Carlo Ballatore

TitleAssociate Professor
InstitutionUniversity of California San Diego
DepartmentSchool of Pharmacy and Pharmaceutical Science
Address9500 Gilman Drive #0756
La Jolla CA 92093
vCardDownload vCard

    Collapse Research 
    Collapse Research Activities and Funding
    Brain Penetrant Microtubule-Stabilizers to treat CNS-invasive parasitic diseases
    NIH/NIAID R21AI133394Jun 1, 2018 - May 31, 2020
    Role: Co-Principal Investigator
    Orally-absorbed, small molecule microtubule-stabilizers for tauopathy treatment
    NIH/NIA R01AG044332Jun 15, 2013 - May 31, 2018
    Role: Co-Principal Investigator

    Collapse ORNG Applications 
    Collapse Websites

    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.
    List All   |   Timeline
    1. Monti L, Wang SC, Oukoloff K, Smith AB, Brunden KR, Caffrey C, Ballatore C. Brain-penetrant, triazolopyrimidine and phenylpyrimidine microtubule-stabilizers as potential leads to treat human African trypanosomiasis. ChemMedChem. 2018 Jul 03. PMID: 29969537.
      View in: PubMed
    2. 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 May 05. PMID: 29764743.
      View in: PubMed
    3. 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 Aug 10; 8(8):864-868. PMID: 28835803.
      View in: PubMed
    4. 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 Jun 22; 60(12):5120-5145. PMID: 28530811.
      View in: PubMed
    5. 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 Sep; 105:328-335. PMID: 28012891.
      View in: PubMed
    6. 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 01 18; 8(1):5-7. PMID: 28095679.
      View in: PubMed
    7. 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 Sep 29; 4(1):106. PMID: 27687527.
      View in: PubMed
    8. 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 Apr 14; 59(7):3183-203. PMID: 26967507; PMCID: PMC4833640.
    9. 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 Pharmacol Exp Ther. 2016 May; 357(2):432-50. PMID: 26980057; PMCID: PMC4851320 [Available on 05/01/17].
    10. Penazzi L, Tackenberg C, Ghori A, Golovyashkina N, Niewidok B, Selle K, Ballatore C, Smith AB, Bakota L, Brandt R. Aß-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. PMID: 26772969; PMCID: PMC4873443 [Available on 06/01/17].
    11. 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 Genet. 2016 Jan 01; 25(1):146-57. PMID: 26604147; PMCID: PMC4690499 [Available on 01/01/17].
    12. Golovyashkina N, Penazzi L, Ballatore C, Smith AB, Bakota L, Brandt R. Region-specific dendritic simplification induced by Aß, mediated by tau via dysregulation of microtubule dynamics: a mechanistic distinct event from other neurodegenerative processes. Mol Neurodegener. 2015 Nov 05; 10:60. PMID: 26541821; PMCID: PMC4634596.
    13. Cornec AS, James MJ, Kovalevich J, Trojanowski JQ, Lee VM, Smith AB, Ballatore C, Brunden KR. Pharmacokinetic, pharmacodynamic and metabolic characterization of a brain retentive microtubule (MT)-stabilizing triazolopyrimidine. Bioorg Med Chem Lett. 2015 Nov 01; 25(21):4980-2. PMID: 25819095; PMCID: PMC4569539 [Available on 11/01/16].
    14. 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. Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists. ACS Med Chem Lett. 2014 Sep 11; 5(9):1015-20. PMID: 25221659; PMCID: PMC4160754.
    15. Ballatore C, Gay B, Huang L, Robinson KH, James MJ, Trojanowski JQ, Lee VM, Brunden KR, Smith AB. 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. PMID: 25127105; PMCID: PMC4146692.
    16. Lou K, Yao Y, Hoye AT, James MJ, Cornec AS, Hyde E, Gay B, Lee VM, Trojanowski JQ, Smith AB, Brunden KR, Ballatore C. 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. PMID: 24992153; PMCID: PMC4111403.
    17. Ballatore C, Smith AB, Lee VM, Trojanowski JQ, Brunden KR. Aminothienopyridazines as imaging probes of tau pathology: a patent evaluation of WO2013090497. Expert Opin Ther Pat. 2014 Mar; 24(3):355-60. PMID: 24387030; PMCID: PMC4399384.
    18. Brunden KR, Trojanowski JQ, Smith AB, Lee VM, Ballatore C. Microtubule-stabilizing agents as potential therapeutics for neurodegenerative disease. Bioorg Med Chem. 2014 Sep 15; 22(18):5040-9. PMID: 24433963; PMCID: PMC4076391.
