Carlo Ballatore

Title(s)Professor, School of Pharmacy and Pharmaceutical Science
SchoolVc-health Sciences-schools
Address9500 Gilman Drive #
La Jolla CA 92093
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    Collapse Overview 
    Collapse Overview
    Over the past several years my laboratory has been engaged in NIH-funded multidisciplinary drug/probe discovery programs by providing expertise in medicinal chemistry and drug design. Such collaborations include programs directed towards the discovery and development of candidate treatments for: (a) neurodegenerative tauopathies (e.g., Alzheimer’s disease), in collaboration with the Center for Neurodegenerative Diseases Research at University of Pennsylvania; and (b) parasitic infections, such as trypanosomiasis and schistosomiasis, in collaboration with the Center for Discovery and Innovation in Parasitic Diseases at UCSD. In addition, my laboratory has also been actively involved in the investigation of basic, fundamental principles in medicinal chemistry, such as in the area of isosteric replacements.
    I have successfully completed facilitator-led training for effective mentoring delivered by the Center for Improvement of Mentored Experiences in Research (CIMER)-trained instructors and developed a mentoring philosophy for mentoring certification. I am available to serve as a career or research mentor for early career faculty, postdoctoral scholars, and graduate students. The Health Sciences campus-wide Faculty Mentor Training Program (FMTP) initiative is sponsored by the Health Sciences Office of Faculty Affairs (OFA) with support from the Chancellor’s Office, VC-EDI and VCHS.

    Collapse Research 
    Collapse Research Activities and Funding
    Development of thiophen-2-yl-phenylpyrimidines for treatment of schistosomiasis
    NIH R21AI156554Sep 23, 2021 - Aug 31, 2023
    Role: Co-Principal Investigator
    Optimization of microtubule-stabilizing triazolopyrimidines as therapeutics for Alzheimer's disease and related tauopathies
    NIH U01AG061173Mar 1, 2019 - Feb 28, 2023
    Role: Co-Principal Investigator
    Brain Penetrant Microtubule-Stabilizers to Treat CNS-invasive Parasitic Diseases
    NIH R21AI141210Feb 1, 2019 - Jan 31, 2021
    Role: Principal Investigator
    Brain Penetrant Microtubule-Stabilizers to treat CNS-invasive parasitic diseases
    NIH R21AI133394Jun 1, 2018 - May 31, 2021
    Role: Co-Principal Investigator
    Orally-absorbed, small molecule microtubule-stabilizers for tauopathy treatment
    NIH R01AG044332Jun 15, 2013 - Nov 30, 2018
    Role: Co-Principal Investigator

    Collapse Bibliographic 
    Collapse Publications
    Publications listed below are automatically derived from MEDLINE/PubMed and other sources, which might result in incorrect or missing publications. Researchers can login to make corrections and additions, or contact us for help. to make corrections and additions.
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    Altmetrics Details PMC Citations indicate the number of times the publication was cited by articles in PubMed Central, and the Altmetric score represents citations in news articles and social media. (Note that publications are often cited in additional ways that are not shown here.) Fields are based on how the National Library of Medicine (NLM) classifies the publication's journal and might not represent the specific topic of the publication. Translation tags are based on the publication type and the MeSH terms NLM assigns to the publication. Some publications (especially newer ones and publications not in PubMed) might not yet be assigned Field or Translation tags.) Click a Field or Translation tag to filter the publications.
    1. A small-molecule microtubule-stabilizing agent safely reduces Aß plaque and tau pathology in transgenic mouse models of Alzheimer's disease. Alzheimers Dement. 2024 Jun 17. Yao Y, Muench M, Alle T, Zhang B, Lucero B, Perez-Tremble R, McGrosso D, Newman M, Gonzalez DJ, Lee VM, Ballatore C, Brunden KR. PMID: 38884283.
      View in: PubMed   Mentions:
    2. High-throughput Virtual Screening- and Molecular Docking-based Prediction for Acetylcholinesterase Inhibitors and Exploring its Mechanisms against Alzheimer’s Disease based on Network Pharmacology. Biomedical Sciences and Clinical Medicine. 2024; 63(3). Takomthong P, Waiwut P, Ballatore C, Choowongkomon K, Arsito PN, Chulikhit Y, Boonyarat C. View Publication.
    3. AI is a viable alternative to high throughput screening: a 318-target study. Sci Rep. 2024 04 02; 14(1):7526. Atomwise AIMS Program. PMID: 38565852; PMCID: PMC10987645.
      View in: PubMed   Mentions:    Fields:    
    4. Design, Synthesis, and Evaluation of An Anti-trypanosomal [1,2,4]Triazolo[1,5-a]pyrimidine Probe for Photoaffinity Labeling Studies. ChemMedChem. 2024 Jan 26; e202300656. Lucero B, Francisco KR, Varricchio C, Liu LJ, Yao Y, Brancale A, Brunden KR, Caffrey CR, Ballatore C. PMID: 38277231.
