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Discovery of an APP-selective BACE1 inhibitor for Alzheimer's disease. Neurotherapeutics. 2025 Sep; 22(5):e00610. Campagna J, Jagodzinska B, Wi D, Zhu C, Lee J, Cohn W, Jun M, Elias C, Padder S, Descamps O, Peters-Libeu C, Zhang Q, Gorostiza O, Poksay K, Spilman P, Bredesen D, John V. PMID: 40399225; PMCID: PMC12491701.
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Discovery of a small molecule secreted clusterin enhancer that improves memory in Alzheimer's disease mice. NPJ Drug Discov. 2025; 2(1):7. Cohn W, Campagna J, Wi D, Lee JT, Beniwal S, Elezi G, Zhu C, Jagodzinska B, Whitelegge J, Damoiseaux R, John V. PMID: 40322539; PMCID: PMC12048343.
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Discovery of an ApoE4-targeted small-molecule SirT1 enhancer for the treatment of Alzheimer's disease. Sci Rep. 2025 Apr 23; 15(1):14028. Campagna J, Chandra S, Teter B, Cohn W, Pham J, Kim YS, Jagodzinska B, Vadivel K, Alam P, Bilousova T, Young M, Elias C, Marcucci J, Flacau I, Jackman A, Padder S, Wi D, Zhu C, Spilman P, Jung ME, Bredesen DE, John V. PMID: 40269061; PMCID: PMC12019328.
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A therapeutic small molecule enhances γ-oscillations and improves cognition/memory in Alzheimer's disease model mice. Proc Natl Acad Sci U S A. 2024 Aug 13; 121(33):e2400420121. Wei X, Campagna JJ, Jagodzinska B, Wi D, Cohn W, Lee JT, Zhu C, Huang CS, Molnár L, Houser CR, John V, Mody I. PMID: 39106304; PMCID: PMC11331084.
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Simultaneous isolation of intact brain cells and cell-specific extracellular vesicles from cryopreserved Alzheimer's disease cortex. J Neurosci Methods. 2024 06; 406:110137. Melnik M, Miyoshi E, Ma R, Corrada M, Kawas C, Bohannan R, Caraway C, Miller CA, Hinman JD, John V, Bilousova T, Gylys KH. PMID: 38626853.
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A therapeutic small molecule lead enhances γ-oscillations and improves cognition/memory in Alzheimer's disease model mice. bioRxiv. 2023 Dec 06. Wei X, Campagna JJ, Jagodzinska B, Wi D, Cohn W, Lee J, Zhu C, Huang CS, Molnár L, Houser CR, John V, Mody I. PMID: 38106006; PMCID: PMC10723366.
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Pharmacological Inhibition of p-21 Activated Kinase (PAK) Restores Impaired Neurite Outgrowth and Remodeling in a Cellular Model of Down Syndrome. Neurotox Res. 2023 Jun; 41(3):256-269. Barraza-Núñez N, Pérez-Núñez R, Gaete-Ramírez B, Barrios-Garrido A, Arriagada C, Poksay K, John V, Barnier JV, Cárdenas AM, Caviedes P. PMID: 36867391.
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Distinct Patterns of Gene Expression Changes in the Colon and Striatum of Young Mice Overexpressing Alpha-Synuclein Support Parkinson's Disease as a Multi-System Process. J Parkinsons Dis. 2023; 13(7):1127-1147. Videlock EJ, Hatami A, Zhu C, Kawaguchi R, Chen H, Khan T, Yehya AHS, Stiles L, Joshi S, Hoffman JM, Law KM, Rankin CR, Chang L, Maidment NT, John V, Geschwind DH, Pothoulakis C. PMID: 37638450; PMCID: PMC10657720.
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Fluorescent risedronate analogue 800CW-pRIS improves tooth extraction-associated abnormal wound healing in zoledronate-treated mice. Commun Med (Lond). 2022; 2:112. Okawa H, Kondo T, Hokugo A, Cherian P, Sundberg O, Campagna JJ, Kashemirov BA, John V, Sun S, Ebetino FH, McKenna CE, Nishimura I. PMID: 36082175; PMCID: PMC9445170.
