Peptidomimetic toolbox for drug discovery

E Lenci, A Trabocchi - Chemical Society Reviews, 2020 - pubs.rsc.org
The art of transforming peptides into drug leads is still a dynamic and fertile field in medicinal
chemistry and drug discovery. Peptidomimetics can respond to peptide limitations by …

Structure‐based design of inhibitors of protein–protein interactions: mimicking peptide binding epitopes

M Pelay‐Gimeno, A Glas, O Koch… - Angewandte Chemie …, 2015 - Wiley Online Library
Protein–protein interactions (PPIs) are involved at all levels of cellular organization, thus
making the development of PPI inhibitors extremely valuable. The identification of selective …

Biomedical importance of indoles

NK Kaushik, N Kaushik, P Attri, N Kumar, CH Kim… - Molecules, 2013 - mdpi.com
The indole nucleus is an important element of many natural and synthetic molecules with
significant biological activity. This review covers some of the relevant and recent …

Synthetic therapeutic peptides: science and market

P Vlieghe, V Lisowski, J Martinez, M Khrestchatisky - Drug discovery today, 2010 - Elsevier
The decreasing number of approved drugs produced by the pharmaceutical industry, which
has been accompanied by increasing expenses for R&D, demands alternative approaches …

A field guide to foldamers

DJ Hill, MJ Mio, RB Prince, TS Hughes… - Chemical …, 2001 - ACS Publications
The breadth of structure and function displayed by the molecules of biology is remarkable.
Considering that there are only three major biopolymer backbones (proteins, ribonucleic …

Chemical modifications designed to improve peptide stability: incorporation of non-natural amino acids, pseudo-peptide bonds, and cyclization

L Gentilucci, R De Marco… - Current pharmaceutical …, 2010 - ingentaconnect.com
Functions and properties of native peptides vary from highly specific antibiotics or cytotoxic
antitumor drugs, to hormones, neurotransmitters, immunomodulators, etc. Despite their …

Strategies for fine-tuning the conformations of cyclic peptides

R Jwad, D Weissberger, L Hunter - Chemical Reviews, 2020 - ACS Publications
Cyclic peptides are promising scaffolds for drug development, attributable in part to their
increased conformational order compared to linear peptides. However, when optimizing the …

Peptidomimetics, a synthetic tool of drug discovery

J Vagner, H Qu, VJ Hruby - Current opinion in chemical biology, 2008 - Elsevier
The demand for modified peptides with improved stability profiles and pharmacokinetic
properties is driving extensive research effort in this field. Many structural modifications of …

New developments in the chemistry of N-acyliminium ions and related intermediates

WN Speckamp, MJ Moolenaar - Tetrahedron, 2000 - Elsevier
Reactions between N-acyliminium ions and nucleophiles–also described as
amidoalkylation or Mannich type condensations–have been frequently utilized to introduce …

Phosphine-catalyzed annulations of azomethine imines: allene-dependent [3+ 2],[3+ 3],[4+ 3], and [3+ 2+ 3] pathways

R Na, C Jing, Q Xu, H Jiang, X Wu, J Shi… - Journal of the …, 2011 - ACS Publications
In this paper we describe the phosphine-catalyzed [3+ 2],[3+ 3],[4+ 3], and [3+ 2+ 3]
annulations of azomethine imines and allenoates. These processes mark the first use of …