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 …

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 …

PROTACs: past, present and future

K Li, CM Crews - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules consisting of
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …

Stimuli-activatable PROTACs for precise protein degradation and cancer therapy

J Gao, L Yang, S Lei, F Zhou, H Nie, B Peng, T Xu… - Science bulletin, 2023 - Elsevier
The proteolysis targeting chimeras (PROTACs) approach has attracted extensive attention in
the past decade, which represents an emerging therapeutic modality with the potential to …

[HTML][HTML] PROteolysis TArgeting Chimeras (PROTACs)—past, present and future

M Pettersson, CM Crews - Drug Discovery Today: Technologies, 2019 - Elsevier
The majority of currently used therapeutics are small molecule-based and utilize occupancy-
driven pharmacology as the mode of action (MOA), in which the protein function is …

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 …

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 …

Enriching proteolysis targeting chimeras with a second modality: When two are better than one

A Salerno, F Seghetti, J Caciolla, E Uliassi… - Journal of Medicinal …, 2022 - ACS Publications
Proteolysis targeting chimera (PROTAC)-mediated protein degradation has prompted a
radical rethink and is at a crucial stage in driving a drug discovery transition. To fully harness …

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 …

Proteolysis-targeting chimera (PROTAC) delivery system: advancing protein degraders towards clinical translation

Y Chen, I Tandon, W Heelan, Y Wang… - Chemical Society …, 2022 - pubs.rsc.org
Proteolysis Targeting Chimeras (PROTACs), an emerging therapeutic entity designed to
degrade target proteins by hijacking the ubiquitin–proteasome system, have the potential to …