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1. Full Text Tau-mediated neurodegeneration in Alzheimer's disease and related disorders
by Lee, Virginia M.-Y and Trojanowski, John Q and Ballatore, Carlo
Nature Reviews Neuroscience, ISSN 1471-003X, 09/2007, Volume 8, Issue 9, pp. 663 - 672
Advances in our understanding of the mechanisms of tau- mediated neurodegeneration in Alzheimer's disease ( AD) and related tauopathies, which are... 
NEUROFIBRILLARY TANGLES | O-GLCNACYLATION | PROTEIN AGGREGATION | P301L TAU | MOUSE MODEL | IN-VIVO | PAIRED HELICAL FILAMENTS | PROMINENT AXONOPATHY | AXONAL-TRANSPORT | NEUROSCIENCES | TRANSGENIC ANIMAL-MODELS | Tauopathies - metabolism | Animals | tau Proteins - genetics | Models, Biological | tau Proteins - physiology | Humans | Alzheimer Disease - metabolism | Tauopathies - pathology | Nerve Degeneration | Alzheimer Disease - pathology | Physiological aspects | Research | Alzheimer's disease | Amyloid beta-protein
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2. Full Text Carboxylic Acid (Bio)Isosteres in Drug Design
by Ballatore, Carlo and Huryn, Donna M and Smith, Amos B
ChemMedChem, ISSN 1860-7179, 03/2013, Volume 8, Issue 3, pp. 385 - 395
The carboxylic acid functional group can be an important constituent of a pharmacophore, however, the presence of this moiety can also be responsible for... 
bioisosteres | drug design | isosteric replacement | carboxylic acids | Drug design | Carboxylic acids | Bioisosteres | Isosteric replacement | ANGIOTENSIN-II RECEPTOR | CHEMISTRY, MEDICINAL | HYDROXAMIC ACIDS | THIOIBOTENIC ACID | 3-ISOXAZOLOL GABA(A) ANTAGONISTS | TETRAMIC ACIDS | GLYCINE SITE | NMDA ANTAGONISTS | MEDICINAL CHEMISTRY | GLUTAMATE RECEPTORS | PHARMACOLOGY & PHARMACY | IBOTENIC ACID | Furans - metabolism | Sulfonamides - chemistry | Azoles - metabolism | Hydroxamic Acids - chemistry | Phosphorous Acids - metabolism | Sulfonic Acids - metabolism | Azoles - chemistry | Hydroxamic Acids - metabolism | Sulfonic Acids - chemistry | Phosphorous Acids - chemistry | Furans - chemistry | Carboxylic Acids - chemistry | Drug Design | Ketones - chemistry | Sulfonamides - metabolism | Carboxylic Acids - metabolism | Kinetics | Ketones - metabolism | Organic acids | Analytical chemistry | Acids | Index Medicus
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3. Full Text 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
by Penazzi, Lorène and Tackenberg, Christian and Ghori, Adnan and Golovyashkina, Nataliya and Niewidok, Benedikt and Selle, Karolin and Ballatore, Carlo and Smith, Amos B and Bakota, Lidia and Brandt, Roland
Neuropharmacology, ISSN 0028-3908, 06/2016, Volume 105, pp. 84 - 95
Dendritic spines represent the major postsynaptic input of excitatory synapses. Loss of spines and changes in their morphology correlate with cognitive... 
