Journal ArticleDOI
Evolution in non-peptide α-helix mimetics on the road to effective protein-protein interaction modulators.
Reads0
Chats0
TLDR
This appraisal describes the recent progress in the non-peptide α-helix mimetics field, which has evolved from single-face to multi-face reproducing compounds and from oligomeric to monomeric scaffolds able to bear different substituents in similar spatial dispositions as the side-chains in canonical helices.About:
This article is published in European Journal of Medicinal Chemistry.The article was published on 2021-02-05. It has received 10 citations till now.read more
Citations
More filters
Journal ArticleDOI
OUP accepted manuscript
TL;DR: In this paper , a PAOA (pimeloylanilide o-aminoanilide) derivative, called NKL54, was shown to support MEF2-dependent transcription through several actions, including potentiation of chromatin binding.
Journal ArticleDOI
Transcriptomic and genomic studies classify NKL54 as a histone deacetylase inhibitor with indirect influence on MEF2-dependent transcription
Martina Minisini,Eros Di Giorgio,Emanuela Kerschbamer,Emiliano Dalla,Massimo Faggiani,Elisa Franforte,Franz-Josef Meyer-Almes,Rino Ragno,Lorenzo Antonini,A. Maio,Francesco Fiorentino,Dante Rotili,M. Chinellato,Stefano Perin,Laura Cendron,Christian X. Weichenberger,Alessandro Angelini,Claudio Brancolini +17 more
TL;DR: Although NKL54 cannot outcompete MEF2 from binding to class IIa HDACs, it supportsMEF2-dependent transcription through several actions, including potentiation of chromatin binding.
Journal ArticleDOI
Flat, Cα,β -Didehydroalanine Foldamers with Ferrocene Pendants: Assessing the Role of α-Peptide Dipolar Moments.
Saverio Santi,Annalisa Bisello,Roberta Cardena,Silvia Tomelleri,Renato Schiesari,Barbara Biondi,Marco Crisma,Fernando Formaggio +7 more
TL;DR: In this article, a flat foldamers based on the natural, but non-coded, Cα,β -didehydroalanine α-amino acid, and covalently linked to them two ferrocene (Fc) moieties, as redox probes, were synthesized.
Journal ArticleDOI
Aromatic oligoesters as novel helix mimetic scaffolds
M. Serajul Haque,Theo Flack,Ravindra V. Singh,Archie Wall,Guilherme Vieira de Castro,Andrew J. P. White,Anna Barnard +6 more
TL;DR: In this article , the design, synthesis, and conformational analysis of a novel aromatic oligoester helix mimetic scaffold was reported, where a range of amino acid-type side-chain functionality can be readily incorporated into monomer building blocks over three facile synthetic steps.
Journal ArticleDOI
Tetrasubstituted Pyrrole Derivative Mimetics of Protein–Protein Interaction Hot-Spot Residues: A Promising Class of Anticancer Agents Targeting Melanoma Cells
Marco Persico,Paola Galatello,Maria Grazia Ferraro,Carlo Irace,Maria da Penha Píccolo,A. Abduvakhidov,O. Tkachuk,Maria Luisa d’Aulisio Garigliota,Pietro Campiglia,Patrizia Iannece,Michela Varra,Anna Ramunno,Caterina Fattorusso +12 more
TL;DR: In this paper, a tetrasubstituted pyrrole derivatives (TSPs) were synthesized based on a previously developed hypothesis on their ability to mimic hydrophobic protein motifs.
References
More filters
Journal ArticleDOI
In vivo activation of the p53 pathway by small-molecule antagonists of MDM2.
Lyubomir T. Vassilev,Binh Thanh Vu,Bradford Graves,Daisy Carvajal,Frank John Podlaski,Zoran Filipovic,Norman Kong,Ursula Kammlott,Christine Lukacs,Christian Klein,Nader Fotouhi,Liu Emily Aijun +11 more
TL;DR: In this article, the authors identify potent and selective small-molecule antagonists of MDM2 and confirm their mode of action through the crystal structures of complexes, leading to cell cycle arrest, apoptosis, and growth inhibition of human tumor xenografts.
Journal ArticleDOI
The spontaneous insertion of proteins into and across membranes: the helical hairpin hypothesis
TL;DR: It is proposed that the initial event in the secretion of proteins across membranes and their insertion into membranes is the spontaneous penetration of the hydrophobic portion of the bilayer by a helical hairpin.
Journal ArticleDOI
Estimating the size of the human interactome
Michael P. H. Stumpf,Thomas Thorne,Eric de Silva,Ron Stewart,Hyeong Jun An,Michael Lappe,Carsten Wiuf +6 more
TL;DR: It is found that the human interaction network is one order of magnitude bigger than the Drosophila melanogaster interactome and ≈3 times bigger than in Caenorhabditis elegans.
Journal ArticleDOI
Foldamers with Heterogeneous Backbones
W. Seth Horne,Samuel H. Gellman +1 more
TL;DR: The promise of heterogeneous backbone foldamers is illustrated by focusing on examples containing both alpha- and beta-amino acid residues, which offer new platforms for mimicry of the molecular surfaces involved in specific protein-protein recognition events.
Journal ArticleDOI
Inhibition of α-helix-mediated protein–protein interactions using designed molecules
TL;DR: This Review discusses the relevance of PPIs and, in particular, the importance of α-helix-mediated PPIs to chemical biology and drug discovery with a focus on designing inhibitors, including constrained peptides, foldamers and proteomimetic-derived ligands.