Results 21 to 30 of about 11,685 (174)

Rational design, synthesis and structural characterization of peptides and peptidomimetics to target Hsp90/Cdc37 interaction for treating hepatocellular carcinoma

Computational and Structural Biotechnology Journal, 2023
Heat shock protein 90 (Hsp90) and cell division cycle 37 (Cdc37) work together as a molecular chaperone complex to regulate the activity of a multitude of client protein kinases.
Surya Sukumaran, Mingdian Tan, Shulamit Fluss Ben-Uliel, Hui Zhang, Marta De Zotti, Mei-Sze Chua, Samuel K. So, Nir Qvit   +7 more
doaj   +1 more source

Combinatorial assembly of small molecules into bivalent antagonists of TrkC or TrkA receptors.

PLoS ONE, 2014
A library of peptidomimetics was assembled combinatorially into dimers on a triazine-based core. The pharmacophore corresponds to β-turns of the neurotrophin polypeptides neurotrophin-3 (NT-3), nerve growth factor (NGF), or brain-derived neurotrophic ...
Fouad Brahimi, Eunhwa Ko, Andrey Malakhov, Kevin Burgess, H Uri Saragovi   +4 more
doaj   +1 more source

Development of peptidomimetic ligands of Pro-Leu-Gly-NH2 as allosteric modulators of the dopamine D2 receptor

Beilstein Journal of Organic Chemistry, 2013
A variety of stable, small-molecule peptidomimetic ligands have been developed to elucidate the mechanism by which the neuropeptide Pro-Leu-Gly-NH2 (PLG) modulates dopaminergic neurotransmission.
Swapna Bhagwanth, Ram K. Mishra, Rodney L. Johnson   +2 more
doaj   +1 more source

Exploitation of the Ugi 5-Center-4-Component Reaction (U-5C-4CR) for the Generation of Diverse Libraries of Polycyclic (Spiro)Compounds

Frontiers in Chemistry, 2018
An Ugi multicomponent reaction with chiral cyclic amino acids, benzyl isocyanide and cyclic ketones (or acetone) has been exploited as key step for the generation of peptidomimetics.
Lisa Moni, Fabio De Moliner, Silvia Garbarino, Jörn Saupe, Christian Mang, Andrea Basso   +5 more
doaj   +1 more source

Downsizing Electrophilic MAX‐Derived Helical Zipper Peptides to Covalently Bind and Degrade Oncogenic MYC

Angewandte Chemie, EarlyView.
Oncogenic MYC is a transcription factor that is difficult to inhibit. However, precise positioning of an acrylamide electrophile in MAX to covalently bond to the unique Cys438 in MYC, enabled shortening and optimizing of MAX‐derived, helix‐constrained peptides with high‐affinity and selectivity.
Aline Dantas de Araujo, Lei Luo, Mahan Azad, Miao Yu, Jody M. Mason, Junxian Lim, Timothy A. Hill, David P. Fairlie   +7 more
wiley   +2 more sources

Polyproline: A Synthetic Polypeptide With Unique Properties

Angewandte Chemie, EarlyView.
Poly‐L‐proline is a unique polypeptide distinguished by its well‐defined secondary structures and unusual thermal behavior. This mini review highlights recent advances in the synthesis of poly‐L‐proline by N‐carboxyanhydride (NCA) polymerization, the formation of structurally defined architectures and nanostructures, and emerging strategies that ...
Rosanna Le Scouarnec, Josué M. Galindo, Colin Bonduelle, Andreas Heise   +3 more
wiley   +2 more sources

Control of Helix Screw‐Sense Preference in Dynamic Foldamers of meso Symmetry Built From Chiral Monomeric Units

Angewandte Chemie, EarlyView.
Sequence‐diverse meso and “near‐meso” oligourea foldamers are reported and exhibit stimulus‐responsive helix screw‐sense control governed by terminal‐group desymmetrization and sequence‐encoded helix stability. ABSTRACT Meso oligoureas are dynamic hydrogen‐bonded foldamers capable of reversible helix polarity inversion but have so far been limited to ...
Naveen Gupta, Mégane Bornerie, Bo Li, Antoine Hacihasanoglu, Orlando Villegas Bello, Stéphanie Antunes, Estelle Morvan, Jean‐Marc Sotiropoulos, Philippe Carbonnière, Morgane Pasco, Brice Kauffmann, Céline Douat, Sung Hyun Yoo, Gilles Guichard   +13 more
wiley   +2 more sources

Improvement on Permeability of Cyclic Peptide/Peptidomimetic: Backbone N-Methylation as A Useful Tool

Marine Drugs, 2021
Peptides have a three-dimensional configuration that can adopt particular conformations for binding to proteins, which are well suited to interact with larger contact surface areas on target proteins.
Yang Li, Wang Li, Zhengshuang Xu
doaj   +1 more source

The Synthesis and Evaluation of Aminocoumarin Peptidomimetics as Cytotoxic Agents on Model Bacterial E. coli Strains

, 2021
This work presents the successful synthesis of a library of novel peptidomimetics via Ugi multicomponent reaction. Most of these peptidomimetics contain differently substituted aminocoumarin; 7-amino-4-methylcoumarin and 7-amino-4-(trifluoromethyl ...
Ryszard Ostaszewski, Paweł Kowalczyk, Grzegorz Skiba, Mateusz Szymczak, Karol Kramkowski, Dorota Sulejczak, Stanisława Raj, Patrycja Kleczkowska, Monika Wilk, Parul Parul   +9 more
core   +1 more source

A readily applicable strategy to convert peptides to peptoid-based therapeutics. [PDF]

PLoS ONE, 2013
Incorporation of unnatural amino acids and peptidomimetic residues into therapeutic peptides is highly efficacious and commonly employed, but generally requires laborious trial-and-error approaches.
Minyoung Park, Modi Wetzler, Theodore S Jardetzky, Annelise E Barron   +3 more
doaj   +1 more source