Up-down regulation of HIF-1α in cancer progression

M Rashid, LR Zadeh, B Baradaran, O Molavi… - Gene, 2021 - Elsevier
Hypoxia induicible factor-1 alpha (HIF-1α) is a key transcription factor in cancer progression
and target therapy in cancer. HIF-1α acts differently depending on presence or absence of …

[HTML][HTML] HIF-1α pathway: role, regulation and intervention for cancer therapy

GN Masoud, W Li - Acta Pharmaceutica Sinica B, 2015 - Elsevier
Abstract Hypoxia-inducible factor-1 (HIF-1) has been recognized as an important cancer
drug target. Many recent studies have provided convincing evidences of strong correlation …

Catalytic in vivo protein knockdown by small-molecule PROTACs

DP Bondeson, A Mares, IED Smith, E Ko… - Nature chemical …, 2015 - nature.com
The current predominant therapeutic paradigm is based on maximizing drug-receptor
occupancy to achieve clinical benefit. This strategy, however, generally requires excessive …

Delineating the role of cooperativity in the design of potent PROTACs for BTK

A Zorba, C Nguyen, Y Xu, J Starr… - Proceedings of the …, 2018 - National Acad Sciences
Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that
simultaneously bind to a target protein and an E3 ligase, thereby leading to ubiquitination …

Targeting hypoxia-inducible factors: therapeutic opportunities and challenges

X Yuan, W Ruan, B Bobrow, P Carmeliet… - Nature Reviews Drug …, 2024 - nature.com
Hypoxia-inducible factors (HIFs) are highly conserved transcription factors that are crucial for
adaptation of metazoans to limited oxygen availability. Recently, HIF activation and …

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 …

Identification and characterization of Von Hippel-Lindau-recruiting proteolysis targeting chimeras (PROTACs) of TANK-binding kinase 1

AP Crew, K Raina, H Dong, Y Qian… - Journal of medicinal …, 2018 - ACS Publications
Proteolysis targeting chimeras (PROTACs) are bifunctional molecules that recruit an E3
ligase to a target protein to facilitate ubiquitination and subsequent degradation of that …

HECT and RING finger families of E3 ubiquitin ligases at a glance

MB Metzger, VA Hristova… - Journal of cell …, 2012 - journals.biologists.com
This article is part of a Minifocus on Ubiquitin. For further reading, please see related
articles: ʻUbiquitin and SUMO in DNA repair at a glanceʼ by Helle D. Ulrich (J. Cell Sci …

The 2007 WHO classification of tumours of the central nervous system

DN Louis, H Ohgaki, OD Wiestler, WK Cavenee… - Acta …, 2007 - Springer
The fourth edition of the World Health Organization (WHO) classification of tumours of the
central nervous system, published in 2007, lists several new entities, including angiocentric …

Targeting of HIF-α to the von Hippel-Lindau Ubiquitylation Complex by O2-Regulated Prolyl Hydroxylation

P Jaakkola, DR Mole, YM Tian, MI Wilson, J Gielbert… - Science, 2001 - science.org
Hypoxia-inducible factor (HIF) is a transcriptional complex that plays a central role in the
regulation of gene expression by oxygen. In oxygenated and iron replete cells, HIF-α …