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 …
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 …
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 …
kinase inhibitors yield significant benefit in patients with ALK fusion-positive (ALK+) lung …
PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …
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 …
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 …
specificity and low toxicity have emerged as a powerful technology of targeted protein …
PROTAC therapy as a new targeted therapy for lung cancer
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 …
cancer deaths. Currently, limited targeted therapy options and acquired drug resistance …
Catalytic degraders effectively address kinase site mutations in EML4-ALK oncogenic fusions
Heterobifunctional degraders, known as proteolysis targeting chimeras (PROTACs),
theoretically possess a catalytic mode-of-action, yet few studies have either confirmed or …
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 …
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 …
synthesized based on proteolysis-targeting chimera (PROTAC) technology by linking two …