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 …

Chemistries of bifunctional PROTAC degraders

C Cao, M He, L Wang, Y He, Y Rao - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …

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 …

Advancing targeted protein degradation for cancer therapy

B Dale, M Cheng, KS Park, HÜ Kaniskan… - Nature Reviews …, 2021 - nature.com
The human proteome contains approximately 20,000 proteins, and it is estimated that more
than 600 of them are functionally important for various types of cancers, including nearly 400 …

RAF-MEK-ERK pathway in cancer evolution and treatment

R Ullah, Q Yin, AH Snell, L Wan - Seminars in cancer biology, 2022 - Elsevier
Abstract The RAF-MEK-ERK signaling cascade is a well-characterized MAPK pathway
involved in cell proliferation and survival. The three-layered MAPK signaling cascade is …

Rare molecular subtypes of lung cancer

G Harada, SR Yang, E Cocco, A Drilon - Nature Reviews Clinical …, 2023 - nature.com
Oncogenes that occur in≤ 5% of non-small-cell lung cancers have been defined as 'rare';
nonetheless, this frequency can correspond to a substantial number of patients diagnosed …

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 …

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 …

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 …

An overview of PROTACs: a promising drug discovery paradigm

Z Liu, M Hu, Y Yang, C Du, H Zhou, C Liu, Y Chen… - Molecular …, 2022 - Springer
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …