64411-38-7Relevant academic research and scientific papers
Small-molecule inhibitors that target protein-protein interactions in the RAD51 family of recombinases
Scott, Duncan E.,Coyne, Anthony G.,Venkitaraman, Ashok,Blundell, Tom L.,Abell, Chris,Hyv?nen, Marko
supporting information, p. 296 - 303 (2015/02/05)
The development of small molecules that inhibit protein-protein interactions continues to be a challenge in chemical biology and drug discovery. Herein we report the development of indole-based fragments that bind in a shallow surface pocket of a humanised surrogate of RAD51. RAD51 is an ATP-dependent recombinase that plays a key role in the repair of doublestrand DNA breaks. It both self-associates, forming filament structures with DNA, and interacts with the BRCA2 protein through a common "FxxA" tetrapeptide motif. We elaborated previously identified fragment hits that target the FxxA motif site and developed small-molecule inhibitors that are approximately 500-fold more potent than the initial fragments. The lead compounds were shown to compete with the BRCA2-derived Ac-FHTA-NH2 peptide and the self-association peptide of RAD51, but they had no effect on ATP binding. This study is the first reported elaboration of small-molecular-weight fragments against this challenging target.
Preparation of boc-amino-acid or peptide aldehydes via reduction of corresponding phenyl esters
Zlatoidsky
, p. 150 - 154 (2007/10/02)
A new alternative method for the preparation of amino-acid and peptide aldehydes based on reduction of corresponding phenyl esters with lithium tri(tert-butoxy)aluminium hydride is described.
ACTIVATION OF A CARBOXY GROUP BY DIALKYL PYROCARBONATES. SYNTHESIS OF SYMMETRICAL ANHYDRIDES AND ARYL ESTERS OF N-PROTECTED AMINO ACIDS USING DI-tert-BUTYL PYROCARBONATE AS CONDENSING REAGENT
Pozdnev, V. F.,Chernaya, M. Yu.
, p. 333 - 337 (2007/10/02)
It has been shown that di-tert-butyl pyrocarbonate can be used as a condensing reagent in the production of anhydrides and some aryl esters of carboxylic acids.The synthesis of anhydrides and of phenyl, p-nitrophenyl, β-naphtyl, and quinolin-8-yl esters of N-protected amino acids is described.
