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  • About
  • The Global ETD Search service is a free service for researchers to find electronic theses and dissertations. This service is provided by the Networked Digital Library of Theses and Dissertations.
    Our metadata is collected from universities around the world. If you manage a university/consortium/country archive and want to be added, details can be found on the NDLTD website.
1

Re-engineering of the Duocarmycin Structural Architecture Enables Bioprecursor Development Targeting CYP1A1 and CYP2W1 for Biological Activity

Sheldrake, Helen M., Travica, S., Johansson, I., Loadman, Paul, Sutherland, Mark, Elsalem, Lina M.I., Illingworth, Nicola A., Cresswell, Alexander J., Reuillon, Tristan, Shnyder, Steven, Mkrtchian, S., Searcey, M., Ingelman-Sundberg, M., Patterson, Laurence H., Pors, Klaus 11 July 2013 (has links)
Yes / A library of duocarmycin bioprecursors based on the CPI and CBI scaffolds was synthesized and used to probe selective activation by cells expressing CYP1A1 and 2W1, CYPs known to be expressed in high frequency in some tumors. Several CPI-based compounds were pM–nM potent in CYP1A1 expressing cells. CYP2W1 was also shown to sensitize proliferating cells to several compounds, demonstrating its potential as a target for tumor selective activation of duocarmycin bioprecursors.

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