Structure-activity relationships of 2',5'-oligoadenylate analogue modifications of prostate-specific membrane antigen (PSMA) antagonists
Prostate-specific membrane antigen (PSMA) is an ideal biomarker for prostate cancer. A previously reported 2-5A conjugate RBI1033 (3) showed binding affinity more than 10 times higher than the parent urea-based compound (S)-2-(3-((S)-5-amino-1-carboxypentyl)ureido) pentanedioic acid (1). The purpose of this work is to further optimize the structure of 3 to identify highly selective ligands of PSMA. It was found that conjugates having 2-5A in their structure showed extraordinary improved binding affinity to PSMA compared with compound 1. Removal of 2-5A significantly reduced its biological activity. The results will provide a path to agents for targeted imaging and treatment of prostate cancer.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2012 |
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| Erschienen: |
2012 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:31 |
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| Enthalten in: |
Nucleosides, nucleotides & nucleic acids - 31(2012), 5 vom: 08. Mai, Seite 432-44 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Wang, Xinning [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 12.10.2012 Date Revised 23.08.2018 published: Print Citation Status MEDLINE |
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| doi: |
10.1080/15257770.2012.671988 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM216963702 |
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| 100 | 1 | |a Wang, Xinning |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Structure-activity relationships of 2',5'-oligoadenylate analogue modifications of prostate-specific membrane antigen (PSMA) antagonists |
| 264 | 1 | |c 2012 | |
| 336 | |a Text |b txt |2 rdacontent | ||
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| 500 | |a Date Completed 12.10.2012 | ||
| 500 | |a Date Revised 23.08.2018 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Prostate-specific membrane antigen (PSMA) is an ideal biomarker for prostate cancer. A previously reported 2-5A conjugate RBI1033 (3) showed binding affinity more than 10 times higher than the parent urea-based compound (S)-2-(3-((S)-5-amino-1-carboxypentyl)ureido) pentanedioic acid (1). The purpose of this work is to further optimize the structure of 3 to identify highly selective ligands of PSMA. It was found that conjugates having 2-5A in their structure showed extraordinary improved binding affinity to PSMA compared with compound 1. Removal of 2-5A significantly reduced its biological activity. The results will provide a path to agents for targeted imaging and treatment of prostate cancer | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, N.I.H., Extramural | |
| 650 | 4 | |a Research Support, U.S. Gov't, Non-P.H.S. | |
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| 650 | 7 | |a Antigens, Surface |2 NLM | |
| 650 | 7 | |a Ligands |2 NLM | |
| 650 | 7 | |a Oligoribonucleotides |2 NLM | |
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| 650 | 7 | |a 2',5'-oligoadenylate |2 NLM | |
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| 700 | 1 | |a Tian, Haibin |e verfasserin |4 aut | |
| 700 | 1 | |a Lee, Zhenghong |e verfasserin |4 aut | |
| 700 | 1 | |a Heston, Warren D W |e verfasserin |4 aut | |
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