      View in: PubMed   Mentions:    Fields:    
    5. Targeted Reversible Covalent Modification of a Noncatalytic Lysine of the Krev Interaction Trapped 1 Protein Enables Site-Directed Screening for Protein-Protein Interaction Inhibitors. ACS Pharmacol Transl Sci. 2023 Nov 10; 6(11):1651-1658. Francisco KR, Bruystens J, Varricchio C, McCurdy S, Wu J, Lopez-Ramirez MA, Ginsberg M, Caffrey CR, Brancale A, Gingras AR, Hixon MS, Ballatore C. PMID: 37974623; PMCID: PMC10644391.
      View in: PubMed   Mentions:
    6. A microtubule stabilizer ameliorates protein pathogenesis and neurodegeneration in mouse models of repetitive traumatic brain injury. Sci Transl Med. 2023 09 13; 15(713):eabo6889. Zhao X, Zeng W, Xu H, Sun Z, Hu Y, Peng B, McBride JD, Duan J, Deng J, Zhang B, Kim SJ, Zoll B, Saito T, Sasaguri H, Saido TC, Ballatore C, Yao H, Wang Z, Trojanowski JQ, Brunden KR, Lee VM, He Z. PMID: 37703352; PMCID: PMC10787216.
      View in: PubMed   Mentions:    Fields:    Translation:AnimalsCells
    7. Structure-Activity Relationships, Tolerability and Efficacy of Microtubule-Active 1,2,4-Triazolo[1,5-a]pyrimidines as Potential Candidates to Treat Human African Trypanosomiasis. ChemMedChem. 2023 10 17; 18(20):e202300193. Monti L, Liu LJ, Varricchio C, Lucero B, Alle T, Yang W, Bem-Shalom I, Gilson M, Brunden KR, Brancale A, Caffrey CR, Ballatore C. PMID: 37429821; PMCID: PMC10615688.
      View in: PubMed   Mentions:    Fields:    Translation:HumansAnimalsCells
    8. Structure-property relationships of fluorinated carboxylic acid bioisosteres. Bioorg Med Chem Lett. 2023 07 15; 91:129363. Alle T, Joyasawal S, Oukoloff K, Long K, Owyang Z, Francisco KR, Cahard D, Huryn DM, Ballatore C. PMID: 37295616; PMCID: PMC11003450.
      View in: PubMed   Mentions: 1     Fields:    
    9. Protein-protein interactions: developing small-molecule inhibitors/stabilizers through covalent strategies. Trends Pharmacol Sci. 2023 07; 44(7):474-488. Lucero B, Francisco KR, Liu LJ, Caffrey CR, Ballatore C. PMID: 37263826; PMCID: PMC11003449.
      View in: PubMed   Mentions: 4     Fields:    Translation:HumansCells
    10. Hydrogen Bonding Parameters by Rapid Colorimetric Assessment: Evaluation of Structural Components Found in Biological Ligands and Organocatalysts. Chemistry. 2023 Jul 14; 29(40):e202300696. Roenfanz HF, Paniak TJ, Berlin CB, Tran V, Francisco KR, Lassalas P, Devas A, Landes O, Rosenberger A, Rotella ME, Ballatore C, Kozlowski MC. PMID: 36917701; PMCID: PMC10363249.
      View in: PubMed   Mentions: 1     Fields:    Translation:Cells
    11. Microtubule-Stabilizing 1,2,4-Triazolo[1,5-a]pyrimidines as Candidate Therapeutics for Neurodegenerative Disease: Matched Molecular Pair Analyses and Computational Studies Reveal New Structure-Activity Insights. J Med Chem. 2023 01 12; 66(1):435-459. Alle T, Varricchio C, Yao Y, Lucero B, Nzou G, Demuro S, Muench M, Vuong KD, Oukoloff K, Cornec AS, Francisco KR, Caffrey CR, Lee VM, Smith AB, Brancale A, Brunden KR, Ballatore C. PMID: 36534051; PMCID: PMC9841533.
      View in: PubMed   Mentions: 4     Fields:    Translation:HumansCells
    12. Identification of SARS-CoV-2 inhibitors targeting Mpro and PLpro using in-cell-protease assay. Commun Biol. 2022 02 25; 5(1):169. Narayanan A, Narwal M, Majowicz SA, Varricchio C, Toner SA, Ballatore C, Brancale A, Murakami KS, Jose J. PMID: 35217718; PMCID: PMC8881501.
      View in: PubMed   Mentions: 53  Translation:HumansCells
    13. Thietanes and Derivatives thereof in Medicinal Chemistry. Curr Top Med Chem. 2022; 22(15):1219-1234. Francisco KR, Ballatore C. PMID: 35546768.
      View in: PubMed   Mentions:    Fields:    
    14. New Heights for ProTides? J Med Chem. 2021 11 25; 64(22):16422-16424. Ballatore C. PMID: 34783565.
      View in: PubMed   Mentions: 1     Fields:    
    15. Corrigendum to "structure property relationships of N-Acylsulfonamides and related bioisosteres" European journal of medicinal chemistry, 218 (2021), 113399. Eur J Med Chem. 2021 Dec 15; 226:113894. Francisco KR, Varricchio C, Paniak TJ, Kozlowski MC, Brancale A, Ballatore C. PMID: 34678530.