    19. 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. 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-3ß inhibitors. J Med Chem. 2013 Dec 27; 56(24):10066-78. PMID: 24295046.
      View in: PubMed
    20. Brunden KR, Gardner NM, James MJ, Yao Y, Trojanowski JQ, Lee VM, Paterson I, Ballatore C, Smith AB. MT-Stabilizer, Dictyostatin, Exhibits Prolonged Brain Retention and Activity: Potential Therapeutic Implications. ACS Med Chem Lett. 2013 Sep 12; 4(9):886-9. PMID: 24900764; PMCID: PMC4027543.
    21. Crowe A, James MJ, Lee VM, Smith AB, Trojanowski JQ, Ballatore C, Brunden KR. Aminothienopyridazines and methylene blue affect Tau fibrillization via cysteine oxidation. J Biol Chem. 2013 Apr 19; 288(16):11024-37. PMID: 23443659; PMCID: PMC3630889.
    22. Ballatore C, Huryn DM, Smith AB. Carboxylic acid (bio)isosteres in drug design. ChemMedChem. 2013 Mar; 8(3):385-95. PMID: 23361977; PMCID: PMC3640829.
    23. Ballatore C, Brunden KR, Huryn DM, Trojanowski JQ, Lee VM, Smith AB. Microtubule stabilizing agents as potential treatment for Alzheimer's disease and related neurodegenerative tauopathies. J Med Chem. 2012 Nov 08; 55(21):8979-96. PMID: 23020671; PMCID: PMC3493881.
    24. Brunden KR, Ballatore C, Lee VM, Smith AB, Trojanowski JQ. Brain-penetrant microtubule-stabilizing compounds as potential therapeutic agents for tauopathies. Biochem Soc Trans. 2012 Aug; 40(4):661-6. PMID: 22817712; PMCID: PMC3431553.
    25. Soper JH, Sugiyama S, Herbst-Robinson K, James MJ, Wang X, Trojanowski JQ, Smith AB, Lee VM, Ballatore C, Brunden KR. 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. PMID: 23173073; PMCID: PMC3503350.
    26. Ballatore C, Crowe A, Piscitelli F, James M, Lou K, Rossidivito G, Yao Y, Trojanowski JQ, Lee VM, Brunden KR, Smith AB. 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. PMID: 22717239; PMCID: PMC4304654.
    27. Zhang B, Carroll J, Trojanowski JQ, Yao Y, Iba M, Potuzak JS, Hogan AM, Xie SX, Ballatore C, Smith AB, Lee VM, Brunden KR. 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. PMID: 22423084; PMCID: PMC3321513.
    28. Ballatore C, Soper JH, Piscitelli F, James M, Huang L, Atasoylu O, Huryn DM, Trojanowski JQ, Lee VM, Brunden KR, Smith AB. 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. PMID: 21863799; PMCID: PMC3188681.
    29. Ballatore C, Brunden KR, Trojanowski JQ, Lee VM, Smith AB, Huryn DM. Modulation of protein-protein interactions as a therapeutic strategy for the treatment of neurodegenerative tauopathies. Curr Top Med Chem. 2011; 11(3):317-30. PMID: 21320060; PMCID: PMC3069499.
    30. Brunden KR, Yao Y, Potuzak JS, Ferrer NI, Ballatore C, James MJ, Hogan AM, Trojanowski JQ, Smith AB, Lee VM. 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. PMID: 21163349; PMCID: PMC3042036.
    31. 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. 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. PMID: 20943926; PMCID: PMC2958430.
    32. Ballatore C, Brunden KR, Piscitelli F, James MJ, Crowe A, Yao Y, Hyde E, Trojanowski JQ, Lee VM, Smith AB. Discovery of brain-penetrant, orally bioavailable aminothienopyridazine inhibitors of tau aggregation. J Med Chem. 2010 May 13; 53(9):3739-47. PMID: 20392114; PMCID: PMC2872922.
    33. Piscitelli F, Ballatore C, Smith AB. Solid phase synthesis of 2-aminobenzothiazoles. Bioorg Med Chem Lett. 2010 Jan 15; 20(2):644-8. PMID: 19954974; PMCID: PMC2818510.
    34. Brunden KR, Ballatore C, Crowe A, Smith AB, Lee VM, Trojanowski JQ. 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. PMID: 19744482; PMCID: PMC2864354.
