Monomeric and dimeric 68Ga-labeled bombesin Analogues for Positron Emission Tomography (PET) imaging of tumors expressing Gastrin-Releasing Peptide Receptors (GRPrs)
The GRPr, highly expressed in prostate PCa and breast cancer BCa, is a promising target for the development of new PET radiotracers. The chelator HBED-CC (N,N′-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N′-diacetic acid) was coupled to the bombesin peptides: HBED-C-BN(2-14) 1, HBED-CC-PE...
Gespeichert in:
| Hauptverfasser: | , , , , , , , |
|---|---|
| Dokumenttyp: | Article (Journal) |
| Sprache: | Englisch |
| Veröffentlicht: |
February 12, 2018
|
| In: |
Journal of medicinal chemistry
Year: 2018, Jahrgang: 61, Heft: 5, Pages: 2062-2074 |
| ISSN: | 1520-4804 |
| DOI: | 10.1021/acs.jmedchem.7b01856 |
| Online-Zugang: | Verlag, Volltext: https://doi.org/10.1021/acs.jmedchem.7b01856 Verlag: https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01856 
|
| Verfasserangaben: | Christos Liolios, Benjamin Buchmuller, Ulrike Bauder-Wüst, Martin Schäfer, Karin Leotta, Uwe Haberkorn, Matthias Eder, and Klaus Kopka |
MARC
| LEADER | 00000caa a2200000 c 4500 | ||
|---|---|---|---|
| 001 | 1690920491 | ||
| 003 | DE-627 | ||
| 005 | 20220818000317.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 200225s2018 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.1021/acs.jmedchem.7b01856 |2 doi | |
| 035 | |a (DE-627)1690920491 | ||
| 035 | |a (DE-599)KXP1690920491 | ||
| 035 | |a (OCoLC)1341308004 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rda | ||
| 041 | |a eng | ||
| 084 | |a 30 |2 sdnb | ||
| 100 | 1 | |a Liolios, Christos |e VerfasserIn |0 (DE-588)1205337059 |0 (DE-627)1690922826 |4 aut | |
| 245 | 1 | 0 | |a Monomeric and dimeric 68Ga-labeled bombesin Analogues for Positron Emission Tomography (PET) imaging of tumors expressing Gastrin-Releasing Peptide Receptors (GRPrs) |c Christos Liolios, Benjamin Buchmuller, Ulrike Bauder-Wüst, Martin Schäfer, Karin Leotta, Uwe Haberkorn, Matthias Eder, and Klaus Kopka |
| 264 | 1 | |c February 12, 2018 | |
| 300 | |a 13 | ||
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a Computermedien |b c |2 rdamedia | ||
| 338 | |a Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Im Titel ist "68" in 68Ga-labeled hochgestellt | ||
| 500 | |a Gesehen am 25.02.2020 | ||
| 520 | |a The GRPr, highly expressed in prostate PCa and breast cancer BCa, is a promising target for the development of new PET radiotracers. The chelator HBED-CC (N,N′-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N′-diacetic acid) was coupled to the bombesin peptides: HBED-C-BN(2-14) 1, HBED-CC-PEG2-[d-Tyr6,β-Ala11,Thi13,Nle14]-BN(6-14) 2, HBED-CC-Y-[d-Phe6,Sta13,Leu14]-BN(6-14) (Y = 4-amino-1-carboxymethylpiperidine) 3, and HBED-CC-{PEG2-Y-[d-Phe6,Sta13,Leu14]-BN(6-14)}2 4 (homodimer). Compounds 1-4 presented high binding affinities for GRPr (T47D, 0.56-3.51 nM; PC-3, 2.12-4.68 nM). In PC-3 and T47D cells, agonists [68Ga]1 and [68Ga]2 were mainly internalized while antagonists [68Ga]3 and [68Ga]4 were surface bound. Cell-related radioactivity reached a maximum after 45 min, while tracer levels followed GRPr expression (PC-3 > T47D > LNCaP > MDA-MB-231). [68Ga]4 showed the highest cell-bound radioactivity (PC-3 and T47D). In vivo, tumor (PC-3) targeting for [68Ga]3 and [68Ga]4 increased over time, with dynamic μPET showing clearer tumors images at later time points. [68Ga]3 and [68Ga]4 can be considered suitable PET tracers for imaging PCa and BCa expressing GRPr. | ||
| 700 | 1 | |a Buchmuller, Benjamin |d 1991- |e VerfasserIn |0 (DE-588)1186278366 |0 (DE-627)1665788240 |4 aut | |
| 700 | 1 | |a Bauder-Wüst, Ulrike |e VerfasserIn |4 aut | |
| 700 | 1 | |a Schäfer, Martin |e VerfasserIn |4 aut | |
| 700 | 1 | |a Leotta, Karin |e VerfasserIn |4 aut | |
| 700 | 1 | |a Haberkorn, Uwe |d 1959- |e VerfasserIn |0 (DE-588)1022913905 |0 (DE-627)717331245 |0 (DE-576)366166352 |4 aut | |
