Peptidomimetic toolbox for drug discovery

E Lenci, A Trabocchi - Chemical Society Reviews, 2020 - pubs.rsc.org
The art of transforming peptides into drug leads is still a dynamic and fertile field in medicinal
chemistry and drug discovery. Peptidomimetics can respond to peptide limitations by …

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 …

Macrocyclization strategies for cyclic peptides and peptidomimetics

C Bechtler, C Lamers - RSC medicinal chemistry, 2021 - pubs.rsc.org
Peptides are a growing therapeutic class due to their unique spatial characteristics that can
target traditionally “undruggable” protein–protein interactions and surfaces. Despite their …

Antimicrobial peptides–Advances in development of therapeutic applications

HX Luong, TT Thanh, TH Tran - Life sciences, 2020 - Elsevier
The severe infection is becoming a significant health problem which threaten the lives of
patients and the safety and economy of society. In the way of finding new strategy …

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 …

Getting across the cell membrane: an overview for small molecules, peptides, and proteins

NJ Yang, MJ Hinner - Site-Specific Protein Labeling: Methods and …, 2014 - Springer
The ability to efficiently access cytosolic proteins is desired in both biological research and
medicine. However, targeting intracellular proteins is often challenging, because to reach …

The future of peptide‐based drugs

DJ Craik, DP Fairlie, S Liras… - Chemical biology & drug …, 2013 - Wiley Online Library
The suite of currently used drugs can be divided into two categories–traditional 'small
molecule'drugs with typical molecular weights of< 500 Da but with oral bioavailability, and …

New modalities for challenging targets in drug discovery

E Valeur, SM Guéret, H Adihou… - Angewandte Chemie …, 2017 - Wiley Online Library
Our ever‐increasing understanding of biological systems is providing a range of exciting
novel biological targets, whose modulation may enable novel therapeutic options for many …

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 …

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, C Tovar… - Proceedings of the …, 2013 - pnas.org
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 …