BACE2 as a new diabetes target: a patent review (2010 – 2012)

Bibliography

• Lam DW, LeRoith D. The worldwide diabetes epidemic. Curr Opin Endocrinol Diabetes Obes 2012;19:93-6
   PubMed Web of Science ®Google Scholar
• El-Kaissi S, Sherbeeni S. Pharmacological management of type 2 diabetes mellitus: an update. Curr Diabetes Rev 2011;7:392-405
   PubMedGoogle Scholar
• Esterhazy D, Stutzer I, Wang H, Bace2 is a beta cell-enriched protease that regulates pancreatic beta cell function and mass. Cell Metab 2011;14:365-77
   PubMed Web of Science ®Google Scholar
• Akpinar P, Kuwajima S, Krutzfeldt J, Stoffel M. Tmem27: a cleaved and shed plasma membrane protein that stimulates pancreatic beta cell proliferation. Cell Metab 2005;2:385-97
   PubMed Web of Science ®Google Scholar
• Finzi G, Franzi F, Placidi C, BACE2 is stored in secretory granules of mouse and rat pancreatic beta cells. Ultrastruct Pathol 2008;32:246-51
   PubMed Web of Science ®Google Scholar
• Hussain I, Powell D, Howlett DR, Identification of a novel aspartic protease (Asp 2) as beta-secretase. Mol Cell Neurosci 1999;14:419-27
   PubMed Web of Science ®Google Scholar
• Vassar R, Bennett B, Babu-Khan S, Beta-secretase cleavage of Alzheimer's amyloid precursor protein by the transmembrane aspartic protease BACE. Science (New York, N.Y.) 1999;286:735-41
   PubMed Web of Science ®Google Scholar
• Yan R, Bienkowski M, Shuck M, Membrane-anchored aspartyl protease with Alzheimer's disease beta-secretase activity. Nature 1999;402:533-7
   PubMed Web of Science ®Google Scholar
• Sinha S, Anderson J, Barbour R, Purification and cloning of amyloid precursor protein beta-secretase from human brain. Nature 1999;402:537-40
   PubMed Web of Science ®Google Scholar
• Hussain I, Powell DJ, Howlett DR, ASP1 (BACE2) cleaves the amyloid precursor protein at the beta-secretase site. Mol Cell Neurosci 2000;16:609-19
   PubMed Web of Science ®Google Scholar
• Lin X, Koelsch G, Wu S, Human aspartic protease memapsin 2 cleaves the beta-secretase site of beta-amyloid precursor protein. Proc Nat Acad Sci USA 2000;97:1456-60
   PubMed Web of Science ®Google Scholar
• Acquati F, Accarino M, Nucci C, The gene encoding DRAP (BACE2), a glycosylated transmembrane protein of the aspartic protease family, maps to the down critical region. FEBS Lett 2000;468:59-64
   PubMed Web of Science ®Google Scholar
• Farzan M, Schnitzler C, Vasilieva N, BACE2, a beta-secretase homolog, cleaves at the beta site and within the amyloid-beta region of the amyloid-beta precursor protein. Proc Nat Acad Sci USA 2000;97:9712-17
   PubMed Web of Science ®Google Scholar
• Beecham S. Aspartic proteinase 2 (ASP2). EP0855444; 1997
   Google Scholar
• Beecham S. Aspartic protease ASP1. EP0848062; 1998
   Google Scholar
• Ghosh AK, Brindisi M, Tang J. Developing beta-secretase inhibitors for treatment of Alzheimer's disease. J Neurochem 2012;120(Suppl):71-83
   PubMed Web of Science ®Google Scholar
• Probst G, Xu YZ. Small-molecule BACE1 inhibitors: a patent literature review (2006 - 2011). Expert Opin Ther Pat 2012;22:511-40
   PubMed Web of Science ®Google Scholar
• Fleck D, Garratt A, Haass C, Willem M. BACE1 dependent neuregulin proteolysis. Curr Alzheimer Res 2012;9(2):178-83
   PubMed Web of Science ®Google Scholar
• EPO - Espacenet. Available from: http://worldwide.espacenet.com/advancedSearch?locale=en_EP [Acessed January 2013]
   Google Scholar
• WIPO PATENTSCOPE. Available from: http://patentscope.wipo.int/search/en/search.jsf [Acessed January 2013]
   Google Scholar
• FPO IP Research & Communities. Available from: http://www.freepatentsonline.com/ [Acessed January 2013]
   Google Scholar
• Europe PubMed Central. Available from: http://europepmc.org/ [Acessed January 2013]
   Google Scholar
• SureChemOpen. Available from: https://open.surechem.com/en/ [Acessed January 2013]
   Google Scholar
• Southan C. InChI in the wild: an Assessment of InChIKey searching in Google. J Cheminform 2013;5:10
   PubMed Web of Science ®Google Scholar
• The PubChem Project. Available from: http://pubchem.ncbi.nlm.nih.gov/ [Acessed January 2013]
   Google Scholar
• ChEMBLdb. Available from: https://www.ebi.ac.uk/chembldb/index.php [Acessed January 2013]
   Google Scholar
• Ostermann N, Eder J, Eidhoff U, Crystal structure of human BACE2 in complex with a hydroxyethylamine transition-state inhibitor. J Mol Biol 2006;355:249-61
   PubMed Web of Science ®Google Scholar
