Results 1 to 10 of about 8,887,267 (401)
Modular Assembled Targeting Chimera Enables Multimodal Targeted Protein Degradation. [PDF]
Zhu W +5 more
europepmc +2 more sources
Structure-based design of a phosphotyrosine-masked covalent ligand targeting the E3 ligase SOCS2
The Src homology 2 (SH2) domain recognizes phosphotyrosine (pY) post translational modifications in partner proteins to trigger downstream signaling. Drug discovery efforts targeting the SH2 domains have long been stymied by the poor drug-like properties
Sarath Ramachandran +10 more
doaj +1 more source
Targeting proteins for degradation [PDF]
Protein degradation plays a central role in many cellular functions. Misfolded and damaged proteins are removed from the cell to avoid toxicity. The concentrations of regulatory proteins are adjusted by degradation at the appropriate time. Both foreign and native proteins are digested into small peptides as part of the adaptive immune response.
Erin K, Schrader +2 more
openaire +2 more sources
Background LINC00173 had been reported as a cisplatin (cis-diamminedichloroplatinum, DDP) chemotherapy-resistant inducer in small-cell lung cancer (SCLC) and lung squamous cell carcinoma (LUSC). This study aimed to display reverse data for LINC00173 as a
Xingyu Tao +10 more
doaj +1 more source
A core‐shell‐structured Cu2O@Mn3Cu3O8 (CMCO) nanozyme is constructed to serve as a tumor microenvironment (TME)‐activated copper ionophore to achieve safe and efficient cuproptosis.
Wei Chen +6 more
doaj +1 more source
CHD1L augments autophagy-mediated migration of hepatocellular carcinoma through targeting ZKSCAN3
Autophagy is an important biological process in normal cells. However, how it affects tumor progression still remains poorly understood. Herein, we demonstrated that the oncogenic protein Chromodomain-helicase-DNA-binding-protein 1-like gene (CHD1L ...
Xiaofeng Zhang +14 more
doaj +1 more source
Protein degradation in mitochondria [PDF]
The biogenesis of mitochondria and the maintenance of mitochondrial functions depends on an autonomous proteolytic system in the organelle which is highly conserved throughout evolution. Components of this system include processing peptidases and ATP-dependent proteases, as well as molecular chaperone proteins and protein complexes with apparently ...
Kaser, M., Langer, T.
openaire +3 more sources
An amendment to this paper has been published and can be accessed via a link at the top of the paper.
Qingzi Chen +12 more
doaj +1 more source
A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo
Protein degraders are an emerging drug modality; however, their properties lie beyond typical drug-like space. Here the authors report optimisation via structure-based exit vector and linker design towards the VHL-recruiting PROTAC ACBI2, an orally ...
Christiane Kofink +29 more
doaj +1 more source
Hyperglycemia triggers HIPK2 protein degradation [PDF]
Homeodomain interacting protein kinase-2 (HIPK2) is an evolutionary conserved kinase that modulates several key molecular pathways to restrain tumor growth and induce p53-depending apoptotic cell-death in response to anticancer therapies. HIPK2 silencing
Baldari, Silvia +6 more
core +2 more sources

