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 …
enabling and regulating the function of individual proteins. Thus, PPIs represent high-value …
Selection of Nucleotide-Encoded Mass Libraries of Macrocyclic Peptides for Inaccessible Drug Targets
K Colas, D Bindl, H Suga - Chemical Reviews, 2024 - ACS Publications
Technological advances and breakthrough developments in the pharmaceutical field are
knocking at the door of the “undruggable” fortress with increasing insistence. Notably, the …
knocking at the door of the “undruggable” fortress with increasing insistence. Notably, the …
Covalent proteomimetic inhibitor of the bacterial FtsQB divisome complex
FM Paulussen, GK Schouten, C Moertl… - Journal of the …, 2022 - ACS Publications
The use of antibiotics is threatened by the emergence and spread of multidrug-resistant
strains of bacteria. Thus, there is a need to develop antibiotics that address new targets. In …
strains of bacteria. Thus, there is a need to develop antibiotics that address new targets. In …
Myo-differentiation reporter screen reveals NF-Y as an activator of PAX3–FOXO1 in rhabdomyosarcoma
MW Sroka, D Skopelitis, MW Vermunt… - Proceedings of the …, 2023 - National Acad Sciences
Recurrent chromosomal rearrangements found in rhabdomyosarcoma (RMS) produce the
PAX3–FOXO1 fusion protein, which is an oncogenic driver and a dependency in this …
PAX3–FOXO1 fusion protein, which is an oncogenic driver and a dependency in this …
Designing stapled peptides to inhibit protein‐protein interactions: an analysis of successes in a rapidly changing field
MTJ Bluntzer, J O'Connell, TS Baker, J Michel… - Peptide …, 2021 - Wiley Online Library
Two decades after their discovery, stapled peptide methodologies have evolved to a point
where they can be used with confidence to generate therapeutic leads. Research groups …
where they can be used with confidence to generate therapeutic leads. Research groups …
First-in-class cyclic Temporin L analogue: Design, synthesis, and antimicrobial assessment
R Bellavita, B Casciaro, S Di Maro… - Journal of medicinal …, 2021 - ACS Publications
The pharmacodynamic and pharmacokinetic properties of bioactive peptides can be
modulated by introducing conformational constraints such as intramolecular …
modulated by introducing conformational constraints such as intramolecular …
Structure-Based Design and Synthesis of Stapled 10Panx1 Analogues for Use in Cardiovascular Inflammatory Diseases
A Lamouroux, M Tournier, D Iaculli… - Journal of medicinal …, 2023 - ACS Publications
Following a rational design, a series of macrocyclic (“stapled”) peptidomimetics of 10Panx1,
the most established peptide inhibitor of Pannexin1 (Panx1) channels, were developed and …
the most established peptide inhibitor of Pannexin1 (Panx1) channels, were developed and …
NFYA promotes malignant behavior of triple-negative breast cancer in mice through the regulation of lipid metabolism
N Okada, C Ueki, M Shimazaki, G Tsujimoto… - Communications …, 2023 - nature.com
Two splicing variants exist in NFYA that exhibit high expression in many human tumour
types. The balance in their expression correlates with prognosis in breast cancer, but …
types. The balance in their expression correlates with prognosis in breast cancer, but …
A host–guest approach to combining enzymatic and artificial catalysis for catalyzing biomimetic monooxygenation
L Zhao, J Cai, Y Li, J Wei, C Duan - Nature Communications, 2020 - nature.com
Direct transfer of protons and electrons between two tandem reactions is still a great
challenge, because overall reaction kinetics is seriously affected by diffusion rate of the …
challenge, because overall reaction kinetics is seriously affected by diffusion rate of the …
Stapling of Peptides Potentiates the Antibiotic Treatment of Acinetobacter baumannii In Vivo
The rising incidence of multidrug resistance in Gram-negative bacteria underlines the
urgency for novel treatment options. One promising new approach is the synergistic …
urgency for novel treatment options. One promising new approach is the synergistic …