Research Topics
| Kurt R BrundenSummaryAffiliation: University of Pennsylvania Country: USA Publications
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Publications
Brain-penetrant microtubule-stabilizing compounds as potential therapeutic agents for tauopathiesKurt 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...- Tau-directed drug discovery for Alzheimer's disease and related tauopathies: a focus on tau assembly inhibitorsKurt 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... - Advances in tau-focused drug discovery for Alzheimer's disease and related tauopathiesKurt R Brunden
Center for Neurodegenerative Disease Research, Institute on Aging, Department of Pathology and Laboratory Medicine, School of Medicine, University of Pennsylvania, 3600 Spruce Street, Philadelphia, PA 19104 4283, USA
Nat Rev Drug Discov 8:783-93. 2009..Here, we focus on strategies directed at reducing misfolded tau and compensating for the loss of normal tau function... - The characterization of microtubule-stabilizing drugs as possible therapeutic agents for Alzheimer's disease and related tauopathiesKurt 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.... - Epothilone D improves microtubule density, axonal integrity, and cognition in a transgenic mouse model of tauopathyKurt 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... - The microtubule-stabilizing agent, epothilone D, reduces axonal dysfunction, neurotoxicity, cognitive deficits, and Alzheimer-like pathology in an interventional study with aged tau transgenic miceBin 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... 
Aminothienopyridazine inhibitors of tau aggregation: evaluation of structure-activity relationship leads to selection of candidates with desirable in vivo propertiesCarlo 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...- Discovery of brain-penetrant, orally bioavailable aminothienopyridazine inhibitors of tau aggregationCarlo 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... - Microtubule stabilizing agents as potential treatment for Alzheimer's disease and related neurodegenerative tauopathiesCarlo 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.... - Developing therapeutic approaches to tau, selected kinases, and related neuronal protein targetsVirginia M Y Lee
Center for Neurodegenerative Disease Research, Institute on Aging, Department of Pathology and Laboratory Medicine, School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
Cold Spring Harb Perspect Med 1:a006437. 2011..Finally, we discuss the challenges and potential benefits of tau-directed drug discovery programs... - Chronic stress exacerbates tau pathology, neurodegeneration, and cognitive performance through a corticotropin-releasing factor receptor-dependent mechanism in a transgenic mouse model of tauopathyJenna C Carroll
Center for Neurodegenerative Disease Research, Department of Pathology and Laboratory Medicine, School of Medicine and Institute on Aging, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
J Neurosci 31:14436-49. 2011..These studies also implicate CRF in AD pathophysiology and suggest that pharmacological manipulation of this neuropeptide may be a potential therapeutic strategy for AD... - Brain-penetrant tetrahydronaphthalene thromboxane A2-prostanoid (TP) receptor antagonists as prototype therapeutics for Alzheimer's diseaseJames 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... - Characterization of tau fibrillization in vitroShaohua Xu
The Center for Neurodegenerative Disease Research, Department of Pathology and Laboratory Medicine, and Institute on Aging, University of Pennsylvania School of Medicine, Philadelphia, USA
Alzheimers Dement 6:110-7. 2010..By using recombinant human tau, we have delineated events leading to the conversion of normal soluble tau into tau fibrils... - Effects of TNFalpha-converting enzyme inhibition on amyloid beta production and APP processing in vitro and in vivoMinkyu L Kim
Center for Neurodegenerative Disease Research, Department of Pathology and Laboratory Medicine, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104, USA
J Neurosci 28:12052-61. 2008..Accordingly, it is possible that TACE inhibitors could reduce TNFalpha levels without increasing Abeta levels within the AD brain... - A model for improving the treatment and care of Alzheimer's disease patients through interdisciplinary researchJohn Q Trojanowski
Institute on Aging, University of Pennsylvania, Philadelphia, PA, USA Center for Neurodegenerative Disease Research, University of Pennsylvania, Philadelphia, PA, USA Department of Pathology and Laboratory Medicine, Perelman School of Medicine, University of Pennsylvania, Philadelphia, PA, USA Electronic address
Alzheimers Dement 8:564-73. 2012..The "Ware-UPenn" program has been presented in this report as a useful prototype for partnerships between private philanthropy and academia in planning and developing programs to address a major national public health problem... - Cyclopentane-1,3-dione: a novel isostere for the carboxylic acid functional group. Application to the design of potent thromboxane (A2) receptor antagonistsCarlo 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... - Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screeningAlex 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... - Exogenous alpha-synuclein fibrils seed the formation of Lewy body-like intracellular inclusions in cultured cellsKelvin C Luk
Department of Pathology and Laboratory Medicine, University of Pennsylvania School of Medicine, Center for Neurodegenerative Disease Research, Institute on Aging, Philadelphia, PA 19104 4283, USA
Proc Natl Acad Sci U S A 106:20051-6. 2009.... - Evidence that non-fibrillar tau causes pathology linked to neurodegeneration and behavioral impairmentsKurt R Brunden
Department of Pathology and Laboratory Medicine, Center for Neurodegenerative Disease Research, School of Medicine, University of Pennsylvania, Philadelphia, PA 19104, USA
J Alzheimers Dis 14:393-9. 2008.... - Advancing Alzheimer's disease diagnosis, treatment, and care: recommendations from the Ware Invitational SummitMary D Naylor
Institute on Aging, University of Pennsylvania, Philadelphia, USA
Alzheimers Dement 8:445-52. 2012..The workgroups shared, discussed, and compiled an integrated set of priorities, recommendations, and action plans, which are presented in this article...