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 …

Peptide therapeutics: targeting the undruggable space

N Tsomaia - European journal of medicinal chemistry, 2015 - Elsevier
Rapid advancements in genomics have brought a better understanding of molecular
mechanisms for various pathologies and identified a number of highly attractive target …

Modulating protein–protein interactions: the potential of peptides

L Nevola, E Giralt - Chemical Communications, 2015 - pubs.rsc.org
Protein–protein interactions (PPIs) have emerged as important and challenging targets in
chemical biology and medicinal chemistry. The main difficulty encountered in the discovery …

Features of protein–protein interactions that translate into potent inhibitors: topology, surface area and affinity

MC Smith, JE Gestwicki - Expert reviews in molecular medicine, 2012 - cambridge.org
Protein–protein interactions (PPIs) control the assembly of multi-protein complexes and,
thus, these contacts have enormous potential as drug targets. However, the field has …

Structural basis for high-affinity peptide inhibition of p53 interactions with MDM2 and MDMX

M Pazgier, M Liu, G Zou, W Yuan, C Li… - Proceedings of the …, 2009 - National Acad Sciences
The oncoproteins MDM2 and MDMX negatively regulate the activity and stability of the tumor
suppressor protein p53—a cellular process initiated by MDM2 and/or MDMX binding to the …

Peptide-based inhibitors of protein–protein interactions

P Wójcik, Ł Berlicki - Bioorganic & medicinal chemistry letters, 2016 - Elsevier
Protein–protein interactions (PPIs) are key elements of several important biological
processes and have emerged as valuable targets in medicinal chemistry. Importantly …

In vivo activation of the p53 tumor suppressor pathway by an engineered cyclotide

Y Ji, S Majumder, M Millard, R Borra, T Bi… - Journal of the …, 2013 - ACS Publications
The overexpression of Hdm2 and HdmX is a common mechanism used by many tumor cells
to inactive the p53 tumor suppressor pathway promoting cell survival. Targeting Hdm2 and …

Targeting protein–protein interactions for therapeutic intervention: a challenge for the future

G Zinzalla, DE Thurston - Future medicinal chemistry, 2009 - Taylor & Francis
Background: Over the last two decades, an increasing research effort in academia and
industry has focused on the modulation (both inhibition and stabilization) of protein–protein …

Targeting protein–protein interactions: lessons from p53/MDM2

JK Murray, SH Gellman - Peptide Science: Original Research …, 2007 - Wiley Online Library
The tremendous challenge of inhibiting therapeutically important protein–protein
interactions has created the opportunity to extend traditional medicinal chemistry to a new …

Intrinsically cell-permeable miniature proteins based on a minimal cationic PPII motif

DS Daniels, A Schepartz - Journal of the American Chemical …, 2007 - ACS Publications
Cell-penetrating peptides (CPPs) provide promising tools for the cellular delivery of
molecular cargos ranging in size from small molecules and peptides to proteins and …