Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer's Disease.
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Qin Jiang | William J Greenlee | Xia Chen | Lynn A. Hyde | W. Greenlee | A. Stamford | J. Cumming | R. Hodgson | M. Forman | K. Cox | Yusheng Wu | P. Orth | C. Strickland | J. Voigt | U. Iserloh | M. Kennedy | R. Kuvelkar | E. Parker | J. Misiaszek | Xia Chen | L. Hyde | J. Stone | Julie Stone | Q. Jiang | Hongwu Wang | Jared N Cumming | Reshma Kuvelkar | Matthew E Kennedy | Kathleen Cox | Peter Orth | Irina Kazakevich | Eric M Parker | Andrew W Stamford | A. Brunskill | Johannes H Voigt | Jack D Scott | Sarah W Li | Andrew P J Brunskill | Mark Forman | Eric J Gilbert | Robert A Hodgson | Lynn A Hyde | Ulrich Iserloh | Hong Mei | John Meredith | Jeffrey Misiaszek | Lana M Rossiter | Meagan Slater | Corey O Strickland | Ganfeng Wang | Yusheng Wu | H. Mei | Jack D. Scott | Hongwu Wang | E. Gilbert | M. Slater | I. Kazakevich | Jackson Meredith | Ganfeng Wang
[1] Alfredo G. Tomasselli,et al. Membrane-anchored aspartyl protease with Alzheimer's disease β-secretase activity , 1999, Nature.
[2] J. Tang,et al. Human aspartic protease memapsin 2 cleaves the beta-secretase site of beta-amyloid precursor protein. , 2000, Proceedings of the National Academy of Sciences of the United States of America.
[3] William Greenlee,et al. Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation. , 2012, Journal of medicinal chemistry.
[4] Alexander Alex,et al. Intramolecular hydrogen bonding to improve membrane permeability and absorption in beyond rule of five chemical space , 2011 .
[5] James E Audia,et al. Robust Central Reduction of Amyloid-β in Humans with an Orally Available, Non-Peptidic β-Secretase Inhibitor , 2011, The Journal of Neuroscience.
[6] Daniel Oehlrich,et al. The evolution of amidine-based brain penetrant BACE1 inhibitors. , 2014, Bioorganic & medicinal chemistry letters.
[7] Suresh Babu,et al. Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aβ Reduction. , 2012, ACS medicinal chemistry letters.
[8] P. Selzer,et al. Fast calculation of molecular polar surface area as a sum of fragment-based contributions and its application to the prediction of drug transport properties. , 2000, Journal of medicinal chemistry.
[9] Steven P. Miller,et al. Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer's Disease. , 2016, Organic letters.
[10] Shankar Venkatraman,et al. Structure-based design of β-site APP cleaving enzyme 1 (BACE1) inhibitors for the treatment of Alzheimer's disease. , 2013, Journal of medicinal chemistry.
[11] K. Nave,et al. Bace1 and Neuregulin-1 cooperate to control formation and maintenance of muscle spindles , 2013, The EMBO journal.
[12] P. Coleman,et al. Kinesin spindle protein (KSP) inhibitors. Part V: discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by beta-fluorination to overcome cellular efflux by P-glycoprotein. , 2007, Bioorganic & medicinal chemistry letters.
[13] Michael Czarniecki,et al. Application of fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design to identify novel microM leads for the development of nM BACE-1 (beta-site APP cleaving enzyme 1) inhibitors. , 2010, Journal of medicinal chemistry.
[14] Matthias Rarey,et al. Torsion angle preferences in druglike chemical space: a comprehensive guide. , 2013, Journal of medicinal chemistry.
[15] K. Parris,et al. Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design. , 2015, Journal of medicinal chemistry.
[16] J. Treanor,et al. Beta-secretase cleavage of Alzheimer's amyloid precursor protein by the transmembrane aspartic protease BACE. , 1999, Science.
[17] B. de Strooper,et al. BACE2 processes PMEL to form the melanosome amyloid matrix in pigment cells , 2013, Proceedings of the National Academy of Sciences.
[18] Lynn A. Hyde,et al. Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates. , 2016, Journal of medicinal chemistry.
[19] Marc Wortmann. Dementia: a global health priority - highlights from an ADI and World Health Organization report , 2012, Alzheimer's Research & Therapy.
[20] M. Fielden,et al. Retinal Toxicity Induced by a Novel β-secretase Inhibitor in the Sprague-Dawley Rat , 2015, Toxicologic pathology.
[21] D. Selkoe,et al. Soluble protein oligomers in neurodegeneration: lessons from the Alzheimer's amyloid β-peptide , 2007, Nature Reviews Molecular Cell Biology.
[22] R. Tanzi. The genetics of Alzheimer disease. , 2012, Cold Spring Harbor perspectives in medicine.
[23] J. Macor,et al. Discovery of a novel series of quinolone α7 nicotinic acetylcholine receptor agonists. , 2013, Bioorganic & medicinal chemistry letters.
[24] David J. Diller,et al. In Silico hERG Modeling: Challenges and Progress , 2009 .