    35. 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. Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening. Biochemistry. 2009 Aug 18; 48(32):7732-45. PMID: 19580328; PMCID: PMC2773749.
    36. Ballatore C, Zhang B, Trojanowski JQ, Lee VM, Smith AB. In situ blood-brain barrier permeability of a C-10 paclitaxel carbamate. Bioorg Med Chem Lett. 2008 Dec 01; 18(23):6119-21. PMID: 18947993; PMCID: PMC2603177.
    37. Ballatore C, Lee VM, Trojanowski JQ. Tau-mediated neurodegeneration in Alzheimer's disease and related disorders. Nat Rev Neurosci. 2007 Sep; 8(9):663-72. PMID: 17684513.
      View in: PubMed
    38. Ballatore C, Hyde E, Deiches RF, Lee VM, Trojanowski JQ, Huryn D, Smith AB. Paclitaxel C-10 carbamates: potential candidates for the treatment of neurodegenerative tauopathies. Bioorg Med Chem Lett. 2007 Jul 01; 17(13):3642-6. PMID: 17485207; PMCID: PMC2648301.
    39. Crowe A, Ballatore C, Hyde E, Trojanowski JQ, Lee VM. High throughput screening for small molecule inhibitors of heparin-induced tau fibril formation. Biochem Biophys Res Commun. 2007 Jun 22; 358(1):1-6. PMID: 17482143; PMCID: PMC2646256.
    40. Kim Y, Lillo AM, Steiniger SC, Liu Y, Ballatore C, Anichini A, Mortarini R, Kaufmann GF, Zhou B, Felding-Habermann B, Janda KD. 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. PMID: 16878978.
      View in: PubMed
    41. Aspland SE, Ballatore C, Castillo R, Desharnais J, Eustaquio T, Goelet P, Guo Z, Li Q, Nelson D, Sun C, Castellino AJ, Newman MJ. 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. PMID: 16870428.
      View in: PubMed
    42. Sun C, Aspland SE, Ballatore C, Castillo R, Smith AB, Castellino AJ. 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. PMID: 16242325.
      View in: PubMed
    43. Ballatore C, Aspland SE, Castillo R, Desharnais J, Eustaquio T, Sun C, Castellino AJ, Smith AB. A facile route to paclitaxel C-10 carbamates. Bioorg Med Chem Lett. 2005 May 16; 15(10):2477-80. PMID: 15863300.
      View in: PubMed
    44. Ballatore C, McGuigan C, De Clercq E, Balzarini J. Synthesis and evaluation of novel amidate prodrugs of PMEA and PMPA. Bioorg Med Chem Lett. 2001 Apr 23; 11(8):1053-6. PMID: 11327587.
      View in: PubMed
    45. McGuigan C, Bidois L, Hiouni A, Ballatore C, De Clercq E, Balzarini J. Phosphoramidate derivatives of stavudine as inhibitors of HIV: unnatural amino acids may substitute for alanine. Antivir Chem Chemother. 2000 Mar; 11(2):111-6. PMID: 10819435.
      View in: PubMed
    46. Siddiqui A, McGuigan C, Ballatore C, Srinivasan S, De Clercq E, Balzarini J. Enhancing the aqueous solubility of d4T-based phosphoramidate prodrugs. Bioorg Med Chem Lett. 2000 Feb 21; 10(4):381-4. PMID: 10714505.
      View in: PubMed
    47. Siddiqui AQ, McGuigan C, Ballatore C, Zuccotto F, Gilbert IH, De Clercq E, Balzarini J. 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. PMID: 10514282.
      View in: PubMed
    48. Siddiqui AQ, McGuigan C, Ballatore C, Wedgwood O, De Clercq E, Balzarini J. 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. PMID: 10498207.
      View in: PubMed
    49. Ballatore C, McGuigan C, De Clercq E, Balzarini J. 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 Apr-May; 18(4-5):967-9. PMID: 10432721.
      View in: PubMed
    50. Siddiqui AQ, Ballatore C, McGuigan C, De Clercq E, Balzarini J. 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. PMID: 9986709.
      View in: PubMed
    51. McGuigan C, Cahard D, Ballatore C, Siddiqui A, De Clercq E, Balzarini J. 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. PMID: 9873653.
      View in: PubMed
    Carlo's Networks
    Derived automatically from this person's publications.
    People in Profiles who have published with this person.
    Related Authors
    People who share related concepts with this person.