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Mechanism of bisphosphonate-related osteonecrosis of the jaw (BRONJ) revealed by targeted removal of legacy bisphosphonate from jawbone using competing inert hydroxymethylene diphosphonate. Elife. 2022 08 26; 11. Okawa H, Kondo T, Hokugo A, Cherian P, Campagna JJ, Lentini NA, Sung EC, Chiang S, Lin YL, Ebetino FH, John V, Sun S, McKenna CE, Nishimura I. PMID: 36017995; PMCID: PMC9489207.
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Integrated Multiomics Analysis of Salivary Exosomes to Identify Biomarkers Associated with Changes in Mood States and Fatigue. Int J Mol Sci. 2022 May 09; 23(9). Cohn W, Zhu C, Campagna J, Bilousova T, Spilman P, Teter B, Li F, Guo R, Elashoff D, Cole GM, Avidan A, Faull KF, Whitelegge J, Wong DTW, John V. PMID: 35563647; PMCID: PMC9105576.
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Multi-Omics Analysis of Microglial Extracellular Vesicles From Human Alzheimer's Disease Brain Tissue Reveals Disease-Associated Signatures. Front Pharmacol. 2021; 12:766082. Cohn W, Melnik M, Huang C, Teter B, Chandra S, Zhu C, McIntire LB, John V, Gylys KH, Bilousova T. PMID: 34925024; PMCID: PMC8675946.
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Exosomal tau with seeding activity is released from Alzheimer's disease synapses, and seeding potential is associated with amyloid beta. Lab Invest. 2021 12; 101(12):1605-1617. Miyoshi E, Bilousova T, Melnik M, Fakhrutdinov D, Poon WW, Vinters HV, Miller CA, Corrada M, Kawas C, Bohannan R, Caraway C, Elias C, Maina KN, Campagna JJ, John V, Gylys KH. PMID: 34462532; PMCID: PMC8590975.
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Correction to: Pharmacological inhibition of nSMase2 reduces brain exosome release and α-synuclein pathology in a Parkinson's disease model. Mol Brain. 2021 Jul 08; 14(1):108. Zhu C, Bilousova T, Focht S, Jun M, Elias CJ, Melnik M, Chandra S, Campagna J, Cohn W, Hatami A, Spilman P, Gylys KH, John V. PMID: 34238327; PMCID: PMC8265003.
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Pharmacological inhibition of nSMase2 reduces brain exosome release and α-synuclein pathology in a Parkinson's disease model. Mol Brain. 2021 04 19; 14(1):70. Zhu C, Bilousova T, Focht S, Jun M, Elias CJ, Melnik M, Chandra S, Campagna J, Cohn W, Hatami A, Spilman P, Gylys KH, John V. PMID: 33875010; PMCID: PMC8056538.
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Behavioral Deficits and Brain α-Synuclein and Phosphorylated Serine-129 α-Synuclein in Male and Female Mice Overexpressing Human α-Synuclein. J Alzheimers Dis. 2021; 79(2):875-893. Gabrielyan L, Liang H, Minalyan A, Hatami A, John V, Wang L. PMID: 33361597; PMCID: PMC8577576.
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A Small-Molecule Approach to Restore a Slow-Oxidative Phenotype and Defective CaMKIIβ Signaling in Limb Girdle Muscular Dystrophy. Cell Rep Med. 2020 10 20; 1(7):100122. Liu J, Campagna J, John V, Damoiseaux R, Mokhonova E, Becerra D, Meng H, McNally EM, Pyle AD, Kramerova I, Spencer MJ. PMID: 33205074; PMCID: PMC7659555.
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High-throughput screening identifies modulators of sarcospan that stabilize muscle cells and exhibit activity in the mouse model of Duchenne muscular dystrophy. Skelet Muscle. 2020 09 18; 10(1):26. Shu C, Parfenova L, Mokhonova E, Collado JR, Damoiseaux R, Campagna J, John V, Crosbie RH. PMID: 32948250; PMCID: PMC7499884.
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Dual Neutral Sphingomyelinase-2/Acetylcholinesterase Inhibitors for the Treatment of Alzheimer's Disease. ACS Chem Biol. 2020 06 19; 15(6):1671-1684. Bilousova T, Simmons BJ, Knapp RR, Elias CJ, Campagna J, Melnik M, Chandra S, Focht S, Zhu C, Vadivel K, Jagodzinska B, Cohn W, Spilman P, Gylys KH, Garg NK, John V. PMID: 32352753; PMCID: PMC8297715.