[25] D. Theil,et al. Pharmacological BACE1 and BACE2 inhibition induces hair depigmentation by inhibiting PMEL17 processing in mice , 2016, Scientific Reports.
[26] H. Nakanishi,et al. Cathepsin D Deficiency Induces Lysosomal Storage with Ceroid Lipofuscin in Mouse CNS Neurons , 2000, The Journal of Neuroscience.
[27] L. Yip,et al. Synthesis and properties of the sulfonyl analogues of 4(5)-aminoimidazole-5(4)-carboxamide, 4(5)-(formylamino)imidazole-5(4)-carboxamide, guanine, and xanthine. , 1980, Journal of medicinal chemistry.
[28] N. Ostermann,et al. Crystal structure of human BACE2 in complex with a hydroxyethylamine transition-state inhibitor. , 2006, Journal of molecular biology.
[29] David G. Tew,et al. Identification of a Novel Aspartic Protease (Asp 2) as β-Secretase , 1999, Molecular and Cellular Neuroscience.
[30] D. Roden. Drug-induced prolongation of the QT interval. , 2004, The New England journal of medicine.
[31] A. Stamford,et al. Inhibitors of BACE for treating Alzheimer's disease: a fragment-based drug discovery story. , 2013, Current opinion in chemical biology.
[32] Lynn A. Hyde,et al. Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor. , 2012, Bioorganic & medicinal chemistry letters.
[33] P. Saftig,et al. Control of Peripheral Nerve Myelination by the ß-Secretase BACE1 , 2006, Science.
[34] A. Lehesjoki,et al. Cathepsin D deficiency underlies congenital human neuronal ceroid-lipofuscinosis. , 2006, Brain : a journal of neurology.
[35] Jean-Michel Rondeau,et al. Discovery of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid β-peptides. , 2012, Journal of medicinal chemistry.
[36] R E Cachau,et al. Crystal structures of native and inhibited forms of human cathepsin D: implications for lysosomal targeting and drug design. , 1994, Proceedings of the National Academy of Sciences of the United States of America.
[37] B. Strooper,et al. The amyloid cascade hypothesis for Alzheimer's disease: an appraisal for the development of therapeutics , 2011, Nature Reviews Drug Discovery.
[38] Manuel Buttini,et al. Partial Reduction of BACE1 Has Dramatic Effects on Alzheimer Plaque and Synaptic Pathology in APP Transgenic Mice* , 2007, Journal of Biological Chemistry.
[39] J. Klimeš,et al. Outcomes of Alzheimer's disease therapy with acetylcholinesterase inhibitors and memantine , 2014, Expert opinion on drug safety.
[40] P. Wong,et al. Bace1 modulates myelination in the central and peripheral nervous system , 2006, Nature Neuroscience.
[41] Lingyan Wang,et al. Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation. , 2010, Journal of medicinal chemistry.
[42] P. Wong,et al. Function, therapeutic potential and cell biology of BACE proteases: current status and future prospects , 2014, Journal of neurochemistry.
[43] I. Kola,et al. BACE knockout mice are healthy despite lacking the primary beta-secretase activity in brain: implications for Alzheimer's disease therapeutics. , 2001, Human molecular genetics.
[44] J. Hardy,et al. The Amyloid Hypothesis of Alzheimer ’ s Disease : Progress and Problems on the Road to Therapeutics , 2009 .
[45] R. Aebersold,et al. Bace2 is a β cell-enriched protease that regulates pancreatic β cell function and mass. , 2011, Cell metabolism.
[46] Ole A. Andreassen,et al. A mutation in APP protects against Alzheimer’s disease and age-related cognitive decline , 2012, Nature.
[47] R. Barbour,et al. Purification and cloning of amyloid precursor protein β-secretase from human brain , 1999, Nature.
[48] Denis M. Bayada,et al. Polar Molecular Surface as a Dominating Determinant for Oral Absorption and Brain Penetration of Drugs , 1999, Pharmaceutical Research.
[49] J. Malmström,et al. Core refinement toward permeable β-secretase (BACE-1) inhibitors with low hERG activity. , 2013, Journal of medicinal chemistry.
[50] Huadong Tang,et al. A NOVEL MODEL FOR PREDICTION OF HUMAN DRUG CLEARANCE BY ALLOMETRIC SCALING , 2005, Drug Metabolism and Disposition.
[51] Michael Tanen,et al. The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer’s disease patients , 2016, Science Translational Medicine.
[52] M. Staufenbiel,et al. Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application. , 2010, Bioorganic & medicinal chemistry letters.
[53] A. McPhail,et al. Stereoselective Synthesis of β-Substituted β-Amino Sulfones and Sulfonamides via Addition of Sulfonyl Anions to Chiral N-Sulfinyl Imines , 2006 .
[54] Ying-zi Xu,et al. Small-molecule BACE1 inhibitors: a patent literature review (2006 – 2011) , 2012, Expert opinion on therapeutic patents.
[55] M. Citron,et al. Alzheimer's disease: strategies for disease modification , 2010, Nature Reviews Drug Discovery.
[56] J R Chretien,et al. Estimation of blood-brain barrier crossing of drugs using molecular size and shape, and H-bonding descriptors. , 1998, Journal of drug targeting.