[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 …
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 …
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …
Cell cycle on the crossroad of tumorigenesis and cancer therapy
Aberrancy in cell cycle progression is one of the fundamental mechanisms underlying
tumorigenesis, making regulators of the cell cycle machinery rational anticancer therapeutic …
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 …
diseases would be therapeutically benefited by targeted protein stabilization (TPS). Here we …
[HTML][HTML] An overview of PROTACs: a promising drug discovery paradigm
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …
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 …
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
Indoleamine 2, 3-dioxygenase 1 (IDO1) is a potent immunosuppressive enzyme that inhibits
the antitumor immune response through both tryptophan metabolism and non-enzymatic …
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 …
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 …
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 …
phosphorylating CDK1 when DNA is damaged to allow time for DNA to repair, disruption of …