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 …

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 …

ALK-positive lung cancer: a moving target

JL Schneider, JJ Lin, AT Shaw - Nature cancer, 2023 - nature.com
Anaplastic lymphoma kinase (ALK) is a potent oncogenic driver in lung cancer. ALK tyrosine
kinase inhibitors yield significant benefit in patients with ALK fusion-positive (ALK+) lung …

PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy

JM Kelm, DS Pandey, E Malin, H Kansou, S Arora… - Molecular Cancer, 2023 - Springer
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …

Developments of CRBN-based PROTACs as potential therapeutic agents

C Wang, Y Zhang, Y Wu, D Xing - European journal of medicinal chemistry, 2021 - Elsevier
Protease-targeted chimeras (PROTACs) are a new technology that is receiving much
attention in the treatment of diseases. The mechanism is to inhibit protein function by …

Peptide-based PROTAC degrader of FOXM1 suppresses cancer and decreases GLUT1 and PD-L1 expression

K Wang, X Dai, A Yu, C Feng, K Liu… - Journal of Experimental & …, 2022 - Springer
Background Peptide proteolysis-targeting chimeras (p-PROTACs) with advantages of high
specificity and low toxicity have emerged as a powerful technology of targeted protein …

PROTAC therapy as a new targeted therapy for lung cancer

JW Li, G Zheng, FJ Kaye, L Wu - Molecular therapy, 2023 - cell.com
Despite recent advances in molecular therapeutics, lung cancer is still a leading cause of
cancer deaths. Currently, limited targeted therapy options and acquired drug resistance …

Catalytic degraders effectively address kinase site mutations in EML4-ALK oncogenic fusions

Y Gao, B Jiang, H Kim, MJ Berberich… - Journal of Medicinal …, 2023 - ACS Publications
Heterobifunctional degraders, known as proteolysis targeting chimeras (PROTACs),
theoretically possess a catalytic mode-of-action, yet few studies have either confirmed or …

Molecular strategies to target protein aggregation in Huntington's disease

OD Jarosińska, SGD Rüdiger - Frontiers in molecular biosciences, 2021 - frontiersin.org
Huntington's disease (HD) is a neurodegenerative disorder caused by the aggregation of
the mutant huntingtin (mHTT) protein in nerve cells. mHTT self-aggregates to form soluble …

Development of alectinib-based PROTACs as novel potent degraders of anaplastic lymphoma kinase (ALK)

S Xie, Y Sun, Y Liu, X Li, X Li, W Zhong… - Journal of medicinal …, 2021 - ACS Publications
A series of novel anaplastic lymphoma kinase (ALK) degraders were designed and
synthesized based on proteolysis-targeting chimera (PROTAC) technology by linking two …