90514-72-0Relevant articles and documents
Synthesis and antimicrobial activity of novel 2-[4-(1H-benzimidazol-1-yl) phenyl]-1H-benzimidazoles
Alp, Mehmet,Goker, Ali Hakan,Altanlar, Nurten
, p. 152 - 156 (2014)
A new class of 2-[4-(1H-benzimidazol-1-yl)phenyl]-1H-benzimidazoles (13-22) were synthesized via cyclocondensation reaction of the substituted 1,2-phenylenediamines (1, 4-12) and 1-(4-formylpheny)-1H-benzimidazole (3). The synthesized compounds were evalu
PROTEIN-PROTEIN INTERACTION STABILIZERS
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Paragraph 0953-0954; 0959, (2021/10/11)
Provided herein, inter alia, are stabilizers of protein-protein interactions and methods of identifying and using the same.
Reversible Covalent Imine-Tethering for Selective Stabilization of 14-3-3 Hub Protein Interactions
Brunsveld, Luc,Cossar, Peter J.,Levy, Laura M.,Ottmann, Christian,Valenti, Dario,Van Dijck, Lars,Wolter, Madita
supporting information, p. 8454 - 8464 (2021/06/27)
The stabilization of protein complexes has emerged as a promising modality, expanding the number of entry points for novel therapeutic intervention. Targeting proteins that mediate protein-protein interactions (PPIs), such as hub proteins, is equally challenging and rewarding as they offer an intervention platform for a variety of diseases, due to their large interactome. 14-3-3 hub proteins bind phosphorylated motifs of their interaction partners in a conserved binding channel. The 14-3-3 PPI interface is consequently only diversified by its different interaction partners. Therefore, it is essential to consider, additionally to the potency, also the selectivity of stabilizer molecules. Targeting a lysine residue at the interface of the composite 14-3-3 complex, which can be targeted explicitly via aldimine-forming fragments, we studied the de novo design of PPI stabilizers under consideration of potential selectivity. By applying cooperativity analysis of ternary complex formation, we developed a reversible covalent molecular glue for the 14-3-3/Pin1 interaction. This small fragment led to a more than 250-fold stabilization of the 14-3-3/Pin1 interaction by selective interfacing with a unique tryptophan in Pin1. This study illustrates how cooperative complex formation drives selective PPI stabilization. Further, it highlights how specific interactions within a hub proteins interactome can be stabilized over other interactions with a common binding motif.
Benzimidazolyl benzaldehyde condensed rhodamine hydrazine hydrate Schiff base and preparation method thereof
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Paragraph 0022; 0029-0030; 0033-0034; 0037-0038; 0041; ..., (2021/07/14)
The invention belongs to the field of fluorescent probes, and particularly relates to a benzimidazolyl benzaldehyde rhodamine hydrazine hydrate Schiff base fluorescent probe. A fluorescent switch is turned on in the presence of iron ions by utilizing a ph