Carlo Ballatore

Summary

Affiliation: University of Pennsylvania
Country: USA

Publications

  1. doi request reprint Aminothienopyridazines as imaging probes of tau pathology: a patent evaluation of WO2013090497
    Carlo Ballatore
    University of Pennsylvania, Perelman School of Medicine, Center for Neurodegenerative Disease Research, 3600 Spruce Street, Philadelphia, PA 19104 6323, USA
    Expert Opin Ther Pat 24:355-60. 2014
  2. pmc Carboxylic acid (bio)isosteres in drug design
    Carlo Ballatore
    Department of Chemistry, University of Pennsylvania, 231 South 34th St, Philadelphia, PA 19104, USA
    ChemMedChem 8:385-95. 2013
  3. pmc Microtubule stabilizing agents as potential treatment for Alzheimer's disease and related neurodegenerative tauopathies
    Carlo Ballatore
    Department of Chemistry, School of Arts and Sciences, University of Pennsylvania, 231 South 34th Street, Philadelphia, Pennsylvania 19104 6323, United States
    J Med Chem 55:8979-96. 2012
  4. doi request reprint Aminothienopyridazine inhibitors of tau aggregation: evaluation of structure-activity relationship leads to selection of candidates with desirable in vivo properties
    Carlo Ballatore
    Department of Chemistry, University of Pennsylvania, 231 South 34th Street, Philadelphia, PA 19104 6323, USA
    Bioorg Med Chem 20:4451-61. 2012
  5. pmc Modulation of protein-protein interactions as a therapeutic strategy for the treatment of neurodegenerative tauopathies
    C Ballatore
    Department of Chemistry, School of Arts and Sciences, University of Pennsylvania, 231 South 34th St, Philadelphia, PA 19104 6323, USA
    Curr Top Med Chem 11:317-30. 2011
  6. pmc Discovery of brain-penetrant, orally bioavailable aminothienopyridazine inhibitors of tau aggregation
    Carlo Ballatore
    Department of Chemistry, School of Arts and Sciences, University of Pennsylvania, 231 South 34th Street, Philadelphia, Pennsylvania 19104 6323, USA
    J Med Chem 53:3739-47. 2010
  7. pmc Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonists
    Carlo Ballatore
    Department of Chemistry, School of Arts and Sciences, University of Pennsylvania, 231 South 34th Street, Philadelphia, Pennsylvania 19104 6323, United States
    J Med Chem 54:6969-83. 2011
  8. pmc In situ blood-brain barrier permeability of a C-10 paclitaxel carbamate
    Carlo Ballatore
    Center for Neurodegenerative Diseases Research, Institute on Aging, University of Pennsylvania, 3600 Spruce Street, Philadelphia, PA 19104 6323, USA
    Bioorg Med Chem Lett 18:6119-21. 2008
  9. pmc Paclitaxel C-10 carbamates: potential candidates for the treatment of neurodegenerative tauopathies
    Carlo Ballatore
    Department of Chemistry, University of Pennsylvania, 231 South 34th St, Philadelphia, PA 19104 6323, USA
    Bioorg Med Chem Lett 17:3642-6. 2007
  10. pmc 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
    Bin Zhang
    Center for Neurodegenerative Disease Research, Institute on Aging and Department of Pathology and Laboratory Medicine, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    J Neurosci 32:3601-11. 2012

