Trends in Biotechnology
FocusThe ‘peptoid’ approach to the design of non-peptide, small molecule agonists and antagonists of neuropeptides
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Peptides: Important tools for the treatment of central nervous system disorders
2011, NeuropeptidesCitation Excerpt :The first approaches were based on simple modifications of N- or C-terminus, N- and Cα-methylation, or single amino acid replacement with their d-amino acid equivalent (Sasubilli and Gutheil, 2004; Sagan et al., 2004). With the introduction of isosteric groups, peptide bond modifications (Ahn et al., 2002) resulted in a variety of peptidomimetic classes, such as peptoids (Horwell, 1995), retro-inverso peptides (Fletcher and Campbell, 1998), azapeptides (Zega, 2005), urea-peptidomimetics (Bakshi and Wolfe, 2004) and sulphonamide peptides/peptoids (Brouwer and Liskamp, 2004). Several examples of sugar amino acid scaffolds have been used in biologically active peptide sequences, such as RGD-containing integrin antagonists, somatostatin, LHRH, and enkephalins (von Roedern et al., 1996).
Design and pharmacology of peptoids and peptide-peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence
2003, Bioorganic and Medicinal Chemistry LettersNeurokinins activate local glutamatergic inputs to serotonergic neurons of the dorsal raphe nucleus
2002, NeuropsychopharmacologyParticipation of GABA<inf>A</inf> receptors in the modulation of experimental anxiety by tachykinin agonists and antagonists in mice
2002, Progress in Neuro-Psychopharmacology and Biological PsychiatryMolecular Basis for Selectivity of High Affinity Peptide Antagonists for the Gastrin-releasing Peptide Receptor
2001, Journal of Biological ChemistryCitation Excerpt :This is in large part because, for many, specific receptor antagonists do not exist, and for others, only recently have high affinity antagonists been developed (51). The antagonists for these receptors generally fall into one of three types: nonpeptide antagonists (the largest group); peptide antagonists; or, in a few cases, peptoid antagonists, which have features of both peptides and nonpeptides (52, 53). There are a number of studies of the molecular basis of action of nonpeptide antagonists for various GI hormone receptors (14, 54-57); however, there are only a few studies for peptide antagonists (14, 16, 17, 55).