Trends in kinase drug discovery: targets, indications and inhibitor design

MM Attwood, D Fabbro, AV Sokolov, S Knapp… - Nature Reviews Drug …, 2021 - nature.com
The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …

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 …

Proteolysis-targeting chimeras (PROTACs) in cancer therapy

X Li, W Pu, Q Zheng, M Ai, S Chen, Y Peng - Molecular cancer, 2022 - Springer
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …

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 …

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 …

E3 ligase ligand chemistries: from building blocks to protein degraders

I Sosič, A Bricelj, C Steinebach - Chemical Society Reviews, 2022 - pubs.rsc.org
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …

Intracellular delivery of glutathione peroxidase degrader induces ferroptosis in vivo

T Luo, Q Zheng, L Shao, T Ma, L Mao… - Angewandte …, 2022 - Wiley Online Library
Ferroptosis is a new form of regulated, non‐apoptotic cell death driven by iron‐dependent
phospholipid peroxidation. Its therapeutic potential is however, greatly limited by the low …

[HTML][HTML] NRAS mutant melanoma: Towards better therapies

T Randic, I Kozar, C Margue, J Utikal, S Kreis - Cancer treatment reviews, 2021 - Elsevier
Genetic alterations affecting RAS proteins are commonly found in human cancers. Roughly
a fourth of melanoma patients carry activating NRAS mutations, rendering this malignancy …