      View in: PubMed   Mentions:    Fields:    
    16. Evaluation of log P, pKa, and log D predictions from the SAMPL7 blind challenge. J Comput Aided Mol Des. 2021 07; 35(7):771-802. Bergazin TD, Tielker N, Zhang Y, Mao J, Gunner MR, Francisco K, Ballatore C, Kast SM, Mobley DL. PMID: 34169394; PMCID: PMC8224998.
      View in: PubMed   Mentions: 16     Fields:    Translation:Humans
    17. Burger’s Medicinal Chemistry and Drug Discovery. Drug Discovery and Development for Kinetoplastid Diseases. 2021. Caffrey CR, Steverding D, Ferreira RS, de Oliveira RB, O’Donoghue AJ, Monti L, Ballatore C, Bachovchin KA, Ferrins L, Pollastri MP, Zorn KM, Foil DH, Clark AM, Mottin M, Andrade CH, de Siqueira-Neto JL, Ekins S. View Publication.
    18. Structure property relationships of N-acylsulfonamides and related bioisosteres. Eur J Med Chem. 2021 Jun 05; 218:113399. Francisco KR, Varricchio C, Paniak TJ, Kozlowski MC, Brancale A, Ballatore C. PMID: 33823393; PMCID: PMC8105289.
      View in: PubMed   Mentions: 11     Fields:    Translation:Cells
    19. The Prolyl-tRNA Synthetase Inhibitor Halofuginone Inhibits SARS-CoV-2 Infection. bioRxiv. 2021 Mar 26. Sandoval DR, Clausen TM, Nora C, Cribbs AP, Denardo A, Clark AE, Garretson AF, Coker JKC, Narayanan A, Majowicz SA, Philpott M, Johansson C, Dunford JE, Spliid CB, Golden GJ, Payne NC, Tye MA, Nowell CJ, Griffis ER, Piermatteo A, Grunddal KV, Alle T, Magida JA, Hauser BM, Feldman J, Caradonna TM, Pu Y, Yin X, McVicar RN, Kwong EM, Weiss RJ, Downes M, Tsimikas S, Smidt AG, Ballatore C, Zengler K, Evans RM, Chanda SK, Croker BA, Leibel SL, Jose J, Mazitschek R, Oppermann U, Esko JD, Carlin AF, Gordts PLSM. PMID: 33791697; PMCID: PMC8010724.
      View in: PubMed   Mentions: 2  
    20. Inhibition of the HEG1-KRIT1 interaction increases KLF4 and KLF2 expression in endothelial cells. FASEB Bioadv. 2021 May; 3(5):334-355. Lopez-Ramirez MA, McCurdy S, Li W, Haynes MK, Hale P, Francisco K, Oukoloff K, Bautista M, Choi CHJ, Sun H, Gongol B, Shyy JY, Ballatore C, Sklar LA, Gingras AR. PMID: 33977234; PMCID: PMC8103725.
      View in: PubMed   Mentions: 3  
    21. Evaluation of the Structure-Activity Relationship of Microtubule-Targeting 1,2,4-Triazolo[1,5-a]pyrimidines Identifies New Candidates for Neurodegenerative Tauopathies. J Med Chem. 2021 01 28; 64(2):1073-1102. Oukoloff K, Nzou G, Varricchio C, Lucero B, Alle T, Kovalevich J, Monti L, Cornec AS, Yao Y, James MJ, Trojanowski JQ, Lee VM, Smith AB, Brancale A, Brunden KR, Ballatore C. PMID: 33411523; PMCID: PMC8569887.
      View in: PubMed   Mentions: 10     Fields:    Translation:HumansAnimalsCells
    22. Congeners Derived from Microtubule-Active Phenylpyrimidines Produce a Potent and Long-Lasting Paralysis of Schistosoma mansoni In Vitro. ACS Infect Dis. 2021 05 14; 7(5):1089-1103. Monti L, Cornec AS, Oukoloff K, Kovalevich J, Prijs K, Alle T, Brunden KR, Smith AB, El-Sakkary N, Liu LJ, Syed A, Skinner DE, Ballatore C, Caffrey CR. PMID: 33135408; PMCID: PMC8641298.
      View in: PubMed   Mentions: 5     Fields:    Translation:HumansAnimalsCells
    23. Correction of microtubule defects within Aβ plaque-associated dystrophic axons results in lowered Aβ release and plaque deposition. Alzheimers Dement. 2020 10; 16(10):1345-1357. Yao Y, Nzou G, Alle T, Tsering W, Maimaiti S, Trojanowski JQ, Lee VM, Ballatore C, Brunden KR. PMID: 32918367; PMCID: PMC7652013.
      View in: PubMed   Mentions: 7     Fields:    Translation:HumansAnimalsCells
    24. Rational design, synthesis, and evaluation of uncharged, "smart" bis-oxime antidotes of organophosphate-inhibited human acetylcholinesterase. J Biol Chem. 2020 03 27; 295(13):4079-4092. Gorecki L, Gerlits O, Kong X, Cheng X, Blumenthal DK, Taylor P, Ballatore C, Kovalevsky A, Radic Z. PMID: 32019865; PMCID: PMC7105318.
