O5‐04‐05: A NEW THERAPEUTIC STRATEGY FOR TAUOPATHIES: DISCOVERY OF HIGHLY POTENT BRAIN PENETRANT PROTAC<sup>TM</sup> DEGRADER MOLECULES THAT TARGET PATHOLOGIC TAU PROTEIN SPECIES

Cacace, Angela; Chandler, Julian; Flanagan, John J.; Berlin, Michael; Cadelina, Gregory; Pizzano, Jennifer; Bookbinder, Mark; Crews, CM; Crew, Andrew P.; Taylor, I; Houston, John

doi:10.1016/j.jalz.2019.06.4856

Cited by 2 publications

(1 citation statement)

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“…Based on the abstract of a scientific meeting, Arvinas, Inc. appears to have discovered small‐molecular PROTACs that potently degrade pathologic tau species in tauopathy mice [64] . Notably, these PROTACs can be administered peripherally and cross the BBB to show activity.…”

Section: Proteolysis‐targeting Chimeras For Nds Therapymentioning

confidence: 99%

PROTACs and Other Chemical Protein Degradation Technologies for the Treatment of Neurodegenerative Disorders

Tomoshige

Ishikawa

2020

Angewandte Chemie

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Neurodegenerative disorders (NDs) are a group of diseases that cause neural cell damage, leading to motility and/or cognitive dysfunctions. One of the causative agents is misfolded protein aggregates, which are considered as undruggable in terms of conventional tools, such as inhibitors and agonists/antagonists. Indeed, there is currently no FDA‐approved drug for the causal treatment of NDs. However, emerging technologies for chemical protein degradation are opening up the possibility of selective elimination of target proteins through physiological protein degradation machineries, which do not depend on the functions of the target proteins. Here, we review recent efforts towards the treatment of NDs using chemical protein degradation technologies, and we briefly discuss the challenges and prospects.

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Section: Proteolysis‐targeting Chimeras For Nds Therapymentioning

confidence: 99%

PROTACs and Other Chemical Protein Degradation Technologies for the Treatment of Neurodegenerative Disorders

Tomoshige

Ishikawa

2020

Angewandte Chemie

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PROTACs and Other Chemical Protein Degradation Technologies for the Treatment of Neurodegenerative Disorders

Tomoshige

Ishikawa

2020

Angew Chem Int Ed

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O5‐04‐05: A NEW THERAPEUTIC STRATEGY FOR TAUOPATHIES: DISCOVERY OF HIGHLY POTENT BRAIN PENETRANT PROTAC^TM DEGRADER MOLECULES THAT TARGET PATHOLOGIC TAU PROTEIN SPECIES

Cited by 2 publications

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PROTACs and Other Chemical Protein Degradation Technologies for the Treatment of Neurodegenerative Disorders

PROTACs and Other Chemical Protein Degradation Technologies for the Treatment of Neurodegenerative Disorders

PROTACs and Other Chemical Protein Degradation Technologies for the Treatment of Neurodegenerative Disorders

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O5‐04‐05: A NEW THERAPEUTIC STRATEGY FOR TAUOPATHIES: DISCOVERY OF HIGHLY POTENT BRAIN PENETRANT PROTACTM DEGRADER MOLECULES THAT TARGET PATHOLOGIC TAU PROTEIN SPECIES

Cited by 2 publications

References 0 publications

PROTACs and Other Chemical Protein Degradation Technologies for the Treatment of Neurodegenerative Disorders

PROTACs and Other Chemical Protein Degradation Technologies for the Treatment of Neurodegenerative Disorders

PROTACs and Other Chemical Protein Degradation Technologies for the Treatment of Neurodegenerative Disorders

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Product

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O5‐04‐05: A NEW THERAPEUTIC STRATEGY FOR TAUOPATHIES: DISCOVERY OF HIGHLY POTENT BRAIN PENETRANT PROTAC^TM DEGRADER MOLECULES THAT TARGET PATHOLOGIC TAU PROTEIN SPECIES