Discovery of Novel Pyrazolo-Pyridone DCN1 Inhibitors Controlling Cullin Neddylation.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00410
Abstract: Chemical control of cullin neddylation is attracting increased attention based largely on the successes of the NEDD8-activating enzyme (E1) inhibitor Pevonedistat. Recently reported chemical probes enable selective and time-dependent inhibition of downstream members of the… read more here.
Keywords: pyrazolo pyridone; cullin neddylation; discovery novel; dcn1 ... See more keywords
Cullin neddylation inhibitor attenuates hyperglycemia by enhancing hepatic insulin signaling through insulin receptor substrate stabilization
Sign Up to like & getrecommendations! Published in 2022 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2111737119
Abstract: Significance Hepatic insulin resistance is a well-recognized cause of hepatic glucose overproduction and fasting hyperglycemia in fatty liver disease and type-2 diabetes. Here, we have discovered that pharmacological inhibition of cullin neddylation by NAE1 inhibitor… read more here.
Keywords: cullin neddylation; cullin; insulin signaling; insulin ... See more keywords
Targeting Protein Neddylation to Inactivate Cullin-RING Ligases by Gossypol: A Lucky Hit or a New Start?
Sign Up to like & getrecommendations! Published in 2021 at "Drug Design, Development and Therapy"
DOI: 10.2147/dddt.s286373
Abstract: Abstract Cullin-RING E3 ligases (CRLs) are the largest family of E3 ubiquitin ligases, responsible for about 20% of the protein degradation by the ubiquitin-proteasome system (UPS). Given their vital roles in multiple cellular processes, and… read more here.
Keywords: cullin ring; cullin neddylation; ring ligases; neddylation ... See more keywords