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 …

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 …

Antibody–drug conjugates come of age in oncology

C Dumontet, JM Reichert, PD Senter… - Nature Reviews Drug …, 2023 - nature.com
Antibody–drug conjugates (ADCs) combine the specificity of monoclonal antibodies with the
potency of highly cytotoxic agents, potentially reducing the severity of side effects by …

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …

Payload diversification: a key step in the development of antibody–drug conjugates

L Conilh, L Sadilkova, W Viricel, C Dumontet - Journal of Hematology & …, 2023 - Springer
Antibody–drug conjugates (ADCs) is a fast moving class of targeted biotherapeutics that
currently combines the selectivity of monoclonal antibodies with the potency of a payload …

Exploring the next generation of antibody–drug conjugates

K Tsuchikama, Y Anami, SYY Ha… - Nature Reviews Clinical …, 2024 - nature.com
Antibody–drug conjugates (ADCs) are a promising cancer treatment modality that enables
the selective delivery of highly cytotoxic payloads to tumours. However, realizing the full …

Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders

CJ Diehl, A Ciulli - Chemical Society Reviews, 2022 - pubs.rsc.org
The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …

The dawn of a new era: targeting the “undruggables” with antibody-based therapeutics

L Qian, X Lin, X Gao, RU Khan, JY Liao, S Du… - Chemical …, 2023 - ACS Publications
The high selectivity and affinity of antibodies toward their antigens have made them a highly
valuable tool in disease therapy, diagnosis, and basic research. A plethora of chemical and …

Aptamer‐protac conjugates (apcs) for tumor‐specific targeting in breast cancer

S He, F Gao, J Ma, H Ma, G Dong… - Angewandte …, 2021 - Wiley Online Library
Abstract Development of proteolysis targeting chimeras (PROTACs) is emerging as a
promising strategy for targeted protein degradation. However, the drug development using …

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 …