Soluble Receptors

Mwatha, J.K., Kimani, G., Kamau, T., Mbugua, G.G., Ouma, J.H., Mumo, J., Fulford, A.J., Jones, F.M., Butterworth, A.E., Roberts, M.B. and Dunne, D.W. (1998) High levels of TNF, solubleTNF receptors, soluble ICAM-1 and IFN-gamma, but low levels of IL-5, are associated with hepatosplenic disease in human schistosomiasis mansoni. The Journal of Immunology 160, 1992-1999. 

Sublingual immunotherapy Allergy Interleukin-2 receptor Soluble intercellular adhesion molecule-1 Immunoglobulin G4 sE-selectin Interleukin Immunoglobulin E... 

Intracellular receptors include both nuclear receptors and cytoplasmic receptors, soluble proteins that are localised within the nucleoplasm and the cytoplasm, respectively. Typical ligands include the steroid hormones (e.g. testosterone, progesterone, cortisol) and derivatives of vitamins A and D, which freely diffuse through the plasma membrane. 

Stem cell factor (SCF) is a dimeric protein that stimulates hematopoietic progenitor cells in bone marrow. The interaction of SCF expressed in E. coli and its receptor, soluble Kit (sKit), was studied (5). The extinction coefficient of the SCF was obtained as 0.534 by using Gill s amino acid composition method and 0.585 by using the method described in this paper [note 0.62 ml/(mg-cm) was reported in reference 11 by the amino acid analysis method]. In this complicated case, a self-consistent three-detector method described in reference 2 was used to determine the stoichiometry of the complex. The results of using these two extinction coefficients are summarized in tables IIIA and IIIB. Both results indicate that the stem cell factor dimerizes its receptor, sKit. 

For some cytokine receptors, including the growth hormone receptor and several interleukin receptors, soluble isoforms have been described that comprise all or part of the extracellular domain and may be able to bind the extracellular ligands. By association with other subunits of heterooligomeric receptors, e. g., the gpl30 subunit, these soluble isoforms can function as agonists or antagonists. 

Two types of soluble binding protein have been described, nonspecific serum proteins and cytokine-specific soluble receptor proteins. The major nonspecific serum protein capable of binding cytokines appears to be a2-macroglobuIin (B57, B58, Mil). A number of soluble cytokine inhibitors related to the relevant receptor have been described. The soluble form of the IL-2R a chain has been found in the serum of apparently normal individuals and is increased in the serum of individuals with inflammatory diseases such as rheumatoid arthritis (W31). Similar molecules have been described for IL-1, IL-6, IFNy, and IL-7 (F7, N14, S62). The mechanism of release has not been properly established but appears to require proteolytic cleavage of the membrane-bound receptor. Soluble inhibitors for two other cytokines, IL-4 and TNF, appear to be derived by alternative RNA splicing sites that give rise to receptors lacking a transmembrane sequence and that are secreted (M50, S22). 

Following its synthesis NO, both in endothelial cells and in the adjacent smooth muscle cells, activates what has been termed its intracellular receptor, soluble guanylate cyclase. NO binds to the heme iron in the catalytic domain of the enzyme and by increasing its activity leads to an enhanced formation of cGMP (Drexler et al., 1989 Martin et al.,... 

Transferrin (asialo, tan, beta-2-) Transferrin receptor (soluble) Transthyretin... 

Targets Intracellular (kinases) Extracellular (cell surface receptors, soluble ligands)... 

Indazoles may be assembled via thermolysis as well. Treatment of diphenylcarbamoyl chloride with sodium azide gives rise to diphenyl-carbamoyl azide. Thermolysis of the diphenyl-carbamoyl azide then afforded indazolol. Subsequent alkylation of the indazolol then produced a series of indazole derivatives as activators of the nitric oxide receptor, soluble guanylate cyclise. 

Rec tor. Receptors are membrane-bound or soluble proteins or protein complexes exerting a physiological effect after binding of an agonist. 

Moreover, multivariate optimization, the simultaneous optimization of several properties, will increasingly come into focus. A drug should have high selectivity in binding to different receptors and minimal toxicity, good solubility and penetration, and so on. A hair color should have a brilliant shine, be absorbed well, not be washed out, not damage the hair, not be toxic, and be stable under sunlight, etc. 

Gustation. A taste sense, the receptors of which He in the mucous membrane covering the tongue, and the stimuli for which consist of certain soluble chemicals, eg, salts, acid, and sugar. 

Diphenoxylate Hydrochloride. l-(3-Cyano-3,3-diphenylpropyl)-4-phenyl-4-piperidinecarboxyhc acidmonohydrochlorhydrate [3810-80-8] (Lomotil) (13) is a white, odorless, crystalline powder that melts at 220—226°C. It is soluble ia methanol, spariagly soluble ia ethanol and acetone, slightly soluble ia water and isopropyl alcohol, freely soluble ia chloroform, and practically iasoluble ia ether and hexane. The method of preparation for diphenoxylate hydrochloride is available (11). Diphenoxylate hydrochloride [3810-80-8] (13) is an antidiarrheal that acts through an opiate receptor. It has effects both on propulsive motility and intestinal secretion. Commercial forms are mixed with atropiae to discourage abuse. 

FK-506 (37) interferes with IL-2 synthesis and release and has a cyclosporin-like profile, but is considerably more potent in vitro. IC q values are approximately 100-fold lower. This neutral macroHde suppresses the mixed lymphocyte reaction T-ceU proliferation generation of cytotoxic T-ceUs production of T-ceU derived soluble mediators, such as IL-2, IL-3, and y-IFN and IL-2 receptor expression (83). StmcturaHy, FK-506 is similar to sirolimus. Mycophenolate mofetil (33), brequinar (34), and deoxyspergualin are in various phases of clinical evaluation. Identification of therapeutic efficacy and safety are important factors in the deterrnination of their utiUty as immunosuppressive agents. 

Acetylcholine. Acetylcholiae (ACh) (1) is a crystalliae material that is very soluble ia water and alcohol. ACh, synthesized by the enzyme choline acetyltransferase (3), iateracts with two main classes of receptor ia mammals muscarinic (mAChR), defiaed oa the basis of the agonist activity of the alkaloid muscarine (4), and nicotinic (nAChR), based on the agonist activity of nicotine (5) (Table 1). m AChRs are GPCRs (21) n AChRs are LGICs (22). 

Administration of dipyridamole-AMP to mice 5—25 min after 1 Gy (100 rad) of TBI y-kradiation is also protective, as indicated by plasma thymidine levels and the amount of saline soluble polynucleotides in the thymus (112). Adding dipyridamole-AMP to in vitro kradiated suspensions of thymocytes enhances the rejoining of DNA strand breaks (112). These post-kradiation effects ate presumably mediated by the activation of extraceUulat adenosine receptors. 

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