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Lysine-Targeting Inhibitors of Amyloidogenic Protein Aggregation: A Promise for Neurodegenerative Proteinopathies. JACS Au. 2025 Aug 25; 5(8):3680-3700. Murakami K, Nguyen THV, Nagao C, Mizuguchi K, Bitan G. PMID: 40881400; PMCID: PMC12381728.
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Mass spectrometry structural analysis of intrinsically disordered phosphoproteins. Int J Mass Spectrom. 2025 Jul; 513. Lantz C, Zenaidee MA, Tran D, Biggs K, Bitan G, Ogorzalek Loo RR, Loo JA. PMID: 41613339; PMCID: PMC12851516.
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Broad repetitive transcranial magnetic stimulation (rTMS) of the precuneus in Alzheimer's disease: A rationale and study design. Alzheimers Dement (N Y). 2025 Jan-Mar; 11(1):e70043. Leuchter MK, Oughli HA, Durbin KA, Jackson NJ, Elashoff D, Chang TS, Corlier J, Ngo D, Matthews C, Wong D, Fogel BL, Bitan G, Leuchter AF, Vossel K, Suthana N. PMID: 40065917; PMCID: PMC11891574.
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Allosteric Modulation of Pathological Ataxin-3 Aggregation: A Path to Spinocerebellar Ataxia Type-3 Therapies. bioRxiv. 2025 Jan 24. Silva A, Duarte-Silva S, Martins PM, Rodrigues B, Serrenho D, Vilasboas-Campos D, Teixeira-Castro A, Vieyto-Nuñez J, Mieres-Perez J, Figueiredo F, Fraga J, Noble J, Lantz C, Sepanj N, Monteiro-Fernandes D, Guerreiro S, Neves-Carvalho A, Pereira-Sousa J, Klärner FG, Schrader T, Loo JA, Pastore A, Sanchez-Garcia E, Bitan G, Carvalho AL, Maciel P, Macedo-Ribeiro S. PMID: 39896516; PMCID: PMC11785186.
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Editorial: Extracellular vesicles: emerging roles in the aged and neurodegenerative brain. Front Cell Neurosci. 2024; 18:1522499. Vasilopoulou F, Pocock J, Bitan G, Hermann DM. PMID: 39717388; PMCID: PMC11663929.
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Anti-amyloid treatment is broadly effective in neuronopathic mucopolysaccharidoses and synergizes with gene therapy in MPS-IIIA. Mol Ther. 2024 Nov 06; 32(11):4108-4121. Giaccio M, Monaco A, Galiano L, Parente A, Borzacchiello L, Rubino R, Klärner FG, Killa D, Perna C, Piccolo P, Marotta M, Pan X, Khijniak M, Siddique I, Schrader T, Pshezhetsky AV, Sorrentino NC, Bitan G, Fraldi A. PMID: 39342429; PMCID: PMC11573617.
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Author Correction: Anakinra in Sanfilippo syndrome: a phase 1/2 trial. Nat Med. 2024 Sep; 30(9):2693. Polgreen LE, Chen AH, Pak Y, Luzzi A, Morales Garval A, Acevedo J, Bitan G, Iacovino M, O'Neill C, Eisengart JB. PMID: 39075282; PMCID: PMC11405256.
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Anakinra in Sanfilippo syndrome: a phase 1/2 trial. Nat Med. 2024 Sep; 30(9):2473-2479. Polgreen LE, Chen AH, Pak Y, Luzzi A, Morales Garval A, Acevedo J, Bitan G, Iacovino M, O'Neill C, Eisengart JB. PMID: 38907160; PMCID: PMC11405265.
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Novel avenues of tau research. Alzheimers Dement. 2024 03; 20(3):2240-2261. Sexton CE, Bitan G, Bowles KR, Brys M, Buée L, Maina MB, Clelland CD, Cohen AD, Crary JF, Dage JL, Diaz K, Frost B, Gan L, Goate AM, Golbe LI, Hansson O, Karch CM, Kolb HC, La Joie R, Lee SE, Matallana D, Miller BL, Onyike CU, Quiroz YT, Rexach JE, Rohrer JD, Rommel A, Sadri-Vakili G, Schindler SE, Schneider JA, Sperling RA, Teunissen CE, Weninger SC, Worley SL, Zheng H, Carrillo MC. PMID: 38170841; PMCID: PMC10984447.
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Recent advances and future therapy development for Alzheimer's disease and related disorders. Neural Regen Res. 2024 Sep 01; 19(9):1877-1878. Hong M, Bitan G. PMID: 38227506; PMCID: PMC11040305.
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Characterization of Molecular Tweezer Binding on α-Synuclein with Native Top-Down Mass Spectrometry and Ion Mobility-Mass Spectrometry Reveals a Mechanism for Aggregation Inhibition. J Am Soc Mass Spectrom. 2023 Dec 06; 34(12):2739-2747. Lantz C, Lopez J, Goring AK, Zenaidee MA, Biggs K, Whitelegge JP, Ogorzalek Loo RR, Klärner FG, Schrader T, Bitan G, Loo JA. PMID: 37936057; PMCID: PMC10959575.
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IM-MS and ECD-MS/MS Provide Insight into Modulation of Amyloid Proteins Self-Assembly by Peptides and Small Molecules. J Am Soc Mass Spectrom. 2023 Oct 04; 34(10):2066-2086. Taha HB, Chawla E, Bitan G. PMID: 37607351.
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Biomarkers for parkinsonian disorders in CNS-originating EVs: promise and challenges. Acta Neuropathol. 2023 05; 145(5):515-540. Dutta S, Hornung S, Taha HB, Bitan G. PMID: 37012443; PMCID: PMC10071251.
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Toward a biomarker panel measured in CNS-originating extracellular vesicles for improved differential diagnosis of Parkinson's disease and multiple system atrophy. Transl Neurodegener. 2023 03 20; 12(1):14. Taha HB, Hornung S, Dutta S, Fenwick L, Lahgui O, Howe K, Elabed N, Del Rosario I, Wong DY, Duarte Folle A, Markovic D, Palma JA, Kang UJ, Alcalay RN, Sklerov M, Kaufmann H, Fogel BL, Bronstein JM, Ritz B, Bitan G. PMID: 36935518; PMCID: PMC10026428.
