[HTML][HTML] PROTAC targeted protein degraders: the past is prologue
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …
tackle disease-causing proteins that have historically been highly challenging to target with …
Protein degraders enter the clinic—a new approach to cancer therapy
D Chirnomas, KR Hornberger, CM Crews - Nature Reviews Clinical …, 2023 - nature.com
Heterobifunctional protein degraders, such as PROteolysis TArgeting Chimera (PROTAC)
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …
[HTML][HTML] Targeted protein degradation: mechanisms, strategies and application
L Zhao, J Zhao, K Zhong, A Tong, D Jia - Signal transduction and …, 2022 - nature.com
Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …
development and application of protein activity modulators, particularly inhibitors, has been …
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 …
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
Advancing targeted protein degradation for cancer therapy
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 …
than 600 of them are functionally important for various types of cancers, including nearly 400 …
The manipulation of apoptosis for cancer therapy using BH3-mimetic drugs
ST Diepstraten, MA Anderson, PE Czabotar… - Nature Reviews …, 2022 - nature.com
Apoptosis is a form of programmed cell death that is regulated by the balance between
prosurvival and proapoptotic BCL-2 protein family members. Evasion of apoptosis is a …
prosurvival and proapoptotic BCL-2 protein family members. Evasion of apoptosis is a …
[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 …
[HTML][HTML] Targeting STAT3 in cancer immunotherapy
S Zou, Q Tong, B Liu, W Huang, Y Tian, X Fu - Molecular cancer, 2020 - Springer
As a point of convergence for numerous oncogenic signaling pathways, signal transducer
and activator of transcription 3 (STAT3) is central in regulating the anti-tumor immune …
and activator of transcription 3 (STAT3) is central in regulating the anti-tumor immune …
[HTML][HTML] Semiconducting polymer nano-PROTACs for activatable photo-immunometabolic cancer therapy
Immunometabolic intervention has been applied to treat cancer via inhibition of certain
enzymes associated with intratumoral metabolism. However, small-molecule inhibitors and …
enzymes associated with intratumoral metabolism. However, small-molecule inhibitors and …