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 …

Inhibition of α-helix-mediated protein–protein interactions using designed molecules

V Azzarito, K Long, NS Murphy, AJ Wilson - Nature chemistry, 2013 - nature.com
Inhibition of protein–protein interactions (PPIs) represents a significant challenge because it
is unclear how they can be effectively and selectively targeted using small molecules …

Constraining cyclic peptides to mimic protein structure motifs

TA Hill, NE Shepherd, F Diness… - Angewandte Chemie …, 2014 - Wiley Online Library
Many proteins exert their biological activities through small exposed surface regions called
epitopes that are folded peptides of well‐defined three‐dimensional structures. Short …

Design and structure of stapled peptides binding to estrogen receptors

C Phillips, LR Roberts, M Schade, R Bazin… - Journal of the …, 2011 - ACS Publications
Synthetic peptides that specifically bind nuclear hormone receptors offer an alternative
approach to small molecules for the modulation of receptor signaling and subsequent gene …

International Union of Basic and Clinical Pharmacology. XC. multisite pharmacology: recommendations for the nomenclature of receptor allosterism and allosteric …

A Christopoulos, JP Changeux, WA Catterall… - Pharmacological …, 2014 - ASPET
Allosteric interactions play vital roles in metabolic processes and signal transduction and,
more recently, have become the focus of numerous pharmacological studies because of the …

Sphingosine-1-phosphate promotes expansion of cancer stem cells via S1PR3 by a ligand-independent Notch activation

N Hirata, S Yamada, T Shoda, M Kurihara… - Nature …, 2014 - nature.com
Many tumours originate from cancer stem cells (CSCs), which is a small population of cells
that display stem cell properties. However, the molecular mechanisms that regulate CSC …

Steroid receptor coactivators 1, 2, and 3: critical regulators of nuclear receptor activity and steroid receptor modulator (SRM)-based cancer therapy

AB Johnson, BW O'Malley - Molecular and cellular endocrinology, 2012 - Elsevier
Coactivators are a diverse group of non-DNA binding proteins that induce structural
changes in agonist-bound nuclear receptors (NRs) that are essential for NR-mediated …

Minireview: Not picking pockets: nuclear receptor alternate-site modulators (NRAMs)

TW Moore, CG Mayne… - Molecular …, 2010 - academic.oup.com
Because of their central importance in gene regulation and mediating the actions of many
hormones, the nuclear receptors (NRs) have long been recognized as very important …

Design and synthesis of α-helical peptides and mimetics

J Garner, MM Harding - Organic & biomolecular chemistry, 2007 - pubs.rsc.org
The α-helix is the most abundant secondary structural element in proteins and is an
important structural domain for mediating protein–protein and protein–nucleic acid …

Crosslinked aspartic acids as helix‐nucleating templates

H Zhao, QS Liu, H Geng, Y Tian, M Cheng… - Angewandte …, 2016 - Wiley Online Library
Described is a facile helix‐nucleating template based on a tethered aspartic acid at the N‐
terminus [terminal aspartic acid (TD)]. The nucleating effect of the template is subtly …