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Development of a Novel Electrochemiluminescence ELISA for Quantification of α-Synuclein Phosphorylated at Ser129 in Biological Samples. ACS Chem Neurosci. 2023 04 05; 14(7):1238-1248. Dutta S, Hornung S, Taha HB, Biggs K, Siddique I, Chamoun LM, Shahpasand-Kroner H, Lantz C, Herrera-Vaquero M, Stefanova N, Loo JA, Bitan G. PMID: 36920792; PMCID: PMC10080651.
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Editorial: Trends in biomarkers for neurodegenerative diseases: Current research and future perspectives. Front Aging Neurosci. 2023; 15:1153932. Dutta S, Sklerov M, Teunissen CE, Bitan G. PMID: 36875706; PMCID: PMC9978689.
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Using FRET-Based Biosensor Cells to Study the Seeding Activity of Tau and α-Synuclein. Methods Mol Biol. 2023; 2551:125-145. Maina KN, Smet-Nocca C, Bitan G. PMID: 36310201; PMCID: PMC9836052.
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Molecular Tweezers: Supramolecular Hosts with Broad-Spectrum Biological Applications. Pharmacol Rev. 2023 03; 75(2):263-308. Shahpasand-Kroner H, Siddique I, Malik R, Linares GR, Ivanova MI, Ichida J, Weil T, Münch J, Sanchez-Garcia E, Klärner FG, Schrader T, Bitan G. PMID: 36549866; PMCID: PMC9976797.
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The Amyloid Inhibitor CLR01 Relieves Autophagy and Ameliorates Neuropathology in a Severe Lysosomal Storage Disease. Mol Ther. 2022 Nov 02; 30(11):3499. Monaco A, Maffia V, Sorrentino NC, Sambri I, Ezhova Y, Giuliano T, Cacace V, Nusco E, De Risi M, De Leonibus E, Schrader T, Klärner FG, Bitan G, Fraldi A. PMID: 36261045; PMCID: PMC9637752.
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A minute fraction of α-synuclein in extracellular vesicles may be a major contributor to α-synuclein spreading following autophagy inhibition. Front Mol Neurosci. 2022; 15:1001382. Taha HB, Kearney B, Bitan G. PMID: 36245921; PMCID: PMC9554483.
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Editorial: Exosomes: Message in a vesicle. Front Pharmacol. 2022; 13:1018928. Dutta S, Nimse SB, Van Keuren-Jensen K, Bitan G. PMID: 36160457; PMCID: PMC9494591.
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mTOR Inhibition with Sirolimus in Multiple System Atrophy: A Randomized, Double-Blind, Placebo-Controlled Futility Trial and 1-Year Biomarker Longitudinal Analysis. Mov Disord. 2022 04; 37(4):778-789. Palma JA, Martinez J, Millar Vernetti P, Ma T, Perez MA, Zhong J, Qian Y, Dutta S, Maina KN, Siddique I, Bitan G, Ades-Aron B, Shepherd TM, Kang UJ, Kaufmann H. PMID: 35040506; PMCID: PMC9018525.
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Three-repeat and four-repeat tau isoforms form different oligomers. Protein Sci. 2022 03; 31(3):613-627. Shahpasand-Kroner H, Portillo J, Lantz C, Seidler PM, Sarafian N, Loo JA, Bitan G. PMID: 34902187; PMCID: PMC8862439.
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Aptamers targeting amyloidogenic proteins and their emerging role in neurodegenerative diseases. J Biol Chem. 2022 01; 298(1):101478. Murakami K, Izuo N, Bitan G. PMID: 34896392; PMCID: PMC8728582.
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Lysine-selective molecular tweezers are cell penetrant and concentrate in lysosomes. Commun Biol. 2021 09 14; 4(1):1076. Li Z, Siddique I, Hadrovic I, Kirupakaran A, Li J, Zhang Y, Klärner FG, Schrader T, Bitan G. PMID: 34521989; PMCID: PMC8440717.
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α-Synuclein in blood exosomes immunoprecipitated using neuronal and oligodendroglial markers distinguishes Parkinson's disease from multiple system atrophy. Acta Neuropathol. 2021 09; 142(3):495-511. Dutta S, Hornung S, Kruayatidee A, Maina KN, Del Rosario I, Paul KC, Wong DY, Duarte Folle A, Markovic D, Palma JA, Serrano GE, Adler CH, Perlman SL, Poon WW, Kang UJ, Alcalay RN, Sklerov M, Gylys KH, Kaufmann H, Fogel BL, Bronstein JM, Ritz B, Bitan G. PMID: 33991233; PMCID: PMC8357708.
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Inhibition of Staphylococcus aureus biofilm-forming functional amyloid by molecular tweezers. Cell Chem Biol. 2021 09 16; 28(9):1310-1320.e5. Malishev R, Salinas N, Gibson J, Eden AB, Mieres-Perez J, Ruiz-Blanco YB, Malka O, Kolusheva S, Klärner FG, Schrader T, Sanchez-Garcia E, Wang C, Landau M, Bitan G, Jelinek R. PMID: 33852903; PMCID: PMC9377279.
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The molecular tweezer CLR01 improves behavioral deficits and reduces tau pathology in P301S-tau transgenic mice. Alzheimers Res Ther. 2021 01 04; 13(1):6. Di J, Siddique I, Li Z, Malki G, Hornung S, Dutta S, Hurst I, Ishaaya E, Wang A, Tu S, Boghos A, Ericsson I, Klärner FG, Schrader T, Bitan G. PMID: 33397489; PMCID: PMC7784007.
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Supramolecular Mechanism of Viral Envelope Disruption by Molecular Tweezers. J Am Chem Soc. 2020 10 07; 142(40):17024-17038. Weil T, Groß R, Röcker A, Bravo-Rodriguez K, Heid C, Sowislok A, Le MH, Erwin N, Dwivedi M, Bart SM, Bates P, Wettstein L, Müller JA, Harms M, Sparrer K, Ruiz-Blanco YB, Stürzel CM, von Einem J, Lippold S, Read C, Walther P, Hebel M, Kreppel F, Klärner FG, Bitan G, Ehrmann M, Weil T, Winter R, Schrader T, Shorter J, Sanchez-Garcia E, Münch J. PMID: 32926779; PMCID: PMC7523239.