Epothilone | Dendritic spine | Amyloid beta | Alzheimer's disease | Microtubules | ALZHEIMERS-DISEASE | SYNAPTIC PLASTICITY | NEUROSCIENCES | WILD-TYPE TAU | DENDRITIC SPINES | DYNAMIC MICROTUBULES | TAU TRANSGENIC MICE | MUSHROOM SPINES | AMYLOID-BETA | PHARMACOLOGY & PHARMACY | LIVING NEURONS | COGNITIVE DEFICITS | Tubulin Modulators - pharmacology | Mice, Inbred C57BL | Cells, Cultured | Nocodazole - pharmacology | Epothilones - pharmacology | Rats | Mice, Transgenic | Hippocampus - pathology | Hippocampus - drug effects | PC12 Cells | Alzheimer Disease - pathology | Amyloid beta-Protein Precursor - genetics | Animals | Dendritic Spines - drug effects | Dendritic Spines - pathology | Amyloid beta-Protein Precursor - metabolism | Diamines - pharmacology | Mice | Thiazoles - pharmacology | Alzheimer Disease - genetics
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4. Full Text Brain‐Penetrant Triazolopyrimidine and Phenylpyrimidine Microtubule Stabilizers as Potential Leads to Treat Human African Trypanosomiasis
by Monti, Ludovica and Wang, Steven C and Oukoloff, Killian and Smith, Amos B and Brunden, Kurt R and Caffrey, Conor R and Ballatore, Carlo
ChemMedChem, ISSN 1860-7179, 09/2018, Volume 13, Issue 17, pp. 1751 - 1754
In vitro whole‐organism screens of Trypanosoma brucei with representative examples of brain‐penetrant microtubule (MT)‐stabilizing agents identified lethal... 
triazolopyrimidines | human African trypanosomiasis | microtubules | Trypanosoma brucei | phenylpyrimidines | FUNGICIDAL ACTIVITY | CHEMISTRY, MEDICINAL | BRUCEI-GAMBIENSE TRYPANOSOMIASIS | ALZHEIMERS-DISEASE | ANTICANCER AGENTS | DRUG DISCOVERY | IDENTIFICATION | IN-VITRO | MELARSOPROL | TAXOL | PHARMACOLOGY & PHARMACY | TUBULIN | Trypanosomiasis | Lubrication and lubricants | Vector-borne diseases | Stabilizers (agents) | Brain | Tubulin | Pharmacology | Bioavailability | Screens | African trypanosomiasis | Mammalian cells | Triazolopyrimidine | Human African Trypanosomiasis | Microtubules
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5. Full Text 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
by Zhang, Bin and Carroll, Jenna and Trojanowski, John Q and Yao, Yuemang and Iba, Michiyo and Potuzak, Justin S and Hogan, Anne-Marie L and Xie, Sharon X and Ballatore, Carlo and Smith III, Amos B and Lee, Virginia M.-Y and Brunden, Kurt R
Journal of Neuroscience, ISSN 0270-6474, 03/2012, Volume 32, Issue 11, pp. 3601 - 3611
Neurodegenerative tauopathies, such as Alzheimer's disease (AD), are characterized by insoluble deposits of hyperphosphorylated tau protein within brain... 
NEUROFIBRILLARY TANGLES | WATER MAZE | TRANSPORT | MOUSE MODEL | IN-VIVO | NEURODEGENERATIVE TAUOPATHIES | DISEASE | HUMAN-BRAIN | SPATIAL MEMORY | BARNES MAZE | NEUROSCIENCES | Tubulin Modulators - pharmacology | Humans | Aging - drug effects | Epothilones - pharmacology | Tauopathies - pathology | Male | Epothilones - therapeutic use | Neurotoxicity Syndromes - drug therapy | Alzheimer Disease - pathology | Neurotoxicity Syndromes - psychology | tau Proteins - genetics | Neurotoxicity Syndromes - pathology | Microtubules - drug effects | Tauopathies - psychology | Alzheimer Disease - psychology | Cognition Disorders - psychology | Cognition Disorders - pathology | Alzheimer Disease - drug therapy | Axons - drug effects | Aging - psychology | Mice, Transgenic | Cognition Disorders - drug therapy | Microtubules - pathology | Tubulin Modulators - therapeutic use | Aging - pathology | Animals | Axons - pathology | Mice | Tauopathies - drug therapy
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6. Full Text Microtubule stabilizing agents as potential treatment for alzheimers disease and related neurodegenerative tauopathies
by Ballatore, Carlo and Brunden, Kurt R and Huryn, Donna M and Trojanowski, John Q and Lee, Virginia M.-Y and Smith, Amos B
Journal of Medicinal Chemistry, ISSN 0022-2623, 11/2012, Volume 55, Issue 21, pp. 8979 - 8996
The microtubule (MT) associated protein tau, which is highly expressed in the axons of neurons, is an endogenous MT-stabilizing agent that plays an important... 
