Oral administration of a potent and selective non-peptidic BACE-1 inhibitor decreases beta-cleavage of amyloid precursor protein and amyloid-beta production in vivo.

PubWeight™: 1.20‹?› | Rank: Top 10%

🔗 View Article (PMID 17156133)

Published in J Neurochem on February 01, 2007

Authors

Ishrut Hussain1, Julie Hawkins, David Harrison, Christopher Hille, Gareth Wayne, Leanne Cutler, Tania Buck, Daryl Walter, Emmanuel Demont, Colin Howes, Alan Naylor, Philip Jeffrey, Maria I Gonzalez, Colin Dingwall, Anton Michel, Sally Redshaw, John B Davis

Author Affiliations

1: Neurology and GastroIntestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline Research & Development Ltd, Harlow, Essex, UK. Ishrut_2_Hussain@gsk.com

Articles citing this

Genetics of Alzheimer's disease: recent advances. Genome Med (2009) 1.95

beta-Secretase as a therapeutic target for Alzheimer's disease. Neurotherapeutics (2008) 1.74

Identification of beta-secretase (BACE1) substrates using quantitative proteomics. PLoS One (2009) 1.52

Function, therapeutic potential and cell biology of BACE proteases: current status and future prospects. J Neurochem (2014) 1.37

Developing β-secretase inhibitors for treatment of Alzheimer's disease. J Neurochem (2011) 1.37

Inhibition of GSK3β-mediated BACE1 expression reduces Alzheimer-associated phenotypes. J Clin Invest (2012) 1.32

Animal models of Alzheimer disease. Cold Spring Harb Perspect Med (2012) 1.18

Phospho-eIF2α level is important for determining abilities of BACE1 reduction to rescue cholinergic neurodegeneration and memory defects in 5XFAD mice. PLoS One (2010) 1.11

Soluble amyloid precursor protein-α modulates β-secretase activity and amyloid-β generation. Nat Commun (2012) 1.07

Integrating ADNI results into Alzheimer's disease drug development programs. Neurobiol Aging (2010) 1.03

Recent rodent models for Alzheimer's disease: clinical implications and basic research. J Neural Transm (Vienna) (2011) 0.99

beta-Secretase inhibitor potency is decreased by aberrant beta-cleavage location of the "Swedish mutant" amyloid precursor protein. J Biol Chem (2009) 0.96

Molecular consequences of amyloid precursor protein and presenilin mutations causing autosomal-dominant Alzheimer's disease. Alzheimers Res Ther (2012) 0.95

Intraperitoneal injection of the pancreatic peptide amylin potently reduces behavioral impairment and brain amyloid pathology in murine models of Alzheimer's disease. Mol Psychiatry (2014) 0.94

Inhibition of BACE1 for therapeutic use in Alzheimer's disease. Int J Clin Exp Pathol (2010) 0.92

Generation of aggregation prone N-terminally truncated amyloid β peptides by meprin β depends on the sequence specificity at the cleavage site. Mol Neurodegener (2016) 0.88

Expression of reticulon 3 in Alzheimer's disease brain. Neuropathol Appl Neurobiol (2009) 0.88

Cell surface expression of the major amyloid-β peptide (Aβ)-degrading enzyme, neprilysin, depends on phosphorylation by mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK) and dephosphorylation by protein phosphatase 1a. J Biol Chem (2012) 0.88

Transgenic mouse models of Alzheimer disease: developing a better model as a tool for therapeutic interventions. Curr Pharm Des (2012) 0.88

Inhibition of beta-secretase in vivo via antibody binding to unique loops (D and F) of BACE1. J Biol Chem (2011) 0.86

Consequences of inhibiting amyloid precursor protein processing enzymes on synaptic function and plasticity. Neural Plast (2012) 0.86

CNS amyloid-β, soluble APP-α and -β kinetics during BACE inhibition. J Neurosci (2014) 0.84

Neuronal death in Alzheimer's disease and therapeutic opportunities. J Cell Mol Med (2009) 0.84

Mechanisms that lessen benefits of β-secretase reduction in a mouse model of Alzheimer's disease. Transl Psychiatry (2013) 0.84

Flavonoids as therapeutic compounds targeting key proteins involved in Alzheimer's disease. ACS Chem Neurosci (2014) 0.82

BACE-1 inhibition prevents the γ-secretase inhibitor evoked Aβ rise in human neuroblastoma SH-SY5Y cells. J Biomed Sci (2011) 0.81

Can BACE1 inhibition mitigate early axonal pathology in neurological diseases? J Alzheimers Dis (2014) 0.80

