Optimization of α-amido boronic acids via cryo-electron microscopy analysis: Discovery of a novel highly selective immunoproteasome subunit LMP7 (β5i)/LMP2 (β1i) dual inhibitor

[Display omitted] The immunoproteasome subunit LMP7 (β5i)/LMP2 (β1i) dual blockade has been reported to suppress B cell differentiation and activation, suggesting that the dual inhibition of LMP7/LMP2 is a promising approach for treating autoimmune diseases. In contrast, the inhibition of the consti...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2024-07, Vol.109, p.117790, Article 117790
Hauptverfasser:	Arai, Yuuki, Shitama, Hiroaki, Yamagishi, Masahito, Ono, Satoshi, Kashima, Akiko, Hiraizumi, Masahiro, Tsuda, Naoki, Katayama, Koushirou, Tanaka, Kouji, Koda, Yuzo, Kato, Sayuka, Sakata, Kei, Nureki, Osamu, Miyazaki, Hiroshi
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Autoimmune disease Boronic Acids - chemical synthesis Boronic Acids - chemistry Boronic Acids - pharmacology Constitutive proteasome Cryo-EM Cryoelectron Microscopy Cysteine Endopeptidases - metabolism Drug Discovery Humans Immunoproteasome LMP2 LMP7 Mice Molecular Dynamics Simulation Molecular Structure Proteasome Endopeptidase Complex - chemistry Proteasome Endopeptidase Complex - metabolism Proteasome Inhibitors - chemical synthesis Proteasome Inhibitors - chemistry Proteasome Inhibitors - pharmacology Structure-Activity Relationship β5c
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