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Peptoids (1):
Recent article
Peptoids
Abstract
We present a structure-activity relationship study of a potent, peptide-based PKB/Akt inhibitor, PTR6154. The study was designed to evaluate backbone modifications on the inhibitory activity of PTR6154. Two peptidomimetic libraries, peptoid and N(alpha)-methylation, based on PTR6154, were synthesize...
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PMID: 20347317
PDF is available here.
PDF is available here.
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Abstract
A rapid array-based protocol is presented by which a modest affinity protein-binding small molecule can be appended to a library of peptoids via click chemistry. The array can then be screened for improved ligands that exhibit a higher affinity for the protein target.
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PMID: 19380225
PDF is available here.
PDF is available here.
Abstract
Peptoids are oligomers of N-substituted glycine units. These molecules are almost perfectly suited for combinatorial approaches to drug discovery because large libraries can be synthesized easily from readily available primary amines. Moreover, major advances in screening methodology have allowed pe...
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PMID: 19479663
PDF is available here.
PDF is available here.
Abstract
We anticipate these connections will provide a pathway toward the de novo design of functional peptoids. In this perspective, we review several of the peptoid structure-function relationships that have been delineated over the past five years....
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PMID: 19343235
PDF is available here.
PDF is available here.
Abstract
These results could provide a foundation for further structural optimization of Shc SH2 domain-binding peptide mimetics....
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PMID: 19226165
PDF is available here.
PDF is available here.
Abstract
Abstract
We describe new approaches to direct the conformation of the peptoid backbone, leading to secondary structures such as helices, loops, and turns. These advances are enabling the discovery of bioactive peptoids and will establish modules for the design and assembly of protein mimetics....
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PMID: 18786652
PDF is available here.
PDF is available here.
Abstract
We identify the pharmacophore in a peptoid that antagonizes Vascular Endothelial Growth Factor Receptor-2 (VEGFR2) in vitro and in vivo. Only three of the side chains in the peptoid are required for activity. Surprisingly, however, main chain atoms also form critical interactions with the receptor....
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PMID: 18653335
PDF is available here.
PDF is available here.
Abstract
Novel peptidomimetic backbone designs with stability towards proteases are of interest for several pharmaceutical applications including intracellular delivery. The present study concerns the cellular uptake and membrane-destabilising effects of various cationic chimeras comprised of alternating N-al...
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PMID: 18675778
PDF is available here.
PDF is available here.
Abstract
Peptoids are oligomeric N-substituted glycines with potential as biologically relevant compounds. Helical peptoids provide an attractive fold for the generation of protein-protein interaction inhibitors. The generation of helical peptoid folds in organic and aqueous media has been limited to strict...
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PMID: 18688493
PDF is available here.
PDF is available here.
Abstract
N-Substituted glycine peptoid oligomers were synthesized to incorporate a photoresponsive azobenzene side chain. The ability of this side chain to undergo reversible photoisomerization was established, and the cis- to trans-azobenzene thermal isomerization of this side chain was investigated. Circul...
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PMID: 18600272
PDF is available here.
PDF is available here.
Neuroscience Letters (439)1 2008
Abstract
We examined whether intranasal peptoid CHIR5585, an antagonist of the urokinase plasminogen activator receptor (uPAR), is delivered to the CNS. Peptoids are a novel class of peptide isomers that are oligomeric N-substituted glycine peptides. Anesthetized male rats were administered peptoid CHIR5585...
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PMID: 18501511
PDF is available here.
PDF is available here.
Abstract
We recently described a novel peptoid antagonist of VEGF Receptor 2 (VEGFR2) that binds to the extracellular domain of the receptor and inhibits VEGF-mediated autophosphorylation and subsequent downstream signaling. Given the structural similarities between peptides and peptoids, an obvious model fo...
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PMID: 18501615
PDF is available here.
PDF is available here.
Abstract
We report the strengths and limitations of a high-throughput cell-based permeability assay that registers the relative ability of steroid-conjugated peptides and peptoids to enter a cell. A comparative investigation of the physicochemical properties and side chain composition of peptoids and peptide...
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PMID: 18490170
PDF is available here.
PDF is available here.
Abstract
We report a two-color, cell-based screen to identify specific receptor-binding compounds in a combinatorial library of peptoids displayed on beads. We apply this strategy to the isolation of vascular endothelial growth factor receptor 2 (VEGFR2)-binding peptoids. A dimeric derivative of one of these...
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PMID: 18386897
PDF is available here.
PDF is available here.
Abstract
We identified pyrimidinone-peptoid hybrid molecules that inhibit cell proliferation with greater potency than previously described Hsp70 modulators. In many cases, anti-proliferative activity correlated with inhibition of J domain stimulation of Hsp70....
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PMID: 18164205
PDF is available here.
PDF is available here.
