Design and synthesis of a PSMA inhibitor-doxorubicin conjugate for targeted prostate cancer therapy
Prostate-specific membrane antigen (PSMA) provides an attractive target for the
development of targeted chemotherapeutics for prostate cancer. We have designed and
synthesized a bioconjugate 1 that comprises the cytotoxic drug doxorubicin and one of our
previously described urea-based PSMA inhibitors. While this bioconjugate retained high
binding affinity for PSMA, it inhibited only 30% of C4-2 cell growth at a concentration of 5.0
μM.
development of targeted chemotherapeutics for prostate cancer. We have designed and
synthesized a bioconjugate 1 that comprises the cytotoxic drug doxorubicin and one of our
previously described urea-based PSMA inhibitors. While this bioconjugate retained high
binding affinity for PSMA, it inhibited only 30% of C4-2 cell growth at a concentration of 5.0
μM.
Abstract
Prostate-specific membrane antigen (PSMA) provides an attractive target for the development of targeted chemotherapeutics for prostate cancer. We have designed and synthesized a bioconjugate 1 that comprises the cytotoxic drug doxorubicin and one of our previously described urea-based PSMA inhibitors. While this bioconjugate retained high binding affinity for PSMA, it inhibited only 30% of C4-2 cell growth at a concentration of 5.0 μM.
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