PROTAC targeted protein degraders: the past is prologue

M Békés, DR Langley, CM Crews - Nature Reviews Drug Discovery, 2022 - nature.com
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …

Advances in targeting 'undruggable'transcription factors with small molecules

MJ Henley, AN Koehler - Nature Reviews Drug Discovery, 2021 - nature.com
Transcription factors (TFs) represent key biological players in diseases including cancer,
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …

The AUTOTAC chemical biology platform for targeted protein degradation via the autophagy-lysosome system

CH Ji, HY Kim, MJ Lee, AJ Heo, DY Park, S Lim… - Nature …, 2022 - nature.com
Targeted protein degradation allows targeting undruggable proteins for therapeutic
applications as well as eliminating proteins of interest for research purposes. While several …

Ubiquitin signalling in neurodegeneration: mechanisms and therapeutic opportunities

MF Schmidt, ZY Gan, D Komander… - Cell Death & …, 2021 - nature.com
Neurodegenerative diseases are characterised by progressive damage to the nervous
system including the selective loss of vulnerable populations of neurons leading to motor …

Targeted protein degradation: expanding the toolbox

M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …

PROTACs: great opportunities for academia and industry

X Sun, H Gao, Y Yang, M He, Y Wu, Y Song… - Signal transduction and …, 2019 - nature.com
Although many kinds of therapies are applied in the clinic, drug-resistance is a major and
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …

PROTACs: an emerging therapeutic modality in precision medicine

DA Nalawansha, CM Crews - Cell chemical biology, 2020 - cell.com
Targeted protein degradation (TPD) has emerged as an exciting new era in chemical
biology and drug discovery. PROteolysis TArgeting Chimera (PROTAC) technology targets …

Revisiting the grammar of Tau aggregation and pathology formation: how new insights from brain pathology are shaping how we study and target Tauopathies

G Limorenko, HA Lashuel - Chemical Society Reviews, 2022 - pubs.rsc.org
Converging evidence continues to point towards Tau aggregation and pathology formation
as central events in the pathogenesis of Alzheimer's disease and other Tauopathies …

Tau: Enabler of diverse brain disorders and target of rapidly evolving therapeutic strategies

CW Chang, E Shao, L Mucke - Science, 2021 - science.org
BACKGROUND The microtubule-associated protein tau has been implicated in the
pathogenesis of Alzheimer's disease and a range of other neurodegenerative disorders …

Proteolysis-targeting chimeras as therapeutics and tools for biological discovery

GM Burslem, CM Crews - Cell, 2020 - cell.com
New biological tools provide new techniques to probe fundamental biological processes.
Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which …