2016
DOI: 10.1097/ppo.0000000000000221
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Prostate-Specific Membrane Antigen–Directed Therapy for Metastatic Castration-Resistant Prostate Cancer

Abstract: Prostate-specific membrane antigen (PSMA) is highly expressed on both benign and malignant prostatic tissue. Prostate-specific membrane antigen–directed therapy is conceptually promising, with a potential to additionally serve as a theranostic model in management of advanced prostate cancer. To date, various approaches have been devised and tested, including radiolabeled PSMA antibodies and inhibitor and antibody-drug conjugates. However, development and progress have faced challenges in determining the optima… Show more

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Cited by 12 publications
(15 citation statements)
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“…Through the past decade, a variety of PSMA-targeted ligands has been systematically evaluated for their modification to radiopharmaceuticals [65]. Among them, two distinct approaches have been used for targeting PSMA, the first approach taking advantage of the macromolecular protein structure of PSMA to provide specific monoclonal antibodies and antibody-based molecules as targeting vectors [66]. The second approach takes advantage of the enzyme activity of PSMA and uses small-molecule enzyme inhibitors or binding agents as target seeking agents [67].…”
Section: Psma Ligands For Targeted Radiotherapymentioning
confidence: 99%
“…Through the past decade, a variety of PSMA-targeted ligands has been systematically evaluated for their modification to radiopharmaceuticals [65]. Among them, two distinct approaches have been used for targeting PSMA, the first approach taking advantage of the macromolecular protein structure of PSMA to provide specific monoclonal antibodies and antibody-based molecules as targeting vectors [66]. The second approach takes advantage of the enzyme activity of PSMA and uses small-molecule enzyme inhibitors or binding agents as target seeking agents [67].…”
Section: Psma Ligands For Targeted Radiotherapymentioning
confidence: 99%
“…PSMA is a transmembrane type II glycoprotein also called folate hydrolase I or glutamate carboxipeptidase II, which has a 19-amino-acid intracellular portion, a 24-amino-acid transmembrane portion and a 707-amino-acid extracellular portion ( 41 ). PSMA is expressed by prostate cells and overexpressed in PCa cells.…”
Section: Evidence Synthesismentioning
confidence: 99%
“…Furthermore, numerous other small molecule inhibitors have been derived and some of those are currently being studied in clinical trials (Table 1). An elaborate overview of PSMA-targeting tracer development in the past two decades can be found in earlier published reviews [15,16,17,18,19,20,21].…”
Section: Introductionmentioning
confidence: 99%