L655,240, acting as a competitive BACE1 inhibitor, efficiently decreases β-amyloid peptide production in HEK293-APPswe cells. Acta Pharmacol Sin (2012) 0.79

Do amyloid oligomers act as traps for misfolded proteins? A hypothesis. Amyloid (2008) 0.79

Comparison of pharmacological modulation of APP metabolism in primary chicken telencephalic neurons and in a human neuroglioma cell line. J Mol Neurosci (2010) 0.78

Pharmacological Treatment of Alzheimer's Disease: Is it Progressing Adequately? Open Neurol J (2009) 0.75

The Metalloprotease Meprin β Is an Alternative β-Secretase of APP. Front Mol Neurosci (2017) 0.75

Quantum mechanics study of the hydroxyethylamines-BACE-1 active site interaction energies. J Comput Aided Mol Des (2011) 0.75

Prediction of intracellular exposure bridges the gap between target- and cell-based drug discovery. Proc Natl Acad Sci U S A (2017) 0.75

Articles by these authors

Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives. J Biol Chem (2002) 3.14

Partial carotid ligation is a model of acutely induced disturbed flow, leading to rapid endothelial dysfunction and atherosclerosis. Am J Physiol Heart Circ Physiol (2009) 3.11

The serine protease Omi/HtrA2 regulates apoptosis by binding XIAP through a reaper-like motif. J Biol Chem (2001) 2.47

The diversity in the vanilloid (TRPV) receptor family of ion channels. Trends Pharmacol Sci (2002) 2.45

'Matching Michigan': a 2-year stepped interventional programme to minimise central venous catheter-blood stream infections in intensive care units in England. BMJ Qual Saf (2012) 2.44

Protease-activated receptor 2 sensitizes the capsaicin receptor transient receptor potential vanilloid receptor 1 to induce hyperalgesia. J Neurosci (2004) 2.42

Matrix assembly, regulation, and survival functions of laminin and its receptors in embryonic stem cell differentiation. J Cell Biol (2002) 2.34

Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. J Med Chem (2013) 2.09

Exclusively targeting beta-secretase to lipid rafts by GPI-anchor addition up-regulates beta-site processing of the amyloid precursor protein. Proc Natl Acad Sci U S A (2003) 2.03

COX-2, CB2 and P2X7-immunoreactivities are increased in activated microglial cells/macrophages of multiple sclerosis and amyotrophic lateral sclerosis spinal cord. BMC Neurol (2006) 1.87

Caspase-6 gene disruption reveals a requirement for lamin A cleavage in apoptotic chromatin condensation. EMBO J (2002) 1.82

Implications of prognostic pessimism in patients with chronic obstructive pulmonary disease (COPD) or asthma admitted to intensive care in the UK within the COPD and asthma outcome study (CAOS): multicentre observational cohort study. BMJ (2007) 1.81

WT1 is a key regulator of podocyte function: reduced expression levels cause crescentic glomerulonephritis and mesangial sclerosis. Hum Mol Genet (2002) 1.70

Neuronal membrane cholesterol loss enhances amyloid peptide generation. J Cell Biol (2004) 1.66

TRPV channels as temperature sensors. Cell Calcium (2003) 1.63

Jejunal afferent nerve sensitivity in wild-type and TRPV1 knockout mice. J Physiol (2004) 1.63

Dda helicase tightly couples translocation on single-stranded DNA to unwinding of duplex DNA: Dda is an optimally active helicase. J Mol Biol (2012) 1.57

The mouse as a model for understanding chronic diseases of aging: the histopathologic basis of aging in inbred mice. Pathobiol Aging Age Relat Dis (2011) 1.56

Medullary amyloidosis associated with apolipoprotein A-IV deposition. Kidney Int (2011) 1.56

[3H]Resiniferatoxin autoradiography in the CNS of wild-type and TRPV1 null mice defines TRPV1 (VR-1) protein distribution. Brain Res (2004) 1.54

BACE1 (beta-secretase) transgenic and knockout mice: identification of neurochemical deficits and behavioral changes. Mol Cell Neurosci (2003) 1.52

The T4 phage SF1B helicase Dda is structurally optimized to perform DNA strand separation. Structure (2012) 1.52

Role of laminin terminal globular domains in basement membrane assembly. J Biol Chem (2007) 1.50

Diagnostic accuracy of chest X-rays acquired using a digital camera for low-cost teleradiology. Int J Med Inform (2004) 1.49

