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.
| Identifer | oai:union.ndltd.org:BRADFORD/oai:bradscholars.brad.ac.uk:10454/9998 |
| Date | 11 July 2013 |
| Creators | 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 |
| Source Sets | Bradford Scholars |
| Language | English |
| Detected Language | English |
| Type | Article, Published version |
| Rights | © 2013 American Chemical Society. This is an Open Access article licensed under the Creative Commons CC-BY-NC-ND license (http://pubs.acs.org/page/policy/authorchoice_ccbyncnd_termsofuse.html), CC-BY-NC-ND |
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