Piperlongumine and some of its analogs inhibit selectively the human immunoproteasome over the constitutive proteasome - CNRS - Centre national de la recherche scientifique Accéder directement au contenu
Article Dans Une Revue Biochemical and Biophysical Research Communications Année : 2018

Piperlongumine and some of its analogs inhibit selectively the human immunoproteasome over the constitutive proteasome

Résumé

The natural small molecule piperlongumine A is toxic selectively to cancer cells in vitro and in vivo. This toxicity has been correlated with cancer cell ROS, DNA damage and apoptotic cell death increases. We demonstrate here a new mechanistic property of piperlongumine: it inhibits selectively human immunoproteasome with no noticeable inhibition of human constitutive proteasome. This result suggests that immunoproteasome inhibition, a mechanism independent of ROS elevation, may also partly play a role in the anticancer effects observed with piperlongumine. Structure-activity relationships of piperlongumine analogs suggest that the lactam (piperidonic) ring of piperlongumine A may be replaced by the linear olefin -NHCO-CH2=CH2 to improve both in vitro inhibitory efficiency against immunoproteasome and cellular toxicity.

Dates et versions

hal-03997837 , version 1 (20-02-2023)

Identifiants

Citer

Elodie Bosc, Jhennifer Nastri, Valérie Lefort, Marilia Valli, Fernando Contiguiba, et al.. Piperlongumine and some of its analogs inhibit selectively the human immunoproteasome over the constitutive proteasome. Biochemical and Biophysical Research Communications, 2018, 496 (3), pp.961-966. ⟨10.1016/j.bbrc.2018.01.100⟩. ⟨hal-03997837⟩
10 Consultations
0 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More