[HTML][HTML] Current strategies for the design of PROTAC linkers: a critical review

RI Troup, C Fallan, MGJ Baud - Exploration of Targeted Anti-tumor …, 2020 - ncbi.nlm.nih.gov
Abstract PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …

Tumour hypoxia induces a metabolic shift causing acidosis: a common feature in cancer

J Chiche, MC Brahimi‐Horn… - Journal of cellular and …, 2010 - Wiley Online Library
Introduction• Intracellular pH regulation controls energy balance and cell proliferation:
chemical and biological proof of principle‐Chemical proof of principle‐Biological proof of …

Targeting the von Hippel–Lindau E3 ubiquitin ligase using small molecules to disrupt the VHL/HIF-1α interaction

DL Buckley, I Van Molle, PC Gareiss… - Journal of the …, 2012 - ACS Publications
E3 ubiquitin ligases, which bind protein targets, leading to their ubiquitination and
subsequent degradation, are attractive drug targets due to their exquisite substrate …

The chemical biology of nitric oxide: implications in cellular signaling

DD Thomas, LA Ridnour, JS Isenberg… - Free Radical Biology …, 2008 - Elsevier
Nitric oxide (NO) has earned the reputation of being a signaling mediator with many diverse
and often opposing biological activities. The diversity in response to this simple diatomic …

Hypoxia-inducible factor 1 (HIF-1) pathway

GL Semenza - Science's STKE, 2007 - science.org
Hypoxia-inducible factor 1 (HIF-1) is a basic helix-loop-helix-PAS domain transcription factor
that is expressed in all metazoan organisms and is composed of HIF-1α and HIF-1β …

Causes and consequences of increased glucose metabolism of cancers

RJ Gillies, I Robey, RA Gatenby - Journal of Nuclear Medicine, 2008 - Soc Nuclear Med
In this review we examine the mechanisms (causes) underlying the increased glucose
consumption observed in tumors within a teleological context (consequences). In other …

eNOS activation by physical forces: from short-term regulation of contraction to chronic remodeling of cardiovascular tissues

JL Balligand, O Feron, C Dessy - Physiological reviews, 2009 - journals.physiology.org
Nitric oxide production in response to flow-dependent shear forces applied on the surface of
endothelial cells is a fundamental mechanism of regulation of vascular tone, peripheral …

Nitric oxide release: part III. Measurement and reporting

PN Coneski, MH Schoenfisch - Chemical Society Reviews, 2012 - pubs.rsc.org
Nitric oxide's expansive physiological and regulatory roles have driven the development of
therapies for human disease that would benefit from exogenous NO administration. Already …

Nutrient-sensitized screening for drugs that shift energy metabolism from mitochondrial respiration to glycolysis

VM Gohil, SA Sheth, R Nilsson, AP Wojtovich… - Nature …, 2010 - nature.com
Most cells have the inherent capacity to shift their reliance on glycolysis relative to oxidative
metabolism, and studies in model systems have shown that targeting such shifts may be …

Hypoxia up-regulates hypoxia-inducible factor-1α transcription by involving phosphatidylinositol 3-kinase and nuclear factor κB in pulmonary artery smooth muscle …

RS BelAiba, S Bonello, C Zähringer… - Molecular biology of …, 2007 - Am Soc Cell Biol
The oxygen sensitive α-subunit of the hypoxia-inducible factor-1 (HIF-1) is a major trigger of
the cellular response to hypoxia. Although the posttranslational regulation of HIF-1α by …