[HTML][HTML] 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 …

[HTML][HTML] 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 …

Cell cycle on the crossroad of tumorigenesis and cancer therapy

J Liu, Y Peng, W Wei - Trends in cell biology, 2022 - cell.com
Aberrancy in cell cycle progression is one of the fundamental mechanisms underlying
tumorigenesis, making regulators of the cell cycle machinery rational anticancer therapeutic …

[HTML][HTML] Deubiquitinase-targeting chimeras for targeted protein stabilization

NJ Henning, L Boike, JN Spradlin, CC Ward… - Nature chemical …, 2022 - nature.com
Many diseases are driven by proteins that are aberrantly ubiquitinated and degraded. These
diseases would be therapeutically benefited by targeted protein stabilization (TPS). Here we …

[HTML][HTML] 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 …

Recent advances in DDR (DNA damage response) inhibitors for cancer therapy

B Cheng, W Pan, Y Xing, Y Xiao, J Chen… - European Journal of …, 2022 - Elsevier
DDR (DNA damage response) defects in cells drive tumor formation by promoting DNA
mutations, which also provides cancer-specific vulnerabilities that can be targeted by …

Identification and characterization of a novel indoleamine 2, 3-dioxygenase 1 protein degrader for glioblastoma

LR Bollu, PV Bommi, PJ Monsen, L Zhai… - Journal of Medicinal …, 2022 - ACS Publications
Indoleamine 2, 3-dioxygenase 1 (IDO1) is a potent immunosuppressive enzyme that inhibits
the antitumor immune response through both tryptophan metabolism and non-enzymatic …

[HTML][HTML] Targeting the DNA damage response pathway as a novel therapeutic strategy in colorectal cancer

F Catalano, R Borea, S Puglisi, A Boutros, A Gandini… - Cancers, 2022 - mdpi.com
Simple Summary Defective DNA damage response (DDR) is a hallmark of cancer leading to
genomic instability. Up to 15–20% of colorectal cancers carry alterations in DDR. However …

Cell cycle involvement in cancer therapy; WEE1 kinase, a potential target as therapeutic strategy

S Vakili-Samiani, OJ Khanghah, E Gholipour… - Mutation Research …, 2022 - Elsevier
Mitosis is the process of cell division and is regulated by checkpoints in the cell cycle. G1-S,
S, and G2-M are the three main checkpoints that prevent initiation of the next phase of the …

[HTML][HTML] Selective Wee1 degradation by PROTAC degraders recruiting VHL and CRBN E3 ubiquitin ligases

MC Aublette, TA Harrison, EJ Thorpe… - Bioorganic & Medicinal …, 2022 - Elsevier
Abstract The Ser/Thr protein kinase Wee1 plays a regulatory role at the G 2/M checkpoint by
phosphorylating CDK1 when DNA is damaged to allow time for DNA to repair, disruption of …