Abstract
We have discovered molecules that bind to a central protein component of the apoptosome, Apaf-1, and inhibits its activity. These new first-in-class apoptosome inhibitors have been further improved by modifications directed to enhance their cellular penetration to yield compounds that decrease cell...
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PMID: 18197610
PDF is available here.
PDF is available here.
Abstract
Efficient drug delivery is essential for many therapeutic applications. Some cell-penetrating peptides, peptide mimetics, and peptoids express transport function that, however, lack in most cases specific intracellular destination. In this study, carrier-peptoids with either amino or guanidinium sid...
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PMID: 18215012
PDF is available here.
PDF is available here.
Organic Letters (10)2 2008
Abstract
A new strategy for the synthesis of cyclic peptoids was developed. The approach is based on the use of consecutive Ugi reactions for the assembly of the acyclic peptoid and for the ring closure. Cyclopentapeptoid analogues of the RGD peptides were designed and synthesized using this methodology. The...
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PMID: 18088132
PDF is available here.
PDF is available here.
Chemotherapy (54)2 2008
Abstract
The lysine-peptoid hybrids proved to be active against all strains tested, except K. pneumoniae. For each susceptible strain, we identified at least 4 lysine-peptoid hybrids showing excellent activity. The most active compounds displayed minimal inhibitory concentrations ranging from < or =1.6 to 6....
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PMID: 18332629
PDF is available here.
PDF is available here.
Biofouling (24)6 2008
Abstract
Surface modification techniques that create surfaces capable of killing adherent bacteria are promising solutions to infections associated with implantable medical devices. Antimicrobial (AM) peptoid oligomers (ampetoids) that were designed to mimic helical AM peptides were synthesised with a peptoi...
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PMID: 18696290
PDF is available here.
PDF is available here.
Abstract
We describe the solid-phase synthesis of a series of indole-based peptoids (N-alkylglycines) and the biological activity of the peptoids as novel TRPV1 antagonists. The potency and selectivity of the compounds were determined by electrophysiological recordings in Xenopus oocytes. The most potent and...
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PMID: 17985859
PDF is available here.
PDF is available here.
Abstract
ChemBioChem (8)15 2007
Abstract
Abstract
We report the results of a study of the kinetics and equilibria of cis/trans isomerization of the amide bonds of N-acetylated peptoid monomers, dipeptoids, and tripeptoids by NMR spectroscopy. Resonance intensities indicate the cis conformation of the backbone amide bonds of the peptoids studied is...
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PMID: 17824612
PDF is available here.
PDF is available here.
Abstract
Enzyme-linked lectin assay (ELLA) was performed for oligomannosylpeptoids, which were immobilized on microtiter plates through a streptavidin-biotin interaction. The other immobilization methods, a hydrophobic adsorption and a covalent attachment, were found inapplicable to the oligomannosylpeptoids...
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PMID: 17689075
PDF is available here.
PDF is available here.
Abstract
We designed a novel cell-selective antimicrobial peptide (TPk) with intracellular mode of action from Pro --> Nlys (Lys peptoid residue) substitution in a noncell-selective cathelicidin-derived Trp/Pro-rich antimicrobial peptide, tritrpticin-amide (TP; VRRFPWWWPFLRR-NH(2)) (Biochemistry 2006; 45: 13...
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PMID: 17604338
PDF is available here.
PDF is available here.
Biochimica et Biophysica Acta (1768)6 2007
Abstract
We attempted to generate novel cell-selective peptides by substituting amino acids in the leucine zipper sequence of ME with peptoid residues. We generated a series of ME analogues by replacing Leu-6, Lue-13 and Ile-20 with Nala, Nleu, Nphe, or Nlys, and we examined their secondary structure, self-a...
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PMID: 17462584
PDF is available here.
PDF is available here.
Abstract
Libraries of new, small peptoid monomers and dipeptoids were synthesized and assayed for antiproliferative activity against representative human neoplastic cell lines. The C-terminal N-alkyl amide peptoids are cytotoxic and are the smallest peptoids reported to have such activity. These compounds we...
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PMID: 17432841
PDF is available here.
PDF is available here.
Abstract
We have identified a family of peptoids that inhibits in vitro the activity of the apoptosome, a macromolecular complex that activates mitochondrial-dependent apoptosis pathways. The analysis of peptide-based cell compatible delivery systems of the most active peptoid is presented. The active peptoi...
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PMID: 17408805
PDF is available here.
PDF is available here.
Abstract
The highly amyloidogenic peptide sequence of amylin(20-29) was transformed into its corresponding peptoid and retropeptoid sequences to design a novel class of beta-sheet breaker peptides as amyloid inhibitors. This report describes the synthesis of the chiral peptoid building block of L-isoleucine,...
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PMID: 17276062
PDF is available here.
PDF is available here.
