Featured Publications
Publications since 2016:
For a full list of publications click here
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. “A small-molecule microtubule-stabilizing agent safely reduces Aβ plaque and tau pathology in transgenic mouse models of Alzheimer’s disease”. Alzheimer’s Dement. 2024. doi.org/10.1002/alz.13875
Lucero B, Francisco KR, Varricchio C, Liu LJ, Yao Y, Brancale A, Brunden KR, Caffrey CR, Ballatore C. Design, Synthesis, and Evaluation of An Anti-trypanosomal [1,2,4]Triazolo[1,5-a]pyrimidine Probe for Photoaffinity Labeling Studies. ChemMedChem. 2024 Vol. 19 Issue 8 Pages e202300656. doi: 10.1002/cmdc.202300656. PMID: 38277231.
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. “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, 6, 11, 1651 – 1658, PMID: 37974623.
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. “A microtubule stabilizer ameliorates protein pathogenesis and neurodegeneration in mouse models of repetitive traumatic brain injury”. Sci Transl. Med. 2023 Vol. 15 Issue 713 Pages eabo6889. PMID: 37703352.
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. “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, e202300193, PMID: 37429821.
Alle T, Joyasawal S, Oukoloff K, Long K, Owyang Z, Francisco KR, Cahard D, Huryn DM, Ballatore C. “Structure property relationships of fluorinated carboxylic acid bioisosteres”. Bioorg. Med. Chem. Lett. 2023, 91, 129363, PMID: 37295616.
Lucero B, Francisco KR, Liu LJ, Caffrey CR, Ballatore C. “Protein-protein interactions: developing small-molecule inhibitors/stabilizers through covalent strategies”. Trends Pharmacol. Sci., 2023, Vol. 44, No. 7, 474-488. PMID: 37263826
HF, Paniak TJ, Berlin CB, Tran V, Francisco KR, Lassalas P, Devas A, Landes O, Rosenberger A, Rotella ME, Ballatore C, Kozlowski MC. “Hydrogen Bonding Parameters by Rapid Colorimetric Assessment: Evaluation of Structural Components Found in Biological Ligands and Organocatalysts”. Chem. Eur. J. 2023, e202300696. PMID: 36917701.
Alle T, Varricchio C, Yao Y, Lucero B, Nzou G, Demuro S, Muench M, Vuong KD, Oukoloff K, Cornec A-S, Francisco KR, Caffrey CR, Lee VM-Y, Smith AB III, Brancale A, Brunden KR, Ballatore C. “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, 66, 1, 435–459. PMCID: PMC9841533
Francisco KR, Ballatore C. “Thietanes and derivatives thereof in medicinal chemistry” Curr. Top. Med. Chem. 2022, 22(15):1219. PMID: 35546768.
Narayanan A, Narwal M, Majowicz SA, Varricchio C, Toner SA, Ballatore C, Brancale A, Murakami KS, Jose J. “Identification of SARS-CoV-2 inhibitors targeting Mpro and PLpro using in-cell-protease assay.” Commun. Biol. 2022, 5, 169. PMID: 35217718.
Ballatore C. “New Heights for ProTides?” J. Med. Chem. 2021, 64, 16422. PMID: 34783565.
Bergazin TD, Tielker N, Zhang Y, Mao J, Gunner MR, Francisco K, Ballatore C, Kast SM, Mobley DL. “Evaluation of log P, pKa, and log D predictions from the SAMPL7 blind challenge” J. Comput. Aided Mol. Des. 2021, 35, 771. PMID: 34169394.
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. “Drug Discovery and Development for Kinetoplastid Diseases”, Chapter 4, pp.255-334 in Burger’s Medicinal Chemistry and Drug Discovery 8th Edition, Donald J. Abraham (Editor-in-Chief) and Michael Myers (Consulting Editor), ISBN: 978-1-119-53030-5, Wiley, April 2021.
Francisco KR, Varricchio C, Paniak TJ, Kozlowski MC, Brancale A, Ballatore C. “Structure Property Relationships of N-Acylsulfonamides and Related Bioisosteres” Eur. J. Med. Chem. 2021, 218, 113399. PMID: 33823393.
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. “Inhibition of the HEG1–KRIT1 interaction increases KLF4 and KLF2 expression in endothelial cells” FASEB BioAdv. 2021, 3: 334-355. PMID: 33977234
Oukoloff K, Nzou G, Varricchio C, Lucero B, Alle T, Kovalevich J, Monti L, Cornec AS, Yao Y, James MJ, Trojanowski JQ, Lee MY, Smith AB, Brancale A, Brunden KR, Ballatore C. “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, 64(2):1073-1102. PMID: 33411523
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. “Congeners derived from microtubule-active phenylpyrimidines produce a potent and long-lasting paralysis of Schistosoma mansoni in vitro” ACS Infect. Dis. 2021, 7(5):1089-1103. PMID: 33135408.
Yao Y, Nzou G, Alle T, Tsering W, Maimaiti S, Trojanowski JQ, Lee VM, Ballatore C, Brunden KR. “Correction of microtubule defects within Aβ plaque-associated dystrophic axons results in lowered Aβ release and plaque deposition.” Alzheimer’s Dement. 2020, 16, 1345–1357. PMID: 32918367.
