Featured
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Article |
Large-scale chemical–genetics yields new M. tuberculosis inhibitor classes
A high-throughput chemical–genetic screening approach for the discovery of targets and chemicals to treat Mycobacterium tuberculosis yields tenfold more hit compounds than conventional whole-cell screening methods.
- Eachan O. Johnson
- , Emily LaVerriere
- & Deborah T. Hung
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Letter |
A Cdk9–PP1 switch regulates the elongation–termination transition of RNA polymerase II
The kinase Cdk9 and the phosphatase Dis2 regulate the termination of transcription in fission yeast in part by controlling the phosphorylation state of the elongation factor Spt5.
- Pabitra K. Parua
- , Gregory T. Booth
- & Robert P. Fisher
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Letter |
Transcription control by the ENL YEATS domain in acute leukaemia
ENL, identified in a genome-scale loss-of-function screen as a crucial requirement for proliferation of acute leukaemia, is required for leukaemic gene expression, and its YEATS chromatin-reader domain is essential for leukaemic growth.
- Michael A. Erb
- , Thomas G. Scott
- & James E. Bradner
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Article |
Targeting Plasmodium PI(4)K to eliminate malaria
The lipid kinase phosphatidylinositol-4-OH kinase (PI(4)K) is identified as a target of the imidazopyrazines, a new antimalarial compound class that can inhibit several Plasmodium species at each stage of the parasite life cycle; the imidazopyrazines exert their inhibitory action by interacting with the ATP-binding pocket of PI(4)K.
- Case W. McNamara
- , Marcus C. S. Lee
- & Elizabeth A. Winzeler
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Article |
Chemical genetic discovery of targets and anti-targets for cancer polypharmacology
Using Ret-driven models of multiple endocrine neoplasia, it is shown that optimal kinase inhibition must aim to target an ideal spectrum of tumour-relevant kinases while avoiding ‘anti-targets’ that cause unwanted toxicity.
- Arvin C. Dar
- , Tirtha K. Das
- & Ross L. Cagan
Selective control of parasitic nematodes using bioactivated nematicides