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CLR01 protects dopaminergic neurons in vitro and in mouse models of Parkinson's disease. Nat Commun. 2020 09 28; 11(1):4885. Bengoa-Vergniory N, Faggiani E, Ramos-Gonzalez P, Kirkiz E, Connor-Robson N, Brown LV, Siddique I, Li Z, Vingill S, Cioroch M, Cavaliere F, Threlfell S, Roberts B, Schrader T, Klärner FG, Cragg S, Dehay B, Bitan G, Matute C, Bezard E, Wade-Martins R. PMID: 32985503; PMCID: PMC7522721.
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Examination of SOD1 aggregation modulators and their effect on SOD1 enzymatic activity as a proxy for potential toxicity. FASEB J. 2020 09; 34(9):11957-11969. Malik R, Corrales C, Linsenmeier M, Alalami H, Sepanj N, Bitan G. PMID: 32701214; PMCID: PMC7903925.
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Different Inhibitors of Aβ42-Induced Toxicity Have Distinct Metal-Ion Dependency. ACS Chem Neurosci. 2020 08 05; 11(15):2243-2255. Mason AJ, Hurst I, Malik R, Siddique I, Solomonov I, Sagi I, Klärner FG, Schrader T, Bitan G. PMID: 32559370; PMCID: PMC7695034.
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The recent failure of the PROMESA clinical trial for multiple system atrophy raises the question-are polyphenols a viable therapeutic option against proteinopathies? Ann Transl Med. 2020 Jun; 8(11):719. Bitan G. PMID: 32617339; PMCID: PMC7327354.
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CNS-Derived Blood Exosomes as a Promising Source of Biomarkers: Opportunities and Challenges. Front Mol Neurosci. 2020; 13:38. Hornung S, Dutta S, Bitan G. PMID: 32265650; PMCID: PMC7096580.
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The Amyloid Inhibitor CLR01 Relieves Autophagy and Ameliorates Neuropathology in a Severe Lysosomal Storage Disease. Mol Ther. 2020 04 08; 28(4):1167-1176. Monaco A, Maffia V, Sorrentino NC, Sambri I, Ezhova Y, Giuliano T, Cacace V, Nusco E, De Risi M, De Leonibus E, Schrader T, Klärner FG, Bitan G, Fraldi A. PMID: 32087148; PMCID: PMC7132627.
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Amyloid β-protein oligomers promote the uptake of tau fibril seeds potentiating intracellular tau aggregation. Alzheimers Res Ther. 2019 10 18; 11(1):86. Shin WS, Di J, Cao Q, Li B, Seidler PM, Murray KA, Bitan G, Jiang L. PMID: 31627745; PMCID: PMC6800506.
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Molecular Lysine Tweezers Counteract Aberrant Protein Aggregation. Front Chem. 2019; 7:657. Hadrovic I, Rebmann P, Klärner FG, Bitan G, Schrader T. PMID: 31632951; PMCID: PMC6779714.
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Ischemic axonal injury up-regulates MARK4 in cortical neurons and primes tau phosphorylation and aggregation. Acta Neuropathol Commun. 2019 08 20; 7(1):135. Hayden EY, Putman J, Nunez S, Shin WS, Oberoi M, Charreton M, Dutta S, Li Z, Komuro Y, Joy MT, Bitan G, MacKenzie-Graham A, Jiang L, Hinman JD. PMID: 31429800; PMCID: PMC6700776.
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Disease-modifying therapy for proteinopathies: Can the exception become the rule? Prog Mol Biol Transl Sci. 2019; 168:277-287. Bitan G. PMID: 31699321; PMCID: PMC7032046.
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The molecular tweezer CLR01 reduces aggregated, pathologic, and seeding-competent α-synuclein in experimental multiple system atrophy. Biochim Biophys Acta Mol Basis Dis. 2019 11 01; 1865(11):165513. Herrera-Vaquero M, Bouquio D, Kallab M, Biggs K, Nair G, Ochoa J, Heras-Garvin A, Heid C, Hadrovic I, Poewe W, Wenning GK, Klärner FG, Schrader T, Bitan G, Stefanova N. PMID: 31319154; PMCID: PMC8425273.
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Major Differences between the Self-Assembly and Seeding Behavior of Heparin-Induced and in Vitro Phosphorylated Tau and Their Modulation by Potential Inhibitors. ACS Chem Biol. 2019 06 21; 14(6):1363-1379. Despres C, Di J, Cantrelle FX, Li Z, Huvent I, Chambraud B, Zhao J, Chen J, Chen S, Lippens G, Zhang F, Linhardt R, Wang C, Klärner FG, Schrader T, Landrieu I, Bitan G, Smet-Nocca C. PMID: 31046227; PMCID: PMC6636790.
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A Label-Free Platform for Identification of Exosomes from Different Sources. ACS Sens. 2019 02 22; 4(2):488-497. Yan Z, Dutta S, Liu Z, Yu X, Mesgarzadeh N, Ji F, Bitan G, Xie YH. PMID: 30644736.
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The molecular tweezer CLR01 inhibits aberrant superoxide dismutase 1 (SOD1) self-assembly in vitro and in the G93A-SOD1 mouse model of ALS. J Biol Chem. 2019 03 08; 294(10):3501-3513. Malik R, Meng H, Wongkongkathep P, Corrales CI, Sepanj N, Atlasi RS, Klärner FG, Schrader T, Spencer MJ, Loo JA, Wiedau M, Bitan G. PMID: 30602569; PMCID: PMC6416427.
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Investigation of Anti-SOD1 Antibodies Yields New Structural Insight into SOD1 Misfolding and Surprising Behavior of the Antibodies Themselves. ACS Chem Biol. 2018 09 21; 13(9):2794-2807. Atlasi RS, Malik R, Corrales CI, Tzeplaeff L, Whitelegge JP, Cashman NR, Bitan G. PMID: 30110532; PMCID: PMC6475120.
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Native Top-Down Mass Spectrometry and Ion Mobility Spectrometry of the Interaction of Tau Protein with a Molecular Tweezer Assembly Modulator. J Am Soc Mass Spectrom. 2019 Jan; 30(1):16-23. Nshanian M, Lantz C, Wongkongkathep P, Schrader T, Klärner FG, Blümke A, Despres C, Ehrmann M, Smet-Nocca C, Bitan G, Loo JA. PMID: 30062477; PMCID: PMC6320309.
