Electric Literature of 2008-04-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.2008-04-0, Name is 2-(Trifluoromethyl)benzo[d]oxazole, molecular formula is C8H4F3NO. In a Article£¬once mentioned of 2008-04-0
Structure-Based Design of Inhibitors Selective for Human Proteasome beta2c or beta2i Subunits
Subunit-selective proteasome inhibitors are valuable tools to assess the biological and medicinal relevance of individual proteasome active sites. Whereas the inhibitors for the beta1c, beta1i, beta5c, and beta5i subunits exploit the differences in the substrate-binding channels identified by X-ray crystallography, compounds selectively targeting beta2c or beta2i could not yet be rationally designed because of the high structural similarity of these two subunits. Here, we report the development, chemical synthesis, and biological screening of a compound library that led to the identification of the beta2c- and beta2i-selective compounds LU-002c (4; IC50 beta2c: 8 nM, IC50 beta2i/beta2c: 40-fold) and LU-002i (5; IC50 beta2i: 220 nM, IC50 beta2c/beta2i: 45-fold), respectively. Co-crystal structures with beta2 humanized yeast proteasomes visualize protein-ligand interactions crucial for subunit specificity. Altogether, organic syntheses, activity-based protein profiling, yeast mutagenesis, and structural biology allowed us to decipher significant differences of beta2 substrate-binding channels and to complete the set of subunit-selective proteasome inhibitors.
A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 2008-04-0
Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem