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Inter- vs Intramolecular Aldehyde-Alkyne-Amine A sup 3 /sup -Reaction in the Solution-Phase Synthesis of a Potent Macrocyclic Azapeptide CD36 Modulator

Author(s): Maarouf-Mesli N; Fonseca JC; Harvey SM; Chauhan PS; Mulumba M; Ahsanullah None; Selka A; Meneksedag Erol D; Chemtob S; Ong H; Polyak F; Lubell WD;

Modern macrocyclic peptides feature unnatural elements that are used to improve the activity and pharmacokinetic properties. Chemistry beyond peptide synthesis must, however, be employed to introduce such elements. Notably, application of the copper-catalyzed aldehyde-alkyne-amine A3-reaction in ...

Article GUID: 42049622


Secondary Structure Stabilization of Macrocyclic Antimicrobial Peptides via Cross-Link Swapping

Author(s): Nazeer N; Kooner N; Ghimire A; Rainey JK; Lubell WD; Meneksedag-Erol D; Ahmed M;

Lactam cross-links have been employed to stabilize the helical secondary structure and enhance the activity and physiological stability of antimicrobial peptides; however, stabilization of ß-sheets via lactamization has not been observed. In the present study, lactams between the side chains of C- and N-terminal residues have been used to stabilize the ß- ...

Article GUID: 38771638


Cyst Reduction in a Polycystic Kidney Disease Drosophila Model Using Smac Mimics.

Author(s): Millet-Boureima C, Chingle R, Lubell WD, Gamberi C

Biomedicines. 2019 Oct 18;7(4): Authors: Millet-Boureima C, Chingle R, Lubell WD, Gamberi C

Article GUID: 31635379


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