) might affect the rate. (wikipedia.org)
Compound1
- Other DPP-4 inhibitors predominantly undergo renal excretion, with 60-85% of each dose eliminated as unchanged parent compound in the urine. (nih.gov)
Interactions2
- Drugs that cause CYP450 drug interactions are referred to as either inhibitors or inducers. (rxlist.com)
- The importance of the N-terminal region of human cystatin C or chicken cystatin for the kinetics of interactions of the inhibitors with four cysteine proteinases was characterized. (lu.se)
Complexes2
- The presence of Ca2+ decreases the rate at which C.hivin.1r complexes with C.hivin.1-inhibitor but does not affect the reactivity of C.hivin.1s. (eurekamag.com)
- The incorporation of C.hivin.1r into C.hivin.1 bound to immune complexes increased the reactivity of C.hivin.1r towards C.hivin.1-inhibitor. (eurekamag.com)
Reaction1
- Heparin stimulates the rate of the reaction of C.hivin.1s with C.hivin.1-inhibitor by a factor of 14-15. (eurekamag.com)
Molecules1
- Many drug molecules are enzyme inhibitors that inhibit an aberrant human enzyme or an enzyme critical for the survival of a pathogen such as a virus , bacterium or parasite . (wikipedia.org)
Incorporation1
- Our model correctly predicts for HIV-1 that resistance against nucleoside analog reverse transcriptase inhibitors (NRTIs) can be conferred by decreasing their incorporation rate, increasing their excision rate, or decreasing their affinity for the polymerase enzyme. (plos.org)
Hepatic1
- With the exception of the primary hydroxylated metabolite of saxagliptin, which is 2-fold less potent than its parent molecule, metabolic products of hepatic biotransformation are minimally active and none appreciably contribute to either the therapeutic or the toxic effects of DPP-4 inhibitors. (nih.gov)
Activation1
- We recently showed that NANOG-mediated induction of Aurora A kinase (AURKA), an upstream kinase for aPKCζ, and repression of Lethal Giant Larva 2 (LGL2 or LLGL2), an aPKCζ inhibitor, leads to aPKCζ upregulation and activation. (nature.com)
Reactions1
- CYP450 inhibitors are used to minimize or prevent such reactions. (rxlist.com)
Concentration1
- Numerical differences in maximum (peak) plasma drug concentrations and areas under the plasma concentration-time curve among the DPP-4 inhibitors vary by an order of magnitude. (nih.gov)
Activity2
- Enzyme inhibitors play an important role in all cells, since they are generally specific to one enzyme each and serve to control that enzyme's activity. (wikipedia.org)
- [7] A special case of protein enzyme inhibitors are zymogens that contain an autoinhibitory N-terminal peptide that binds to the active site of enzyme that intramolecularly blocks its activity as a protective mechanism against uncontrolled catalysis. (wikipedia.org)
Cells1
- Pulmonary inflammation can damage pulmonary vascular endothelial cells and type-II alveolar epithelial cells (AECII), which further increases the expression of tissue factor (TF) and plasminogen activator inhibitor-1 (PAI-1) in these cells, thus activating the exogenous coagulation system. (spandidos-publications.com)
Disease1
- Dipeptidyl peptidase-4 (DPP-4) inhibitors collectively comprise a presently unique form of disease management for persons with type 2 diabetes mellitus. (nih.gov)
Acute1
- Hydrochloric acid (HCl) and carbonic anhydrase inhibitors may be used in some acute situations. (medscape.com)
Rate4
- N-Terminal truncation of the first ten residues of the inhibitor negligibly affected the association rate constant with papain or ficin, but increased the dissociation rate constant approx. (lu.se)
- 60-fold, while minimally affecting the dissociation rate constant. (lu.se)
- 15-fold higher dissociation rate constant than the intact inhibitor. (lu.se)
- The decreased affinity of human cystatin C or chicken cystatin for cysteine proteinases after removal of the N-terminal region is thus due to either a decreased association rate constant or an increased dissociation rate constant, or both, depending on the enzyme. (lu.se)
Similar1
- Systematic reviews of clinical trials suggest that the overall efficacy of DPP-4 inhibitors in patients with type 2 diabetes generally is similar. (nih.gov)
Calculated the association1
- We calculated the association and dissociation prices, the KD and the binding energy by utilizing the Markov fit and compared these values with these we Caspase 3 supplier obtained from our original experiments applying ,-meATP as an agonist. (achrinhibitor.com)
Target1
- Since anti-pathogen inhibitors generally target only one enzyme, such drugs are highly specific and generally produce few side effects in humans, provided that no analogous enzyme is found in humans. (wikipedia.org)
Process1
- We provide evidence that KRas translocation occurs through sequestration of the polybasic-prenyl motif by Ca 2+ /calmodulin (Ca 2+ /CaM) and subsequent release of KRas from the PM, in a process reminiscent of GDP dissociation inhibitor-mediated membrane recycling of Rab and Rho GTPases. (rupress.org)
Results1
- This in turn results in aPKCζ-mediated NUMB phosphorylation, NUMB dissociation from p53, and p53 degradation (Fig. 1a ) 12 . (nature.com)
Capacity1
- However, functional capacity measured in terms of glucose-lowering ability remains comparable among all available DPP-4 inhibitors. (nih.gov)
Small1
- [3] [2] Small molecule enzyme inhibitors also include secondary metabolites , which are not essential to the organism that produces them, but provide the organism with an evolutionary advantage, in that they can be used to repel predators or competing organisms or immobilize prey. (wikipedia.org)
Research1
- Hence the discovery and refinement of enzyme inhibitors is an active area of research in biochemistry and pharmacology . (wikipedia.org)