• Novartis. Three-dimensional structure of the human aspartyl protease beta-site amyloid precursor-protein-cleaving enzyme 2 (BACE2), methods and use thereof. WO2006018287; 2006
   Google Scholar
• Hoffman-La Roche. Screening assays for the identification of BACE2 inhibitors. WO2010063640; 2010
   Google Scholar
• ETH-Zurich. Screening assay for metabolic disease therapeuticals. WO2010063718; 2010
   Google Scholar
• Stachel SJ, Coburn CA, Steele TG, Conformationally biased P3 amide replacements of beta-secretase inhibitors. Bioorg Med Chem Lett 2006;16:641-4
   PubMed Web of Science ®Google Scholar
• Astex/AstraZeneca. Substitute amino compounds and uses thereof. WO2006041404; 2006
   Google Scholar
• Shionogi. Aminodihydrothiazine derivative. WO2007049532; 2007
   Google Scholar
• Hoffman-La Roche. 2-Aminodihydro [1, 3] thiazines as BACE2 inhibitors for the treatment of diabetes. WO2011029803; 2011
   Google Scholar
• Hoffman-La Roche. Dihydropyrimidinones for use as BACE2 inhibitors. WO2010128058; 2010
   Google Scholar
• Hoffman-La-Roche/Sienna Biotech. 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazine derivatives. WO2011020806; 2010
   Google Scholar
• Hoffman-La Roche. Amino oxazine derivatives. WO2011070029; 2011
   Google Scholar
• Hoffman-La Roche/Sienna Biotech. 2-Amino-5, 5-difluoro-5, 6-dihydro-4H-oxazines as BACE1 and/or BACE2 inhibitors. WO2011069934; 2011
   Google Scholar
• Hoffman-La Roche. BACE inhibitors for use in the treatment of diabetes. WO2012028563; 2012
   Google Scholar
• Novartis. BACE-2 inhibitors for the treatment of metabolic disorders. WO2012095521; 2012
   Google Scholar
• Hoffman-La Roche. Oxazine derivatives and their use as BACE inhibitors for the treatment of neurological disorders. WO2011009943; 2011
   Google Scholar
• Novartis. Novel heterocyclic derivatives and their use in the treatment of neurological disorders. WO2012095469; 2012
   Google Scholar
• Hoffman-La Roche. 1,4 Thiazepines/sulfones as BACE1 and/or BACE2 inhibitors. WO2012119883; 2012
   Google Scholar
• Hoffman-La Roche/Sienna Biotech. 1,3 Oxazines as BACE1 and/or BACE2 inhibitors. WO2012139993; 2012
   Google Scholar
• Schering. 5-Substituted iminothiazines,mono- and dioxides as BACE inhibitors, compositions and use. WO2012139425; 2012
   Google Scholar
• Schering. Iminothiadiazine dioxide compounds as BACE inhibitors, compositions and their use. US20120183563; 2012
   Google Scholar
• Esterhazy D, Akpinar P, Stoffel M. Tmem27 dimerization, deglycosylation, plasma membrane depletion, and the extracellular Phe-Phe motif are negative regulators of cleavage by Bace2. Biol Chem 2012;393:473-84
   PubMed Web of Science ®Google Scholar
• Casas S, Casini P, Piquer S, BACE2 plays a role in the insulin receptor trafficking in pancreatic beta-cells. Am J Physiol Endocrinol Metab 2010;299:E1087-95
   Web of Science ®Google Scholar
• Meakin PJ, Harper AJ, Hamilton DL, Reduction in BACE1 decreases body weight, protects against diet-induced obesity and enhances insulin sensitivity in mice. Biochem J 2012;441:285-96
   PubMed Web of Science ®Google Scholar
• Dominguez D, Tournoy J, Hartmann D, Phenotypic and biochemical analyses of BACE1- and BACE2-deficient mice. J Biol Chem 2005;280:30797-806
   PubMed Web of Science ®Google Scholar
• Van Bebber F, Hruscha A, Willem M, Loss of Bace2 in zebrafish affects melanocyte migration and is distinct from Bace1 knock out phenotypes. J Neurochem 2013; Accepted Article
   PubMed Web of Science ®Google Scholar
• Cruchaga C, Haller G, Chakraverty S, Rare variants in APP, PSEN1 and PSEN2 increase risk for AD in late-onset Alzheimer's disease families. PLoS One 2012;7(5):10
   Google Scholar
• Jonsson T, Atwal JK, Steinberg S, A mutation in APP protects against Alzheimer's disease and age-related cognitive decline. Nature 2012;488:96-9
   PubMed Web of Science ®Google Scholar
• Southan C, Boppana K, Jagarlapudi SAA, Muresan S. Analysis of in vitro bioactivity data extracted from drug discovery literature and patents: ranking 1654 human protein targets by assayed compounds and molecular scaffolds. J Cheminform 2011;3:14
   PubMed Web of Science ®Google Scholar
• Abdul-Hay SO, Sahara T, McBride M, Identification of BACE2 as an avid beta-amyloid-degrading protease. Mol Neurodegener 2012;7:46
   PubMed Web of Science ®Google Scholar
• Luchsinger JA. Type 2 diabetes and cognitive impairment: linking mechanisms. J Alzheimer's Dis 2012;30(Suppl):2
   Google Scholar