[HTML][HTML] Deubiquitinase-targeting chimeras for targeted protein stabilization

NJ Henning, L Boike, JN Spradlin, CC Ward… - Nature chemical …, 2022 - nature.com
Many diseases are driven by proteins that are aberrantly ubiquitinated and degraded. These
diseases would be therapeutically benefited by targeted protein stabilization (TPS). Here we …

E3 ligase ligands for PROTACs: how they were found and how to discover new ones

T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …

[HTML][HTML] 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 …

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 …

[HTML][HTML] Mapping the degradable kinome provides a resource for expedited degrader development

KA Donovan, FM Ferguson, JW Bushman, NA Eleuteri… - Cell, 2020 - cell.com
Targeted protein degradation (TPD) refers to the use of small molecules to induce ubiquitin-
dependent degradation of proteins. TPD is of interest in drug development, as it can address …

[HTML][HTML] Current strategies for the design of PROTAC linkers: a critical review

RI Troup, C Fallan, MGJ Baud - Exploration of Targeted Anti-tumor …, 2020 - ncbi.nlm.nih.gov
Abstract PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …

Targeted protein degradation by electrophilic PROTACs that stereoselectively and site-specifically engage DCAF1

Y Tao, D Remillard, EV Vinogradova… - Journal of the …, 2022 - ACS Publications
Targeted protein degradation induced by heterobifunctional compounds and molecular
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …

Recent developments in PROTAC‐mediated protein degradation: from bench to clinic

Z Hu, CM Crews - ChemBioChem, 2022 - Wiley Online Library
Abstract Proteolysis‐targeting chimeras (PROTACs), an emerging paradigm‐shifting
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …

[HTML][HTML] Expanding PROTACtable genome universe of E3 ligases

Y Liu, J Yang, T Wang, M Luo, Y Chen, C Chen… - Nature …, 2023 - nature.com
Proteolysis-targeting chimera (PROTAC) and other targeted protein degradation (TPD)
molecules that induce degradation by the ubiquitin-proteasome system (UPS) offer new …

[HTML][HTML] Major advances in targeted protein degradation: PROTACs, LYTACs, and MADTACs

SB Alabi, CM Crews - Journal of Biological Chemistry, 2021 - ASBMB
Of late, targeted protein degradation (TPD) has surfaced as a novel and innovative chemical
tool and therapeutic modality. By co-opting protein degradation pathways, TPD facilitates …