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Cellular Cyborgs: On the Precipice of a Drug Delivery Revolution 10.1016/j.chembiol.2018.03.003 2018-04-05 Cell-based drug delivery systems offer the prospect of biocompatibility, large-loading capacity, longin vivolifespan, and active targeting of diseased sites. However, these opportunities are offset by an array of challenges, including safeguarding the integri...
The Rheumatoid Arthritis-Associated Citrullinome 10.1016/j.chembiol.2018.03.002 2018-04-05 Increased protein citrullination is linked to various diseases including rheumatoid arthritis (RA), lupus, and cancer. Citrullinated autoantigens, a hallmark of RA, are recognized by anti-citrullinated protein antibodies (ACPAs) which are used to diagnose RA....
Dependence on the Pyrimidine Biosynthetic Enzyme DHODH Is a Synthetic Lethal Vulnerability in Mutant KRAS-Driven Cancers 10.1016/j.chembiol.2018.03.005 2018-04-05 ActivatingKRASmutations are major oncogenic drivers in multiple tumor types. Synthetic lethal screens have previously been used to identify targets critical for the survival ofKRASmutant cells, but their application to drug discovery has proven challenging, p...
The O-GlcNAc Transferase Intellectual Disability Mutation L254F Distorts the TPR Helix 10.1016/j.chembiol.2018.03.004 2018-03-29 O-linked β-N-acetyl-D-glucosamine (O-GlcNAc) transferase (OGT) regulates proteinO-GlcNAcylation, an essential post-translational modification that is abundant in the brain. Recently,OGTmutations have been associated with intellectual disability, although it i...
Targeting Phosphopeptide Recognition by the Human BRCA1 Tandem BRCT Domain to Interrupt BRCA1-Dependent Signaling 10.1016/j.chembiol.2018.02.012 2018-03-29 Intracellular signals triggered by DNA breakage flow through proteins containing BRCT (BRCA1 C-terminal) domains. This family, comprising 23 conserved phosphopeptide-binding modules in man, is inaccessible to small-molecule chemical inhibitors. Here, we devel...
Bacterial Alkaloid Biosynthesis: Structural Diversity via a Minimalistic Nonribosomal Peptide Synthetase 10.1016/j.chembiol.2018.02.013 2018-03-29 Chemical and biochemical analyses of one of the most basic nonribosomal peptide synthetases (NRPS) from aPseudomonas fluorescensstrain revealed its striking plasticity. Determination of the potential substrate scope enabled us to anticipate novel secondary me...
Copper-Binding Small Molecule Induces Oxidative Stress and Cell-Cycle Arrest in Glioblastoma-Patient-Derived Cells 10.1016/j.chembiol.2018.02.010 2018-03-22 Transition metals are essential, but deregulation of their metabolism causes toxicity. Here, we report that the compound NSC319726 binds copper to induce oxidative stress and arrest glioblastoma-patient-derived cells at picomolar concentrations. Pharmacogenom...
Dual Modifications of α-Galactosylceramide Synergize to Promote Activation of Human Invariant Natural Killer T Cells and Stimulate Anti-tumor Immunity 10.1016/j.chembiol.2018.02.009 2018-03-22 Glycosylceramides that activate CD1d-restricted invariant natural killer T (iNKT) cells have potential therapeutic applications for augmenting immune responses against cancer and infections. Previous studies using mouse models identified sphinganine variants ...
Structural Insights into the Forward and Reverse Enzymatic Reactions in Human Adenine Phosphoribosyltransferase 10.1016/j.chembiol.2018.02.011 2018-03-22 Phosphoribosyltransferases catalyze the displacement of a PRPP α-1′-pyrophosphate to a nitrogen-containing nucleobase. How they control the balance of substrates/products binding and activities is poorly understood. Here, we investigated the human adenine pho...
Analysis of the Pseudouridimycin Biosynthetic Pathway Provides Insights into the Formation of C-nucleoside Antibiotics 10.1016/j.chembiol.2018.02.008 2018-03-15 Pseudouridimycin (PUM) is a selective nucleoside-analog inhibitor of bacterial RNA polymerase with activity against Gram-positive and Gram-negative bacteria. PUM, produced byStreptomycessp. ID38640, consists of a formamidinylated,N-hydroxylated Gly-Gln dipept...

