[HTML][HTML] Stapled peptides inhibitors: a new window for target drug discovery

AM Ali, J Atmaj, N Van Oosterwijk, MR Groves… - Computational and …, 2019 - Elsevier
Protein-protein interaction (PPI) is a hot topic in clinical research as protein networking has a
major impact in human disease. Such PPIs are potential drugs targets, leading to the need …

Hydrocarbon stapled peptides as modulators of biological function

PM Cromm, J Spiegel, TN Grossmann - ACS chemical biology, 2015 - ACS Publications
Peptide-based drug discovery has experienced a significant upturn within the past decade
since the introduction of chemical modifications and unnatural amino acids has allowed for …

The roles of MDM2 and MDMX in cancer

O Karni-Schmidt, M Lokshin… - Annual Review of …, 2016 - annualreviews.org
For more than 25 years, MDM2 and its homolog MDMX (also known as MDM4) have been
shown to exert oncogenic activity. These two proteins are best understood as negative …

Peptide-based inhibitors of protein–protein interactions: biophysical, structural and cellular consequences of introducing a constraint

H Wang, RS Dawber, P Zhang, M Walko, AJ Wilson… - Chemical …, 2021 - pubs.rsc.org
Protein–protein interactions (PPIs) are implicated in the majority of cellular processes by
enabling and regulating the function of individual proteins. Thus, PPIs represent high-value …

How to design a successful p53–MDM2/X interaction inhibitor: a thorough overview based on crystal structures

N Estrada‐Ortiz, CG Neochoritis, A Dömling - ChemMedChem, 2016 - Wiley Online Library
A recent therapeutic strategy in oncology is based on blocking the protein–protein
interaction between the murine double minute (MDM) homologues MDM2/X and the tumor …

Medicinal chemistry strategies to disrupt the p53–MDM2/MDMX interaction

A Lemos, M Leao, J Soares, A Palmeira… - Medicinal research …, 2016 - Wiley Online Library
The growth inhibitory activity of p53 tumor suppressor is tightly regulated by interaction with
two negative regulatory proteins, murine double minute 2 (MDM2) and X (MDMX), which are …

Classes of cell-penetrating peptides

M Pooga, Ü Langel - Cell-penetrating peptides: methods and protocols, 2015 - Springer
During the three decades of cell-penetrating peptides era the superfamily of CPPs has
rapidly expanded, and the quest for new sequences continues. CPPs have been well …

Artificial macrocycles as potent p53–MDM2 inhibitors

N Estrada-Ortiz, CG Neochoritis… - ACS medicinal …, 2017 - ACS Publications
Based on a combination of an Ugi four component reaction and a ring closing metathesis, a
library of novel artificial macrocyclic inhibitors of the p53–MDM2 interaction was designed …

Dichotomous transactivation domains contribute to growth inhibitory and promotion functions of TAp73

D Li, CYL Kok, C Wang, D Ray… - Proceedings of the …, 2024 - National Acad Sciences
The transcription factor p73, a member of the p53 tumor-suppressor family, regulates cell
death and also supports tumorigenesis, although the mechanistic basis for the dichotomous …

Benzene probes in molecular dynamics simulations reveal novel binding sites for ligand design

YS Tan, J Reeks, CJ Brown, D Thean… - The Journal of …, 2016 - ACS Publications
Protein flexibility poses a major challenge in binding site identification. Several
computational pocket detection methods that utilize small-molecule probes in molecular …