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The molecular tweezer CLR01 inhibits Ebola and Zika virus infection. Antiviral Res. 2018 04; 152:26-35. Röcker AE, Müller JA, Dietzel E, Harms M, Krüger F, Heid C, Sowislok A, Riber CF, Kupke A, Lippold S, von Einem J, Beer J, Knöll B, Becker S, Schmidt-Chanasit J, Otto M, Vapalahti O, Zelikin AN, Bitan G, Schrader T, Münch J. PMID: 29428508; PMCID: PMC7113745.
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Using Molecular Tweezers to Remodel Abnormal Protein Self-Assembly and Inhibit the Toxicity of Amyloidogenic Proteins. Methods Mol Biol. 2018; 1777:369-386. Malik R, Di J, Nair G, Attar A, Taylor K, Teng E, Klärner FG, Schrader T, Bitan G. PMID: 29744849; PMCID: PMC6459406.
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Preparation of Pure Populations of Amyloid β-Protein Oligomers of Defined Size. Methods Mol Biol. 2018; 1779:3-12. Hayden EY, Conovaloff JL, Mason A, Bitan G, Teplow DB. PMID: 29886523; PMCID: PMC6490168.
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Recommendations of the Global Multiple System Atrophy Research Roadmap Meeting. Neurology. 2018 01 09; 90(2):74-82. Walsh RR, Krismer F, Galpern WR, Wenning GK, Low PA, Halliday G, Koroshetz WJ, Holton J, Quinn NP, Rascol O, Shaw LM, Eidelberg D, Bower P, Cummings JL, Abler V, Biedenharn J, Bitan G, Brooks DJ, Brundin P, Fernandez H, Fortier P, Freeman R, Gasser T, Hewitt A, Höglinger GU, Huentelman MJ, Jensen PH, Jeromin A, Kang UJ, Kaufmann H, Kellerman L, Khurana V, Klockgether T, Kim WS, Langer C, LeWitt P, Masliah E, Meissner W, Melki R, Ostrowitzki S, Piantadosi S, Poewe W, Robertson D, Roemer C, Schenk D, Schlossmacher M, Schmahmann JD, Seppi K, Shih L, Siderowf A, Stebbins GT, Stefanova N, Tsuji S, Sutton S, Zhang J. PMID: 29237794; PMCID: PMC5772155.
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A Molecular Tweezer Ameliorates Motor Deficits in Mice Overexpressing α-Synuclein. Neurotherapeutics. 2017 Oct; 14(4):1107-1119. Richter F, Subramaniam SR, Magen I, Lee P, Hayes J, Attar A, Zhu C, Franich NR, Bove N, De La Rosa K, Kwong J, Klärner FG, Schrader T, Chesselet MF, Bitan G. PMID: 28585223; PMCID: PMC5722755.
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Inhibition of Mutant αB Crystallin-Induced Protein Aggregation by a Molecular Tweezer. J Am Heart Assoc. 2017 Aug 08; 6(8). Xu N, Bitan G, Schrader T, Klärner FG, Osinska H, Robbins J. PMID: 28862927; PMCID: PMC5586456.
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Inhibition of Huntingtin Exon-1 Aggregation by the Molecular Tweezer CLR01. J Am Chem Soc. 2017 04 26; 139(16):5640-5643. Vöpel T, Bravo-Rodriguez K, Mittal S, Vachharajani S, Gnutt D, Sharma A, Steinhof A, Fatoba O, Ellrichmann G, Nshanian M, Heid C, Loo JA, Klärner FG, Schrader T, Bitan G, Wanker EE, Ebbinghaus S, Sanchez-Garcia E. PMID: 28406616; PMCID: PMC5506490.
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Computational On-Chip Imaging of Nanoparticles and Biomolecules using Ultraviolet Light. Sci Rep. 2017 03 09; 7:44157. Daloglu MU, Ray A, Gorocs Z, Xiong M, Malik R, Bitan G, McLeod E, Ozcan A. PMID: 28276489; PMCID: PMC5343455.
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Preparation of pure populations of covalently stabilized amyloid β-protein oligomers of specific sizes. Anal Biochem. 2017 Feb 01; 518:78-85. Hayden EY, Conovaloff JL, Mason A, Bitan G, Teplow DB. PMID: 27810329; PMCID: PMC5474095.
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Molecular tweezers for lysine and arginine - powerful inhibitors of pathologic protein aggregation. Chem Commun (Camb). 2016 Oct 15; 52(76):11318-34. Schrader T, Bitan G, Klärner FG. PMID: 27546596; PMCID: PMC5026632.
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Modulation of Amyloid β-Protein (Aβ) Assembly by Homologous C-Terminal Fragments as a Strategy for Inhibiting Aβ Toxicity. ACS Chem Neurosci. 2016 07 20; 7(7):845-56. Li H, Rahimi F, Bitan G. PMID: 27322435; PMCID: PMC5450937.
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Neurotoxicity of the Parkinson Disease-Associated Pesticide Ziram Is Synuclein-Dependent in Zebrafish Embryos. Environ Health Perspect. 2016 Nov; 124(11):1766-1775. Lulla A, Barnhill L, Bitan G, Ivanova MI, Nguyen B, O'Donnell K, Stahl MC, Yamashiro C, Klärner FG, Schrader T, Sagasti A, Bronstein JM. PMID: 27301718; PMCID: PMC5089875.
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Reducing synuclein accumulation improves neuronal survival after spinal cord injury. Exp Neurol. 2016 Apr; 278:105-15. Fogerson SM, van Brummen AJ, Busch DJ, Allen SR, Roychaudhuri R, Banks SM, Klärner FG, Schrader T, Bitan G, Morgan JR. PMID: 26854933; PMCID: PMC4788542.
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Role of Species-Specific Primary Structure Differences in Aβ42 Assembly and Neurotoxicity. ACS Chem Neurosci. 2015 Dec 16; 6(12):1941-55. Roychaudhuri R, Zheng X, Lomakin A, Maiti P, Condron MM, Benedek GB, Bitan G, Bowers MT, Teplow DB. PMID: 26421877; PMCID: PMC4844016.
