[PDF][PDF] Targeted protein degradation: A promise for undruggable proteins

KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
Summary Protein homeostasis, or" proteostasis," is indispensable for a balanced, healthy
environment within the cell. However, when natural proteostasis mechanisms are …

Targeted protein degradation: elements of PROTAC design

SL Paiva, CM Crews - Current opinion in chemical biology, 2019 - Elsevier
Targeted protein degradation using Proteolysis Targeting Chimeras (PROTACs) has
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …

Targeted protein degradation: mechanisms, strategies and application

L Zhao, J Zhao, K Zhong, A Tong, D Jia - Signal transduction and …, 2022 - nature.com
Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …

Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation

MJ Bond, CM Crews - RSC chemical biology, 2021 - pubs.rsc.org
With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …

[PDF][PDF] 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 …

[HTML][HTML] The rise and rise of protein degradation: opportunities and challenges ahead

SJ Hughes, A Testa, N Thompson, I Churcher - Drug Discovery Today, 2021 - Elsevier
The transformational mechanism of action underpinning targeted protein degradation
strategies, including proteolysis-targeting chimeras (PROTACs), gives potential for potent in …

Blocking non-enzymatic functions by PROTAC-mediated targeted protein degradation

D Sun, J Zhang, G Dong, S He… - Journal of Medicinal …, 2022 - ACS Publications
The non-enzymatic functions of target proteins play key roles in the regulation of various cell
signaling pathways and are closely related to numerous human diseases. However …

Targeted protein degradation in vivo with Proteolysis Targeting Chimeras: Current status and future considerations

GF Watt, P Scott-Stevens, L Gaohua - Drug Discovery Today: Technologies, 2019 - Elsevier
Proteolysis Targeting Chimeras (PROTACs) are a rapidly expanding new therapeutic
modality inducing selective protein degradation and offering the potential of a differentiated …

PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy

JM Kelm, DS Pandey, E Malin, H Kansou, S Arora… - Molecular Cancer, 2023 - Springer
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …

Proteolysis-targeting chimeras: induced protein degradation as a therapeutic strategy

P Ottis, CM Crews - ACS chemical biology, 2017 - ACS Publications
Until recently, the only ways to reduce specific protein signaling were to either knock down
the target by RNAi or to interfere with the signaling by inhibiting an enzyme or receptor …