Cellular Cyborgs: On the Precipice of a Drug Delivery Revolution

10.1016/j.chembiol.2018.03.003

2018-04-05

Cell-based drug delivery systems offer the prospect of biocompatibility, large-loading capacity, longin vivolifespan, and active targeting of diseased sites. However, these opportunities are offset by an array of challenges, including safeguarding the integri...

The Rheumatoid Arthritis-Associated Citrullinome

10.1016/j.chembiol.2018.03.002

2018-04-05

Increased protein citrullination is linked to various diseases including rheumatoid arthritis (RA), lupus, and cancer. Citrullinated autoantigens, a hallmark of RA, are recognized by anti-citrullinated protein antibodies (ACPAs) which are used to diagnose RA....

Dependence on the Pyrimidine Biosynthetic Enzyme DHODH Is a Synthetic Lethal Vulnerability in Mutant KRAS-Driven Cancers

10.1016/j.chembiol.2018.03.005

2018-04-05

ActivatingKRASmutations are major oncogenic drivers in multiple tumor types. Synthetic lethal screens have previously been used to identify targets critical for the survival ofKRASmutant cells, but their application to drug discovery has proven challenging, p...

The O-GlcNAc Transferase Intellectual Disability Mutation L254F Distorts the TPR Helix

10.1016/j.chembiol.2018.03.004

2018-03-29

O-linked β-N-acetyl-D-glucosamine (O-GlcNAc) transferase (OGT) regulates proteinO-GlcNAcylation, an essential post-translational modification that is abundant in the brain. Recently,OGTmutations have been associated with intellectual disability, although it i...

Targeting Phosphopeptide Recognition by the Human BRCA1 Tandem BRCT Domain to Interrupt BRCA1-Dependent Signaling

10.1016/j.chembiol.2018.02.012

2018-03-29

Intracellular signals triggered by DNA breakage flow through proteins containing BRCT (BRCA1 C-terminal) domains. This family, comprising 23 conserved phosphopeptide-binding modules in man, is inaccessible to small-molecule chemical inhibitors. Here, we devel...

Bacterial Alkaloid Biosynthesis: Structural Diversity via a Minimalistic Nonribosomal Peptide Synthetase

10.1016/j.chembiol.2018.02.013

2018-03-29

Chemical and biochemical analyses of one of the most basic nonribosomal peptide synthetases (NRPS) from aPseudomonas fluorescensstrain revealed its striking plasticity. Determination of the potential substrate scope enabled us to anticipate novel secondary me...

Copper-Binding Small Molecule Induces Oxidative Stress and Cell-Cycle Arrest in Glioblastoma-Patient-Derived Cells

10.1016/j.chembiol.2018.02.010

2018-03-22

Transition metals are essential, but deregulation of their metabolism causes toxicity. Here, we report that the compound NSC319726 binds copper to induce oxidative stress and arrest glioblastoma-patient-derived cells at picomolar concentrations. Pharmacogenom...

Dual Modifications of α-Galactosylceramide Synergize to Promote Activation of Human Invariant Natural Killer T Cells and Stimulate Anti-tumor Immunity

10.1016/j.chembiol.2018.02.009

2018-03-22

Glycosylceramides that activate CD1d-restricted invariant natural killer T (iNKT) cells have potential therapeutic applications for augmenting immune responses against cancer and infections. Previous studies using mouse models identified sphinganine variants ...

Structural Insights into the Forward and Reverse Enzymatic Reactions in Human Adenine Phosphoribosyltransferase

10.1016/j.chembiol.2018.02.011

2018-03-22

Phosphoribosyltransferases catalyze the displacement of a PRPP α-1′-pyrophosphate to a nitrogen-containing nucleobase. How they control the balance of substrates/products binding and activities is poorly understood. Here, we investigated the human adenine pho...

Analysis of the Pseudouridimycin Biosynthetic Pathway Provides Insights into the Formation of C-nucleoside Antibiotics

10.1016/j.chembiol.2018.02.008

2018-03-15

Pseudouridimycin (PUM) is a selective nucleoside-analog inhibitor of bacterial RNA polymerase with activity against Gram-positive and Gram-negative bacteria. PUM, produced byStreptomycessp. ID38640, consists of a formamidinylated,N-hydroxylated Gly-Gln dipept...