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Mechanism of C-Terminal Fragments of Amyloid β-Protein as Aβ Inhibitors: Do C-Terminal Interactions Play a Key Role in Their Inhibitory Activity? J Phys Chem B. 2016 Mar 03; 120(8):1615-23. Zheng X, Wu C, Liu D, Li H, Bitan G, Shea JE, Bowers MT. PMID: 26439281; PMCID: PMC4777659.
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Toxicity inhibitors protect lipid membranes from disruption by Aβ42. ACS Chem Neurosci. 2015 Nov 18; 6(11):1860-9. Malishev R, Nandi S, Kolusheva S, Levi-Kalisman Y, Klärner FG, Schrader T, Bitan G, Jelinek R. PMID: 26317327.
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A molecular tweezer antagonizes seminal amyloids and HIV infection. Elife. 2015 Aug 18; 4. Lump E, Castellano LM, Meier C, Seeliger J, Erwin N, Sperlich B, Stürzel CM, Usmani S, Hammond RM, von Einem J, Gerold G, Kreppel F, Bravo-Rodriguez K, Pietschmann T, Holmes VM, Palesch D, Zirafi O, Weissman D, Sowislok A, Wettig B, Heid C, Kirchhoff F, Weil T, Klärner FG, Schrader T, Bitan G, Sanchez-Garcia E, Winter R, Shorter J, Münch J. PMID: 26284498; PMCID: PMC4536748.
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The Lys-Specific Molecular Tweezer, CLR01, Modulates Aggregation of the Mutant p53 DNA Binding Domain and Inhibits Its Toxicity. Biochemistry. 2015 Jun 23; 54(24):3729-38. Herzog G, Shmueli MD, Levy L, Engel L, Gazit E, Klärner FG, Schrader T, Bitan G, Segal D. PMID: 26030124.
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Molecular tweezers inhibit islet amyloid polypeptide assembly and toxicity by a new mechanism. ACS Chem Biol. 2015 Jun 19; 10(6):1555-69. Lopes DH, Attar A, Nair G, Hayden EY, Du Z, McDaniel K, Dutt S, Bravo-Rodriguez K, Mittal S, Klärner FG, Wang C, Sanchez-Garcia E, Schrader T, Bitan G. PMID: 25844890.
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Amyloid β-protein assembly: The effect of molecular tweezers CLR01 and CLR03. J Phys Chem B. 2015 Apr 09; 119(14):4831-41. Zheng X, Liu D, Klärner FG, Schrader T, Bitan G, Bowers MT. PMID: 25751170; PMCID: PMC4415044.
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Exact modeling of cylindrical metal-dielectric multilayers beyond the effective medium approximation. Opt Lett. 2014 Nov 15; 39(22):6517-20. Aronovich D, Bitan G, Bartal G. PMID: 25490508.
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Safety and pharmacological characterization of the molecular tweezer CLR01 - a broad-spectrum inhibitor of amyloid proteins' toxicity. BMC Pharmacol Toxicol. 2014 Apr 16; 15:23. Attar A, Chan WT, Klärner FG, Schrader T, Bitan G. PMID: 24735982; PMCID: PMC3996151.
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Molecular tweezers targeting transthyretin amyloidosis. Neurotherapeutics. 2014 Apr; 11(2):450-61. Ferreira N, Pereira-Henriques A, Attar A, Klärner FG, Schrader T, Bitan G, Gales L, Saraiva MJ, Almeida MR. PMID: 24459092; PMCID: PMC3996111.
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Molecular basis for preventing α-synuclein aggregation by a molecular tweezer. J Biol Chem. 2014 Apr 11; 289(15):10727-10737. Acharya S, Safaie BM, Wongkongkathep P, Ivanova MI, Attar A, Klärner FG, Schrader T, Loo JA, Bitan G, Lapidus LJ. PMID: 24567327; PMCID: PMC4036189.
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Disrupting self-assembly and toxicity of amyloidogenic protein oligomers by "molecular tweezers" - from the test tube to animal models. Curr Pharm Des. 2014; 20(15):2469-83. Attar A, Bitan G. PMID: 23859557; PMCID: PMC4261945.
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A shortened Barnes maze protocol reveals memory deficits at 4-months of age in the triple-transgenic mouse model of Alzheimer's disease. PLoS One. 2013; 8(11):e80355. Attar A, Liu T, Chan WT, Hayes J, Nejad M, Lei K, Bitan G. PMID: 24236177; PMCID: PMC3827415.
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Tranilast binds to aβ monomers and promotes aβ fibrillation. Biochemistry. 2013 Jun 11; 52(23):3995-4002. Connors CR, Rosenman DJ, Lopes DH, Mittal S, Bitan G, Sorci M, Belfort G, Garcia A, Wang C. PMID: 23679559; PMCID: PMC4082028.
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Protection of primary neurons and mouse brain from Alzheimer's pathology by molecular tweezers. Brain. 2012 Dec; 135(Pt 12):3735-48. Attar A, Ripoli C, Riccardi E, Maiti P, Li Puma DD, Liu T, Hayes J, Jones MR, Lichti-Kaiser K, Yang F, Gale GD, Tseng CH, Tan M, Xie CW, Straudinger JL, Klärner FG, Schrader T, Frautschy SA, Grassi C, Bitan G. PMID: 23183235; PMCID: PMC3525056.
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Effects of different amyloid β-protein analogues on synaptic function. Neurobiol Aging. 2013 Apr; 34(4):1032-44. Ripoli C, Piacentini R, Riccardi E, Leone L, Li Puma DD, Bitan G, Grassi C. PMID: 23046860.
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Plasma methionine sulfoxide in persons with familial Alzheimer's disease mutations. Dement Geriatr Cogn Disord. 2012; 33(4):219-25. Ringman JM, Fithian AT, Gylys K, Cummings JL, Coppola G, Elashoff D, Pratico D, Moskovitz J, Bitan G. PMID: 22584618; PMCID: PMC3568669.
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Zn2+-Aβ40 complexes form metastable quasi-spherical oligomers that are cytotoxic to cultured hippocampal neurons. J Biol Chem. 2012 Jun 08; 287(24):20555-64. Solomonov I, Korkotian E, Born B, Feldman Y, Bitler A, Rahimi F, Li H, Bitan G, Sagi I. PMID: 22528492; PMCID: PMC3370240.
