small molecules as protein-proteininteraction inhibitors

Small Molecules as Protein-Protein Interaction Inhibitors

Protein-protein interactions (PPIs) can be considered as a vast class of therapeutic targets. PPIs play critical roles in all biological functions and are often dysregulated in disease. Despite their functional role both inside and outside the cell, over the past decades PPIs have been neglected as undruggable targets. This was in part due to the fact that PPI interfaces are generally flat and ...

Design, Synthesis and Evaluation of Substituted Aryl-2-Nitrovinyl Derivatives as Small Molecules Proteasome Inhibitors

Based on the existing structure activity relationship for proteasome inhibitors, a number of substituted aryl-2-nitrovinyl derivatives have been synthesized as Michael acceptor and their cytotoxicity and proteasome inhibitory effects were evaluated on two cancer cell lines. Compound 2d exhibited IC50 values of 0.71 and 17.79 μM comparable to bortezomib against MCF-7 and PC-3, respectively. The ...

Design, Synthesis and Evaluation of Substituted Aryl-2-Nitrovinyl Derivatives as Small Molecules Proteasome Inhibitors

Based on the existing structure activity relationship for proteasome inhibitors, a number of substituted aryl-2-nitrovinyl derivatives have been synthesized as Michael acceptor and their cytotoxicity and proteasome inhibitory effects were evaluated on two cancer cell lines. Compound 2d exhibited IC50 values of 0.71 and 17.79 μM comparable to bortezomib against MCF-7 and PC-3, respectively. The ...

Small-molecule inhibitors of protein-protein interactions.

Protein-protein interactions regulate almost all aspects of cellular signaling and aberrant protein-protein interactions have the potential to cause or contribute to human disease. The modulation of these interactions by drug-like molecules would offer previously unavailable opportunities to explore the relevance of pre-selected protein-protein interactions for cellular signaling, as well as be...

INTERACTION OF PROTEINS WITH SMALL MOLECULES

Carbonic Anhydrase Inhibitors and Activators: Small Organic Molecules as Drugs and Prodrugs

This chapter concerns influences of inhibitors and activators on carbonic anhydrase isoenzymes of various living systems. Carbonic anhydrase (EC 4.2.1.1., CA) is a pH regulatory/metabolic enzyme in all life kingdoms, found in organisms all over the phylogenetic tree (Supuran, 2008a,b,c) catalyzing the hydration of carbon dioxide to bicarbonate and the corresponding dehydration of bicarbonate in...