CHEMISTRY, MEDICINAL | LACTAM SYNTHON METHOD | TAU TRANSGENIC MICE | GRAM-SCALE SYNTHESIS | IN-VIVO | RESISTANT CELL-LINES | HUMAN CANCER-CELLS | BLOOD-BRAIN-BARRIER | MARINE SPONGE ORIGIN | ENANTIOSELECTIVE TOTAL-SYNTHESIS | P-GLYCOPROTEIN | Axonal Transport | Humans | Alzheimer Disease - drug therapy | Tauopathies - pathology | tau Proteins - metabolism | Microtubules - pathology | Molecular Targeted Therapy | Alzheimer Disease - pathology | Blood-Brain Barrier - metabolism | Biological Products - chemistry | Tauopathies - metabolism | Animals | Microtubules - drug effects | Alzheimer Disease - metabolism | Tauopathies - drug therapy | Biological Products - therapeutic use
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7. Full Text Microtubule-stabilizing agents as potential therapeutics for neurodegenerative disease
by Brunden, Kurt R and Trojanowski, John Q and Smith, Amos B and Lee, Virginia M.-Y and Ballatore, Carlo
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 09/2014, Volume 22, Issue 18, pp. 5040 - 5049
Microtubules (MTs), cytoskeletal elements found in all mammalian cells, play a significant role in cell structure and in cell division. They are especially... 
Axon | Transport | Neurodegeneration | Microtubules | Paclitaxel | CHEMISTRY, MEDICINAL | ALZHEIMERS-DISEASE | BIOCHEMISTRY & MOLECULAR BIOLOGY | TUBULIN POLYMERIZATION | CHEMISTRY, ORGANIC | AMYOTROPHIC-LATERAL-SCLEROSIS | ALPHA-SYNUCLEIN | HUNTINGTIN-ASSOCIATED PROTEIN-1 | IN-VITRO | TAU TRANSGENIC MICE | PAIRED HELICAL FILAMENTS | FAST AXONAL-TRANSPORT | LINKED SOD1 MUTANTS | Microtubules - metabolism | Tubulin Modulators - chemistry | Animals | Microtubules - drug effects | Tubulin Modulators - pharmacology | Humans | Molecular Structure | Structure-Activity Relationship | Neurodegenerative Diseases - metabolism | Neurodegenerative Diseases - drug therapy | Tubulin Modulators - therapeutic use
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8. Full Text Structure Property Relationships of Carboxylic Acid Isosteres
by Lassalas, Pierrik and Gay, Bryant and Lasfargeas, Caroline and James, Michael J and Tran, Van and Vijayendran, Krishna G and Brunden, Kurt R and Kozlowski, Marisa C and Thomas, Craig J and Smith, Amos B and Huryn, Donna M and Ballatore, Carlo
Journal of Medicinal Chemistry, ISSN 0022-2623, 04/2016, Volume 59, Issue 7, pp. 3183 - 3203
The replacement of a carboxylic acid with a surrogate structure, or (bio)-isostere, is a classical strategy in medicinal chemistry. The general underlying... 
MEDICINAL CHEMISTRY | CHEMISTRY, MEDICINAL | ASYMMETRIC-SYNTHESIS | RECEPTOR ANTAGONISTS | HYDROXAMIC ACIDS | DRUG DESIGN | BIOISOSTERES | PROTEIN-BINDING | INHIBITORS | TETRAZOLE | DERIVATIVES | Carboxylic Acids - chemistry | Mass Spectrometry | Phenylpropionates - chemistry | Plasma - chemistry | Models, Molecular | Molecular Structure | Plasma - drug effects | Structure-Activity Relationship | Chemistry, Pharmaceutical
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9. Full Text 1,2,4-Triazolo[1,5-a]pyrimidines in drug design
by Oukoloff, Killian and Lucero, Bobby and Francisco, Karol R and Brunden, Kurt R and Ballatore, Carlo
European Journal of Medicinal Chemistry, ISSN 0223-5234, 03/2019, Volume 165, pp. 332 - 346
The 1,2,4-triazolo[1,5-a]pyrimidine (TP) heterocycle, in spite of its relatively simple structure, has proved to be remarkably versatile as evidenced by its... 