Collaborators

Detail Information

Publications24

  1. doi request reprint Aminothienopyridazines as imaging probes of tau pathology: a patent evaluation of WO2013090497
    Carlo Ballatore
    University of Pennsylvania, Perelman School of Medicine, Center for Neurodegenerative Disease Research, 3600 Spruce Street, Philadelphia, PA 19104 6323, USA
    Expert Opin Ther Pat 24:355-60. 2014
    ..Moreover, examples of this class of compounds exhibit absorption, distribution, metabolism, excretion and pharmacokinetics (ADME-PK) properties that are appropriate for CNS PET ligands. ..
  2. pmc Carboxylic acid (bio)isosteres in drug design
    Carlo Ballatore
    Department of Chemistry, University of Pennsylvania, 231 South 34th St, Philadelphia, PA 19104, USA
    ChemMedChem 8:385-95. 2013
    ..The goal of this Minireview is to provide an overview of the most commonly employed carboxylic acid (bio)isosteres and to present representative examples demonstrating the use and utility of each isostere in drug design...
  3. pmc Microtubule stabilizing agents as potential treatment for Alzheimer's disease and related neurodegenerative tauopathies
    Carlo Ballatore
    Department of Chemistry, School of Arts and Sciences, University of Pennsylvania, 231 South 34th Street, Philadelphia, Pennsylvania 19104 6323, United States
    J Med Chem 55:8979-96. 2012
    ....
  4. doi request reprint Aminothienopyridazine inhibitors of tau aggregation: evaluation of structure-activity relationship leads to selection of candidates with desirable in vivo properties
    Carlo Ballatore
    Department of Chemistry, University of Pennsylvania, 231 South 34th Street, Philadelphia, PA 19104 6323, USA
    Bioorg Med Chem 20:4451-61. 2012
    ..The latter studies revealed that this compound is well-tolerated with no notable side-effects at an oral dose of 50mg/kg/day...
  5. pmc Modulation of protein-protein interactions as a therapeutic strategy for the treatment of neurodegenerative tauopathies
    C Ballatore
    Department of Chemistry, School of Arts and Sciences, University of Pennsylvania, 231 South 34th St, Philadelphia, PA 19104 6323, USA
    Curr Top Med Chem 11:317-30. 2011
    ....
  6. pmc Discovery of brain-penetrant, orally bioavailable aminothienopyridazine inhibitors of tau aggregation
    Carlo Ballatore
    Department of Chemistry, School of Arts and Sciences, University of Pennsylvania, 231 South 34th Street, Philadelphia, Pennsylvania 19104 6323, USA
    J Med Chem 53:3739-47. 2010
    ..Taken together, these results suggest that examples from the ATPZ class hold promise as candidates for in vivo efficacy studies in animal models of neurodegenerative tauopathies...
  7. pmc Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonists
    Carlo Ballatore
    Department of Chemistry, School of Arts and Sciences, University of Pennsylvania, 231 South 34th Street, Philadelphia, Pennsylvania 19104 6323, United States
    J Med Chem 54:6969-83. 2011
    ..Given the combination of the relatively strong acidity, tunable lipophilicity, and versatility of the structure, the cyclopentane-1,3-dione moiety may constitute a valuable addition to the palette of carboxylic acid isosteres...
  8. pmc In situ blood-brain barrier permeability of a C-10 paclitaxel carbamate
    Carlo Ballatore
    Center for Neurodegenerative Diseases Research, Institute on Aging, University of Pennsylvania, 3600 Spruce Street, Philadelphia, PA 19104 6323, USA
    Bioorg Med Chem Lett 18:6119-21. 2008
    ..Further studies however are needed to evaluate the therapeutic potential of the C-10 carbamates paclitaxel derivatives for the treatment of CNS diseases...
  9. pmc Paclitaxel C-10 carbamates: potential candidates for the treatment of neurodegenerative tauopathies
    Carlo Ballatore
    Department of Chemistry, University of Pennsylvania, 231 South 34th St, Philadelphia, PA 19104 6323, USA
    Bioorg Med Chem Lett 17:3642-6. 2007
    ....
  10. pmc 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
    Bin Zhang
    Center for Neurodegenerative Disease Research, Institute on Aging and Department of Pathology and Laboratory Medicine, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    J Neurosci 32:3601-11. 2012
    ..These data reveal that brain-penetrant MT-stabilizing drugs hold promise for the treatment of AD and related tauopathies, and that EpoD could be a candidate for clinical testing...
  11. pmc The characterization of microtubule-stabilizing drugs as possible therapeutic agents for Alzheimer's disease and related tauopathies
    Kurt R Brunden
    Center for Neurodegenerative Disease Research and Institute on Aging, Department of Pathology and Laboratory Medicine, School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, United States
    Pharmacol Res 63:341-51. 2011
    ....
  12. pmc Brain-penetrant microtubule-stabilizing compounds as potential therapeutic agents for tauopathies
    Kurt R Brunden
    Center for Neurodegenerative Disease Research, Department of Pathology and Laboratory Medicine, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA
    Biochem Soc Trans 40:661-6. 2012
    ..Importantly, no adverse side effects were observed in the EpoD-treated mice. These results suggest that EpoD might be a viable drug candidate for the treatment of AD and related tauopathies...
