Design and synthesis of a PSMA inhibitor-doxorubicin conjugate for targeted prostate cancer therapy

Sarva Jayaprakash; Xinning Wang; Warren D. Heston; Alan P. Kozikowski

doi:10.1002/cmdc.200500044

Design and synthesis of a PSMA inhibitor-doxorubicin conjugate for targeted prostate cancer therapy

Sarva Jayaprakash, Xinning Wang, Warren D. Heston, Alan P. Kozikowski

Research output: Contribution to journal › Article › peer-review

31 Scopus citations

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.

Original language	English (US)
Pages (from-to)	299-302
Number of pages	4
Journal	ChemMedChem
Volume	1
Issue number	3
DOIs	https://doi.org/10.1002/cmdc.200500044
State	Published - Mar 2006
Externally published	Yes

Keywords

Doxorubicin
Inhibitors
Neurotransmitters
PSMA
Prostate cancer

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Pharmacology
Drug Discovery
Pharmacology, Toxicology and Pharmaceutics(all)
Organic Chemistry

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10.1002/cmdc.200500044

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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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AU - Kozikowski, Alan P.

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AB - 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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KW - Inhibitors

KW - Neurotransmitters

KW - PSMA

KW - Prostate cancer

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Design and synthesis of a PSMA inhibitor-doxorubicin conjugate for targeted prostate cancer therapy

Abstract

Keywords

ASJC Scopus subject areas

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