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Shotgun Proteomic Profiling of Bloodborne Nanoscale Extracellular Vesicles. Methods Mol Biol. 2019; 1897:403-416. Heinzelman P, Powers DN, Wohlschlegel JA, John V. PMID: 30539460.
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Synthesis of Fused Indolines by Interrupted Fischer Indolization in a Microfluidic Reactor. Tetrahedron Lett. 2019 Jan 17; 60(3):322-326. Duong AT, Simmons BJ, Alam MP, Campagna J, Garg NK, John V. PMID: 30631216; PMCID: PMC6322698.
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A small molecule ApoE4-targeted therapeutic candidate that normalizes sirtuin 1 levels and improves cognition in an Alzheimer's disease mouse model. Sci Rep. 2018 12 04; 8(1):17574. Campagna J, Spilman P, Jagodzinska B, Bai D, Hatami A, Zhu C, Bilousova T, Jun M, Elias CJ, Pham J, Cole G, LaDu MJ, Jung ME, Bredesen DE, John V. PMID: 30514854; PMCID: PMC6279743.
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Evaluation of an Allosteric BACE Inhibitor Peptide to Identify Mimetics that Can Interact with the Loop F Region of the Enzyme and Prevent APP Cleavage. J Mol Biol. 2018 05 25; 430(11):1566-1576. Campagna J, Vadivel K, Jagodzinska B, Jun M, Bilousova T, Spilman P, John V. PMID: 29649434.
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Suppression of tau propagation using an inhibitor that targets the DK-switch of nSMase2. Biochem Biophys Res Commun. 2018 05 23; 499(4):751-757. Bilousova T, Elias C, Miyoshi E, Alam MP, Zhu C, Campagna J, Vadivel K, Jagodzinska B, Gylys KH, John V. PMID: 29604274; PMCID: PMC5956110.
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Drug-induced modulation of gp130 signalling prevents articular cartilage degeneration and promotes repair. Ann Rheum Dis. 2018 05; 77(5):760-769. Shkhyan R, Van Handel B, Bogdanov J, Lee S, Yu Y, Scheinberg M, Banks NW, Limfat S, Chernostrik A, Franciozi CE, Alam MP, John V, Wu L, Ferguson GB, Nsair A, Petrigliano FA, Vangsness CT, Vadivel K, Bajaj P, Wang L, Liu NQ, Evseenko D. PMID: 29436471; PMCID: PMC8444286.
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A Small Molecule Mimetic of the Humanin Peptide as a Candidate for Modulating NMDA-Induced Neurotoxicity. ACS Chem Neurosci. 2018 03 21; 9(3):462-468. Alam MP, Bilousova T, Spilman P, Vadivel K, Bai D, Elias CJ, Evseenko D, John V. PMID: 29161500.
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Deformable Nanovesicles Synthesized through an Adaptable Microfluidic Platform for Enhanced Localized Transdermal Drug Delivery. J Drug Deliv. 2017; 2017:4759839. Subbiah N, Campagna J, Spilman P, Alam MP, Sharma S, Hokugo A, Nishimura I, John V. PMID: 28480080; PMCID: PMC5396447.
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Screening for Small Molecule Inhibitors of Statin-Induced APP C-terminal Toxic Fragment Production. Front Pharmacol. 2017; 8:46. Poksay KS, Sheffler DJ, Spilman P, Campagna J, Jagodzinska B, Descamps O, Gorostiza O, Matalis A, Mullenix M, Bredesen DE, Cosford ND, John V. PMID: 28261092; PMCID: PMC5309220.
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C-O bond Formation in a Microfluidic Reactor: High Yield SNAr Substitution of Heteroaryl Chlorides. Tetrahedron Lett. 2016 May 11; 57(19):2059-2062. Alam MP, Jagodzinska B, Campagna J, Spilman P, John V. PMID: 27152054; PMCID: PMC4852388.
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Nanoscale Extracellular Vesicle Analysis in Alzheimer's Disease Diagnosis and Therapy. Int J Alzheimers Dis. 2016; 2016:8053139. Heinzelman P, Bilousova T, Campagna J, John V. PMID: 27213078; PMCID: PMC4861781.