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A novel "molecular tweezer" inhibitor of α-synuclein neurotoxicity in vitro and in vivo. Neurotherapeutics. 2012 Apr; 9(2):464-76. Prabhudesai S, Sinha S, Attar A, Kotagiri A, Fitzmaurice AG, Lakshmanan R, Lakshmanan R, Ivanova MI, Loo JA, Klärner FG, Schrader T, Stahl M, Bitan G, Bronstein JM. PMID: 22373667; PMCID: PMC3337029.
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A key role for lysine residues in amyloid β-protein folding, assembly, and toxicity. ACS Chem Neurosci. 2012 Jun 20; 3(6):473-81. Sinha S, Lopes DH, Bitan G. PMID: 22860216; PMCID: PMC3382451.
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Design of β-amyloid aggregation inhibitors from a predicted structural motif. J Med Chem. 2012 Apr 12; 55(7):3002-10. Novick PA, Lopes DH, Branson KM, Esteras-Chopo A, Graef IA, Bitan G, Pande VS. PMID: 22420626; PMCID: PMC3766731.
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Comparison of three amyloid assembly inhibitors: the sugar scyllo-inositol, the polyphenol epigallocatechin gallate, and the molecular tweezer CLR01. ACS Chem Neurosci. 2012 Jun 20; 3(6):451-8. Sinha S, Du Z, Maiti P, Klärner FG, Schrader T, Wang C, Bitan G. PMID: 22860214; PMCID: PMC3386858.
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Modulating self-assembly of amyloidogenic proteins as a therapeutic approach for neurodegenerative diseases: strategies and mechanisms. ChemMedChem. 2012 Mar 05; 7(3):359-74. Liu T, Bitan G. PMID: 22323134.
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A two-step strategy for structure-activity relationship studies of N-methylated aβ42 C-terminal fragments as aβ42 toxicity inhibitors. ChemMedChem. 2012 Mar 05; 7(3):515-22. Li H, Zemel R, Lopes DH, Monien BH, Bitan G. PMID: 22307963; PMCID: PMC3517043.
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Application of photochemical cross-linking to the study of oligomerization of amyloidogenic proteins. Methods Mol Biol. 2012; 849:11-21. Lopes DH, Sinha S, Rosensweig C, Bitan G. PMID: 22528080.
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Preparation of stable amyloid β-protein oligomers of defined assembly order. Methods Mol Biol. 2012; 849:23-31. Rosensweig C, Ono K, Murakami K, Lowenstein DK, Bitan G, Teplow DB. PMID: 22528081; PMCID: PMC5767166.
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Aβ(39-42) modulates Aβ oligomerization but not fibril formation. Biochemistry. 2012 Jan 10; 51(1):108-17. Gessel MM, Wu C, Li H, Bitan G, Shea JE, Bowers MT. PMID: 22129303; PMCID: PMC3271797.
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C-terminal tetrapeptides inhibit Aβ42-induced neurotoxicity primarily through specific interaction at the N-terminus of Aβ42. J Med Chem. 2011 Dec 22; 54(24):8451-60. Li H, Du Z, Lopes DH, Fradinger EA, Wang C, Bitan G. PMID: 22087474; PMCID: PMC3240737.
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Induction of methionine-sulfoxide reductases protects neurons from amyloid β-protein insults in vitro and in vivo. Biochemistry. 2011 Dec 13; 50(49):10687-97. Moskovitz J, Maiti P, Lopes DH, Oien DB, Attar A, Liu T, Mittal S, Hayes J, Bitan G. PMID: 22059533; PMCID: PMC3235361.
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Lysine-specific molecular tweezers are broad-spectrum inhibitors of assembly and toxicity of amyloid proteins. J Am Chem Soc. 2011 Oct 26; 133(42):16958-69. Sinha S, Lopes DH, Du Z, Pang ES, Shanmugam A, Lomakin A, Talbiersky P, Tennstaedt A, McDaniel K, Bakshi R, Kuo PY, Ehrmann M, Benedek GB, Loo JA, Klärner FG, Schrader T, Wang C, Bitan G. PMID: 21916458; PMCID: PMC3210512.
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Structural basis for Aβ1–42 toxicity inhibition by Aβ C-terminal fragments: discrete molecular dynamics study. J Mol Biol. 2011 Jul 08; 410(2):316-28. Urbanc B, Betnel M, Cruz L, Li H, Fradinger EA, Monien BH, Bitan G. PMID: 21621545; PMCID: PMC3124842.
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Rational design of β-sheet ligands against Aβ42-induced toxicity. J Am Chem Soc. 2011 Mar 30; 133(12):4348-58. Hochdörffer K, März-Berberich J, Nagel-Steger L, Epple M, Meyer-Zaika W, Horn AH, Sticht H, Sinha S, Bitan G, Schrader T. PMID: 21381732.
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Surprising toxicity and assembly behaviour of amyloid β-protein oxidized to sulfone. Biochem J. 2011 Jan 15; 433(2):323-32. Maiti P, Piacentini R, Ripoli C, Grassi C, Bitan G. PMID: 21044048; PMCID: PMC5767168.
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Mechanistic investigation of the inhibition of Abeta42 assembly and neurotoxicity by Abeta42 C-terminal fragments. Biochemistry. 2010 Aug 03; 49(30):6358-64. Li H, Monien BH, Lomakin A, Zemel R, Fradinger EA, Tan M, Spring SM, Urbanc B, Xie CW, Benedek GB, Bitan G. PMID: 20568734; PMCID: PMC2912417.
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Selection of aptamers for amyloid beta-protein, the causative agent of Alzheimer's disease. J Vis Exp. 2010 May 13; (39). Rahimi F, Bitan G. PMID: 20616783; PMCID: PMC2918391.
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Elucidation of amyloid beta-protein oligomerization mechanisms: discrete molecular dynamics study. J Am Chem Soc. 2010 Mar 31; 132(12):4266-80. Urbanc B, Betnel M, Cruz L, Bitan G, Teplow DB. PMID: 20218566; PMCID: PMC5767167.