1,2,4-triazolo[1,5-a]pyrimidine | Medicinal chemistry | Heterocyclic chemistry | BEARING BRIDGEHEAD NITROGEN | MYCOBACTERIUM-TUBERCULOSIS | CHEMISTRY, MEDICINAL | ALZHEIMERS-DISEASE | LEAD OPTIMIZATION | DIHYDROOROTATE DEHYDROGENASE INHIBITORS | MICROTUBULE-STABILIZING AGENT | ACETOHYDROXYACID SYNTHASE INHIBITORS | SMALL-MOLECULE INHIBITORS | INFLUENZA-VIRUS POLYMERASE | RNA-POLYMERASE | Medical colleges | Pyrimidines | Lysine | Parasitic diseases
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10. Full Text Altered microtubule dynamics in neurodegenerative disease: Therapeutic potential of microtubule-stabilizing drugs
by Brunden, Kurt R and Lee, Virginia M-Y and Smith, Amos B and Trojanowski, John Q and Ballatore, Carlo
Neurobiology of Disease, ISSN 0969-9961, 09/2017, Volume 105, pp. 328 - 335
Many neurodegenerative diseases are characterized by deficiencies in neuronal axonal transport, a process in which cellular cargo is shuttled with the aid of... 
Axons | Traumatic brain injury | Neurodegeneration | Microtubules | Amyotrophic lateral sclerosis | Frontotemporal lobar degeneration | Transport | Alzheimer | Parkinson | NEUROFIBRILLARY TANGLES | ALZHEIMERS-DISEASE | AXONAL-TRANSPORT DEFECTS | ALPHA-SYNUCLEIN | DOPAMINERGIC-NEURONS | NEUROSCIENCES | EPOTHILONE D | TAU-HYPERPHOSPHORYLATION | PAIRED HELICAL FILAMENTS | BRAIN-PENETRANT | TRANSGENIC MOUSE MODEL | Microtubules - metabolism | Tubulin Modulators - chemistry | Animals | Microtubules - drug effects | Tubulin Modulators - pharmacology | Humans | Neurodegenerative Diseases - metabolism | Neurodegenerative Diseases - drug therapy | Tubulin Modulators - therapeutic use | Drugs | Brain | Nervous system diseases | Health aspects | Injuries | Medical research | Medical colleges | Neurons | Medicine, Experimental | Superoxide | Chronic brain injury | Alzheimer's disease | Amyotrophic Lateral Sclerosis | Traumatic Brain Injury | Frontotemporal Lobar Degeneration
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11. Full Text Aminothienopyridazines and methylene blue affect Tau fibrillization via cysteine oxidation
by Crowe, Alex and James, Michael J and Virginia M.-Y. Lee, M.-Y. Lee and Smith III, Amos B and Trojanowski, John Q and Ballatore, Carlo and Brunden, Kurt R
Journal of Biological Chemistry, ISSN 0021-9258, 04/2013, Volume 288, Issue 16, pp. 11024 - 11037
Alzheimer disease and several other neurodegenerative disorders are characterized by the accumulation of intraneuronal fibrils comprised of the protein Tau.... 
IN-VITRO | INHIBITION | PEPTIDES | DEMENTIA | ALZHEIMERS-DISEASE | BIOCHEMISTRY & MOLECULAR BIOLOGY | PAIRED HELICAL FILAMENTS | NEURODEGENERATION | MICROTUBULE-ASSOCIATED PROTEIN | AGGREGATION | DISCOVERY | Multiprotein Complexes - metabolism | Multiprotein Complexes - chemistry | tau Proteins - genetics | Oxidation-Reduction | Humans |