Discovery of pyrazole as C-terminus of selective BACE1 inhibitors.
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Yechun Xu | Li Li | Jian Li | B. Xiong | Jing-kang Shen | Jianhua He | Tiantian Chen | Wu-yan Chen | Xin Wang | Lan-ping Ma | Lei Xu | Jia Li | Haiyan Zhang | Yan Fu | Y. Zou | Yiping Zhu | Hai-Yan Zhang | Jingkang Shen | Lanping Ma
[1] W. Thies,et al. 2013 Alzheimer's disease facts and figures , 2013, Alzheimer's & Dementia.
[2] Randy J. Read,et al. Overview of the CCP4 suite and current developments , 2011, Acta crystallographica. Section D, Biological crystallography.
[3] N. Borkakoti,et al. Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core. , 2010, European journal of medicinal chemistry.
[4] Y. Mineur,et al. The membrane cytoskeletal protein adducin is phosphorylated by protein kinase C in D1 neurons of the nucleus accumbens and dorsal striatum following cocaine administration , 2009, Journal of neurochemistry.
[5] John Hardy,et al. The amyloid hypothesis for Alzheimer’s disease: a critical reappraisal , 2009, Journal of neurochemistry.
[6] Wei Wang,et al. Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and beta-secretase. , 2009, Bioorganic & medicinal chemistry.
[7] Gianni Chessari,et al. Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency. , 2007, Journal of medicinal chemistry.
[8] Junya Qu,et al. 2-Amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (beta-site APP cleaving enzyme): Use of structure based design to convert a micromolar hit into a nanomolar lead. , 2007, Journal of medicinal chemistry.
[9] D. Hazuda,et al. Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors. , 2007, Bioorganic & medicinal chemistry letters.
[10] Ó. Lopéz,et al. Click Chemistry - What’s in a Name? Triazole Synthesis and Beyond , 2007 .
[11] Joseph B. Moon,et al. Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase. , 2007, Journal of medicinal chemistry.
[12] D. Dickson,et al. Filling the Gaps in the Aβ Cascade Hypothesis of Alzheimers Disease , 2006 .
[13] Claire Mount,et al. Alzheimer disease: progress or profit? , 2006, Nature Medicine.
[14] Chi‐Huey Wong,et al. Epoxide opening in water and screening in situ for rapid discovery of enzyme inhibitors in microtiter plates. , 2006, Bioorganic & medicinal chemistry.
[15] C. Mathers,et al. Global prevalence of dementia: a Delphi consensus study , 2005, The Lancet.
[16] Kevin Cowtan,et al. research papers Acta Crystallographica Section D Biological , 2005 .
[17] Alison R. Gregro,et al. Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1). , 2004, Journal of medicinal chemistry.
[18] Francois Pognan,et al. Modulation of notch processing by gamma-secretase inhibitors causes intestinal goblet cell metaplasia and induction of genes known to specify gut secretory lineage differentiation. , 2004, Toxicological sciences : an official journal of the Society of Toxicology.
[19] Craig J Hawker,et al. Efficiency and fidelity in a click-chemistry route to triazole dendrimers by the copper(i)-catalyzed ligation of azides and alkynes. , 2004, Angewandte Chemie.
[20] Jay S. Fine,et al. Chronic Treatment with the γ-Secretase Inhibitor LY-411,575 Inhibits β-Amyloid Peptide Production and Alters Lymphopoiesis and Intestinal Cell Differentiation* , 2004, Journal of Biological Chemistry.
[21] H. Kolb,et al. The growing impact of click chemistry on drug discovery. , 2003, Drug discovery today.
[22] W. H. Jordan,et al. Adipsin, a Biomarker of Gastrointestinal Toxicity Mediated by a Functional γ-Secretase Inhibitor* , 2003, Journal of Biological Chemistry.
[23] Randy J Read,et al. Electronic Reprint Biological Crystallography Phenix: Building New Software for Automated Crystallographic Structure Determination Biological Crystallography Phenix: Building New Software for Automated Crystallographic Structure Determination , 2022 .
[24] J. Hardy,et al. The Amyloid Hypothesis of Alzheimer ’ s Disease : Progress and Problems on the Road to Therapeutics , 2009 .
[25] Luke G Green,et al. A stepwise huisgen cycloaddition process: copper(I)-catalyzed regioselective "ligation" of azides and terminal alkynes. , 2002, Angewandte Chemie.
[26] R. Perlmutter,et al. Presenilin-dependent γ-secretase activity modulates thymocyte development , 2001, Proceedings of the National Academy of Sciences of the United States of America.
[27] Gregory D. Longmore,et al. γ-Secretase inhibitors repress thymocyte development , 2001, Proceedings of the National Academy of Sciences of the United States of America.
[28] 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.
[29] M. G. Finn,et al. Click Chemistry: Diverse Chemical Function from a Few Good Reactions. , 2001, Angewandte Chemie.
[30] C. Finch,et al. Targeting small Aβ oligomers: the solution to an Alzheimer's disease conundrum? , 2001, Trends in Neurosciences.
[31] H. Cai,et al. BACE1 is the major β-secretase for generation of Aβ peptides by neurons , 2001, Nature Neuroscience.
[32] W. Richards,et al. Mice deficient in BACE1, the Alzheimer's β-secretase, have normal phenotype and abolished β-amyloid generation , 2001, Nature Neuroscience.
[33] L Hong,et al. Structure of the protease domain of memapsin 2 (beta-secretase) complexed with inhibitor. , 2000, Science.
[34] I. Lieberburg,et al. Cellular mechanisms of beta-amyloid production and secretion. , 1999, Proceedings of the National Academy of Sciences of the United States of America.
[35] J. Hardy,et al. Alzheimer's disease: the amyloid cascade hypothesis. , 1992, Science.
[36] Jianhua He,et al. Flexibility of the flap in the active site of BACE1 as revealed by crystal structures and molecular dynamics simulations. , 2012, Acta crystallographica. Section D, Biological crystallography.
[37] J. Macor,et al. Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1. , 2011, Bioorganic & medicinal chemistry letters.
[38] Z. Otwinowski,et al. [20] Processing of X-ray diffraction data collected in oscillation mode. , 1997, Methods in enzymology.