Systematic targeting of protein–protein interactions

AE Modell, SL Blosser, PS Arora - Trends in pharmacological sciences, 2016 - cell.com
Over the past decade, protein–protein interactions (PPIs) have gone from being neglected
as 'undruggable'to being considered attractive targets for the development of therapeutics …

Internal Peptide Late‐Stage Diversification: Peptide‐Isosteric Triazoles for Primary and Secondary C(sp3)−H Activation

M Bauer, W Wang, MM Lorion, C Dong… - Angewandte Chemie …, 2018 - Wiley Online Library
Abstract Secondary C (sp3)− H arylations were accomplished by palladium catalysis with
triazoles as peptide bond isosteres. The unique power of this approach is highlighted by the …

Facets of click-mediated triazoles in decorating amino acids and peptides

SS Bag, A Banerjee, S Sinha, S Jana - Chemical Communications, 2025 - pubs.rsc.org
Decorating biomolecular building blocks, such as amino acids, to afford desired and
tuneable photophysical/biophysical properties would allow chemical biologists to use them …

[HTML][HTML] β-Turn mimetic synthetic peptides as amyloid-β aggregation inhibitors

S Deike, S Rothemund, B Voigt, S Samantray… - Bioorganic …, 2020 - Elsevier
Aggregation of amyloid peptides results in severe neurodegenerative diseases. While the
fibril structures of Aβ 40 and Aβ 42 have been described recently, resolution of the …

Composition and Conformation of Hetero‐ versus Homo‐Fluorinated Triazolamers Influence their Activity on Islet Amyloid Polypeptide Aggregation

J Laxio Arenas, J Lesma, T Ha‐Duong… - … A European Journal, 2024 - Wiley Online Library
Novel fluorinated foldamers based on aminomethyl‐1, 4‐triazolyl‐difluoroacetic acid (1, 4‐
Tz− CF2) units were synthesized and their conformational behaviour was studied by NMR …

Glucosyltriazole amphiphile treatment attenuates breast cancer by modulating the AMPK signaling

NK Chouhan, A Eedara, MN Talati… - Drug Development …, 2024 - Wiley Online Library
Breast cancer is the second most frequent cancer among women. Out of various subtypes,
triple‐negative breast cancers (TNBCs) account for 15% of breast cancers and exhibit more …

Microwave-assisted synthesis of peptidomimetic trans-delta-aminopent-3-enoic acid and its derivatives

K Saranraj, KMP Raja - New Journal of Chemistry, 2024 - pubs.rsc.org
An environmentally friendly solution-phase synthesis has been developed for producing
trans-5-aminopenta-3-enoic acid (trans-δ-Apa), along with several Nα-and C-terminal …

Synthesis, photophysical properties of triazolyl-donor/acceptor chromophores decorated unnatural amino acids: Incorporation of a pair into Leu-enkephalin peptide …

SS Bag, S Jana, MK Pradhan - Bioorganic & Medicinal Chemistry, 2016 - Elsevier
The research in the field of design and synthesis of unnatural amino acids is growing at a
fast space for the increasing demand of proteins of potential therapeutics and many other …

Application of C-terminal 7-azabicyclo [2.2. 1] heptane to stabilize β-strand-like extended conformation of a neighboring α-amino acid

L Zhai, S Wang, M Nara, K Takeuchi… - The Journal of …, 2018 - ACS Publications
β-Strands are formed by extended linear peptide chains that are usually paired to form β-
sheet structure through interstrand hydrogen bonding. Linking a structured organic molecule …

N-Difluoromethyl-triazole as a constrained scaffold in peptidomimetics

M Mamone, RSB Gonçalves, F Blanchard… - Chemical …, 2017 - pubs.rsc.org
The N-difluoromethyl triazolo-β-aza-ε-amino acid present in the core of peptides led to
constrained conformations due to CH–F and NH–F interactions. Pseudotetrapeptides were …