Serine is a natural ligand and allosteric activator of pyruvate kinase M2

Barbara Chaneton, Petra Hillmann, Liang Zheng, +10

Nature

Pyruvate Kinase M2Natural LigandSignal TransductionMolecular PhysiologyBiochemistry +8

Identification of <i>N</i>-(4-Piperidinyl)-4-(2,6-dichlorobenzoylamino)-1<i>H</i>-pyrazole-3-carboxamide (AT7519), a Novel Cyclin Dependent Kinase Inhibitor Using Fragment-Based X-Ray Crystallography and Structure Based Drug Design

Paul G. Wyatt, Andrew Woodhead, Valério Berdini, +20

Journal of Medicinal Chemistry

Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity

Steven Howard, Valério Berdini, John A. Boulstridge, +20

Journal of Medicinal Chemistry

Drug TargetPyrazol-4-yl UreaClinical CandidateAurora BChemical Biology +16

Crystal structure of human CDK4 in complex with a D-type cyclin

Philip J. Day, Anne Cleasby, Ian J. Tickle, +8

Proceedings of the National Academy of Sciences

Identification of Novel p38α MAP Kinase Inhibitors Using Fragment-Based Lead Generation

Adrian L. Gill, Martyn Frederickson, Anne Cleasby, +16

Journal of Medicinal Chemistry

Combinatorial ChemistryDrug TargetHit IdentificationMolecular BiologyLead Identification +16

4-(Pyrazol-4-yl)-pyrimidines as Selective Inhibitors of Cyclin-Dependent Kinase 4/6

Young Shin Cho, Maria Borland, Christopher T. Brain, +18

Journal of Medicinal Chemistry

Cyclin-dependent Kinase 4/6Combinatorial ChemistryMedicinal ChemistryBioorganic ChemistryBiochemistry +13

Pharmacologic Activation of PKM2 Slows Lung Tumor Xenograft Growth

K. Mark Parnell, Jason M. Foulks, Rebecca N. Nix, +16

Molecular Cancer Therapeutics

Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2

Tom D. Heightman, Valério Berdini, Hannah Braithwaite, +33

Journal of Medicinal Chemistry

Multiple CancersTumor BiologyMedicinal ChemistrySignaling PathwayReceptor Tyrosine Kinase +20

Oligosaccharide substrate binding in Escherichia coli maltodextrin phosphorylase

Marc O’Reilly, Kimberly A. Watson, Reinhard Schinzel, +2

Nature Structural & Molecular Biology

BiosynthesisBiochemistryGlycobiologyPolysaccharideCarbohydrate-protein Interaction +1

Identification of an activating transcription factor (ATF) binding site in the human transforming growth factor-beta 2 promoter.

Marc O’Reilly, Andrew G. Geiser, S.J. Kim, +4

Journal of Biological Chemistry

Promoter ActivityHuman GrowthGeneticsTgf-beta 2Dna Sequences +14