The current state of peptide drug discovery: back to the future?

A Henninot, JC Collins, JM Nuss - Journal of medicinal chemistry, 2018 - ACS Publications
Over the past decade, peptide drug discovery has experienced a revival of interest and
scientific momentum, as the pharmaceutical industry has come to appreciate the role that …

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 …

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 insights into protein–protein interaction modulators in drug discovery and therapeutic advance

H Nada, Y Choi, S Kim, KS Jeong… - … and Targeted Therapy, 2024 - nature.com
Protein-protein interactions (PPIs) are fundamental to cellular signaling and transduction
which marks them as attractive therapeutic drug development targets. What were once …

The medicinal chemistry of peptides

J Nestor - Current medicinal chemistry, 2009 - ingentaconnect.com
The shortcomings of native peptides as pharmaceuticals have been long known: short
duration of action, lack of receptor selectivity, lack of oral bioavailability. However medicinal …

Advances in the chemistry of proline and its derivatives: an excellent amino acid with versatile applications in asymmetric synthesis

SK Panday - Tetrahedron: Asymmetry, 2011 - Elsevier
Non-proteinogenic prolines have been acknowledged as an important pool for the synthesis
of conformationally rigid bioactive peptides, angiotensin converting enzyme inhibitors and …

Intramolecular anodic olefin coupling reactions and the synthesis of cyclic amines

HC Xu, KD Moeller - Journal of the American Chemical Society, 2010 - ACS Publications
Anodic olefin coupling reactions using a tosylamine trapping group have been studied. The
cyclizations are favored by the use of a less-polar radical cation and more basic reaction …

N-Methylated Cyclic Pentaalanine Peptides as Template Structures

J Chatterjee, D Mierke, H Kessler - Journal of the American …, 2006 - ACS Publications
The N-methylation of cyclic peptides can be used to modify the activity and/or selectivity of
biologically active peptides. As N-methylation introduces different flexibility and lipophilicity …

A novel biased allosteric compound inhibitor of parturition selectively impedes the prostaglandin F2α-mediated Rho/ROCK signaling pathway

E Goupil, D Tassy, C Bourguet, C Quiniou… - Journal of Biological …, 2010 - ASBMB
The prostaglandin F2α (PGF2α) receptor (FP) is a key regulator of parturition and a target for
pharmacological management of preterm labor. However, an incomplete understanding of …

Pilicides—small molecules targeting bacterial virulence

V Åberg, F Almqvist - Organic & biomolecular chemistry, 2007 - pubs.rsc.org
In a time of emerging bacterial resistance there is a vital need for new targets and strategies
in antibacterial therapy. Using uropathogenic Escherichia coli as a model pathogen we have …