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Inhibitor, receptor binding

Matrosovich M, Klenk H-D (2003) Natural and synthetic sialic acid-containing inhibitors of influenza virus receptor binding. Rev Med Virol 13 85-97 Matrosovich MN, Matrosovich TY, Gray T, Roberts NA, Klenk H-D (2004) Neuraminidase is important for the initiation of influenza virus infection in human airway epithelium. J Virol 78 12665-12667... [Pg.150]

Reddy, DS and Kulkarni, SK (1998) The role of GABA-A and mitochondrial diazepam-binding inhibitor receptors on the effects of neurosteroids on food intake in mice. Psychopharmacology 137 391-100. [Pg.424]

B-Lactamase inhibitors, 31 (1994) 297 Leprosy, chemotherapy, 20 (1983) 1 Leukocyte elastase inhibition, 31 (1994) 59 Leukotriene D4 antagonists, 38 (2001) 249 Ligand-receptor binding, 23 (1986) 41 Linear free energy, 10 (1974) 205... [Pg.388]

Etanercept is a fully human dimeric fusion protein composed of human TNF-a p75 receptor fused to the Fc portion of human IgG 1.41 It acts as a tumor necrosis factor-a (TNF-a) inhibitor by binding to and inactivating TNF-a, thus preventing interactions with its cell surface receptors.41 This agent is useful for chronic moderate to severe plaque psoriasis and for psoriatic... [Pg.956]

To be successful, SAR studies must be adapted to P-gp by implementing membrane partitioning of substrates, modifiers or inhibitors as suggested previously [36]. The aim of the present chapter is to evaluate the contribution of (i) membrane partitioning and (ii) receptor binding proper to the apparent binding of a compound to P-gp. [Pg.464]

S. Langermann, el al., Receptor binding studies disclose a novel class of high-affinity inhibitors of the Escherichia coli FimH adhesin, Mol. Microbiol., 55 (2005) 441 155. [Pg.363]

What are the mechanisms by which trichothecenes exert their transcriptional and post-transcriptional effects The 60S ribosomal subunit is a well-known molecular target of trichothecenes in leukocytes and other actively proliferating eukaryotic cells,3 whereas attempts to demonstrate alternative receptors have not been successful.37 38 Translational inhibitors that bind to ribosomes rapidly activate mitogen-activated protein kinases (MAPKs) and apoptosis via a mechanism termed the ribotoxic stress response. 39-40... [Pg.295]

The triazolobenzodiazepines alprazolam (19a) and triazolam (19b) are widely used psychotropic drugs. These compounds are also specific inhibitors of PAF-induced human platelet aggregation with respective IC50 values of ca. 5 and 3 /rM [117], rabbit platelet aggregation with IC50 values of 2.5 and 0.6 [166], and [3H]PAF receptor binding on human platelets (IC50... [Pg.338]

Flavonoids Sigma receptor binding PKC inhibitor PTKinase inhibitor IL-6 inhibitor Opioid jL/ and k binding... [Pg.259]

Rommelspacher H, Nanz C, Borbe HO, Fehske KJ, Muller WE, Wollert U. (1980). 1-Methyl-beta-carboline (harmane), a potent endogenous inhibitor of benzodiazepine receptor binding. Naunyn Schmiedebergs Arch Pharmacol. 314(1) 97-100. [Pg.549]

Figure 8 Ubiquitin and endocytosis. Receptors on the plasma membrane undergo monoubiquitination as a result of ligand (e.g., neurotransmitter). Ubiquitinated receptors bind to proteins called epsins, which in turn interact with adaptor proteins (adaptin) bound to clathrin-coated pits. Ubiquitination also functions to sort the internalized membrane protein into early endosomes, which directs them to degradation by lysosome through the multivesicular body. If ubiquitin from the endocytosed receptors is removed by an UBP, the receptor recycles back to the membrane. Proteasome inhibitors block endocytotic degradation of some proteins such as glutamate receptor subunits indicating a possible role for the proteasome. Figure 8 Ubiquitin and endocytosis. Receptors on the plasma membrane undergo monoubiquitination as a result of ligand (e.g., neurotransmitter). Ubiquitinated receptors bind to proteins called epsins, which in turn interact with adaptor proteins (adaptin) bound to clathrin-coated pits. Ubiquitination also functions to sort the internalized membrane protein into early endosomes, which directs them to degradation by lysosome through the multivesicular body. If ubiquitin from the endocytosed receptors is removed by an UBP, the receptor recycles back to the membrane. Proteasome inhibitors block endocytotic degradation of some proteins such as glutamate receptor subunits indicating a possible role for the proteasome.
Fig. 2 X-ray co-crystal structure of diketopiperazine-chitinase complex (PDB ID IWIP). Dike-topiperazine inhibitor is shown as yellow sticks, and the receptor binding site is shown as transparent surface. The hydrogen bonding with the key Trp97, Tyr214, and water (cyan ball) is shown as yellow dots... Fig. 2 X-ray co-crystal structure of diketopiperazine-chitinase complex (PDB ID IWIP). Dike-topiperazine inhibitor is shown as yellow sticks, and the receptor binding site is shown as transparent surface. The hydrogen bonding with the key Trp97, Tyr214, and water (cyan ball) is shown as yellow dots...

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See also in sourсe #XX -- [ Pg.99 ]




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