Hara, Toshiaki published the artcileProbing the Structural Requirements of Peptoids That Inhibit HDM2-p53 Interactions, Safety of tert-Butyl 3-(2-aminoethyl)-1H-indole-1-carboxylate, the publication is Journal of the American Chemical Society (2006), 128(6), 1995-2004, database is CAplus and MEDLINE.
Many cellular processes are controlled by protein-protein interactions, and selective inhibition of these interactions could lead to the development of new therapies for several diseases. For example, overexpression of the protein HDM2 (human double minute 2), which binds to and inactivates the protein p53, has been linked to tumor aggressiveness and drug resistance in cancer. In creating inhibitors of protein-protein interactions, one strategy is to recreate the three-dimensional arrangement of side chains that are involved in the binding of one protein to another, using a nonnatural scaffold as the attachment point for the side chains. Here, the authors used oligomeric peptoids as the scaffold to develop a general strategy to rationally design synthetic mols. that can be optimized for inhibition of protein-protein interactions. Structural information on the HDM2-p53 complex was used to design the first class of peptoid inhibitors, and this work provides, in detail, the strategy to modify peptoids with the appropriate side chains that are effective inhibitors of HDM2-p53 binding. While the authors initially tried to develop rigid, helical peptoids as HDM2 binders, the best inhibitors were surprisingly peptoids that lacked any helix-promoting groups. These results indicate that starting with rigid peptoid scaffolds may not always be optimal to develop new inhibitors.
Journal of the American Chemical Society published new progress about 167015-84-1. 167015-84-1 belongs to indole-building-block, auxiliary class Indols, name is tert-Butyl 3-(2-aminoethyl)-1H-indole-1-carboxylate, and the molecular formula is C15H20N2O2, Safety of tert-Butyl 3-(2-aminoethyl)-1H-indole-1-carboxylate.
Referemce:
https://www.nature.com/articles/s41429-020-0333-2,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles