Prolonged hypoxia alleviates prolyl hydroxylation-mediated suppression of RIPK1 to promote necroptosis and inflammation
T Zhang, D Xu, J Liu, M Wang, LJ Duan, M Liu… - Nature cell …, 2023 - nature.com
The prolyl hydroxylation of hypoxia-inducible factor 1α (HIF-1α) mediated by the EGLN–
pVHL pathway represents a classic signalling mechanism that mediates cellular adaptation …
pVHL pathway represents a classic signalling mechanism that mediates cellular adaptation …
Selective small molecule induced degradation of the BET bromodomain protein BRD4
The Bromo-and Extra-Terminal (BET) proteins BRD2, BRD3, and BRD4 play important roles
in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET …
in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET …
Antibody–PROTAC conjugates enable HER2-dependent targeted protein degradation of BRD4
M Maneiro, N Forte, MM Shchepinova… - ACS chemical …, 2020 - ACS Publications
Targeting protein degradation with Proteolysis-Targeting Chimeras (PROTACs) is an area of
great current interest in drug discovery. Nevertheless, although the high effectiveness of …
great current interest in drug discovery. Nevertheless, although the high effectiveness of …
[HTML][HTML] Driving E3 ligase substrate specificity for targeted protein degradation: lessons from nature and the laboratory
Methods to direct the degradation of protein targets with proximity-inducing molecules that
coopt the cellular degradation machinery are advancing in leaps and bounds, and diverse …
coopt the cellular degradation machinery are advancing in leaps and bounds, and diverse …
Bioorthogonal PROTAC prodrugs enabled by on-target activation
Although proteolysis targeting chimeras (PROTACs) have become promising therapeutic
modalities, important concerns exist about the potential toxicity of the approach owing to …
modalities, important concerns exist about the potential toxicity of the approach owing to …
A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase
ME Matyskiela, G Lu, T Ito, B Pagarigan, CC Lu… - Nature, 2016 - nature.com
Immunomodulatory drugs bind to cereblon (CRBN) to confer differentiated substrate
specificity on the CRL4CRBN E3 ubiquitin ligase. Here we report the identification of a new …
specificity on the CRL4CRBN E3 ubiquitin ligase. Here we report the identification of a new …
[HTML][HTML] Regulation of the hypoxia-inducible factor (HIF) by pro-inflammatory cytokines
Hypoxia and inflammation are frequently co-incidental features of the tissue
microenvironment in a wide range of inflammatory diseases. While the impact of hypoxia on …
microenvironment in a wide range of inflammatory diseases. While the impact of hypoxia on …
[HTML][HTML] Targeted protein degradation: from chemical biology to drug discovery
PM Cromm, CM Crews - Cell chemical biology, 2017 - cell.com
Traditional pharmaceutical drug discovery is almost exclusively focused on directly
controlling protein activity to cure diseases. Modulators of protein activity, especially …
controlling protein activity to cure diseases. Modulators of protein activity, especially …
VHL, the story of a tumour suppressor gene
L Gossage, T Eisen, ER Maher - Nature Reviews Cancer, 2015 - nature.com
Abstract Since the Von Hippel–Lindau (VHL) disease tumour suppressor gene VHL was
identified in 1993 as the genetic basis for a rare disorder, it has proved to be of wide medical …
identified in 1993 as the genetic basis for a rare disorder, it has proved to be of wide medical …
Regulation of erythropoiesis by hypoxia-inducible factors
VH Haase - Blood reviews, 2013 - Elsevier
A classic physiologic response to systemic hypoxia is the increase in red blood cell
production. Hypoxia-inducible factors (HIFs) orchestrate this response by inducing cell-type …
production. Hypoxia-inducible factors (HIFs) orchestrate this response by inducing cell-type …