Amino acids receptor binding

McDonald J. W., Garofalo E. A., Hood T., Sackellares C., Gilman S., McKeever P. E., Troncoso J. C., and Johnston M. V. (1991). Altered excitatory and inhibitory amino acid receptor binding in hippocampus of patients with temporal lobe epilepsy. Ann. Neurol. 29 529-541. 

Cyclosporine A (CsA) is a water-insoluble cyclic peptide from a fungus composed of 11 amino acids. CsA binds to its cytosolic receptor cyclophilin. The CsA/cyclophilin complex reduces the activity of the protein phosphatase calcineurin. Inhibition of this enzyme activity interrupts antigen receptor-induced activation and translocation of the transcription factor NEAT to the nucleus which is essential for the induction of cytokine synthesis in T-lymphocytes. 

Although the single amino acids cannot bind the adhesion receptors on cells, they provide other ehemieal functional groups which may improve the adsorption of eell adhesion-mediating molecules on the material surface. Similar efifeet was observed on ion-implanted polyethylene grafted with the Arg-Gly-Asp (RGD)... 

The DNA-binding of the steroid hormone receptor occurs via an approx. 60 amino acid DNA-binding domain with two zmc-Cys4-motrfs (see also 4.3.2). The structure displays two so-called helix-loop-hehx elements, each with a boimd Zn ion (Fig. 1.6). 

Both phencyclidine and ketamine bind with high affinity to a number of receptors in the brain, but it is now accepted that the primary target is the sigma-PCP receptor site located in the ion channel of the NMDA excitatory amino acid receptor complex. The precise function of this receptor in the brain is still the subject of debate. It is now known that there are two distinct sigma receptor sites in the mammalian brain (ctj and a2) which are not associated with the NMDA receptor complex. Haloperidol and the atypical neuroleptic remoxipride bind with high affinity to such sites, and it has been postulated that some typical and atypical neuroleptics may owe some of their pharmacological effects to their action on such receptors. 

Ketamine binds to the excitatory amino acid receptor known as theN-methyl-D-aspartate (NMDA) receptor complex, which regulates calcium flow through an ion channel (Figure 4.4). Therefore, ketamine s direct action is to block the movement of calcium through this channel.56... 

All members of the steroid/nuclear receptor superfamily have the same overall structural organization (Fig. 3) (39). The 66 amino acid DNA binding domain (DBD) is in the middle... 

Domoic acid (CAS 14277-97-5, C15H21NO6) is produced by Nitzchia pungens. The toxin accumulates in the hepatopancreas of mussels, scallops, and other filter-feeding shellfish. Heat-stable neurotoxic domoic acid is similar in structure to the excitatory dicarboxylic amino acid, kainic acid, and has an antagonistic effect at the glutamate receptor. Domoic acid acts as a potent excitatory neurotransmitter, and it binds to excitatory amino acid receptors in the central nervous system in invertebrates. 

The protein structure model, based on X-ray crystallography, represents the 66 amino-acid DNA binding domain of the glucocorticoid receptor (Luisi, B. F., Xu, W. X., Otwinowski, Z., Freedman, L. P.,... 

The amino acid glycine binds to pentameric glycine receptors (similar structure as nAChR) which are ligand-gated Cl- channels. Inhibitory glycinergic neurons are in the brain stem and spinal cord and regulate involuntary motoric via Renshaw interneurons. 

Due to their high selectivity, DER and DEL were the basis for an extensive structure activity relationship study aimed to understand the essential requisites of p. and 8 activity. More than 200 analogues of DER and DEL C were synthesized, and the role of each amino acid in binding to p and 8 receptors and bioactivity was defined [21-31]. New synthetic products were prepared such as oxymorphindole and related derivatives [32], and (+)-4-[(alfa R)-alfa-((2S,5R)-4-allyl-2.5-dimethyl-l-piperazin-yl)-3-methoxy-benzyl]-N, diethylbenzamide [33]. These products are under investigation for their clinical relevance and provide potential nonpeptide ligands for studies on delta-opioid-receptor. 

Young, A.B. and Egg, G.E. (1991) Excitatory amino acid receptors in the brain membrane binding and receptor autoradiographic approaches. In D. Lodge and G.L. Collin-gridge (Eds.), Trends in Pharmacological Sciences. The Pharmacology of Excitatory Amino Acids, Special Report, Elsevier, Amsterdam, pp. 18-24. 

The next step is to translate this interaction field into a model of the receptor which is composed from single isolated amino acids with chemical properties that satisfy the different types of binding present in the pharmacophore. The relative three-dimensional positions of the amino acid binding sites are defined by the corresponding GRIN/GRID results. The resulting amino acid receptor model is sometimes called a pseudoreceptor. ... 

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