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Despite its role in assembly, methionine 35 is not necessary for amyloid beta-protein toxicity. J Neurochem. 2010 Jun; 113(5):1252-62. Maiti P, Lomakin A, Benedek GB, Bitan G. PMID: 20345758; PMCID: PMC2908238.
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Biophysical characterization of Abeta42 C-terminal fragments: inhibitors of Abeta42 neurotoxicity. Biochemistry. 2010 Feb 16; 49(6):1259-67. Li H, Monien BH, Fradinger EA, Urbanc B, Bitan G. PMID: 20050679; PMCID: PMC2831638.
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RNA aptamers generated against oligomeric Abeta40 recognize common amyloid aptatopes with low specificity but high sensitivity. PLoS One. 2009 Nov 10; 4(11):e7694. Rahimi F, Murakami K, Summers JL, Chen CH, Bitan G. PMID: 19901993; PMCID: PMC2770325.
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Amyloid-β protein oligomerization and the importance of tetramers and dodecamers in the aetiology of Alzheimer's disease. Nat Chem. 2009 Jul; 1(4):326-31. Bernstein SL, Dupuis NF, Lazo ND, Wyttenbach T, Condron MM, Bitan G, Teplow DB, Shea JE, Ruotolo BT, Robinson CV, Bowers MT. PMID: 20703363; PMCID: PMC2918915.
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Amino acid position-specific contributions to amyloid beta-protein oligomerization. J Biol Chem. 2009 Aug 28; 284(35):23580-91. Maji SK, Ogorzalek Loo RR, Inayathullah M, Spring SM, Vollers SS, Condron MM, Bitan G, Loo JA, Teplow DB. PMID: 19567875; PMCID: PMC2749133.
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The structure of Abeta42 C-terminal fragments probed by a combined experimental and theoretical study. J Mol Biol. 2009 Mar 27; 387(2):492-501. Wu C, Murray MM, Bernstein SL, Condron MM, Bitan G, Shea JE, Bowers MT. PMID: 19356595; PMCID: PMC2712569.
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Photo-induced cross-linking of unmodified proteins (PICUP) applied to amyloidogenic peptides. J Vis Exp. 2009 Jan 12; (23). Rahimi F, Maiti P, Bitan G. PMID: 19229175; PMCID: PMC2763294.
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C-terminal peptides coassemble into Abeta42 oligomers and protect neurons against Abeta42-induced neurotoxicity. Proc Natl Acad Sci U S A. 2008 Sep 16; 105(37):14175-80. Fradinger EA, Monien BH, Urbanc B, Lomakin A, Tan M, Li H, Spring SM, Condron MM, Cruz L, Xie CW, Benedek GB, Bitan G. PMID: 18779585; PMCID: PMC2544597.
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Structure-function relationships of pre-fibrillar protein assemblies in Alzheimer's disease and related disorders. Curr Alzheimer Res. 2008 Jun; 5(3):319-41. Rahimi F, Shanmugam A, Bitan G. PMID: 18537546; PMCID: PMC2835858.
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Synthesis and Purification of Highly Hydrophobic Peptides Derived from the C-Terminus of Amyloid β-Protein. Open Biotechnol J. 2008 Jan 01; 2(1):87-93. Condron MM, Monien BH, Bitan G. PMID: 19898686; PMCID: PMC2773559.
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Role of electrostatic interactions in amyloid beta-protein (A beta) oligomer formation: a discrete molecular dynamics study. Biophys J. 2007 Jun 01; 92(11):4064-77. Yun S, Urbanc B, Cruz L, Bitan G, Teplow DB, Stanley HE. PMID: 17307823; PMCID: PMC1868995.
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Early diagnostics and therapeutics for Alzheimer's disease--how early can we get there? Expert Rev Neurother. 2006 Sep; 6(9):1293-306. Monien BH, Apostolova LG, Bitan G. PMID: 17009917; PMCID: PMC2715564.
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Elucidating amyloid beta-protein folding and assembly: A multidisciplinary approach. Acc Chem Res. 2006 Sep; 39(9):635-45. Teplow DB, Lazo ND, Bitan G, Bernstein S, Wyttenbach T, Bowers MT, Baumketner A, Shea JE, Urbanc B, Cruz L, Borreguero J, Stanley HE. PMID: 16981680.
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Dendrimeric Abeta1-15 is an effective immunogen in wildtype and APP-tg mice. Neurobiol Aging. 2007 Jun; 28(6):813-23. Seabrook TJ, Thomas K, Jiang L, Bloom J, Spooner E, Maier M, Bitan G, Lemere CA. PMID: 16725229.
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Amyloid beta-protein monomer structure: a computational and experimental study. Protein Sci. 2006 Mar; 15(3):420-8. Baumketner A, Bernstein SL, Wyttenbach T, Bitan G, Teplow DB, Bowers MT, Shea JE. PMID: 16501222; PMCID: PMC2249763.
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Structural study of metastable amyloidogenic protein oligomers by photo-induced cross-linking of unmodified proteins. Methods Enzymol. 2006; 413:217-36. Bitan G. PMID: 17046399; PMCID: PMC2782599.
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En route to early diagnosis of Alzheimer's disease--are we there yet? Trends Biotechnol. 2005 Nov; 23(11):531-3. Fradinger EA, Bitan G. PMID: 16165236.
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Neurotoxic protein oligomers--what you see is not always what you get. Amyloid. 2005 Jun; 12(2):88-95. Bitan G, Fradinger EA, Spring SM, Teplow DB. PMID: 16011984.
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Amyloid beta-protein: monomer structure and early aggregation states of Abeta42 and its Pro19 alloform. J Am Chem Soc. 2005 Feb 23; 127(7):2075-84. Bernstein SL, Wyttenbach T, Baumketner A, Shea JE, Bitan G, Teplow DB, Bowers MT. PMID: 15713083.
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Determination of Peptide oligomerization state using rapid photochemical crosslinking. Methods Mol Biol. 2005; 299:11-8. Vollers SS, Teplow DB, Bitan G. PMID: 15980592.
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Preparation of aggregate-free, low molecular weight amyloid-beta for assembly and toxicity assays. Methods Mol Biol. 2005; 299:3-9. Bitan G, Teplow DB. PMID: 15980591.
