Targeting apoptosis in cancer therapy

BA Carneiro, WS El-Deiry - Nature reviews Clinical oncology, 2020 - nature.com
For over three decades, a mainstay and goal of clinical oncology has been the development
of therapies promoting the effective elimination of cancer cells by apoptosis. This …

Macrocyclic peptides as drug candidates: recent progress and remaining challenges

AA Vinogradov, Y Yin, H Suga - Journal of the American Chemical …, 2019 - ACS Publications
Peptides as a therapeutic modality attract much attention due to their synthetic accessibility,
high degree of specific binding, and the ability to target protein surfaces traditionally …

BCL-2 family proteins: changing partners in the dance towards death

J Kale, EJ Osterlund, DW Andrews - Cell Death & Differentiation, 2018 - nature.com
The BCL-2 family of proteins controls cell death primarily by direct binding interactions that
regulate mitochondrial outer membrane permeabilization (MOMP) leading to the irreversible …

Understanding cell penetration of cyclic peptides

PG Dougherty, A Sahni, D Pei - Chemical Reviews, 2019 - ACS Publications
Approximately 75% of all disease-relevant human proteins, including those involved in
intracellular protein–protein interactions (PPIs), are undruggable with the current drug …

Recent advances in ruthenium-based olefin metathesis

OM Ogba, NC Warner, DJ O'leary… - Chemical Society …, 2018 - pubs.rsc.org
Ruthenium-based olefin metathesis catalysts, known for their functional group tolerance and
broad applicability in organic synthesis and polymer science, continue to evolve as an …

Stapled helical peptides bearing different anchoring residues

X Li, S Chen, WD Zhang, HG Hu - Chemical Reviews, 2020 - ACS Publications
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 …

Discovery of Sulanemadlin (ALRN-6924), the first cell-permeating, stabilized α-helical peptide in clinical development

V Guerlavais, TK Sawyer, L Carvajal… - Journal of Medicinal …, 2023 - ACS Publications
We report the discovery of sulanemadlin (ALRN-6924), the first cell-permeating, stabilized α-
helical peptide to enter clinical trials. ALRN-6924 is a “stapled peptide” that mimics the N …

Small molecules, big targets: drug discovery faces the protein–protein interaction challenge

DE Scott, AR Bayly, C Abell, J Skidmore - Nature Reviews Drug …, 2016 - nature.com
Protein–protein interactions (PPIs) are of pivotal importance in the regulation of biological
systems and are consequently implicated in the development of disease states. Recent work …

[HTML][HTML] Pro-apoptotic complexes of BAX and BAK on the outer mitochondrial membrane

P Wolf, A Schoeniger, F Edlich - … et Biophysica Acta (BBA)-Molecular Cell …, 2022 - Elsevier
In multicellular organisms the regulated cell death apoptosis is critically important for both
ontogeny and homeostasis. Mitochondria are indispensable for stress-induced apoptosis …

Design of stapled antimicrobial peptides that are stable, nontoxic and kill antibiotic-resistant bacteria in mice

R Mourtada, HD Herce, DJ Yin, JA Moroco… - Nature …, 2019 - nature.com
The clinical translation of cationic α-helical antimicrobial peptides (AMPs) has been
hindered by structural instability, proteolytic degradation and in vivo toxicity from nonspecific …