Laminin-sulfatide binding initiates basement membrane assembly and enables receptor signaling in Schwann cells and fibroblasts. J Cell Biol (2005) 1.46

Risk factors for invasive fungal disease in critically ill adult patients: a systematic review. Crit Care (2011) 1.44

A key role for gp130 expressed on peripheral sensory nerves in pathological pain. J Neurosci (2009) 1.37

Increased capsaicin receptor TRPV1 nerve fibres in the inflamed human oesophagus. Eur J Gastroenterol Hepatol (2004) 1.37

GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models. J Pharmacol Exp Ther (2007) 1.30

Endogenous tumor necrosis factor alpha (TNFalpha) requires TNF receptor type 2 to generate heat hyperalgesia in a mouse cancer model. J Neurosci (2008) 1.30

Early peak temperature and mortality in critically ill patients with or without infection. Intensive Care Med (2012) 1.29

Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A). Bioorg Med Chem Lett (2012) 1.24

Improving the in vitro prediction of in vivo central nervous system penetration: integrating permeability, P-glycoprotein efflux, and free fractions in blood and brain. J Pharmacol Exp Ther (2005) 1.23

Differential expression of hDAB2IPA and hDAB2IPB in normal tissues and promoter methylation of hDAB2IPA in hepatocellular carcinoma. J Hepatol (2006) 1.22

Proteomic identification and early validation of complement 1 inhibitor and pigment epithelium-derived factor: Two novel biomarkers of Alzheimer's disease in human plasma. Proteomics Clin Appl (2008) 1.20

Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy. Bioorg Med Chem Lett (2008) 1.20

Neurogenic responses mediated by vanilloid receptor-1 (TRPV1) are blocked by the high affinity antagonist, iodo-resiniferatoxin. Br J Pharmacol (2003) 1.20

Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood (2013) 1.20

Cloning and functional expression of human short TRP7, a candidate protein for store-operated Ca2+ influx. J Biol Chem (2002) 1.19

Function and distribution of circulating human PCSK9 expressed extrahepatically in transgenic mice. J Lipid Res (2008) 1.18

Assessment and optimization of mortality prediction tools for admissions to pediatric intensive care in the United kingdom. Pediatrics (2006) 1.17

Increased capsaicin receptor TRPV1 in skin nerve fibres and related vanilloid receptors TRPV3 and TRPV4 in keratinocytes in human breast pain. BMC Womens Health (2005) 1.17

Perioperative increase in global blood flow to explicit defined goals and outcomes following surgery. Cochrane Database Syst Rev (2012) 1.12

Heparan sulfate regulates amyloid precursor protein processing by BACE1, the Alzheimer's beta-secretase. J Cell Biol (2003) 1.11

Raft disorganization leads to reduced plasmin activity in Alzheimer's disease brains. EMBO Rep (2003) 1.09

Altered oxidative stress response of the long-lived Snell dwarf mouse. Biochem Biophys Res Commun (2004) 1.08

Identification of dystroglycan as a second laminin receptor in oligodendrocytes, with a role in myelination. Development (2007) 1.08

Evaluation of modernisation of adult critical care services in England: time series and cost effectiveness analysis. BMJ (2009) 1.07

P2X purinergic receptor-mediated ionic current in cardiac myocytes of calsequestrin model of cardiomyopathy: implications for the treatment of heart failure. Am J Physiol Heart Circ Physiol (2006) 1.06

Development of a P-glycoprotein knockout model in rodents to define species differences in its functional effect at the blood-brain barrier. J Pharm Sci (2006) 1.04

p38alpha stress-activated protein kinase phosphorylates neurofilaments and is associated with neurofilament pathology in amyotrophic lateral sclerosis. Mol Cell Neurosci (2004) 1.04

Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain. J Med Chem (2007) 1.03

P2X(7) receptors on microglial cells mediate injury to cortical neurons in vitro. Glia (2006) 1.02

BACE1 cytoplasmic domain interacts with the copper chaperone for superoxide dismutase-1 and binds copper. J Biol Chem (2005) 1.02

FTY720 ameliorates MOG-induced experimental autoimmune encephalomyelitis by suppressing both cellular and humoral immune responses. J Neurosci Res (2010) 1.02

Guidelines and considerations for conducting experiments using tissue microarrays. Histopathology (2013) 1.02

A broad-spectrum fluorescence-based peptide library for the rapid identification of protease substrates. Proteomics (2006) 1.00

Understanding the polymerization mechanism of glycoside-hydrolase family 70 glucansucrases. J Biol Chem (2006) 1.00