Abstract
We report that peptoids undergo highly efficient head-to-tail macrocyclization reactions. A diverse array of peptoid sequences from pentamers to 20mers were converted to macrocyclic products within 5 min at room temperature. The introduction of the covalent constraint enhances conformational orderin...
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PMID: 17323948
PDF is available here.
PDF is available here.
Abstract
Abstract
Helical peptoid oligomers were synthesized in which the positions of nitroxide radical spin probes along the backbone were systematically varied, allowing evaluation of intra-molecular distances and dynamics by electron spin resonance spectroscopy.
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PMID: 17220976
PDF is available here.
PDF is available here.
Bioconjugate Chemistry (18)2 2007
Abstract
For many therapeutic applications, it has become more and more important to find synthetic compounds that have the ability to transport a variety of drugs and cargo molecules into cells and tissues. Like arginine-rich cell-penetrating peptides (CPPs), it is already known that peptide mimetics such a...
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PMID: 17326607
PDF is available here.
PDF is available here.
Abstract
Abstract
Abstract
We report here the first example of a cell-permeable STFM that activates the transcription of a reporter gene in mammalian cells. The compound is composed of a cell-permeable coactivator-binding peptoid fused to a DNA-binding hairpin polyamide. The peptoid was identified by screening a combinatorial...
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PMID: 17530904
PDF is available here.
PDF is available here.
Abstract
Two new groups of cholane-peptoid hybrid macrocycles were produced by implementing novel combinations of the MiB methodology. Steroid-based hybrid macrolactams including heterocycle and aryl moieties were obtained by utilizing cholanic dicarboxylic acids and diamines in a bidirectional double Ugi-Fo...
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PMID: 17960094
PDF is available here.
PDF is available here.
Protein & Peptide Letters (14)10 2007
Abstract
We synthesized a Leu/Lys-rich model peptide, KLW-f (KWKKLLKKfLKLfKKLLK-NH(2)) containing two Phe-peptoid residues in its middle position. KLW-f exhibited high antimicrobial activity (the MIC range: 0.5 approximately 2.0microM) against the tested six bacterial cells. In contrast, KLW-f was no cytotox...
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PMID: 18220998
PDF is available here.
PDF is available here.
Abstract
We report the first study of the effects of pentafluoroaromatic functionality on the conformational profiles of peptoids. This work was enabled by the synthesis of a new, alpha-chiral amine building block, (S)-1-(pentafluorophenyl)ethylamine (S-2), which was found to be highly compatible with peptoi...
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PMID: 17076512
PDF is available here.
PDF is available here.
Biochemistry (Washington) (45)43 2006
Abstract
We synthesized tritrpticin-amide (TP, VRRFPWWWPFLRR-NH(2)) and its peptoid residue-substituted peptides in which two Pro residues at positions 5 and 9 are replaced with Nleu (Leu peptoid residue), Nphe (Phe peptoid residue), or Nlys (Lys peptoid residue). Peptides with Pro --> Nphe (TPf) or Pro -->...
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PMID: 17059217
PDF is available here.
PDF is available here.
Biochemistry (Washington) (45)39 2006
Abstract
We created helical, non-natural mimics of SP-B(1-25) based on sequence-specific peptoid 17mers and demonstrated their biomimetic surface activity. Like SP-B(1-25), the peptoids were designed to adopt helical structures with cationic and nonpolar faces. Here, we compare the surface activities of six...
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PMID: 17002281
PDF is available here.
PDF is available here.
Biotechnology Letters (28)18 2006
Abstract
We investigated the effect of substituting Pro(8) of IsCT-P with the Ala-peptoid residue (N-methylglycine) on the peptide's structure and mechanism of action. Circular dichroism analysis revealed that the modified peptide, IsCT-a, has a much lower alpha-helicity than IsCT-P in membrane mimicking con...
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PMID: 16871429
PDF is available here.
PDF is available here.
Abstract
We describe the synthesis and screening of a biased positional scanning library made up of peptoids (N-alkylglycines) and lysines. The library consisted of 100 mixtures divided into four sub-libraries; OXXXKKK, XOXXKKK, XXOXKKK, and XXXOKKK, O being a defined peptoid building block and X a mixture o...
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PMID: 16524733
PDF is available here.
PDF is available here.
Abstract
An antiapoptotic polymeric nanomedicine, PGA-peptoid 1, has been developed by the conjugation of a novel apoptotic protease activating factor 1 (Apaf-1) inhibitor (peptoid 1) to poly-L-glutamic acid (PGA). Full structural and biophysical characterization of the conjugate by different techniques has...
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PMID: 16789732
PDF is available here.
PDF is available here.
Abstract
The first 3-fold multicomponent macrocyclizations of trifunctional building blocks were developed to produce, in one pot, cryptands, cages, and cryptophanes with peptoid tethers carrying additional recognition motifs. The straightforward, efficient, and diversity-oriented fashion by which these comp...