      View in: PubMed   Mentions: 7     Fields:    Translation:HumansCells
    25. Discovery of New Inhibitors of Hepatitis C Virus NS3/4A Protease and Its D168A Mutant. ACS Omega. 2019 Oct 15; 4(16):16999-17008. Meewan I, Zhang X, Roy S, Ballatore C, O'Donoghue AJ, Schooley RT, Abagyan R. PMID: 31646247; PMCID: PMC6796237.
      View in: PubMed   Mentions: 9  
    26. 1,2,4-Triazolo[1,5-a]pyrimidines in drug design. Eur J Med Chem. 2019 Mar 01; 165:332-346. Oukoloff K, Lucero B, Francisco KR, Brunden KR, Ballatore C. PMID: 30703745; PMCID: PMC6394845.
      View in: PubMed   Mentions: 12     Fields:    Translation:HumansAnimals
    27. A brain-penetrant triazolopyrimidine enhances microtubule-stability, reduces axonal dysfunction and decreases tau pathology in a mouse tauopathy model. Mol Neurodegener. 2018 11 07; 13(1):59. Zhang B, Yao Y, Cornec AS, Oukoloff K, James MJ, Koivula P, Trojanowski JQ, Smith AB, Lee VM, Ballatore C, Brunden KR. PMID: 30404654; PMCID: PMC6223064.
      View in: PubMed   Mentions: 15     Fields:    Translation:HumansAnimalsCells
    28. Brain-Penetrant Triazolopyrimidine and Phenylpyrimidine Microtubule Stabilizers as Potential Leads to Treat Human African Trypanosomiasis. ChemMedChem. 2018 09 06; 13(17):1751-1754. Monti L, Wang SC, Oukoloff K, Smith AB, Brunden KR, Caffrey CR, Ballatore C. PMID: 29969537; PMCID: PMC6286711.
      View in: PubMed   Mentions: 7     Fields:    Translation:HumansAnimalsCells
    29. Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines. Bioorg Med Chem Lett. 2018 07 01; 28(12):2180-2183. Oukoloff K, Kovalevich J, Cornec AS, Yao Y, Owyang ZA, James M, Trojanowski JQ, Lee VM, Smith AB, Brunden KR, Ballatore C. PMID: 29764743; PMCID: PMC5993642.
      View in: PubMed   Mentions: 9     Fields:    Translation:HumansCells
    30. Evaluation of Oxetan-3-ol, Thietan-3-ol, and Derivatives Thereof as Bioisosteres of the Carboxylic Acid Functional Group. ACS Med Chem Lett. 2017 Aug 10; 8(8):864-868. Lassalas P, Oukoloff K, Makani V, James M, Tran V, Yao Y, Huang L, Vijayendran K, Monti L, Trojanowski JQ, Lee VM, Kozlowski MC, Smith AB, Brunden KR, Ballatore C. PMID: 28835803; PMCID: PMC5554911.
      View in: PubMed   Mentions: 13  
    31. Multitargeted Imidazoles: Potential Therapeutic Leads for Alzheimer's and Other Neurodegenerative Diseases. J Med Chem. 2017 06 22; 60(12):5120-5145. Cornec AS, Monti L, Kovalevich J, Makani V, James MJ, Vijayendran KG, Oukoloff K, Yao Y, Lee VM, Trojanowski JQ, Smith AB, Brunden KR, Ballatore C. PMID: 28530811; PMCID: PMC5483893.
      View in: PubMed   Mentions: 7     Fields:    Translation:HumansAnimalsCells
    32. Altered microtubule dynamics in neurodegenerative disease: Therapeutic potential of microtubule-stabilizing drugs. Neurobiol Dis. 2017 Sep; 105:328-335. Brunden KR, Lee VM, Smith AB, Trojanowski JQ, Ballatore C. PMID: 28012891; PMCID: PMC5481496.
      View in: PubMed   Mentions: 36     Fields:    Translation:HumansAnimalsCells
    33. Non-Naturally Occurring Small Molecule Microtubule-Stabilizing Agents: A Potential Tactic for CNS-Directed Therapies. ACS Chem Neurosci. 2017 01 18; 8(1):5-7. Ballatore C, Brunden KR, Trojanowski JQ, Lee VM, Smith AB. PMID: 28095679; PMCID: PMC5292930.
      View in: PubMed   Mentions: 9     Fields:    Translation:HumansAnimalsCells
    34. Evaluation of the brain-penetrant microtubule-stabilizing agent, dictyostatin, in the PS19 tau transgenic mouse model of tauopathy. Acta Neuropathol Commun. 2016 Sep 29; 4(1):106. Makani V, Zhang B, Han H, Yao Y, Lassalas P, Lou K, Paterson I, Lee VM, Trojanowski JQ, Ballatore C, Smith AB, Brunden KR. PMID: 27687527; PMCID: PMC5043530.
      View in: PubMed   Mentions: 22     Fields:    
    35. Structure Property Relationships of Carboxylic Acid Isosteres. J Med Chem. 2016 Apr 14; 59(7):3183-203. Lassalas P, Gay B, Lasfargeas C, James MJ, Tran V, Vijayendran KG, Brunden KR, Kozlowski MC, Thomas CJ, Smith AB, Huryn DM, Ballatore C. PMID: 26967507; PMCID: PMC4833640.