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Netrin-1 Interrupts Amyloid-β Amplification, Increases sAβPPα in vitro and in vivo, and Improves Cognition in a Mouse Model of Alzheimer's Disease. J Alzheimers Dis. 2016 03 08; 52(1):223-42. Spilman PR, Corset V, Gorostiza O, Poksay KS, Galvan V, Zhang J, Rao R, Peters-Libeu C, Vincelette J, McGeehan A, Dvorak-Ewell M, Beyer J, Campagna J, Bankiewicz K, Mehlen P, John V, Bredesen DE. PMID: 27060954.
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Correction to hunter-killer peptide (HKP) for targeted therapy. J Med Chem. 2015 Feb 26; 58(4):2045. Ellerby HM, Bredesen DE, Fujimura S, John V. PMID: 25668572.
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sAβPPα is a Potent Endogenous Inhibitor of BACE1. J Alzheimers Dis. 2015; 47(3):545-55. Peters-Libeu C, Campagna J, Mitsumori M, Poksay KS, Spilman P, Sabogal A, Bredesen DE, John V. PMID: 26401691.
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Paradoxical effect of TrkA inhibition in Alzheimer's disease models. J Alzheimers Dis. 2014; 40(3):605-617. Zhang Q, Descamps O, Hart MJ, Poksay KS, Spilman P, Kane DJ, Gorostiza O, John V, Bredesen DE. PMID: 24531152; PMCID: PMC4091737.
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The multi-functional drug tropisetron binds APP and normalizes cognition in a murine Alzheimer's model. Brain Res. 2014 Mar 10; 1551:25-44. Spilman P, Descamps O, Gorostiza O, Peters-Libeu C, Poksay KS, Matalis A, Campagna J, Patent A, Rao R, John V, Bredesen DE. PMID: 24389031; PMCID: PMC4001856.
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Neuroprotective Sirtuin ratio reversed by ApoE4. Proc Natl Acad Sci U S A. 2013 Nov 05; 110(45):18303-8. Theendakara V, Patent A, Peters Libeu CA, Philpot B, Flores S, Descamps O, Poksay KS, Zhang Q, Cailing G, Hart M, John V, Rao RV, Bredesen DE. PMID: 24145446; PMCID: PMC3831497.
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Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors. Bioorg Med Chem Lett. 2013 Aug 15; 23(16):4674-9. Ng RA, Sun M, Bowers S, Hom RK, Probst GD, John V, Fang LY, Maillard M, Gailunas A, Brogley L, Neitz RJ, Tung JS, Pleiss MA, Konradi AW, Sham HL, Dappen MS, Adler M, Yao N, Zmolek W, Nakamura D, Quinn KP, Sauer JM, Bova MP, Ruslim L, Artis DR, Yednock TA. PMID: 23856050.
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Next generation therapeutics for Alzheimer's disease. EMBO Mol Med. 2013 Jun; 5(6):795-8. Bredesen DE, John V. PMID: 23703924; PMCID: PMC3779441.
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AβPP-selective BACE inhibitors (ASBI): novel class of therapeutic agents for alzheimer's disease. J Alzheimers Dis. 2013; 37(2):343-55. Descamps O, Spilman P, Zhang Q, Libeu CP, Poksay K, Gorostiza O, Campagna J, Jagodzinska B, Bredesen DE, John V. PMID: 23948888; PMCID: PMC3971881.
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Posiphen as a candidate drug to lower CSF amyloid precursor protein, amyloid-β peptide and τ levels: target engagement, tolerability and pharmacokinetics in humans. J Neurol Neurosurg Psychiatry. 2012 Sep; 83(9):894-902. Maccecchini ML, Chang MY, Pan C, John V, Zetterberg H, Greig NH. PMID: 22791904; PMCID: PMC3415310.
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Altering APP proteolysis: increasing sAPPalpha production by targeting dimerization of the APP ectodomain. PLoS One. 2012; 7(6):e40027. Libeu CA, Descamps O, Zhang Q, John V, Bredesen DE. PMID: 22768208; PMCID: PMC3386930.
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Ayurvedic medicinal plants for Alzheimer's disease: a review. Alzheimers Res Ther. 2012 Jun 29; 4(3):22. Rao RV, Descamps O, John V, Bredesen DE. PMID: 22747839; PMCID: PMC3506936.
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Pharmacological induction of neuroglobin expression. Pharmacology. 2011; 87(1-2):81-4. Jin K, Mao XO, Xie L, John V, Greenberg DA. PMID: 21228614; PMCID: PMC3042117.
