Targeted protein degradation: expanding the toolbox

M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
… been explored in targeted protein degradation to date. In … targeted protein degradation and
review the major classes of E3 ligases that may be exploited to expand the PROTAC toolbox. …

Opportunities and challenges of protein-based targeted protein degradation

F Shen, LMK Dassama - Chemical Science, 2023 - pubs.rsc.org
… for targeting proteins, thereby expanding the scope of TPD platforms to include secreted …
Professor Laura MK Dassama is a chemical and structural biologist who uses tools of chemistry …

Targeted protein degradation: A promise for undruggable proteins

KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
Targeted Protein Degradation (TPD) strategies have also been explored to target previously
undruggable proteins… of the proteins targeted by PROTACs and the biological effects of their …

Development of targeted protein degradation therapeutics

PP Chamberlain, LG Hamann - Nature chemical biology, 2019 - nature.com
… validation and chemical tools to accelerate efforts in protein degradation. We anticipate …
Both small-molecule approaches to subverting E3 ligases offer an opportunity to expand the …

Targeted protein degradation: mechanisms, strategies and application

L Zhao, J Zhao, K Zhong, A Tong, D Jia - … transduction and targeted …, 2022 - nature.com
expanding the range of substrates. In this review, we first provide a simple introduction of
protein degradation … , will not only provide powerful tools for biomedical research, but hold great …

Advancing targeted protein degradation for cancer therapy

B Dale, M Cheng, KS Park, HÜ Kaniskan… - Nature Reviews …, 2021 - nature.com
… of the target protein. The broad … that target oncoproteins with tissue, tumour and subcellular
selectivity. In this Review, we first discuss the molecular basis of targeted protein degradation

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 …

The application of targeted protein degradation technologies to G protein‐coupled receptors

AC Keen, M Jörg, ML Halls - British Journal of Pharmacology, 2024 - Wiley Online Library
Targeted protein degraders are extremely useful as biological tools for discovery research.
They have also been developed as novel therapeutics with several targeted protein

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
… To expand the reach of TPD to degrade other “hard to drug” … synthesis, and molecular
biology, tools now exist to identify ligands for almost any protein. This is underscored by the recent …

Covalent ligand screening uncovers a RNF4 E3 ligase recruiter for targeted protein degradation applications

CC Ward, JI Kleinman, SM Brittain, PS Lee… - ACS chemical …, 2019 - ACS Publications
… to E3 ligases remains crucial for expanding the set of E3 … for targeted protein degradation
of a given target of interest and ultimately expand the applicability of this modality to any protein