Inhibition partial

Among one of the more unusual side effects noticed as the use of the sulfonamides became widespread was the increased urine output of many patients treated with these drugs. The fact that the urine was unusually alkaline led to the suspicion, later (Confirmed by independent means, that these agents were responsible for partial inhibition of the enzyme carbonic anhydrase. Inhibition of this enzyme causes increased excretion of sodium and bicarbonate ions as well as water, in effect bringing about diure-... 

It has been only found that some antioxidants and light stabilizers show the ability for partial inhibition of thermal destruction of the polyolefins. 

Most antiplatelet dtugs only partially inhibit platelet activation. In contrast, blockers of GPIIb/llla interfere at the end of the pathway common to platelet aggregation. They prevent fibrinogen and vWf from... 

The most popular assumption for the action of cardiac glycosides is that an inhibition or partial inhibition may induce inotropy of the heart by raising intracellular... 

There are several hundred reported NF-kB inhibitors (see www.nf-kb.org for a complete and updated list). These inhibitors include natural products, chemicals, metabolites, and synthetic compounds. A large majority of these products, in particular commonly used antiinflammatory drugs such as corticosteroids and the nonsteroidal antiinflammatory drugs (NSADDs) aspirin, sulindac, ibuprofen and sulphasalazine, have the ability to partially inhibit NF-kB activity in cell culture. However, the precise mechanism of action and the specific molecular targets of most of these inhibitors remain unclear. 

Figure 4.5 Illustration ofthe concepts of potency that is, it is potent but not very effective. Inhibitor and effectiveness for two enzyme inhibitors. B shows less affinityfortheenzyme (high /<,), but Inhibitor A has a strong affinity for the enzyme it is a much more effective inhibitor when (low ff ), but even when it is maximally bound to maximally bound-that is, it is notvery potent but the enzyme it only achieves partial inhibition - is effective.

Multiple feedback loops can provide additional fine control. For example, as shown in Figure 9—5, the presence of excess product B decteases the tequitement for substrate 3. Howevet, Sj is also tequited fot synthesis of A, C, and D. Excess B should thetefote also curtail synthesis of all font end products. To circumvent this potential difficulty, each end product typically only partially inhibits catalytic activity. The effect of an excess of two or more end products may be strictly additive or, alternatively, may be greater than their individual effect (cooperative feedback inhibition). 

Chemical modification studies with fluorescein-5 -isothiocyanate support the proximity of Lys515 to the ATP binding site [98,113-117,212,339]. Fluorescein-5 -isothiocyanate stoichiometrically reacts with the Ca -ATPase in intact or solubilized sarcoplasmic reticulum at a mildly alkaline pH, causing inhibition of ATPase activity, ATP-dependent Ca transport, and the phosphorylation of the Ca " -ATPase by ATP the Ca uptake energized by acetylphosphate, carbamylphos-phate or j -nitrophenyl phosphate is only partially inhibited [113,114,212,339]. The reaction of -ATPase with FITC is competitively inhibited by ATP, AMPPNP, TNP-ATP, and less effectively by ADP or ITP the concentrations of the various nucleotides required for protection are consistent with their affinities for the ATP binding site of the Ca -ATPase [114,212,340]. 

Before trying to interpret this partial inhibition of S by PCP, we need to consider the influence of membrane potential on the 86Rb efflux. To obtain information about the relationship between component S and membrane potential, we measured S (increase in the slope of 86Rb efflux between 2 and 4 seconds) as a function of [K]0 in the efflux solution, in the absence of drug. These data are shown in figure 3 (solid circles) the calculated depolarization, due to increasing [K]0, is given in the upper abscissa seale. 

CCR8 Effector T cells (Th2) I-309/CCL1 Yes Partial inhibition... 

Less, but still significant, information is available on the surface chemistry of other nitrogen oxides. In terms of N20, that molecule has been shown to be quite reactive on most metals on Rh(110), for instance, it decomposes between 60 and 190 K, and results in N2 desorption [18]. N02 is also fairly reactive, but tends to convert into a mixed layer of adsorbed NO and atomic oxygen [19] on Pd(lll), this happens at 180 K, and is partially inhibited at high coverages. Ultimately, though the chemistry of the catalytic reduction of nitrogen oxide emissions is in most cases controlled by the conversion of NO. 

Zeng, B.F., MacDonald, J.R., Bann, J.G., Reck, K., Gambee, J.E., Boswell, B.A. and Bachinger, H.P. (1998) Chicken FK506-binding protein, FKBP65, a member of the FKBP family of peptidylprolyl cis-lrans isomerases, is only partially inhibited by FK506. BiochemicalJournal 330, 109-114. 

Figure 6. A plot of S(x)/SD(x) versus f for a network in which junction fluctuations are partially inhibited (k 0) and where molecular deformations are less than...

This method was first reported by Winston and others (1998) and it is based on the oxidation of alpha-kclo-y-mcthiolbutyric acid (KMBA) to ethylene by peroxyl radicals produced from AAPH. The ethylene formation, which is partially inhibited... 

Peng, M., Huang, L., Xie, Z., Huang, W. H. and Askari, A. Partial inhibition of Na+/K+-ATPase by ouabain induces the Ca2+-dependent expressions of early-response genes in cardiac myocytes. /. Biol. Chem. 271 10372-10378,1996. 

H, receptors also can stimulate the activity of phospholipase A2 (PLA2), with the subsequent release of arachido-nate and its metabolites. In platelets, this response does not require activation of the phosphoinositide cycle and is inhibited by pertussis toxin, suggesting a second, distinct Gj/o-protein-mediated transduction mechanism. In cells transfected with the H, receptor, PLA2 activation is partially inhibited by pertussis toxin, also suggesting at least two transduction systems [30,34],... 

Exposure to trichothecenes at levels that partially inhibit translation upregulates expression of many inflammatory and immune-related genes including macrophage, Thl and Th2 cytokines as well as chemokines, cyclooxygenase 2 and inducible nitric oxide synthase.1518 Contrastingly, suppressive effects of trichothecenes on leukocyte function are intimately linked with the induction of apoptosis as has been demonstrated in macrophages, T cells and B cells both in vivo and in vitro.19-20... 

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