Discovery of (2,4-Dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a Novel Inhibitor of the Molecular Chaperone Hsp90 by Fragment Based Drug Design

Andrew Woodhead, Hayley C. Angove, Maria G. Carr, +25

Journal of Medicinal Chemistry

Pharmaceutical ScienceNovel InhibitorDrug TargetHit IdentificationBiomolecular Structure Prediction +17

Fragment-Based Drug Discovery Applied to Hsp90. Discovery of Two Lead Series with High Ligand Efficiency

Christopher W. Murray, Maria G. Carr, Owen Callaghan, +15

Journal of Medicinal Chemistry

Molecular DockingHigh Ligand EfficiencyMedicinal ChemistryChaperone Hsp90Fragment Screening +13

Discovery of an allosteric mechanism for the regulation of HCV NS3 protein function

S. Saalau-Bethell, Andrew Woodhead, Gianni Chessari, +10

Nature Chemical Biology

Virus StructureViral ReplicationSignal TransductionMolecular VirologyAllosteric Mechanism +6

A Structural Comparison of Inhibitor Binding to PKB, PKA and PKA-PKB Chimera

Thomas G. Davies, Marcel L. Verdonk, Brent Graham, +9

Journal of Molecular Biology

BiochemistryPka-pkb ChimeraNatural SciencesMedicineMechanism Of Action +9

The heat shock protein 90 inhibitor, <scp>AT</scp>13387, displays a long duration of action <i>in vitro</i> and <i>in vivo</i> in non‐small cell lung cancer

Brent Graham, Jayne Curry, Tomoko Smyth, +11

Cancer Science

Tumor XenograftsChemoprevention StrategyMolecular BiologyCancer BiologyTumor Biology +15

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

AT9283, a potent inhibitor of the Aurora kinases and Jak2, has therapeutic potential in myeloproliferative disorders

Mark A. Dawson, Jayne Curry, Kelly Barber, +10

British Journal of Haematology

Therapeutic PotentialImmunologyTumor BiologyMyeloid NeoplasiaHematological Malignancy +17

Identification of spliced baculovirus RNAs expressed late in infection

Gerald R. Kovacs, Linda A. Guarino, Brent Graham, +1

Virology

Molecular VirologyPathogenesisRna SplicingVirologyVirus Gene +4

Protease Inhibitors Block Multiple Functions of the NS3/4A Protease-Helicase during the Hepatitis C Virus Life Cycle

David R. McGivern, Takahiro Masaki, William Lovell, +3

Journal of Virology

Potent, Selective Inhibitors of Fibroblast Growth Factor Receptor Define Fibroblast Growth Factor Dependence in Preclinical Cancer Models

Matthew Squires, George A. Ward, Gordan Saxty, +33

Molecular Cancer Therapeutics