Gorecki L, Gerlits O, Kong X, Cheng X, Blumenthal DK, Taylor P, Ballatore C, Kovalevsky A, Radic Z. “Rational design, synthesis, and evaluation of uncharged, “smart” bis-oxime antidotes of organophosphate-inhibited human acetylcholinesterase.” J. Biol. Chem. 2020, 295(13):4079-4092. PMID: 32019865.
Meewan I, Zhang X, Roy S, Ballatore C, O’Donoghue AJ, Schooley RT, Abagyan R. “Discovery of New Inhibitors of Hepatitis C Virus NS3/4A Protease and Its D168A Mutant”. ACS Omega. 2019, 4(16):16999-17008. PMID: 31646247.
Oukoloff K, Lucero B, Francisco KR, Brunden KR, Ballatore C. “1,2,4-Triazolo[1,5-a]pyrimidines in drug design”. Eur. J. Med. Chem. 2019, 165:332-346. PMID: 30703745.
Zhang B, Yao Y, Cornec AS, Oukoloff K, James MJ, Koivula P, Trojanowski JQ, Smith AB, Lee VM, Ballatore C, Brunden KR. “A brain-penetrant triazolopyrimidine enhances microtubule-stability, reduces axonal dysfunction and decreases tau pathology in a mouse tauopathy model”. Mol. Neurodegener. 2018, 13(1):59. PMID: 30404654.
Monti L, Wang SC, Oukoloff K, Smith AB, Brunden KR, Caffrey CR, Ballatore C. “Brain-Penetrant Triazolopyrimidine and Phenylpyrimidine Microtubule Stabilizers as Potential Leads to Treat Human African Trypanosomiasis”. ChemMedChem. 2018, 13(17):1751-1754. PMID: 29969537.
Oukoloff K, Kovalevich J, Cornec AS, Yao Y, Owyang ZA, James M, Trojanowski JQ, Lee VM, Smith AB, Brunden KR, Ballatore C. “Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines”. Bioorg. Med. Chem. Lett. 2018, 28(12):2180-2183. PMID: 29764743.
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. “Evaluation of Oxetan-3-ol, Thietan-3-ol, and Derivatives Thereof as Bioisosteres of the Carboxylic Acid Functional Group”. ACS Med. Chem. Lett. 2017, 8(8):864-868. PMID: 28835803.
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. “Multitargeted Imidazoles: Potential Therapeutic Leads for Alzheimer’s and Other Neurodegenerative Diseases”. J. Med. Chem. 2017, 60(12):5120-5145. PMID: 28530811.
Brunden KR, Lee VM, Smith AB, Trojanowski JQ, Ballatore C. “Altered microtubule dynamics in neurodegenerative disease: Therapeutic potential of microtubule-stabilizing drugs”. Neurobiol. Dis. 2017, 105:328-335. PMID: 28012891.
Ballatore C, Brunden KR, Trojanowski JQ, Lee VM, Smith AB. “Non-Naturally Occurring Small Molecule Microtubule-Stabilizing Agents: A Potential Tactic for CNS-Directed Therapies”. ACS Chem. Neurosci. 2017, 8(1):5-7. PMID: 28095679.
Makani V, Zhang B, Han H, Yao Y, Lassalas P, Lou K, Paterson I, Lee VM, Trojanowski JQ, Ballatore C, Smith AB, Brunden KR. “Evaluation of the brain-penetrant microtubule-stabilizing agent, dictyostatin, in the PS19 tau transgenic mouse model of tauopathy”. Acta Neuropathol. Commun. 2016, 4(1):106. PMID: 27687527.
Lassalas P, Gay B, Lasfargeas C, James MJ, Tran V, Vijayendran KG, Brunden KR, Kozlowski MC, Thomas CJ, Smith AB, Huryn DM, Ballatore C. “Structure Property Relationships of Carboxylic Acid Isosteres.” J. Med. Chem. 2016, 59(7):3183-203. PMID: 26967507; PMCID: PMC4833640. [see also “The same and not the same: Carboxylic acids and tetrazoles”]
Kovalevich J, Cornec AS, Yao Y, James M, Crowe A, Lee VM, Trojanowski JQ, Smith AB, Ballatore C, Brunden KR. “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. Pharm. Exp. Ther., 2016, 357 (2):432-450. PMID: 26980057; PMCID: PMC4851320.
Ballatore C, Smith AB, Trojanowski JQ, Lee VM, Brunden KR; Book Chapter “Microtubule Stabilization”, Book Title: “Developing Therapeutics for Alzheimer’s Disease: Progress and Challenges”, 2016, Academic Press.
Ballatore C, Smith AB, Lee VM, Trojanowski JQ, Brunden KR; Book Chapter “Microtubule-Stabilizing Agents for Alzheimer’s and Other Tauopathies”, 2016, In: Wolfe M. (eds) Alzheimer’s Disease II. Topics in Medicinal Chemistry, vol 24. Springer, Cham. https://doi.org/10.1007/7355_2016_15
Penazzi L, Tackenberg C, Ghori A, Golovyashkina N, Niewidok B, Selle K, Ballatore C, Smith AB, Bakota L, Brandt R. “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, 105:84-95. PMID: 26772969; PMCID: PMC4873443.
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. “Altered microtubule dynamics and vesicular transport in mouse and human MeCP2-deficient astrocytes”, Hum. Mol. Gen., 2016, 25(1), 146-57. PMID: 26604147; PMCID: PMC4690499.