      View in: PubMed   Mentions: 65     Fields:    Translation:Cells
    36. Characterization of Brain-Penetrant Pyrimidine-Containing Molecules with Differential Microtubule-Stabilizing Activities Developed as Potential Therapeutic Agents for Alzheimer's Disease and Related Tauopathies. J Pharmacol Exp Ther. 2016 May; 357(2):432-50. Kovalevich J, Cornec AS, Yao Y, James M, Crowe A, Lee VM, Trojanowski JQ, Smith AB, Ballatore C, Brunden KR. PMID: 26980057; PMCID: PMC4851320.
      View in: PubMed   Mentions: 29     Fields:    Translation:AnimalsCells
    37. Aβ-mediated spine changes in the hippocampus are microtubule-dependent and can be reversed by a subnanomolar concentration of the microtubule-stabilizing agent epothilone D. Neuropharmacology. 2016 06; 105:84-95. Penazzi L, Tackenberg C, Ghori A, Golovyashkina N, Niewidok B, Selle K, Ballatore C, Smith AB, Bakota L, Brandt R. PMID: 26772969; PMCID: PMC4873443.
      View in: PubMed   Mentions: 23     Fields:    Translation:AnimalsCells
    38. Developing Therapeutics for Alzheimer's Disease. Microtubule Stabilization. 2016; 305-326. Ballatore C, Smith A B III, Lee V M-Y, Trojanowski J Q Brunden, K. R. View Publication.
    39. Wolfe M. (eds) Alzheimer’s Disease II. Topics in Medicinal Chemistry. Microtubule-Stabilizing Agents for Alzheimer’s and Other Tauopathies. 2016; 24:1-21. Ballatore C Smith A B III Lee V M-Y Trojanowski J Q Brunden, Kurt R. View Publication.
    40. Altered microtubule dynamics and vesicular transport in mouse and human MeCP2-deficient astrocytes. Hum Mol Genet. 2016 Jan 01; 25(1):146-57. Delépine C, Meziane H, Nectoux J, Opitz M, Smith AB, Ballatore C, Saillour Y, Bennaceur-Griscelli A, Chang Q, Williams EC, Dahan M, Duboin A, Billuart P, Herault Y, Bienvenu T. PMID: 26604147; PMCID: PMC4690499.
      View in: PubMed   Mentions: 32     Fields:    Translation:HumansAnimalsCells
    41. Region-specific dendritic simplification induced by Aβ, mediated by tau via dysregulation of microtubule dynamics: a mechanistic distinct event from other neurodegenerative processes. Mol Neurodegener. 2015 Nov 05; 10:60. Golovyashkina N, Penazzi L, Ballatore C, Smith AB, Bakota L, Brandt R. PMID: 26541821; PMCID: PMC4634596.
      View in: PubMed   Mentions: 18     Fields:    Translation:AnimalsCells
    42. Pharmacokinetic, pharmacodynamic and metabolic characterization of a brain retentive microtubule (MT)-stabilizing triazolopyrimidine. Bioorg Med Chem Lett. 2015 Nov 01; 25(21):4980-4982. Cornec AS, James MJ, Kovalevich J, Trojanowski JQ, Lee VM, Smith AB, Ballatore C, Brunden KR. PMID: 25819095; PMCID: PMC4569539.
      View in: PubMed   Mentions: 11     Fields:    Translation:AnimalsCells
    43. Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists. ACS Med Chem Lett. 2014 Sep 11; 5(9):1015-20. Wang X, Liu L, Huang L, Herbst-Robinson K, Cornec AS, James MJ, Sugiyama S, Bassetto M, Brancale A, Trojanowski JQ, Lee VM, Smith AB, Brunden KR, Ballatore C. PMID: 25221659; PMCID: PMC4160754.
      View in: PubMed   Mentions: 2  
    44. Evaluation of the cyclopentane-1,2-dione as a potential bio-isostere of the carboxylic acid functional group. Bioorg Med Chem Lett. 2014 Sep 01; 24(17):4171-5. Ballatore C, Gay B, Huang L, Robinson KH, James MJ, Trojanowski JQ, Lee VM, Brunden KR, Smith AB. PMID: 25127105; PMCID: PMC4146692.
      View in: PubMed   Mentions: 2     Fields:    Translation:HumansCells
    45. Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies. J Med Chem. 2014 Jul 24; 57(14):6116-27. Lou K, Yao Y, Hoye AT, James MJ, Cornec AS, Hyde E, Gay B, Lee VM, Trojanowski JQ, Smith AB, Brunden KR, Ballatore C. PMID: 24992153; PMCID: PMC4111403.
      View in: PubMed   Mentions: 31     Fields:    Translation:HumansAnimalsCells
    46. Aminothienopyridazines as imaging probes of tau pathology: a patent evaluation of WO2013090497. Expert Opin Ther Pat. 2014 Mar; 24(3):355-60. Ballatore C, Smith AB, Lee VM, Trojanowski JQ, Brunden KR. PMID: 24387030; PMCID: PMC4399384.