Persistence, switching, and discontinuation rates among patients receiving sertraline, paroxetine, and citalopram. Pharmacotherapy (2005) 0.99

Early temperature and mortality in critically ill patients with acute neurological diseases: trauma and stroke differ from infection. Intensive Care Med (2015) 0.99

Nitric-oxide supplementation for treatment of long-term complications in argininosuccinic aciduria. Am J Hum Genet (2012) 0.98

Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development. Bioorg Med Chem Lett (2006) 0.98

A detailed methodology of partial hepatectomy in the mouse. Lab Anim (NY) (2008) 0.96

Expression of the complement C3a and C5a receptors after permanent focal ischemia: An alternative interpretation. Glia (2002) 0.95

The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem (2014) 0.94

Relationship between microglial activation and dopaminergic neuronal loss in the substantia nigra: a time course study in a 6-hydroxydopamine model of Parkinson's disease. J Neurochem (2009) 0.94

The tumor suppressor gene DLEC1 is frequently silenced by DNA methylation in hepatocellular carcinoma and induces G1 arrest in cell cycle. J Hepatol (2007) 0.94

Activation of vanilloid receptor 1 by resiniferatoxin mobilizes calcium from inositol 1,4,5-trisphosphate-sensitive stores. Br J Pharmacol (2003) 0.93

Characterization of the ectodomain shedding of the beta-site amyloid precursor protein-cleaving enzyme 1 (BACE1). J Biol Chem (2003) 0.93

Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability. J Med Chem (2008) 0.92

Coexpression of RTI40 with alveolar epithelial type II cell proteins in lungs following injury: identification of alveolar intermediate cell types. Am J Physiol Lung Cell Mol Physiol (2005) 0.92

ADAM9 inhibition increases membrane activity of ADAM10 and controls α-secretase processing of amyloid precursor protein. J Biol Chem (2011) 0.92

The increasing burden of alcoholic liver disease on United Kingdom critical care units: secondary analysis of a high quality clinical database. J Health Serv Res Policy (2008) 0.91

Gonadotropin-releasing hormone receptor levels and cell context affect tumor cell responses to agonist in vitro and in vivo. Cancer Res (2008) 0.91

Capsazepine protects against neuronal injury caused by oxygen glucose deprivation by inhibiting I(h). J Neurosci (2003) 0.91

N-Tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl biaryl carboxamides as antagonists of TRPV1. Bioorg Med Chem Lett (2006) 0.91

The cyclooxygenase-2 inhibitor GW406381X [2-(4-ethoxyphenyl)-3-[4-(methylsulfonyl)phenyl]-pyrazolo[1,5-b]pyridazine] is effective in animal models of neuropathic pain and central sensitization. J Pharmacol Exp Ther (2004) 0.90

Prognostic modelling in traumatic brain injury. BMJ (2008) 0.90

Hospitals' star ratings and clinical outcomes: ecological study. BMJ (2004) 0.89

Cyclin-dependent kinase-5/p35 phosphorylates Presenilin 1 to regulate carboxy-terminal fragment stability. Mol Cell Neurosci (2002) 0.89

Care managers' experiences in a collaborative care program for high risk mothers with depression. Psychosomatics (2012) 0.89

Caspase-7 gene disruption reveals an involvement of the enzyme during the early stages of apoptosis. J Biol Chem (2003) 0.89

Vanilloid receptor 1 expression in human tooth pulp in relation to caries and pain. J Orofac Pain (2005) 0.89

Discovery of GSK345931A: An EP(1) receptor antagonist with efficacy in preclinical models of inflammatory pain. Bioorg Med Chem Lett (2008) 0.89

Down-regulation of the ATP-binding cassette transporter 2 (Abca2) reduces amyloid-β production by altering Nicastrin maturation and intracellular localization. J Biol Chem (2011) 0.88

Applying hierarchical task analysis to medication administration errors. Appl Ergon (2005) 0.88

Neuroprotection by the selective iNOS inhibitor GW274150 in a model of Parkinson disease. Free Radic Biol Med (2010) 0.88

Crystal structure of the human ephrin-A5 ectodomain. Protein Sci (2007) 0.88

The effect of secular trends and specialist neurocritical care on mortality for patients with intracerebral haemorrhage, myasthenia gravis and Guillain-Barré syndrome admitted to critical care : an analysis of the Intensive Care National Audit & Research Centre (ICNARC) national United Kingdom database. Intensive Care Med (2013) 0.88

The discovery and early validation of novel plasma biomarkers in mild-to-moderate Alzheimer's disease patients responding to treatment with rosiglitazone. Biomarkers (2008) 0.87