Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains

Olivier Mirguet, Romain Gosmini, Jérôme Toum, +20

Journal of Medicinal Chemistry

Histone ModificationsChemoprevention StrategyEpigenetic ChangeGeneticsMolecular Biology +20

Orexin-A, an hypothalamic peptide with analgesic properties

Sharon Bingham, Philip T. Davey, Adam J. Babbs, +11

Pain

Pain MedicineHypothalamic Peptide Orexin-aNeuropathic PainMolecular PainHypothalamic Peptide +14

Identification of a novel series of BET family bromodomain inhibitors: Binding mode and profile of I-BET151 (GSK1210151A)

Jonathan T. Seal, Yann Lamotte, Frédéric Donche, +20

Bioorganic & Medicinal Chemistry Letters

Novel SeriesMedicineChemical BiologyPharmacologyBinding Mode +2

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762

Aristeidis Chaidos, Valentina S. Caputo, Katerina Gouvedenou, +22

Blood

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

The Discovery of I-BET726 (GSK1324726A), a Potent Tetrahydroquinoline ApoA1 Up-Regulator and Selective BET Bromodomain Inhibitor

Romain Gosmini, Van Loc Nguyen, Jérôme Toum, +21

Journal of Medicinal Chemistry

Medicinal ChemistryHistone CodeDrug TargetBiochemistryApolipoprotein A1 +10

Improving the in Vitro Prediction of in Vivo Central Nervous System Penetration: Integrating Permeability, P-glycoprotein Efflux, and Free Fractions in Blood and Brain

Scott Summerfield, Alexander J. Stevens, Leanne Cutler, +6

Journal of Pharmacology and Experimental Therapeutics

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

Pharmacokinetics of the novel, high-affinity and selective dopamine D3 receptor antagonist SB-277011 in rat, dog and monkey:<i>in vitro/in vivo</i>correlation and the role of aldehyde oxidase

Nigel Austin, S. J. Baldwin, Leanne Cutler, +8

Xenobiotica

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