      View in: PubMed   Mentions: 1     Fields:    Translation:HumansAnimals
    47. Microtubule-stabilizing agents as potential therapeutics for neurodegenerative disease. Bioorg Med Chem. 2014 Sep 15; 22(18):5040-9. Brunden KR, Trojanowski JQ, Smith AB, Lee VM, Ballatore C. PMID: 24433963; PMCID: PMC4076391.
      View in: PubMed   Mentions: 39     Fields:    Translation:HumansAnimalsCells
    48. Design, synthesis, and biological evaluation of 1-phenylpyrazolo[3,4-e]pyrrolo[3,4-g]indolizine-4,6(1H,5H)-diones as new glycogen synthase kinase-3β inhibitors. J Med Chem. 2013 Dec 27; 56(24):10066-78. La Pietra V, La Regina G, Coluccia A, Famiglini V, Pelliccia S, Plotkin B, Eldar-Finkelman H, Brancale A, Ballatore C, Crowe A, Brunden KR, Marinelli L, Novellino E, Silvestri R. PMID: 24295046.
      View in: PubMed   Mentions: 5     Fields:    Translation:HumansCells
    49. MT-Stabilizer, Dictyostatin, Exhibits Prolonged Brain Retention and Activity: Potential Therapeutic Implications. ACS Med Chem Lett. 2013 Sep 12; 4(9):886-9. Brunden KR, Gardner NM, James MJ, Yao Y, Trojanowski JQ, Lee VM, Paterson I, Ballatore C, Smith AB. PMID: 24900764; PMCID: PMC4027543.
      View in: PubMed   Mentions: 18  
    50. Aminothienopyridazines and methylene blue affect Tau fibrillization via cysteine oxidation. J Biol Chem. 2013 Apr 19; 288(16):11024-37. Crowe A, James MJ, Lee VM, Smith AB, Trojanowski JQ, Ballatore C, Brunden KR. PMID: 23443659; PMCID: PMC3630889.
      View in: PubMed   Mentions: 60     Fields:    Translation:HumansCells
    51. Carboxylic acid (bio)isosteres in drug design. ChemMedChem. 2013 Mar; 8(3):385-95. Ballatore C, Huryn DM, Smith AB. PMID: 23361977; PMCID: PMC3640829.
      View in: PubMed   Mentions: 103     Fields:    
    52. Microtubule stabilizing agents as potential treatment for Alzheimer's disease and related neurodegenerative tauopathies. J Med Chem. 2012 Nov 08; 55(21):8979-96. Ballatore C, Brunden KR, Huryn DM, Trojanowski JQ, Lee VM, Smith AB. PMID: 23020671; PMCID: PMC3493881.
      View in: PubMed   Mentions: 64     Fields:    Translation:HumansAnimalsCells
    53. Brain-penetrant microtubule-stabilizing compounds as potential therapeutic agents for tauopathies. Biochem Soc Trans. 2012 Aug; 40(4):661-6. Brunden KR, Ballatore C, Lee VM, Smith AB, Trojanowski JQ. PMID: 22817712; PMCID: PMC3431553.
      View in: PubMed   Mentions: 24     Fields:    Translation:HumansAnimalsCells
    54. Brain-penetrant tetrahydronaphthalene thromboxane A2-prostanoid (TP) receptor antagonists as prototype therapeutics for Alzheimer's disease. ACS Chem Neurosci. 2012 Nov 21; 3(11):928-40. Soper JH, Sugiyama S, Herbst-Robinson K, James MJ, Wang X, Trojanowski JQ, Smith AB, Lee VM, Ballatore C, Brunden KR. PMID: 23173073; PMCID: PMC3503350.
      View in: PubMed   Mentions: 15     Fields:    Translation:Animals
    55. Aminothienopyridazine inhibitors of tau aggregation: evaluation of structure-activity relationship leads to selection of candidates with desirable in vivo properties. Bioorg Med Chem. 2012 Jul 15; 20(14):4451-61. Ballatore C, Crowe A, Piscitelli F, James M, Lou K, Rossidivito G, Yao Y, Trojanowski JQ, Lee VM, Brunden KR, Smith AB. PMID: 22717239; PMCID: PMC4304654.
      View in: PubMed   Mentions: 7     Fields:    Translation:Animals
    56. The microtubule-stabilizing agent, epothilone D, reduces axonal dysfunction, neurotoxicity, cognitive deficits, and Alzheimer-like pathology in an interventional study with aged tau transgenic mice. J Neurosci. 2012 Mar 14; 32(11):3601-11. Zhang B, Carroll J, Trojanowski JQ, Yao Y, Iba M, Potuzak JS, Hogan AM, Xie SX, Ballatore C, Smith AB, Lee VM, Brunden KR. PMID: 22423084; PMCID: PMC3321513.
      View in: PubMed   Mentions: 172     Fields:    Translation:HumansAnimalsCells
    57. Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonists. J Med Chem. 2011 Oct 13; 54(19):6969-83. Ballatore C, Soper JH, Piscitelli F, James M, Huang L, Atasoylu O, Huryn DM, Trojanowski JQ, Lee VM, Brunden KR, Smith AB. PMID: 21863799; PMCID: PMC3188681.
