The PROTACtable genome

M Schneider, CJ Radoux, A Hercules… - Nature reviews Drug …, 2021 - nature.com
Proteolysis-targeting chimeras (PROTACs) are an emerging drug modality that may offer
new opportunities to circumvent some of the limitations associated with traditional small …

PROTAC degraders as chemical probes for studying target biology and target validation

V Němec, MP Schwalm, S Müller… - Chemical Society Reviews, 2022 - pubs.rsc.org
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …

Transforming targeted cancer therapy with PROTACs: A forward-looking perspective

W Farnaby, M Koegl, DB McConnell, A Ciulli - Current opinion in …, 2021 - Elsevier
Small-molecule targeted protein degraders have in recent years made a great impact on the
strategies of many industry and academic cancer research endeavours. We seek here to …

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 …

PROTACs: emerging targeted protein degradation approaches for advanced druggable strategies

NI Sincere, K Anand, S Ashique, J Yang, C You - Molecules, 2023 - mdpi.com
A potential therapeutic strategy to treat conditions brought on by the aberrant production of a
disease-causing protein is emerging for targeted protein breakdown using the PROTACs …

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 …

[HTML][HTML] Monitoring and deciphering protein degradation pathways inside cells

DL Daniels, KM Riching, M Urh - Drug Discovery Today: Technologies, 2019 - Elsevier
A new series of therapeutic modalities resulting in degradation of target proteins, termed
proteolysis targeting chimeras (PROTACs), hold significant therapeutic potential with …

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 …

PROTAC-DB 2.0: an updated database of PROTACs

G Weng, X Cai, D Cao, H Du, C Shen… - Nucleic acids …, 2023 - academic.oup.com
Proteolysis targeting chimeras (PROTACs), which harness the ubiquitin-proteasome system
to selectively induce targeted protein degradation, represent an emerging therapeutic …

[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 …