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Publications
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Structurally Redesigned Bioorthogonal Reagents for Mitochondria-Specific Prodrug Activation
JACS Au 2020: Early View
The development of abiotic chemical reactions that can be performed in an organelle-specific manner can provide new opportunities in drug delivery and cell and chemical biology. However, due to the complexity of the cellular environment, this remains a significant challenge. Here, we introduce structurally redesigned bioorthogonal tetrazine reagents that spontaneously accumulate in mitochondria of live mammalian cells. The attributes leading to their efficient accumulation in the organelle were optimized to include the right combination of lipophilicity and positive delocalized charge. The best performing mitochondriotropic tetrazines enable subcellular chemical release of TCO-caged compounds as we show using fluorogenic substrates and mitochondrial uncoupler niclosamide. Our work demonstrates that a shrewd redesign of common bioorthogonal reagents can lead to their transformation into organelle-specific probes, opening the possibility to activate prodrugs and manipulate biological…
Druggable Hot Spots in the Schistosomiasis Cathepsin B1 Target Identified by Functional and Binding Mode Analysis of Potent Vinyl Sulfone Inhibitors
ACS Infectious Diseases 2020: Early View
Structural basis of RNA recognition by the SARS-CoV-2 nucleocapsid phosphoprotein
PLOS Pathogens 16 (12): e1009100 (2020)
Monitoring peptide tyrosine nitration by spectroscopic methods
Amino Acids 2020: Early View
Flow cytometric determination of cell cycle progression via direct labeling of replicated DNA
Analytical Biochemistry 2020: Early View