      View in: PubMed   Mentions: 8     Fields:    Translation:HumansAnimalsCells
    58. Modulation of protein-protein interactions as a therapeutic strategy for the treatment of neurodegenerative tauopathies. Curr Top Med Chem. 2011; 11(3):317-30. Ballatore C, Brunden KR, Trojanowski JQ, Lee VM, Smith AB, Huryn DM. PMID: 21320060; PMCID: PMC3069499.
      View in: PubMed   Mentions: 23     Fields:    Translation:HumansAnimalsCells
    59. The characterization of microtubule-stabilizing drugs as possible therapeutic agents for Alzheimer's disease and related tauopathies. Pharmacol Res. 2011 Apr; 63(4):341-51. Brunden KR, Yao Y, Potuzak JS, Ferrer NI, Ballatore C, James MJ, Hogan AM, Trojanowski JQ, Smith AB, Lee VM. PMID: 21163349; PMCID: PMC3042036.
      View in: PubMed   Mentions: 68     Fields:    Translation:HumansAnimalsCells
    60. Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy. J Neurosci. 2010 Oct 13; 30(41):13861-6. Brunden KR, Zhang B, Carroll J, Yao Y, Potuzak JS, Hogan AM, Iba M, James MJ, Xie SX, Ballatore C, Smith AB, Lee VM, Trojanowski JQ. PMID: 20943926; PMCID: PMC2958430.
      View in: PubMed   Mentions: 135     Fields:    Translation:AnimalsCells
    61. Discovery of brain-penetrant, orally bioavailable aminothienopyridazine inhibitors of tau aggregation. J Med Chem. 2010 May 13; 53(9):3739-47. Ballatore C, Brunden KR, Piscitelli F, James MJ, Crowe A, Yao Y, Hyde E, Trojanowski JQ, Lee VM, Smith AB. PMID: 20392114; PMCID: PMC2872922.
      View in: PubMed   Mentions: 24     Fields:    Translation:AnimalsCells
    62. Solid phase synthesis of 2-aminobenzothiazoles. Bioorg Med Chem Lett. 2010 Jan 15; 20(2):644-8. Piscitelli F, Ballatore C, Smith AB. PMID: 19954974; PMCID: PMC2818510.
      View in: PubMed   Mentions: 3     Fields:    Translation:Cells
    63. Tau-directed drug discovery for Alzheimer's disease and related tauopathies: a focus on tau assembly inhibitors. Exp Neurol. 2010 Jun; 223(2):304-10. Brunden KR, Ballatore C, Crowe A, Smith AB, Lee VM, Trojanowski JQ. PMID: 19744482; PMCID: PMC2864354.
      View in: PubMed   Mentions: 44     Fields:    Translation:HumansCells
    64. Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening. Biochemistry. 2009 Aug 18; 48(32):7732-45. Crowe A, Huang W, Ballatore C, Johnson RL, Hogan AM, Huang R, Wichterman J, McCoy J, Huryn D, Auld DS, Smith AB, Inglese J, Trojanowski JQ, Austin CP, Brunden KR, Lee VM. PMID: 19580328; PMCID: PMC2773749.
      View in: PubMed   Mentions: 51     Fields:    Translation:HumansAnimalsCells
    65. In situ blood-brain barrier permeability of a C-10 paclitaxel carbamate. Bioorg Med Chem Lett. 2008 Dec 01; 18(23):6119-21. Ballatore C, Zhang B, Trojanowski JQ, Lee VM, Smith AB. PMID: 18947993; PMCID: PMC2603177.
      View in: PubMed   Mentions: 3     Fields:    Translation:AnimalsCells
    66. Tau-mediated neurodegeneration in Alzheimer's disease and related disorders. Nat Rev Neurosci. 2007 Sep; 8(9):663-72. Ballatore C, Lee VM, Trojanowski JQ. PMID: 17684513.
      View in: PubMed   Mentions: 905     Fields:    Translation:HumansAnimals
    67. Paclitaxel C-10 carbamates: potential candidates for the treatment of neurodegenerative tauopathies. Bioorg Med Chem Lett. 2007 Jul 01; 17(13):3642-6. Ballatore C, Hyde E, Deiches RF, Lee VM, Trojanowski JQ, Huryn D, Smith AB. PMID: 17485207; PMCID: PMC2648301.
      View in: PubMed   Mentions: 10     Fields:    Translation:HumansAnimals
    68. High throughput screening for small molecule inhibitors of heparin-induced tau fibril formation. Biochem Biophys Res Commun. 2007 Jun 22; 358(1):1-6. Crowe A, Ballatore C, Hyde E, Trojanowski JQ, Lee VM. PMID: 17482143; PMCID: PMC2646256.
      View in: PubMed   Mentions: 48     Fields:    Translation:Cells
    69. Targeting heat shock proteins on cancer cells: selection, characterization, and cell-penetrating properties of a peptidic GRP78 ligand. Biochemistry. 2006 Aug 08; 45(31):9434-44. Kim Y, Lillo AM, Steiniger SC, Liu Y, Ballatore C, Anichini A, Mortarini R, Kaufmann GF, Zhou B, Felding-Habermann B, Janda KD. PMID: 16878978.
