Receptor-peptide interactions

Another feature of the Zap-70-T-ceU receptor peptide interaction which is particularly intriguing is that the pTyr binding pocket for the... 

Simantov, R. Childers, D. and Snyder, S. The opiate receptor binding interactions of 3Hmethionine enkephalin, an opioid peptide. Fur J. Pharmacol 47 319-331, 1978. 

Ni Q., Xu H., Partilla J. et al. Opioid peptide receptor studies. Interaction of opioid peptides and other drugs with four subtypes of the K2 receptor in guinea pig brain. Peptides. 16 1083, 1995. 

Garcia, K. C. and Teyton, L. (1998), T-cell receptor peptide-MHC interactions biological lessons from structural studies , Curr. Opinion Biotechnol., 4, 338-343. 

The first identified Ascaris FaRP, AF1 (KNEFIRFamide), and the structurally related peptide, AF2 (KHEYLRFamide), have been found to inhibit locomotory waves when injected into adult worms (Cowden et al., 1989 Cowden and Stretton, 1993). Their effects on body-wall muscle strips are biphasic, comprising a transient relaxation followed by an extended period of increased contractile activity (Maule et al., 1995b Bowman et al., 1996). When using muscle strips that have had the motor nerve cords removed, only the inhibitory actions of AF1 and AF2 are seen (Maule et al., 1995b). This suggests that the inhibitory phase is due to post-synaptic effects on body-wall muscle in the worm. In contrast, the excitatory effects are nerve-cord dependent and are not observed in muscle strips that have been denervated. Another possibility is that the peptides interact with receptors at the post-synaptic junction - these are also removed in specimens that have had the motor nerve cords removed. 

Blake AD, Bot G, Reisine T. Structure-function analysis of the cloned opiate receptors peptide and small molecule interactions. Chem Biol 1996 3 967-972. 

Jason Kindrachuk is a postdoctoral fellow at the University of British Columbia (UBC) in the laboratory of Professor R. E. W. Hancock. Jason received his Ph.D. from the University of Saskatchewan in 2007 where his research focused on host and pathogen sensory systems. During his study he specially focused on TLR-9 receptor—ligand interactions and the interactions between host defense peptides and the PhoPQ two-component sensory system of Salmonella typhimurium. In 2008 Jason received the Canadian Cystic Fibrosis Foundation Kin Canada Fellowship for his research in the area of alternative therapies for treatment of antibiotic- and multidrug-resistant bacteria. Currently his research is focused on the investigation of structure-activity relationships amongst natural and synthetic host defense peptides from the perspective of associated immunomodulatory activities and as well as vaccine formulation strategies. 

Pearce KH, larmone MA, Simmons CA, et al. Discovery of novel nuclear receptor modulating ligands an integral role for peptide interaction profiling. Drug Discov Today 2004 9 741-51. 

The possibility to carry out conformational studies of peptides at low concentrations and in the presence of complex biological systems represents a major advantage of fluorescence spectroscopy over other techniques. Fluorescence quantum yield or lifetime determinations, anisotropy measurements and singlet-singlet resonance energy transfer experiments can be used to study the interaction of peptides with lipid micelles, membranes, proteins, or receptors. These fluorescence techniques can be used to determine binding parameters and to elucidate conformational aspects of the interaction of the peptide with a particular macro-molecular system. The limited scope of this chapter does not permit a comprehensive review of the numerous studies of this kind that have been carried and only a few general aspects are briefly discussed here. Fluorescence studies of peptide interactions with macromolecular systems published prior to 1984 have been reviewed. 

Strong evidence indicates at least a familial pattern and perhaps a hereditary basis for some types of alcoholism ( 393). More recent data show that genotype accounts for approximately 33% of the overall variance in liability ( 394). In addition, specific neurocircuitry and neurochemical systems appear to be important in the etiology of alcoholism (395). Thus, positive reinforcement may be mediated by activation of g-aminobutyric acid (GABA) receptors, release of opioid peptides and dopamine, inhibition of glutamate receptors, and interactions with the 5-HT system. Furthermore, neurobehavioral effects of alcohol and their association with these various neurotransmitters serve as potential targets for novel drug therapies. 

Varying the side groups X in 27b affects both the stability and selectivity of the complexes (lateral discrimination), and allows the receptor-substrate interactions in biological systems to be modelled, for instance, the interaction between nicotinamide and tryptophan [2.109b]. One may attach to 27b amino acid residues (leading to parallel peptides [2.109] as in 27c), nucleic acid bases or nucleosides, saccharides, etc. The structural features of 27 and its remarkable binding properties make it an attractive unit for the construction of macropolycyclic multisite receptors, molecular catalysts, and carriers for membrane transport. Such extensions require sepa-... 

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