Stapled helical peptides bearing different anchoring residues
A large proportion of protein–protein interactions (PPIs) occur between a short peptide and a
globular protein domain; the peptides involved in surface interactions play important roles …
globular protein domain; the peptides involved in surface interactions play important roles …
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 …
making the development of PPI inhibitors extremely valuable. The identification of selective …
The p53 pathway: origins, inactivation in cancer, and emerging therapeutic approaches
AC Joerger, AR Fersht - Annual review of biochemistry, 2016 - annualreviews.org
Inactivation of the transcription factor p53, through either direct mutation or aberrations in
one of its many regulatory pathways, is a hallmark of virtually every tumor. In recent years …
one of its many regulatory pathways, is a hallmark of virtually every tumor. In recent years …
Phase 1 Trial of ALRN-6924, a Dual Inhibitor of MDMX and MDM2, in Patients with Solid Tumors and Lymphomas Bearing Wild-type TP53
Purpose: We describe the first-in-human dose-escalation trial for ALRN-6924, a stabilized,
cell-permeating peptide that disrupts p53 inhibition by mouse double minute 2 (MDM2) and …
cell-permeating peptide that disrupts p53 inhibition by mouse double minute 2 (MDM2) and …
Hydrocarbon-stapled peptides: principles, practice, and progress: miniperspective
LD Walensky, GH Bird - Journal of medicinal chemistry, 2014 - ACS Publications
Protein structure underlies essential biological processes and provides a blueprint for
molecular mimicry that drives drug discovery. Although small molecules represent the lion's …
molecular mimicry that drives drug discovery. Although small molecules represent the lion's …
Drugging the p53 pathway: understanding the route to clinical efficacy
The tumour suppressor p53 is the most frequently mutated gene in human cancer, with more
than half of all human tumours carrying mutations in this particular gene. Intense efforts to …
than half of all human tumours carrying mutations in this particular gene. Intense efforts to …
Peptide stapling techniques based on different macrocyclisation chemistries
Peptide stapling is a strategy for constraining short peptides typically in an alpha-helical
conformation. Stapling is carried out by covalently linking the side-chains of two amino …
conformation. Stapling is carried out by covalently linking the side-chains of two amino …
Stapled α− helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy
YS Chang, B Graves, V Guerlavais… - Proceedings of the …, 2013 - National Acad Sciences
Stapled α− helical peptides have emerged as a promising new modality for a wide range of
therapeutic targets. Here, we report a potent and selective dual inhibitor of MDM2 and …
therapeutic targets. Here, we report a potent and selective dual inhibitor of MDM2 and …
Constraining cyclic peptides to mimic protein structure motifs
Many proteins exert their biological activities through small exposed surface regions called
epitopes that are folded peptides of well‐defined three‐dimensional structures. Short …
epitopes that are folded peptides of well‐defined three‐dimensional structures. Short …
Modulators of protein–protein interactions
LG Milroy, TN Grossmann, S Hennig… - Chemical …, 2014 - ACS Publications
Since Hedin's characterization of trypsin and antitrypsin in 1906,(1) arguably the first
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …