Oral administration of a potent and selective non‐peptidic BACE‐1 inhibitor decreases β‐cleavage of amyloid precursor protein and amyloid‐β production <i>in vivo</i>

Ishrut Hussain, Julie A. Hawkins, David C. Harrison, +14

Journal of Neurochemistry

Molecular PharmacologyAlzheimer's DiseaseBiochemistryMedicineNatural Sciences +11

Heparan sulfate regulates amyloid precursor protein processing by BACE1, the Alzheimer's β-secretase

Zoe Scholefield, Edwin A. Yates, Gareth Wayne, +3

The Journal of Cell Biology

Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery

André Mateus, Laurie Gordon, Gareth Wayne, +9

Proceedings of the National Academy of Sciences

Direct Measurement of Intracellular Compound Concentration by RapidFire Mass Spectrometry Offers Insights into Cell Permeability

Laurie Gordon, Morven Allen, Per Artursson, +7

SLAS DISCOVERY

Cellular AssaysBiological Mass SpectrometryLead IdentificationCellular PhysiologyAnalytical Instrumentation +23

TIMP-3 Inhibition of ADAMTS-4 (Aggrecanase-1) Is Modulated by Interactions between Aggrecan and the C-terminal Domain of ADAMTS-4

Gareth Wayne, Su-Jun Deng, Augustin Amour, +4

Journal of Biological Chemistry

Molecular BiologyChemical BiologyFree Adamts-4OsteoarthritisEfficient Aggrecanase Activity +17

Second Generation of Hydroxyethylamine BACE-1 Inhibitors: Optimizing Potency and Oral Bioavailability

Nicolas Charrier, Brian Clarke, Leanne Cutler, +22

Journal of Medicinal Chemistry

Pharmaceutical ScienceOral BioavailabilityNeurochemical BiomarkersPharmacotherapyPharmaceutical Chemistry +17

BACE-1 inhibitors part 3: Identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells

Paul Beswick, Nicolas Charrier, Brian Clarke, +30

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryPharmaceutical ScienceBiochemistryNanomolar PotencyMedicine +8

BACE-1 inhibitors part 2: Identification of hydroxy ethylamines (HEAs) with reduced peptidic character

Brian Clarke, Emmanuel H. Demont, Colin Dingwall, +24

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryPharmaceutical ChemistryBiochemistryMedicineNatural Sciences +10

Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics

Nicolas Charrier, Brian Clarke, Leanne Cutler, +21

Bioorganic & Medicinal Chemistry Letters

Combinatorial ChemistryMedicinal ChemistryBiochemistryNatural SciencesMedicine +7

Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent

Nicolas Charrier, Brian Clarke, Emmanuel H. Demont, +19

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryNon-prime Side SubstituentBioorganic ChemistryBiochemistryNatural Sciences +11