1233517-63-9Relevant academic research and scientific papers
Selective and potent proteomimetic inhibitors of intracellular protein-protein interactions
Barnard, Anna,Long, Krya,Martin, Heather L.,Miles, Jennifer A.,Edwards, Thomas A.,Tomlinson, Darren C.,Macdonald, Andrew,Wilson, Andrew J.
, p. 2960 - 2965 (2015/06/02)
Inhibition of protein-protein interactions (PPIs) represents a major challenge in chemical biology and drug discovery. α-Helix mediated PPIs may be amenable to modulation using generic chemotypes, termed "proteomimetics", which can be assembled in a modul
N-alkylated oligoamide α-helical proteomimetics
Campbell, Frederick,Plante, Jeffrey P.,Edwards, Thomas A.,Warriner, Stuart L.,Wilson, Andrew J.
supporting information; experimental part, p. 2344 - 2351 (2010/07/08)
Generic approaches for the design and synthesis of small molecule inhibitors of protein-protein interactions (PPIs) represent a key objective in modern chemical biology. Within this context, the α-helix mediated PPIs have received considerable attention as targets for inhibition using small molecules, foldamers and proteomimetics. This manuscript describes a novel N-alkylated aromatic oligoamide proteomimetic scaffold and its solid-phase synthesis - the first time such an approach has been used for proteomimetics. The utility of these scaffolds as proteomimetics is exemplified through the identification of potent μM inhibitors of the p53-hDM2 helix mediated PPI - a key oncogenic target.