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Structural and functional alterations in amyloid-β precursor protein induced by amyloid-β peptides. J Alzheimers Dis. 2011; 25(3):547-66. Libeu CP, Poksay KS, John V, Bredesen DE. PMID: 21471643; PMCID: PMC4001850.
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Induction of the C-terminal proteolytic cleavage of AβPP by statins. J Alzheimers Dis. 2011; 25(1):51-7. Descamps O, Zhang Q, John V, Bredesen DE. PMID: 21422530.
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Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region. Bioorg Med Chem Lett. 2010 Oct 15; 20(20):6034-9. Probst GD, Bowers S, Sealy JM, Stupi B, Dressen D, Jagodzinska BM, Aquino J, Gailunas A, Truong AP, Tso L, Xu YZ, Hom RK, John V, Tung JS, Pleiss MA, Tucker JA, Konradi AW, Sham HL, Jagodzinski J, Toth G, Brecht E, Yao N, Pan H, Lin M, Artis DR, Ruslim L, Bova MP, Sinha S, Yednock TA, Gauby S, Zmolek W, Quinn KP, Sauer JM. PMID: 20822903.
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Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents. Bioorg Med Chem Lett. 2010 Aug 15; 20(16):4789-94. Truong AP, Probst GD, Aquino J, Fang L, Brogley L, Sealy JM, Hom RK, Tucker JA, John V, Tung JS, Pleiss MA, Konradi AW, Sham HL, Dappen MS, Tóth G, Yao N, Brecht E, Pan H, Artis DR, Ruslim L, Bova MP, Sinha S, Yednock TA, Zmolek W, Quinn KP, Sauer JM. PMID: 20634069.
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Importance of the caspase cleavage site in amyloid-β protein precursor. J Alzheimers Dis. 2010; 22(1):57-63. Bredesen DE, John V, Galvan V. PMID: 20847422; PMCID: PMC3968071.
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Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents. Bioorg Med Chem Lett. 2009 Nov 15; 19(22):6386-91. Sealy JM, Truong AP, Tso L, Probst GD, Aquino J, Hom RK, Jagodzinska BM, Dressen D, Wone DW, Brogley L, John V, Tung JS, Pleiss MA, Tucker JA, Konradi AW, Dappen MS, Toth G, Pan H, Ruslim L, Miller J, Bova MP, Sinha S, Quinn KP, Sauer JM. PMID: 19811916.
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Hunter-killer peptide (HKP) for targeted therapy. J Med Chem. 2008 Oct 09; 51(19):5887-92. Ellerby HM, Bredesen DE, Fujimura S, John V. PMID: 18828573.
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Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase. J Med Chem. 2007 Feb 22; 50(4):776-81. Maillard MC, Hom RK, Benson TE, Moon JB, Mamo S, Bienkowski M, Tomasselli AG, Woods DD, Prince DB, Paddock DJ, Emmons TL, Tucker JA, Dappen MS, Brogley L, Thorsett ED, Jewett N, Sinha S, John V. PMID: 17300163.
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Human beta-secretase (BACE) and BACE inhibitors: progress report. Curr Top Med Chem. 2006; 6(6):569-78. John V. PMID: 16712492.
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Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase. J Med Chem. 2004 Jan 01; 47(1):158-64. Hom RK, Gailunas AF, Mamo S, Fang LY, Tung JS, Walker DE, Davis D, Thorsett ED, Jewett NE, Moon JB, John V. PMID: 14695829.
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Human beta-secretase (BACE) and BACE inhibitors. J Med Chem. 2003 Oct 23; 46(22):4625-30. John V, Beck JP, Bienkowski MJ, Sinha S, Heinrikson RL. PMID: 14561080.
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Design and synthesis of statine-based cell-permeable peptidomimetic inhibitors of human beta-secretase. J Med Chem. 2003 May 08; 46(10):1799-802. Hom RK, Fang LY, Mamo S, Tung JS, Guinn AC, Walker DE, Davis DL, Gailunas AF, Thorsett ED, Sinha S, Knops JE, Jewett NE, Anderson JP, John V. PMID: 12723942.
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Design of substrate-based inhibitors of human beta-secretase. J Med Chem. 2002 Jan 17; 45(2):259-62. Tung JS, Davis DL, Anderson JP, Walker DE, Mamo S, Jewett N, Hom RK, Sinha S, Thorsett ED, John V. PMID: 11784130.
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