Receptors hybrid

Barboiu, M. (2004) Supramolecular polymeric macrocyclic receptors-hybrid carrier vs. channel transporters... 

Receptor models presently in use can be classified into one of four categories chemical mass balance, multivariate, microscopic, and source/receptor hybrids. Each classification will be treated individually, though it will become apparent that they are closely related. 

Two more sets of observables are Introduced Into the hybrid models the emissions factors and the dispersion factors. It Is the difficulty of quantifying these that led to the use of a receptor model over the source model In the first place, so It would seem there Is little advantage In reintroducing them. The advantage of the hybridization Is that the number of Individual emission and dispersion factors can be considerably reduced and that the relative values rather than the absolute values are used. These relative values are more accurate In most cases. Still, the uncertainties of emission and dispersion factors need to be evaluated and Incorporated Into any source/receptor hybrid model. 

Source Characterization. All receptor models, even the source/receptor hybrids, require input data about the particulate matter sources. The multivariate models, which can conceivably be used to better estimate source compositions, require an initial knowledge of the chemical species associations in sources. 

Di Marzo V, Bisogno T, De Petrocellis L, Brandi I, Jefferson RG, Winckler RL, Davis JB, Dasse O, Mahadevan A, Razdan RK, Martin BR (2001) Highly selective CBI cannabinoid receptor ligands and novel CB 1/VR1 vanilloid receptor hybrid ligands. Biochem Biophys Res Commun 281 444-451... 

B cells do not express T-cell receptors. Hybridization of T-cell cDNAs with B-cell mRNAs removes cDNAs that are expressed in both cells. Hence, the mixture of cDNAs follovUng... 

Di Marzo, V., Bisogno, T., De Petrocellis, L., et al. (2001) Highly selective CBl cannabinoid receptor ligands and novel CBl/VRl vanilloid receptor hybrid Ug-ands. Biochem. Biophys. Res. Cotrmm. 281,444-451. 

The Liskamp group also examined the ability of peptoid-peptide hybrids to be bound by the MHC Class II receptor, an important component of the human immune system [39]. Two of three peptoid substitutions in the 14-residue peptide caused substantial decreases in binding affinity, despite the fact that these were solvent-exposed residues. These results were attributed to a loss of hydrogen-bond contacts as well as to steric clashes caused by unfavorable positioning of the new side chain groups. 

Varady J, Wu X, Fang X, Min J, Hu Z, Levant B, Wang S. Molecular modeling of the three-dimensional structure of dopamine 3 (D3) subtype receptor discovery of novel and potent D3 ligands through a hybrid pharmacophore-and structure-based database searching approach. / Med Chem 2003 46 4377-92. 

Fig. 9.4 Upregulation of MCPl and CCR2 expression in neurons of the dorsal root ganglia in association with the development of neuropathic pain. Upper panels illustrate expression of CCR2 receptors by in situ hybridization in naive rats (a) and animals subjected to Chronic Compression of the DRG (CCD) a model for neuropathic pain (b). CCR2 is expressed in small sateUite cells and many neurons (white arrows). Bottom panels (c, d) illustrate the expression of MCP-1 (immu-nohistochemistry, red) under the same circumstances. Many neurons (red arrows) express the chemokine (From White et al. 2005)...

Following on from this, and to further exemplify this pharmacophore model, Huffman [182] described a novel hybrid structure that combined the hydroxydibenzopyran ring of THC and the indole moiety of the AAIs into one molecule. It was found that the hybrid molecule (270) had a similar affinity (19 nM) for the CBi receptor in vitro as (67) (41 nM). The compound was also active in vivo in the mouse tetrad model of cannabimimetic activity and had comparable potency to (67) [182]. 

Strotmann J., Wanner I., Helfrich T. and Breer H. (1995). Receptor expression in olfactory neurons during rat development in situ hybridization studies. Eur J Neurosci 7, 492-500. 

Bryant This has not been studied in Drosophila. Several Dig-like MAGUKs have been picked up in a yeast two-hybrid screen using as bait the Erb-B4 receptor (Garcia et al 2000), which is the only one of the mammalian EGF receptor family that has a C-terminus predicted to bind to PDZ domains. This interaction could be involved in controlling receptor localization. Potentially it is the same kind of interaction. 

Sato, K., Zhang, J. H., Saika, T. et al. (1991). Localization of glycine receptor alpha 1 subunit mRNA-containing neurons in the rat brain an analysis using in situ hybridization histochemistry. Neuroscience 43, 381-95. 

---