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• W2895156968 endingPage "2277" @default.
• W2895156968 startingPage "2266" @default.
• W2895156968 abstract "Translesion synthesis (TLS) is a mechanism of replication past damaged DNA through which multiple forms of human cancer survive and acquire resistance to first-line genotoxic chemotherapies. As such, TLS is emerging as a promising target for the development of a new class of anticancer agents. The C-terminal domain of the DNA polymerase Rev1 (Rev1-CT) mediates assembly of the functional TLS complex through protein-protein interactions (PPIs) with Rev1 interacting regions (RIRs) of several other TLS DNA polymerases. Utilizing structural knowledge of the Rev1-CT/RIR interface, we have identified the phenazopyridine scaffold as an inhibitor of this essential TLS PPI. We demonstrate direct binding of this scaffold to Rev1-CT, and the synthesis and evaluation of a small series of analogues have provided important structure-activity relationships for further development of this scaffold. Furthermore, we utilized the umbrella sampling method to predict the free energy of binding to Rev1-CT for each of our analogues. Binding energies calculated through umbrella sampling correlated well with experimentally determined IC50 values, validating this computational tool as a viable approach to predict the biological activity for inhibitors of the Rev1-CT/RIR PPI." @default.
• W2895156968 created "2018-10-12" @default.
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• W2895156968 date "2018-11-26" @default.
• W2895156968 modified "2023-09-27" @default.
• W2895156968 title "Structural Approach To Identify a Lead Scaffold That Targets the Translesion Synthesis Polymerase Rev1." @default.
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• W2895156968 doi "https://doi.org/10.1021/acs.jcim.8b00535" @default.
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• W2895156968 hasPublicationYear "2018" @default.
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