Achieving clinical success with BET inhibitors as anti-cancer agents
The transcriptional upregulation of oncogenes is a driving force behind the progression of
many tumours. However, until a decade ago, the concept of 'switching off'these oncogenic …
many tumours. However, until a decade ago, the concept of 'switching off'these oncogenic …
Liquid–liquid phase separation in tumor biology
X Tong, R Tang, J Xu, W Wang, Y Zhao, X Yu… - Signal Transduction and …, 2022 - nature.com
Liquid–liquid phase separation (LLPS) is a novel principle for explaining the precise spatial
and temporal regulation in living cells. LLPS compartmentalizes proteins and nucleic acids …
and temporal regulation in living cells. LLPS compartmentalizes proteins and nucleic acids …
Acetylation-dependent regulation of PD-L1 nuclear translocation dictates the efficacy of anti-PD-1 immunotherapy
Immunotherapies that target programmed cell death protein 1 (PD-1) and its ligand PD-L1
as well as cytotoxic T-lymphocyte-associated protein 4 (CTLA4) have shown impressive …
as well as cytotoxic T-lymphocyte-associated protein 4 (CTLA4) have shown impressive …
Targeting signaling pathways in prostate cancer: mechanisms and clinical trials
Prostate cancer (PCa) affects millions of men globally. Due to advances in understanding
genomic landscapes and biological functions, the treatment of PCa continues to improve …
genomic landscapes and biological functions, the treatment of PCa continues to improve …
Genetics and biology of prostate cancer
Despite the high long-term survival in localized prostate cancer, metastatic prostate cancer
remains largely incurable even after intensive multimodal therapy. The lethality of advanced …
remains largely incurable even after intensive multimodal therapy. The lethality of advanced …
Cyclin D–CDK4 kinase destabilizes PD-L1 via cullin 3–SPOP to control cancer immune surveillance
Treatments that target immune checkpoints, such as the one mediated by programmed cell
death protein 1 (PD-1) and its ligand PD-L1, have been approved for treating human …
death protein 1 (PD-1) and its ligand PD-L1, have been approved for treating human …
Bromodomains: a new target class for drug development
AG Cochran, AR Conery, RJ Sims III - Nature Reviews Drug Discovery, 2019 - nature.com
Less than a decade ago, it was shown that bromodomains, acetyl lysine 'reader'modules
found in proteins with varied functions, were highly tractable small-molecule targets. This is …
found in proteins with varied functions, were highly tractable small-molecule targets. This is …
Light-induced control of protein destruction by opto-PROTAC
By hijacking endogenous E3 ligase to degrade protein targets via the ubiquitin-proteasome
system, PROTACs (PRoteolysis TArgeting Chimeras) provide a new strategy to inhibit …
system, PROTACs (PRoteolysis TArgeting Chimeras) provide a new strategy to inhibit …
Cancer mutations of the tumor suppressor SPOP disrupt the formation of active, phase-separated compartments
JJ Bouchard, JH Otero, DC Scott, E Szulc, EW Martin… - Molecular cell, 2018 - cell.com
Mutations in the tumor suppressor SPOP (speckle-type POZ protein) cause prostate, breast,
and other solid tumors. SPOP is a substrate adaptor of the cullin3-RING ubiquitin ligase and …
and other solid tumors. SPOP is a substrate adaptor of the cullin3-RING ubiquitin ligase and …
Radiotherapy-triggered proteolysis targeting chimera prodrug activation in tumors
C Yang, Y Yang, Y Li, Q Ni, J Li - Journal of the American …, 2022 - ACS Publications
Proteolysis targeting chimera (PROTAC) is an emerging protein degradation strategy, which
shows excellent advantages in targeting those so-called “undruggable” proteins. However …
shows excellent advantages in targeting those so-called “undruggable” proteins. However …