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PMID: 16734440
PDF is available here.
PDF is available here.
Abstract
The title compound, C10H8F5NO, crystallizes as a racemate with four symmetry-independent molecules in the asymmetric unit. The four molecules form two hydrogen-bonded pairs. Each pair is a building unit of an independent C4 chain propagating parallel to the ab plane.
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PMID: 16679606
PDF is available here.
PDF is available here.
Organic Letters (8)7 2006
Abstract
[structure: see text] Cyclic semipeptoids 1 and 2 represent constrained, secondary structure mimics where the R(1) and R(2) side chains correspond to those of amino acids. Solid-phase syntheses and conformational analyses of these compounds are described.
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PMID: 16562866
PDF is available here.
PDF is available here.
Physical Biology (3)1 2006
Abstract
We provide a complete overview on helix formation in alpha- and beta-peptoids on the basis of systematic theoretical conformational analyses employing the methods of ab initio molecular orbital (MO) theory. It can be shown that the alpha- and beta-peptoid structures form helical structures with both...
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PMID: 16582460
PDF is available here.
PDF is available here.
Abstract
Antimicrobial peptides and their mimetics offer a potential new disinfective tool. beta-Peptoids (oligo-N-substituted beta-alanines) were synthesized and investigated for antimicrobial activity. A block approach whereby di- and tri-beta-peptoids were first prepared and then ligated via amide bond fo...
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PMID: 16384703
PDF is available here.
PDF is available here.
Abstract
We used oligomeric peptoids as the scaffold to begin to develop a general strategy in which we could rationally design synthetic molecules that can be optimized for inhibition of protein-protein interactions. Structural information on the HDM2-p53 complex was used to design our first class of peptoi...
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PMID: 16464101
PDF is available here.
PDF is available here.
Abstract
We describe a family of N-substituted glycine or "peptoid" nonamers that folds into an unusual "threaded loop" structure of exceptional thermal stability and conformational homogeneity in acetonitrile. The structure is chain-length-specific and relies on bulky, chiral side chains and chain-terminati...
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PMID: 16448149
PDF is available here.
PDF is available here.
Abstract
Selenocysteine containing peptoids and peptide-peptoid conjugates were synthesized by combinatorial Ugi-MCRs (multicomponent reactions) in water: for the first time, an acetal (selenoacetal 2a) was used in Ugi-MCR to furnish selenocysteine peptoids in one step as model compounds for selenocysteine p...
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PMID: 16432576
PDF is available here.
PDF is available here.
Methods in Enzymology (413) 2006
Abstract
We consider methods of assaying fibrillogenesis inhibitors, including pitfalls in these assays. We consider binding of inhibitor peptides to their targets, but because this is a specific application of the more general and much larger problem of assessing protein-protein interactions, this topic is...
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PMID: 17046402
PDF is available here.
PDF is available here.
Abstract
We have developed a method for the rapid and unambiguous identification of sequences of hit compounds from one-bead-one-compound combinatorial libraries of peptide and peptoid ligands. The approach uses a cleavable linker that is hydrophilic to help reduce nonspecific binding to biological samples a...
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PMID: 16677012
PDF is available here.
PDF is available here.
Abstract
We synthesized a ME analogue (ME-w) in which the Trp-19 residue of ME was replaced by a Trp-peptoid residue (Nhtrp). ME-w exhibited similar antimicrobial activity compared to ME against the tested six bacteria and C. albicans. However, it was much less cytotoxic against the hRBCs and HeLa and NIH-3T...
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PMID: 17018016
PDF is available here.
PDF is available here.
Abstract
We report the stepwise transformation of a linear peptide epitope recognized by the anti-transforming growth factor alpha monoclonal antibody Tab2 into peptomers and finally into peptoid analogs. The key experiment in this study is the substitution analysis in which each position of the peptide is e...
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PMID: 17073730
PDF is available here.
PDF is available here.
Abstract
We demonstrate that proteases can catalyze the ligation of peptidomimetic oligomers. The enzyme clostripain was used to facilitate the native ligation of N-substituted glycine oligomers, or peptoids. In addition to mediating the efficient condensation of two peptoid fragments, iterative ligation eve...
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PMID: 16332030
PDF is available here.
PDF is available here.
Journal of Peptide Science (11)11 2005
Abstract
We report the design, synthesis and antibacterial activity of 20 lysine-peptoid hybrids. The hybrids are based on the peptoid lead structure [N-(1-naphthalenemethyl)glycyl]-[N-(4-methylbenzyl)glycyl]-[N-(1-naphthalenemethyl)glycyl]-N-(butyl)glycin amide (1) and contain between one and six lysine res...
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PMID: 16161020
PDF is available here.
PDF is available here.