Covalent targeting of non-cysteine residues in PI4KIIIβ
Brett Cosgrove, Emma K. Grant, Sophie Bertrand, Kenneth D. Down, Don O. Somers, John P. Evans, Nicholas C. O. Tomkinson* (思克莱德大学,英国) and Michael D. Barker* (葛兰素史克药物研究中心,英国)
👉 The synthesis and characterisation of fluorosulfate covalent inhibitors of the catalytic lysine, a distal tyrosine or both residues in the lipid kinase PI4KIIIβ is described.
Macrocyclic peptides that inhibit Wnt signalling via interaction with Wnt3a
Manuel E. Otero-Ramirez, Kyoko Matoba, Emiko Mihara, Toby Passioura, Junichi Takagi* (大阪大学,日本) and Hiroaki Suga* (东京大学,日本)
👉 Discovery and optimization of de novo macrocyclic peptide binders of Wnt3a through RaPID screening against an afamin-stabilized Wnt3a complex, capable of inhibiting Wnt signalling by direct interaction to the Wnt protein.
Superoxide-responsive quinone methide precursors (QMP-SOs) to study superoxide biology by proximity labeling and chemoproteomics
Hinyuk Lai and Clive Yik-Sham Chung*(香港大学, 中国)
👉 QMP-SOs are molecular probes capable of proximity labeling of proteins in a superoxide-dependent manner. This enables fluorescence imaging of superoxide and profiling proteins associated with superoxide biology by chemoproteomics.
Probing the metalloproteome: an 8-mercaptoquinoline motif enriches minichromosome maintenance complex components as significant metalloprotein targets in live cells
Sean M. McKenna, Bogdan I. Florea, Daniela M. Zisterer, Sander I. van Kasteren and Joanna F. McGouran* (都柏林圣三一大学,爱尔兰)
👉 A mercaptoquinoline based photo affinity probe for profiling metalloproteins was developed and applied in live cell assays, identifying several novel, therapeutically significant protein targets.
Biosynthesis of the corallorazines, a widespread class of antibiotic cyclic lipodipeptides
Teresa M. Dreckmann, Lisa Fritz, Christian F. Kaiser, Sarah M. Bouhired, Daniel A. Wirtz, Marvin Rausch, Anna Müller, Tanja Schneider, Gabriele M. König and Max Crüsemann*(波恩大学,德国)
👉 Corallorazines are cyclic lipodipeptide natural products produced by the myxobacterium Corallococcus coralloides B035. Corallorazine biosynthesis was analyzed in vitro and in silico, in addition to antibiotic and mode of action studies.