Small-molecule allosteric inhibitors of BAX

February 4th, 2019 by Thomas P. Garner

Small-molecule allosteric inhibitors of BAX

Small-molecule allosteric inhibitors of BAX, Published online: 04 February 2019; doi:10.1038/s41589-018-0223-0

Using biochemical and NMR studies, a class of small-molecule inhibitors termed BAX activation inhibitors were found to bind directly to a previously unrecognized pocket of inactive BAX and allosterically inhibit conformational changes in BAX.

A chemoproteomic portrait of the oncometabolite fumarate

February 4th, 2019 by Rhushikesh A. Kulkarni

A chemoproteomic portrait of the oncometabolite fumarate

A chemoproteomic portrait of the oncometabolite fumarate, Published online: 04 February 2019; doi:10.1038/s41589-018-0217-y

Chemoproteomic mapping of fumarate sensitive cysteines in a hereditary leiomyomatosis and renal cell carcinoma cell line revealed a critical cysteine in the protein–protein interaction interface of the SWI–SNF complex.

[ASAP] Chemical Diversification Based on Substrate Promiscuity of a Standalone Adenylation Domain in a Reconstituted NRPS System

February 4th, 2019 by Mengyi Zhu, Lijuan Wang, Jing He

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ACS Chemical Biology
DOI: 10.1021/acschembio.8b00938
  • Posted in ACS Chemical Biology, Publications
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[ASAP] Metabolic Regulation of the Epitranscriptome

February 1st, 2019 by Justin M. Thomas, Pedro J. Batista, Jordan L. Meier

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ACS Chemical Biology
DOI: 10.1021/acschembio.8b00951

[ASAP] <italic toggle=”yes”>N</italic>-Acyl <sc>l</sc>-Homocysteine Thiolactones Are Potent and Stable Synthetic Modulators of the RhlR Quorum Sensing Receptor in <italic toggle=”yes”>Pseudomonas aeruginosa</italic>

February 1st, 2019 by Michelle E. Boursier, Joshua B. Combs, Helen E. Blackwell

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ACS Chemical Biology
DOI: 10.1021/acschembio.8b01079
  • Posted in ACS Chemical Biology, Publications
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[ASAP] Antisense RNA-Based Strategy for Enhancing Surfactin Production in <italic toggle=”yes”>Bacillus subtilis</italic> TS1726 via Overexpression of the Unconventional Biotin Carboxylase II To Enhance ACCase Activity

January 31st, 2019 by Miaomiao Wang, Huimin Yu, Zhongyao Shen

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ACS Synthetic Biology
DOI: 10.1021/acssynbio.8b00459
  • Posted in ACS Synthetic Biology, Publications
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Combined chemosensitivity and chromatin profiling prioritizes drug combinations in CLL

January 28th, 2019 by Christian Schmidl

Combined chemosensitivity and chromatin profiling prioritizes drug combinations in CLL

Combined chemosensitivity and chromatin profiling prioritizes drug combinations in CLL, Published online: 28 January 2019; doi:10.1038/s41589-018-0205-2

Epigenome profiling in combination with imaging-based chemosensitivity and integrative bioinformatic analysis establishes a method for detecting therapy-induced vulnerabilities, as shown here for ibrutinib-treated chronic lymphocytic leukemia.
  • Posted in Nat Chem Biol, Publications
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An allosteric MALT1 inhibitor is a molecular corrector rescuing function in an immunodeficient patient

January 28th, 2019 by Jean Quancard

An allosteric MALT1 inhibitor is a molecular corrector rescuing function in an immunodeficient patient

An allosteric MALT1 inhibitor is a molecular corrector rescuing function in an immunodeficient patient, Published online: 28 January 2019; doi:10.1038/s41589-018-0222-1

An allosteric inhibitor of the proteolytic activity of the CBM signalosome complex scaffolding protein MALT1 acts as a pharmacological chaperone to stabilize a mutant MALT1 carried by an immunodeficient patient.
  • Posted in Nat Chem Biol, Publications
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Bacterial sensors define intracellular free energies for correct enzyme metalation

January 28th, 2019 by Deenah Osman

Bacterial sensors define intracellular free energies for correct enzyme metalation

Bacterial sensors define intracellular free energies for correct enzyme metalation, Published online: 28 January 2019; doi:10.1038/s41589-018-0211-4

The sensitivities of a set of bacterial metal-sensing transcriptional regulators explain how a protein, such as the cobalt chelatase CbiK, is metalated with its cognate metal in cells rather than mis-metalated with more tightly binding metals.
  • Posted in Nat Chem Biol, Publications
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Freedom of movement

January 21st, 2019 by Ulrich Rass

Freedom of movement

Freedom of movement, Published online: 21 January 2019; doi:10.1038/s41589-019-0224-7

Holliday junction resolvases lock dynamic DNA four-way junctions into specific structural conformations for symmetric DNA cleavage. Single-molecule studies now reveal that resolvases can relax their grip, enabling Holliday junction conformer transitions and branch migration in the enzyme-bound form.