Receptor Modulating Peptide

The dopamine receptor modulating peptide Pro-Leu-Gly-NH2 (PLG) selectively enhances the binding of agonists to dopamine receptors in the mammalian central nervous system. Johnson and co-workers at the University of Minnesota and McMaster University have prepared bicyclic 5,5- and 6,5-thiazolidine lactam peptidomimetics (82, 83) in an attempt to elucidate the bioactive conformations of PLG. 

PLG is believed to exist in a type II p-turn in its bioactive conformation. The random incremental pulse search (RIPS)-MM2 conformational scanning algorithm was used to predict the manner in which the 5,5- and 5,6-bicyclic thiazolidine lactam ring systems would restrict the tli2 and )3 torsional angles, two of the angles that define a p-turn. These studies revealed that low energy conformations of both model compounds present torsional values close 

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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. 

E. J. Trybulski (2001). Vasopressin receptor modulators from non-peptide antagonists to... 

Smith BN, Davis SF, van den Pol AN et al (2002) Selective enhancement of excitatory synaptic activity in the rat nucleus tractus solitarius by hypocretin 2. Neuroscience 115 707-14 Smith-White MA, Herzog H, Potter EK (2002) Role of neuropeptide Y Y2 receptors in modulation of cardiac parasympathetic neurotransmission. Regul Peptides 103 105-11 Stanford IM, Cooper Al (1999) Presynaptic mu and delta opioid receptor modulation of GABAa IPSCs in the rat globus pallidus in vitro. 1 Neurosci 19 4796 4803 Starke K (1977) Regulation of noradrenaline release by presynaptic receptor systems. Rev Physiol Biochem Pharmacol 77 1-124... 

Dixit VD, Schaffer EM, Pyle RS, CoUins GD, Sakthivel SK, Palaniappan R, I.illaid JW, Taub DD (2004) Ghrelin inhibits leptin- and activation-induced proinflammatory cytokine expression by human monocytes and T cells. J CUn Invest 114 57-66 Dmitrieva N, Shelton D, Rice ASC, McMahon SB (1997) The role of nerve growth factor in a model of visceral inflammation. Neuroscience 78 449-459 Doak GJ, Sawynok J (1997) Formalin-induced nodceptive behavior and edema involvement of multiple peripheral 5-hydroxytryptamine receptor subtypes. Neuroscience 80 939-949 Dobner PR (2006) Neurotensin and pain modulation. Peptides 27 2405-2414 Dobolyi A, Ueda H, Uchida H, Palkovits M, Usdin TB (2002) Anatomical and physiological evidence for involvement of tuberoinfundibular peptide of 39 residues in nociception. Proc Natl Acad Sci U S A 99 1651-1656... 

Multiple mechanisms are probably involved in immune-modulating effects of AMPs. A variety of receptors has been described for cathelicidins, however, only one biological function, that of LL-37-mediated chemotaxis of human peripheral blood leukocytes, is associated with a known receptor (formyl peptide receptor like 1), [187]. Human BD-2 recruits mast cells and LL-37 activates epithelial cells through at least 2 classes of receptors [183,202], LL-37 transactivates epidermal growth factor receptor (EGFR) and promotes the release of IL-ip [203], and LL-37-induced maturation of LPS-primed monocytes requires the P2X(7)... 

Zigmond, S. H., Sullivan, S. J., and Lauffenburger, D. A., Kinetic analysis of chemotactic peptide receptor modulation. J. Cell Biot. 92, 34 (1982). 

Glyxins, a group of synthetic peptides acting as NMDA receptor modulators. A potent member of this group is GLYX-13 [J. R. Moskal et al., Neuropharmacolog 2005, 49, 1077]. 

Sullivan, S.J. and Zigmond, S.H. (1980). Chemotactic peptide receptor modulation in polymorphonuclear leukocytes, y. Cell Biol. 88, 644-647. 

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