      View in: PubMed   Mentions: 82     Fields:    Translation:HumansCells
    70. Kinase-mediated trapping of bi-functional conjugates of paclitaxel or vinblastine with thymidine in cancer cells. Bioorg Med Chem Lett. 2006 Oct 01; 16(19):5194-8. Aspland SE, Ballatore C, Castillo R, Desharnais J, Eustaquio T, Goelet P, Guo Z, Li Q, Nelson D, Sun C, Castellino AJ, Newman MJ. PMID: 16870428.
      View in: PubMed   Mentions: 10     Fields:    Translation:HumansCells
    71. The design, synthesis, and evaluation of two universal doxorubicin-linkers: preparation of conjugates that retain topoisomerase II activity. Bioorg Med Chem Lett. 2006 Jan 01; 16(1):104-7. Sun C, Aspland SE, Ballatore C, Castillo R, Smith AB, Castellino AJ. PMID: 16242325.
      View in: PubMed   Mentions:    Fields:    Translation:HumansCells
    72. A facile route to paclitaxel C-10 carbamates. Bioorg Med Chem Lett. 2005 May 16; 15(10):2477-80. Ballatore C, Aspland SE, Castillo R, Desharnais J, Eustaquio T, Sun C, Castellino AJ, Smith AB. PMID: 15863300.
      View in: PubMed   Mentions: 3     Fields:    
    73. Separation of individual antiviral nucleotide prodrugs from synthetic mixtures using cross-reactivity of a molecularly imprinted stationary phase. Analytica Chimica Acta. 2001; 435(1):107-113. Allender, C. J. Brain, K. R. Ballatore, C. Cahard, D. Siddiqui, A. McGuigan, C.
    74. Synthesis and evaluation of novel amidate prodrugs of PMEA and PMPA. Bioorg Med Chem Lett. 2001 Apr 23; 11(8):1053-6. Ballatore C, McGuigan C, De Clercq E, Balzarini J. PMID: 11327587.
      View in: PubMed   Mentions: 13     Fields:    Translation:HumansCells
    75. Phosphoramidate derivatives of stavudine as inhibitors of HIV: unnatural amino acids may substitute for alanine. Antivir Chem Chemother. 2000 Mar; 11(2):111-6. McGuigan C, Bidois L, Hiouni A, Ballatore C, De Clercq E, Balzarini J. PMID: 10819435.
      View in: PubMed   Mentions: 1     Fields:    Translation:HumansCells
    76. Enhancing the aqueous solubility of d4T-based phosphoramidate prodrugs. Bioorg Med Chem Lett. 2000 Feb 21; 10(4):381-4. Siddiqui A, McGuigan C, Ballatore C, Srinivasan S, De Clercq E, Balzarini J. PMID: 10714505.
      View in: PubMed   Mentions:    Fields:    Translation:AnimalsCells
    77. Design and synthesis of lipophilic phosphoramidate d4T-MP prodrugs expressing high potency against HIV in cell culture: structural determinants for in vitro activity and QSAR. J Med Chem. 1999 Oct 07; 42(20):4122-8. Siddiqui AQ, McGuigan C, Ballatore C, Zuccotto F, Gilbert IH, De Clercq E, Balzarini J. PMID: 10514282.
      View in: PubMed   Mentions: 7     Fields:    Translation:Cells
    78. Simple mono-derivatisation of the aryl moiety of D4A and DDA-based phosphoramidate prodrugs significantly enhances their anti-HIV potency in cell culture. Bioorg Med Chem Lett. 1999 Sep 06; 9(17):2555-60. Siddiqui AQ, McGuigan C, Ballatore C, Wedgwood O, De Clercq E, Balzarini J. PMID: 10498207.
      View in: PubMed   Mentions: 3     Fields:    Translation:HumansCells
    79. The presence of substituents on the aryl moiety of the aryl phosphoramidate derivative of d4T enhances anti-HIV efficacy in cell culture: A structure-activity relationship. J Med Chem. 1999 Feb 11; 42(3):393-9. Siddiqui AQ, Ballatore C, McGuigan C, De Clercq E, Balzarini J. PMID: 9986709.
      View in: PubMed   Mentions: 10     Fields:    Translation:HumansAnimalsCells
    80. An in situ pig liver esterase assay as a useful predictive tool for the likely in vitro anti viral activity of phosphoramidate pro-drugs. Nucleosides Nucleotides. 1999; 18(4-5):967-9. Ballatore, C. McGuigan, C. De Clercq, E. Balzarini, J.
    81. Lactate cannot substitute for alanine in d4T-based anti-HIV nucleotide prodrugs--despite efficient esterase-mediated hydrolysis. Bioorg Med Chem Lett. 1998 Nov 03; 8(21):2949-54. McGuigan C, Cahard D, Ballatore C, Siddiqui A, De Clercq E, Balzarini J. PMID: 9873653.
      View in: PubMed   Mentions:    Fields:    Translation:Cells
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