Proteasomes: Attack of cancer drugs

September 20th, 2016 by Mirella Bucci

Nature Chemical Biology 12, 763 (2016). doi:10.1038/nchembio.2198

Author: Mirella Bucci

Stapled peptides: How to be quick on the uptake

September 20th, 2016 by Joshua A Kritzer

Nature Chemical Biology 12, 764 (2016). doi:10.1038/nchembio.2183

Author: Joshua A Kritzer

Stapled helices are promising compounds for inhibiting intracellular protein–protein interactions, but the discovery of peptides with the key property of cellular uptake has taken place largely through trial and error. A new study defines physicochemical parameters for designing hydrocarbon-stapled helices with a greater likelihood of cellular uptake.

Phospholipids: How to flip a flippase

September 20th, 2016 by Caitlin Deane

Nature Chemical Biology 12, 763 (2016). doi:10.1038/nchembio.2199

Author: Caitlin Deane

Single-molecule biophysics: TALEs spin along, but not around

September 20th, 2016 by Sebastian Becker

Nature Chemical Biology 12, 766 (2016). doi:10.1038/nchembio.2182

Authors: Sebastian Becker & Jens Boch

TALE proteins search for target sequences along a DNA substrate in a uniquely one-dimensional and non-rotating fashion.

Host–microbe interactions: DAO does it

September 20th, 2016 by Mirella Bucci

Nature Chemical Biology 12, 763 (2016). doi:10.1038/nchembio.2196

Author: Mirella Bucci

Corrigendum: Structural biology: HDAC6 finally crystal clear

September 20th, 2016 by Yanli Liu

Nature Chemical Biology 12, 885 (2016). doi:10.1038/nchembio1016-885

Author: Yanli Liu, Li Li & Jinrong Min

Post-translational modifications: Bonds that bind

September 20th, 2016 by Marcey L Waters

Nature Chemical Biology 12, 768 (2016). doi:10.1038/nchembio.2186

Author: Marcey L Waters

Scientists find that oxidation of methionine induces favorable interactions with aromatic groups in proteins, contrary to conventional wisdom, providing new molecular insight into the structural and biological impact of methionine oxidation.

Transcriptional regulation: Stuck in traffic

September 20th, 2016 by Grant Miura

Nature Chemical Biology 12, 763 (2016). doi:10.1038/nchembio.2197

Author: Grant Miura

Transcriptional kinases: Caught by a sticky drug

September 20th, 2016 by Dalibor Blazek

Nature Chemical Biology 12, 765 (2016). doi:10.1038/nchembio.2184

Author: Dalibor Blazek

A new study reports THZ531 as a covalent CDK12/CDK13 inhibitor affecting transcription. Application of the compound in cells decreases transcription elongation of DNA damage response genes and key super-enhancer-associated transcription factor genes, with important implications for targeted cancer therapy.

Compounds that select against the tetracycline-resistance efflux pump

September 19th, 2016 by Laura K Stone

Nature Chemical Biology 12, 902 (2016). doi:10.1038/nchembio.2176

Authors: Laura K Stone, Michael Baym, Tami D Lieberman, Remy Chait, Jon Clardy & Roy Kishony

We developed a competition-based screening strategy to identify compounds that invert the selective advantage of antibiotic resistance. Using our assay, we screened over 19,000 compounds for the ability to select against the TetA tetracycline-resistance efflux pump in Escherichia coli and identified two hits, β-thujaplicin and disulfiram. Treating a tetracycline-resistant population with β-thujaplicin selects for loss of the resistance gene, enabling an effective second-phase treatment with doxycycline.

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