Development of a double-stapled peptide stabilizing both α-helix and β-sheet structures for degrading transcription factor AR-V7

B Ma, D Liu, M Zheng, Z Wang, D Zhang, Y Jian, J Ma… - JACS Au, 2024 - ACS Publications
Peptide drugs offer distinct advantages in therapeutics; however, their limited stability and
membrane penetration abilities hinder their widespread application. One strategy to …

Peptide Stapling through Site-Directed Conjugation of Triazine Moieties to the Tyrosine Residues of a Peptide

Y Zhang, R Yin, H Jiang, C Wang, X Wang… - Organic …, 2023 - ACS Publications
Peptide stapling is a strategy for improving the biological properties of peptides. Herein, we
report a novel method for stapling peptides that utilizes bifunctional triazine moieties for two …

[HTML][HTML] Identification of a short ACE2-derived stapled peptide targeting the SARS-CoV-2 spike protein

L Calugi, G Sautariello, E Lenci, ML Mattei… - European Journal of …, 2023 - Elsevier
The design and synthesis of a series of peptide derivatives based on a short ACE2 α-helix 1
epitope and subsequent [i-i+ 4] stapling of the secondary structure resulted in the …

Comparative Analysis of Cyclization Techniques in Stapled Peptides: Structural Insights into Protein–Protein Interactions in a SARS-CoV-2 Spike RBD/hACE2 Model …

S Ferková, U Froehlich, MÉ Nepveu-Traversy… - International Journal of …, 2023 - mdpi.com
Medicinal chemistry is constantly searching for new approaches to develop more effective
and targeted therapeutic molecules. The design of peptidomimetics is a promising emerging …

[HTML][HTML] Synthesis of Novel Planar-Chiral Charge-Compensated nido-Carborane-Based Amino Acid

DA Gruzdev, AA Telegina, MA Ezhikova, MI Kodess… - Molecules, 2024 - mdpi.com
Amino acids with unusual types of chirality and their derivatives have recently attracted
attention as precursors in the synthesis of chiral catalysts and peptide analogues with …

[HTML][HTML] Conformational Analysis and Organocatalytic Activity of Helical Stapled Peptides Containing α-Carbocyclic α, α-Disubstituted α-Amino Acids

A Iyoshi, A Ueda, T Umeno, T Kato, K Hirayama, M Doi… - Molecules, 2024 - mdpi.com
Conformational freedom-restricted peptides, such as stapled peptides, play a crucial role in
the advancement of functional peptide development. We synthesized stapled octapeptides …

Cyclopeptide Synthesis by Ring-Closing Metathesis

H Yamamoto, T Hattori - Synfacts, 2022 - thieme-connect.com
Cyclopeptide Synthesis by Ring-Closing Metathesis Page 1 © 2022. Thieme. All rights reserved.
Georg Thieme Verlag KG, Rüdigerstraße 14, 70469 Stuttgart, Germany 565 A. UEDA*, Y …

[PDF][PDF] 環状アミノ酸を利用した立体選択的ペプチド側鎖架橋

真倉唯 - 2023 - nagasaki-u.repo.nii.ac.jp
[背景・目的] タンパク質は 20 種類の L-α-アミノ酸の織りなす多様な配列により構成されており,
生理機能の発現では α-ヘリックス構造が重要である. タンパク質に比べ合成が容易なペプチドは …

[引用][C] Synthesis and application of helical peptide foldamer using α, α-disubstituted α-amino acids

A Ueda, K Sato, Y Makura, T Umeno, S Kakazu…