  13. pmc Tau-directed drug discovery for Alzheimer's disease and related tauopathies: a focus on tau assembly inhibitors
    Kurt R Brunden
    Center for Neurodegenerative Disease Research, Institute on Aging, and Department of Pathology and Laboratory Medicine, University of Pennsylvania School of Medicine, Philadelphia, PA 19104, USA
    Exp Neurol 223:304-10. 2010
    ..We briefly review recent advances in tau-based drug discovery, with an emphasis on the identification of compounds that inhibit the assembly of tau into multimers and fibrils...
  14. pmc Aminothienopyridazines and methylene blue affect Tau fibrillization via cysteine oxidation
    Alex Crowe
    Center for Neurodegenerative Disease Research, Department of Pathology and Laboratory Medicine, Perelman School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    J Biol Chem 288:11024-37. 2013
    ..These findings reveal that the ATPZs and methylene blue act by a mechanism that may affect their viability as potential therapeutic agents...
  15. pmc Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathy
    Kurt R Brunden
    Center for Neurodegenerative Disease Research, Department of Pathology and Laboratory Medicine, School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    J Neurosci 30:13861-6. 2010
    ..These results suggest that certain brain-penetrant MT-stabilizing agents might provide a viable therapeutic strategy for the treatment of AD and FTDs...
  16. pmc Brain-penetrant tetrahydronaphthalene thromboxane A2-prostanoid (TP) receptor antagonists as prototype therapeutics for Alzheimer's disease
    James H Soper
    Center for Neurodegenerative Disease Research, Institute on Aging, Perlman School of Medicine, University of Pennsylvania, 3600 Spruce Street, Philadelphia, Pennsylvania, 19104 6323
    ACS Chem Neurosci 3:928-40. 2012
    ..Compounds of this type hold promise as potential lead structures to develop drug candidates for the treatment of AD...
  17. pmc High throughput screening for small molecule inhibitors of heparin-induced tau fibril formation
    Alex Crowe
    Center for Neurodegenerative Disease Research, Institute on Aging, University of Pennsylvania, 3600 Spruce Street, Philadelphia, PA 19104, USA
    Biochem Biophys Res Commun 358:1-6. 2007
    ..This study delineates focused strategies for HTS of tau fibrillization inhibitors that are relevant to drug discovery for Alzheimer's disease and related tauopathies...
  18. pmc Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening
    Alex Crowe
    Center for Neurodegenerative Disease Research, Institute on Aging, and Department of Pathology and Laboratory Medicine, School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    Biochemistry 48:7732-45. 2009
    ..Thus, the ATPZ molecules described here represent a novel class of tau assembly inhibitors that merit further development for testing in animal models of AD-like tau pathology...
  19. ncbi request reprint Tau-mediated neurodegeneration in Alzheimer's disease and related disorders
    Carlo Ballatore
    Center for Neurodegenerative Disease Research, Department of Pathology and Laboratory Medicine, University of Pennsylvania, 3600 Spruce Street, Philadelphia, Pennsylvania 19104 4283, USA
    Nat Rev Neurosci 8:663-72. 2007
    ....
  20. pmc Solid phase synthesis of 2-aminobenzothiazoles
    Francesco Piscitelli
    Department of Chemistry, University of Pennsylvania, 231 South 34th St, Philadelphia, PA 19104 6323, United States
    Bioorg Med Chem Lett 20:644-8. 2010
    ..A small, focused library of 2-aminobenzothiazoles was prepared...
  21. ncbi request reprint The design, synthesis, and evaluation of two universal doxorubicin-linkers: preparation of conjugates that retain topoisomerase II activity
    Chengzao Sun
    Acidophil, LLC, Suite 250, 10835 Road to the Cure, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 16:104-7. 2006
    ..Seven DOX-amino acid conjugates were prepared, each displaying similar inhibitory activity as the parent drug...
  22. ncbi request reprint Kinase-mediated trapping of bi-functional conjugates of paclitaxel or vinblastine with thymidine in cancer cells
    Simon E Aspland
    Acidophil LLC, 2330 W Joppa Road, Suite 330, Lutherville, MD 21093, USA
    Bioorg Med Chem Lett 16:5194-8. 2006
    ..This work provides the first account of 'kinase-mediated trapping' of cancer therapeutics...
  23. ncbi request reprint Targeting heat shock proteins on cancer cells: selection, characterization, and cell-penetrating properties of a peptidic GRP78 ligand
    Youngsoo Kim
    The Skaggs Institute for Chemical Biology and Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037, USA
    Biochemistry 45:9434-44. 2006
    ..In summary, the data presented suggest that cyclic peptide Pep42 might be a powerful tool in the construction of drug conjugates designed to selectively kill malignant cancer cells...
  24. ncbi request reprint A facile route to paclitaxel C-10 carbamates
    Carlo Ballatore
    Acidophil, LLC, Suite 250, 10835 Road to the Cure, San Diego, CA 92121, USA
    Bioorg Med Chem Lett 15:2477-80. 2005
    ..This method is effective for the synthesis of paclitaxel C-10 derivatives, including bifunctional molecules...