Structure-guided development of YEATS domain inhibitors by targeting π-π-π stacking

October 29th, 2018 by Xin Li

Structure-guided development of YEATS domain inhibitors by targeting π-π-π stacking

Structure-guided development of YEATS domain inhibitors by targeting π-π-π stacking, Published online: 29 October 2018; doi:10.1038/s41589-018-0144-y

An inhibitor of the YEATS domain was developed by targeting a unique π-π-π stacking in the YEATS–Kcr recognition. An ENL YEATS-selective inhibitor, XL-13m, helps probe the YEATS-dependent role of ENL in the leukemogenic transcription program.
  • Posted in Nat Chem Biol, Publications
  • Comments Off on Structure-guided development of YEATS domain inhibitors by targeting π-π-π stacking

Enzyme promiscuity drives branched-chain fatty acid synthesis in adipose tissues

October 16th, 2018 by Martina Wallace

Enzyme promiscuity drives branched-chain fatty acid synthesis in adipose tissues

Enzyme promiscuity drives branched-chain fatty acid synthesis in adipose tissues, Published online: 16 October 2018; doi:10.1038/s41589-018-0132-2

mmBCFAs are endogenous fatty acids synthesized from BCAAs by brown and white adipose tissue via CrAT and FASN promiscuity. BCAA catabolism and mmBCFA lipogenesis are decreased by obesity-induced adipose hypoxia and influenced by the microbiome.
  • Posted in Nat Chem Biol, Publications
  • Comments Off on Enzyme promiscuity drives branched-chain fatty acid synthesis in adipose tissues

No more ESKAPE

October 16th, 2018 by Mirella Bucci

No more ESKAPE

No more ESKAPE, Published online: 16 October 2018; doi:10.1038/s41589-018-0156-7

No more ESKAPE

Small-molecule-based regulation of RNA-delivered circuits in mammalian cells

October 16th, 2018 by Tyler E. Wagner

Small-molecule-based regulation of RNA-delivered circuits in mammalian cells

Small-molecule-based regulation of RNA-delivered circuits in mammalian cells, Published online: 16 October 2018; doi:10.1038/s41589-018-0146-9

Engineering of small-molecule-responsive RNA-binding proteins enables chemical regulation of modified mRNA or RNA replicon expression within mammalian cells for applications in synthetic circuit design and RNA-centered therapeutics.
  • Posted in Nat Chem Biol, Publications
  • Comments Off on Small-molecule-based regulation of RNA-delivered circuits in mammalian cells

Trading on thionoesters

October 16th, 2018 by Caitlin Deane

Trading on thionoesters

Trading on thionoesters, Published online: 16 October 2018; doi:10.1038/s41589-018-0158-5

Trading on thionoesters

Structural insights into binding specificity, efficacy and bias of a β<sub>2</sub>AR partial agonist

October 16th, 2018 by Matthieu Masureel

Structural insights into binding specificity, efficacy and bias of a β2AR partial agonist

Structural insights into binding specificity, efficacy and bias of a β<sub>2</sub>AR partial agonist, Published online: 16 October 2018; doi:10.1038/s41589-018-0145-x

The active-state structure of a GPCR occupied by a partial agonist, β2AR with salmeterol, together with mutagenesis and biophysical studies, explains this ligand's unusual pharmacological profile.
  • Posted in Nat Chem Biol, Publications
  • Comments Off on Structural insights into binding specificity, efficacy and bias of a β<sub>2</sub>AR partial agonist

A new spot for PKR

October 16th, 2018 by Yiyun Song

A new spot for PKR

A new spot for PKR, Published online: 16 October 2018; doi:10.1038/s41589-018-0159-4

A new spot for PKR

Metabolic repair through emergence of new pathways in <i>Escherichia coli</i>

October 16th, 2018 by Sammy Pontrelli

Metabolic repair through emergence of new pathways in Escherichia coli

Metabolic repair through emergence of new pathways in <i>Escherichia coli</i>, Published online: 16 October 2018; doi:10.1038/s41589-018-0149-6

In response to the deletion of key genes involved in biosynthesis of the essential CoA precursor β-alanine, Escherichia coli overcomes this pathway damage by successively evolving alternative metabolic pathways.
  • Posted in Nat Chem Biol, Publications
  • Comments Off on Metabolic repair through emergence of new pathways in <i>Escherichia coli</i>

Chaperoning partners

October 16th, 2018 by Grant Miura

Chaperoning partners

Chaperoning partners, Published online: 16 October 2018; doi:10.1038/s41589-018-0157-6

Chaperoning partners

Small molecules that target group II introns are potent antifungal agents

October 15th, 2018 by Olga Fedorova

Small molecules that target group II introns are potent antifungal agents

Small molecules that target group II introns are potent antifungal agents, Published online: 15 October 2018; doi:10.1038/s41589-018-0142-0

High-throughput screening followed by an examination of structure–activity relationship-based optimization resulted in the identification of potent small-molecule inhibitors of group IIB intron splicing in fungal organisms.
  • Posted in Nat Chem Biol, Publications
  • Comments Off on Small molecules that target group II introns are potent antifungal agents