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In silico study of amyloid beta-protein folding and oligomerization. Proc Natl Acad Sci U S A. 2004 Dec 14; 101(50):17345-50. Urbanc B, Cruz L, Yun S, Buldyrev SV, Bitan G, Teplow DB, Stanley HE. PMID: 15583128; PMCID: PMC536046.
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Rapid photochemical cross-linking--a new tool for studies of metastable, amyloidogenic protein assemblies. Acc Chem Res. 2004 Jun; 37(6):357-64. Bitan G, Teplow DB. PMID: 15196045.
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A molecular switch in amyloid assembly: Met35 and amyloid beta-protein oligomerization. J Am Chem Soc. 2003 Dec 17; 125(50):15359-65. Bitan G, Tarus B, Vollers SS, Lashuel HA, Condron MM, Straub JE, Teplow DB. PMID: 14664580.
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Increased T cell reactivity to amyloid beta protein in older humans and patients with Alzheimer disease. J Clin Invest. 2003 Aug; 112(3):415-22. Monsonego A, Zota V, Karni A, Krieger JI, Bar-Or A, Bitan G, Budson AE, Sperling R, Selkoe DJ, Weiner HL. PMID: 12897209; PMCID: PMC166296.
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Elucidation of primary structure elements controlling early amyloid beta-protein oligomerization. J Biol Chem. 2003 Sep 12; 278(37):34882-9. Bitan G, Vollers SS, Teplow DB. PMID: 12840029.
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Amyloid beta -protein (Abeta) assembly: Abeta 40 and Abeta 42 oligomerize through distinct pathways. Proc Natl Acad Sci U S A. 2003 Jan 07; 100(1):330-5. Bitan G, Kirkitadze MD, Lomakin A, Vollers SS, Benedek GB, Teplow DB. PMID: 12506200; PMCID: PMC140968.
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Polyglutamine repeat length-dependent proteolysis of huntingtin. Neurobiol Dis. 2002 Oct; 11(1):111-22. Sun B, Fan W, Balciunas A, Cooper JK, Bitan G, Steavenson S, Denis PE, Young Y, Adler B, Daugherty L, Manoukian R, Elliott G, Shen W, Talvenheimo J, Teplow DB, Haniu M, Haldankar R, Wypych J, Ross CA, Citron M, Richards WG. PMID: 12460551.
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Paradigm shifts in Alzheimer's disease and other neurodegenerative disorders: the emerging role of oligomeric assemblies. J Neurosci Res. 2002 Sep 01; 69(5):567-77. Kirkitadze MD, Bitan G, Teplow DB. PMID: 12210822.
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Identification of a contact domain between echistatin and the integrin alpha(v)beta(3) by photoaffinity cross-linking. Biochemistry. 2001 Dec 18; 40(50):15117-26. Scheibler L, Mierke DF, Bitan G, Rosenblatt M, Chorev M. PMID: 11735394.
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Amyloid beta-protein oligomerization: prenucleation interactions revealed by photo-induced cross-linking of unmodified proteins. J Biol Chem. 2001 Sep 14; 276(37):35176-84. Bitan G, Lomakin A, Teplow DB. PMID: 11441003.
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The relationship between homology length and crossing over during the repair of a broken chromosome. J Biol Chem. 2000 Oct 06; 275(40):30833-8. Inbar O, Liefshitz B, Bitan G, Kupiec M. PMID: 10924495.
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Ligand-integrin alpha v beta 3 interaction determined by photoaffinity cross-linking: a challenge to the prevailing model. Biochemistry. 2000 Sep 12; 39(36):11014-23. Bitan G, Scheibler L, Mierke DF, Rosenblatt M, Chorev M. PMID: 10998238.
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Design and evaluation of benzophenone-containing conformationally constrained ligands as tools for photoaffinity scanning of the integrin alphaVbeta3-ligand bimolecular interaction. J Pept Res. 2000 Mar; 55(3):181-94. Bitan G, Scheibler L, Teng H, Rosenblatt M, Chorev M. PMID: 10727100.
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Photoaffinity cross-linking identifies differences in the interactions of an agonist and an antagonist with the parathyroid hormone/parathyroid hormone-related protein receptor. J Biol Chem. 2000 Jan 07; 275(1):9-17. Behar V, Bisello A, Bitan G, Rosenblatt M, Chorev M. PMID: 10617579.
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Mapping the integrin alpha V beta 3-ligand interface by photoaffinity cross-linking. Biochemistry. 1999 Mar 16; 38(11):3414-20. Bitan G, Scheibler L, Greenberg Z, Rosenblatt M, Chorev M. PMID: 10079087.
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Synthesis and biological activity of novel backbone-bicyclic substance-P analogs containing lactam and disulfide bridges. J Pept Res. 1997 May; 49(5):421-6. Bitan G, Sukhotinsky I, Mashriki Y, Hanani M, Selinger Z, Gilon C. PMID: 9211223.
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Building Units for N-Backbone Cyclic Peptides. 3. Synthesis of Protected N(alpha)-(omega-Aminoalkyl)amino Acids and N(alpha)-(omega-Carboxyalkyl)amino Acids. J Org Chem. 1997 Jan 24; 62(2):411-416. Muller D, Zeltser I, Bitan G, Gilon C. PMID: 11671417.
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Structure-activity relationship of the ring portion in backbone-cyclic C-terminal hexapeptide analogs of substance P. NMR and molecular dynamics. Int J Pept Protein Res. 1996 Dec; 48(6):569-79. Behrens S, Mathä B, Bitan G, Gilon C, Kessler H. PMID: 8985790.
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Synthesis and biological activity of NK-1 selective, N-backbone cyclic analogs of the C-terminal hexapeptide of substance P. J Med Chem. 1996 Aug 02; 39(16):3174-8. Byk G, Halle D, Zeltser I, Bitan G, Selinger Z, Gilon C. PMID: 8759639.
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Backbone cyclization of the C-terminal part of substance P. Part 1: The important role of the sulphur in position 11. J Pept Sci. 1996 Jul-Aug; 2(4):261-9. Bitan G, Zeltser I, Byk G, Halle D, Mashriki Y, Gluhov EV, Sukhotinsky I, Hanani M, Selinger Z, Gilon C. PMID: 9231334.
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