Catalytic in vivo protein knockdown by small-molecule PROTACs

Daniel P. Bondeson, Alina Mares, Ian E. Smith, +26

Nature Chemical Biology

BiochemistryProtein AssemblyNatural SciencesVivo ProteinSmall Molecules

Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription

Matthew P. Coghlan, Ainsley A. Culbert, Darren A.E. Cross, +14

Chemistry & Biology

BiochemistryNatural SciencesGlycobiologyMetabolic RemodelingGene Transcription +5

The Structure of Phosphorylated GSK-3β Complexed with a Peptide, FRATtide, that Inhibits β-Catenin Phosphorylation

B.D. Bax, Paul S. Carter, Ceri Lewis, +9

Structure

Protein FunctionSignal TransductionSignaling PathwayBiochemistryNatural Sciences +9

The antimicrobial natural product chuangxinmycin and Some synthetic analogues are potent and selective inhibitors of bacterial tryptophanyl tRNA synthetase

Murray J. B. Brown, Paul S. Carter, Ashley Fenwick, +11

Bioorganic & Medicinal Chemistry Letters

Natural Product SynthesisAntibioticsMedicineSynthetic AnaloguesSelective Inhibitors +8

Expression, Purification, and Functional Analysis of the Human Serine Protease HtrA2

John W. Savopoulos, Paul S. Carter, Sandra Turconi, +6

Protein Expression and Purification

Protease InhibitorsProtein FunctionProtein ExpressionBiochemistryProtein Folding +6

Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor

John Liddle, Francis Atkinson, Michael D. Barker, +26

Bioorganic & Medicinal Chemistry Letters

G Protein-coupled ReceptorMedicineReceptor Tyrosine KinasePharmacologyCell Biology +3

The Structure of MSK1 Reveals a Novel Autoinhibitory Conformation for a Dual Kinase Protein

Kathrine J. Smith, Paul S. Carter, Angela Bridges, +9

Structure

Msk1 RevealsProtein FunctionSignal TransductionSignaling PathwayProtein Folding +10

Rapid Lentiviral Vector Producer Cell Line Generation Using a Single DNA Construct

Yu Hua Chen, Celeste Pallant, Chris Sampson, +24

Molecular Therapy — Methods & Clinical Development

The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits

Sophie M. Bertrand, Nicolas Ancellin, Benjamin Beaufils, +29

Journal of Medicinal Chemistry

Ligand EfficiencyMolecular BiologyPharmacotherapyHts HitsChemical Biology +15

Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening

Alan D. Borthwick, Nicolas Ancellin, Sophie M. Bertrand, +15

Journal of Medicinal Chemistry

Bioorganic ChemistryStructural BioinformaticsBiomolecular Structure PredictionMolecular BiologyLead Identification +18