scholarly journals Identification of pharmacodynamics readouts through acute dosing of a small molecule inhibitor of tau self‐association in a tauopathy mouse model

2021 ◽  
Vol 17 (S9) ◽  
Author(s):  
Dhruv R. Patel ◽  
Chaya Sussman ◽  
Mindy Greco ◽  
Edward H. Cheesman ◽  
Patricia Lopez ◽  
...  
Keyword(s):  
Mouse Model ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor ◽  
Self Association

scholarly journals In Vivo Validation of a Small Molecule Inhibitor of Tau Self-Association in htau Mice

2020 ◽  
Vol 73 (1) ◽  
pp. 147-161 ◽  
Author(s):  
Eliot J. Davidowitz ◽  
Pavan K. Krishnamurthy ◽  
Patricia Lopez ◽  
Heidy Jimenez ◽  
Leslie Adrien ◽  
...  
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor ◽  
Self Association ◽  
In Vivo Validation

Prevention of chemotherapy-induced peripheral neuropathy by the small-molecule inhibitor Pifithrin-mu in a mouse model

2015 ◽  
Vol 49 ◽  
pp. e25-e26
Author(s):  
K. Krukowski ◽  
C.H. Nijboer ◽  
X. Huo ◽  
M. Maj ◽  
A. Kavelaars ◽  
...  
Keyword(s):  
Peripheral Neuropathy ◽  
Mouse Model ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor

Abstract 4874: Small molecule inhibitor of ezrin inhibits metastasis in a transgenic mouse model of osteosarcoma

2012 ◽  
Author(s):  
Jared T. Murdoch ◽  
Sung-Hyeok Hong ◽  
Gulay Bulut ◽  
George W. Kosturko ◽  
Lauren E. Drebing ◽  
...  
Keyword(s):  
Mouse Model ◽  
Transgenic Mouse ◽  
Small Molecule ◽  
Transgenic Mouse Model ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor

P2-506: Efficacy and safety of systemic versus intracerebroventricular delivery of a β-secretase (BACE1) small molecule inhibitor in a mouse model of Alzheimer's disease

2011 ◽  
Vol 7 ◽  
pp. S474-S474
Author(s):  
Deepak Thakker ◽  
Sethu Sankaranarayanan ◽  
Marcy Weatherspoon ◽  
Jonathan Harrison ◽  
Maria Pierdomenico ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Mouse Model ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Efficacy And Safety ◽  
Model Of Alzheimer’S Disease ◽  
Molecule Inhibitor

scholarly journals The Small Molecule Inhibitor G6 Significantly Reduces Bone Marrow Fibrosis and the Mutant Burden in a Mouse Model of Jak2-Mediated Myelofibrosis

2012 ◽  
Vol 181 (3) ◽  
pp. 858-865 ◽  
Author(s):  
Annet Kirabo ◽  
Sung O. Park ◽  
Heather L. Wamsley ◽  
Meghanath Gali ◽  
Rebekah Baskin ◽  
...  
Keyword(s):  
Bone Marrow ◽  
Mouse Model ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Bone Marrow Fibrosis ◽  
Molecule Inhibitor ◽  
Marrow Fibrosis

scholarly journals A small molecule inhibitor of mutant IDH2 rescues cardiomyopathy in a D-2-hydroxyglutaric aciduria type II mouse model

2016 ◽  
Vol 39 (6) ◽  
pp. 807-820 ◽  
Author(s):  
Fang Wang ◽  
Jeremy Travins ◽  
Zhizhong Lin ◽  
Yaguang Si ◽  
Yue Chen ◽  
...  
Keyword(s):  
Mouse Model ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Type Ii ◽  
Molecule Inhibitor

Abstract 2949: YK-4-279 is a small molecule inhibitor of ETV1 and inhibits metastasis in a mouse model

2014 ◽  
Author(s):  
Said Rahim ◽  
Sarah Justvig ◽  
Sung-Hyeok Hong ◽  
Perrer Tosso ◽  
Haydar Celik ◽  
...  
Keyword(s):  
Mouse Model ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor

scholarly journals A small-molecule inhibitor of SOD1-Derlin-1 interaction ameliorates pathology in an ALS mouse model

2018 ◽  
Vol 9 (1) ◽  
Author(s):  
Naomi Tsuburaya ◽  
Kengo Homma ◽  
Tsunehiko Higuchi ◽  
Andrii Balia ◽  
Hiroyuki Yamakoshi ◽  
...  
Keyword(s):  
Mouse Model ◽  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Molecule Inhibitor

scholarly journals Suppressing aberrant phospholipase D1 signaling in 3xTg Alzheimer’s disease mouse model promotes synaptic resilience

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Krystyn Z. Bourne ◽  
Chandramouli Natarajan ◽  
Carlos X. Medina Perez ◽  
Batbayar Tumurbaatar ◽  
Giulio Taglialatela ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Mouse Model ◽  
Cognitive Decline ◽  
Small Molecule ◽  
Memory Deficits ◽  
Treated Group ◽  
Small Molecule Inhibitor ◽  
Synaptic Dysfunction ◽  
Early Stages ◽  
Molecule Inhibitor

AbstractCurrent approaches in treatment of Alzheimer’s disease (AD) is focused on early stages of cognitive decline. Identifying therapeutic targets that promote synaptic resilience during early stages may prevent progressive memory deficits by preserving memory mechanisms. We recently reported that the inducible isoform of phospholipase D (PLD1) was significantly increased in synaptosomes from post-mortem AD brains compared to age-matched controls. Using mouse models, we reported that the aberrantly elevated neuronal PLD1 is key for oligomeric amyloid driven synaptic dysfunction and underlying memory deficits. Here, we demonstrate that chronic inhibition using a well-tolerated PLD1 specific small molecule inhibitor is sufficient to prevent the progression of synaptic dysfunction during early stages in the 3xTg-AD mouse model. Firstly, we report prevention of cognitive decline in the inhibitor-treated group using novel object recognition (NOR) and fear conditioning (FC). Secondly, we provide electrophysiological assessment of better synaptic function in the inhibitor-treated group. Lastly, using Golgi staining, we report that preservation of dendritic spine integrity as one of the mechanisms underlying the action of the small molecule inhibitor. Collectively, these studies provide evidence for inhibition of PLD1 as a potential therapeutic strategy in preventing progression of cognitive decline associated with AD and related dementia.

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