Tommaso Moschetti
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View article: Selective Aurora A-TPX2 Interaction Inhibitors Have <i>In Vivo</i> Efficacy as Targeted Antimitotic Agents
Selective Aurora A-TPX2 Interaction Inhibitors Have <i>In Vivo</i> Efficacy as Targeted Antimitotic Agents Open
Aurora A kinase, a cell division regulator, is frequently overexpressed in various cancers, provoking genome instability and resistance to antimitotic chemotherapy. Localization and enzymatic activity of Aurora A are regulated by its inter…
View article: Selective Aurora A-TPX2 interaction inhibitors have<i>in vivo</i>efficacy as targeted anti-mitotic agents
Selective Aurora A-TPX2 interaction inhibitors have<i>in vivo</i>efficacy as targeted anti-mitotic agents Open
The protein kinase Aurora A, and its close relative, Aurora B, regulate human cell division. Aurora A is frequently overexpressed in cancers of the breast, ovary, pancreas and blood, provoking genome instability and resistance to anti-mito…
View article: A small-molecule inhibitor of the BRCA2-RAD51 interaction modulates RAD51 assembly and potentiates DNA damage-induced cell death
A small-molecule inhibitor of the BRCA2-RAD51 interaction modulates RAD51 assembly and potentiates DNA damage-induced cell death Open
SUMMARY BRCA2 controls RAD51 recombinase during homologous DNA recombination (HDR) through eight evolutionarily-conserved BRC repeats, which individually engage RAD51 via the motif Phe-x-x-Ala. Using structure-guided molecular design, temp…
View article: Development of a multipurpose scaffold for the display of peptide loops
Development of a multipurpose scaffold for the display of peptide loops Open
Protein–protein interactions (PPIs) determine a wide range of biological processes and analysis of these dynamic networks is increasingly becoming a mandatory tool for studying protein function. Using the globular ATPase domain of recombin…
View article: Quantitative Affinity Determination by Fluorescence Anisotropy Measurements of Individual Nanoliter Droplets
Quantitative Affinity Determination by Fluorescence Anisotropy Measurements of Individual Nanoliter Droplets Open
Fluorescence anisotropy measurements of reagents compartmentalized into individual nanoliter droplets are shown to yield high-resolution binding curves from which precise dissociation constants (K$_{d}$) for protein-peptide interactions ca…