Identification of Promiscuous Small Molecule Activators in High-Throughput Enzyme Activation Screens
摘要:
It is recognized that high-throughput enzyme inhibition screens often return nonspecific inhibitors as. "hits". Recently, high-throughput screens for enzyme activators have led to the identification of several compounds with novel and potent biological activity. Here, we show that enzyme activation screens can also uncover compounds that activate multiple enzymes in a nonspecific fashion. Described herein are the general structural features of such compounds and methods to differentiate between specific and general enzyme activation.
One-Pot Anti-Markovnikov Hydroamination of Unactivated Alkenes by Hydrozirconation and Amination
作者:Alexandra E. Strom、John F. Hartwig
DOI:10.1021/jo401498w
日期:2013.9.6
A one-pot anti-Markovnikov hydroamination of alkenes is reported. The synthesis of primary and secondary amines from unactivated olefins was accomplished in the presence of a variety of functional groups. Hydrozirconation, followed by amination with nitrogen electrophiles, provides exclusive anti-Markovnikov selectivity. Most products are isolated in high yields without the use of column chromatography
Identification of Promiscuous Small Molecule Activators in High-Throughput Enzyme Activation Screens
作者:David R. Goode、Ryan K. Totten、James T. Heeres、Paul J. Hergenrother
DOI:10.1021/jm701583b
日期:2008.4.1
It is recognized that high-throughput enzyme inhibition screens often return nonspecific inhibitors as. "hits". Recently, high-throughput screens for enzyme activators have led to the identification of several compounds with novel and potent biological activity. Here, we show that enzyme activation screens can also uncover compounds that activate multiple enzymes in a nonspecific fashion. Described herein are the general structural features of such compounds and methods to differentiate between specific and general enzyme activation.
Surnin, V. A.; Stadnichuk, M. D., Journal of general chemistry of the USSR, 1985, vol. 55, # 9, p. 1822 - 1829