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A chemical-genetic method for the generation of target-specific protein kinase inhibitors has
been developed recently. This strategy utilizes a functionally silent active-site mutation to …

Genome editing with CRISPR-Cas nucleases has been applied successfully to a wide range
of cells and organisms. There is, however, considerable variation in the efficiency of …

Protein kinases have proved to be largely resistant to the design of highly specific inhibitors,
even with the aid of combinatorial chemistry. The lack of these reagents has complicated …

In eukaryotic cells, nutrient starvation induces the bulk degradation of cellular materials; this
process is called autophagy. In the yeast Saccharomyces cerevisiae, most of the ATG (aut …

The kinase Akt plays a central role as a regulator of multiple growth factor input signals, thus
making it an attractive anticancer drug target. A-443654 is an ATP-competitive Akt inhibitor …

Meiosis is thought to require the protein kinase Ime2 early for DNA replication and the cyclin-
dependent kinase Cdc28 late for chromosome segregation. To elucidate the roles of these …

Background Small-molecule inhibitors that can target individual kinases are powerful tools
for use in signal transduction research. It is difficult to find such compounds because of the …

A strategy for targeting protein kinases with large ATP-binding sites by using bulky and rigid
octahedral ruthenium complexes as structural scaffolds is presented. A highly potent and …

1. INTRODUCTION Nitrogen-containing heterocycles are widely distributed in nature and
essential for life, playing a vital role in the metabolism of all living cells. Among the many …