| 700 | 1 | |a Eder, Matthias |d 1979- |e VerfasserIn |0 (DE-588)140263217 |0 (DE-627)616969279 |0 (DE-576)316151092 |4 aut | |
| 700 | 1 | |a Kopka, Klaus |d 1968- |e VerfasserIn |0 (DE-588)173031862 |0 (DE-627)69795661X |0 (DE-576)133884724 |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Journal of medicinal chemistry |d Washington, DC : ACS, 1959 |g 61(2018), 5, Seite 2062-2074 |h Online-Ressource |w (DE-627)302468846 |w (DE-600)1491411-6 |w (DE-576)090855132 |x 1520-4804 |7 nnas |a Monomeric and dimeric 68Ga-labeled bombesin Analogues for Positron Emission Tomography (PET) imaging of tumors expressing Gastrin-Releasing Peptide Receptors (GRPrs) |
| 773 | 1 | 8 | |g volume:61 |g year:2018 |g number:5 |g pages:2062-2074 |g extent:13 |a Monomeric and dimeric 68Ga-labeled bombesin Analogues for Positron Emission Tomography (PET) imaging of tumors expressing Gastrin-Releasing Peptide Receptors (GRPrs) |
| 856 | 4 | 0 | |u https://doi.org/10.1021/acs.jmedchem.7b01856 |x Verlag |x Resolving-System |3 Volltext |
| 856 | 4 | 0 | |u https://pubs.acs.org/doi/10.1021/acs.jmedchem.7b01856 |x Verlag |
| 951 | |a AR | ||
| 992 | |a 20200225 | ||
| 993 | |a Article | ||
| 994 | |a 2018 | ||
| 998 | |g 173031862 |a Kopka, Klaus |m 173031862:Kopka, Klaus |p 8 |y j | ||
| 998 | |g 140263217 |a Eder, Matthias |m 140263217:Eder, Matthias |p 7 | ||
| 998 | |g 1022913905 |a Haberkorn, Uwe |m 1022913905:Haberkorn, Uwe |d 910000 |d 911400 |e 910000PH1022913905 |e 911400PH1022913905 |k 0/910000/ |k 1/910000/911400/ |p 6 | ||
| 998 | |g 1186278366 |a Buchmuller, Benjamin C. |m 1186278366:Buchmuller, Benjamin C. |p 2 | ||
| 998 | |g 1205337059 |a Liolios, Christos |m 1205337059:Liolios, Christos |d 50000 |e 50000PL1205337059 |k 0/50000/ |p 1 |x j | ||
| 999 | |a KXP-PPN1690920491 |e 3598168438 | ||
| BIB | |a Y | ||
| SER | |a journal | ||
| JSO | |a {"type":{"media":"Online-Ressource","bibl":"article-journal"},"title":[{"title":"Monomeric and dimeric 68Ga-labeled bombesin Analogues for Positron Emission Tomography (PET) imaging of tumors expressing Gastrin-Releasing Peptide Receptors (GRPrs)","title_sort":"Monomeric and dimeric 68Ga-labeled bombesin Analogues for Positron Emission Tomography (PET) imaging of tumors expressing Gastrin-Releasing Peptide Receptors (GRPrs)"}],"physDesc":[{"extent":"13 S."}],"id":{"doi":["10.1021/acs.jmedchem.7b01856"],"eki":["1690920491"]},"relHost":[{"language":["eng"],"part":{"volume":"61","year":"2018","issue":"5","pages":"2062-2074","extent":"13","text":"61(2018), 5, Seite 2062-2074"},"pubHistory":["1.1959 -"],"note":["Gesehen am 02.10.2020"],"disp":"Monomeric and dimeric 68Ga-labeled bombesin Analogues for Positron Emission Tomography (PET) imaging of tumors expressing Gastrin-Releasing Peptide Receptors (GRPrs)Journal of medicinal chemistry","type":{"bibl":"periodical","media":"Online-Ressource"},"name":{"displayForm":["American Chemical Society"]},"recId":"302468846","title":[{"title":"Journal of medicinal chemistry","title_sort":"Journal of medicinal chemistry"}],"id":{"zdb":["1491411-6"],"eki":["302468846"],"issn":["1520-4804"]},"physDesc":[{"extent":"Online-Ressource"}],"origin":[{"dateIssuedKey":"1959","publisherPlace":"Washington, DC ; Easton, Pa.","publisher":"ACS ; ACS","dateIssuedDisp":"1959-"}]}],"origin":[{"dateIssuedDisp":"February 12, 2018","dateIssuedKey":"2018"}],"language":["eng"],"name":{"displayForm":["Christos Liolios, Benjamin Buchmuller, Ulrike Bauder-Wüst, Martin Schäfer, Karin Leotta, Uwe Haberkorn, Matthias Eder, and Klaus Kopka"]},"recId":"1690920491","person":[{"family":"Liolios","role":"aut","display":"Liolios, Christos","given":"Christos"},{"given":"Benjamin","display":"Buchmuller, Benjamin","family":"Buchmuller","role":"aut"},{"family":"Bauder-Wüst","role":"aut","display":"Bauder-Wüst, Ulrike","given":"Ulrike"},{"given":"Martin","display":"Schäfer, Martin","family":"Schäfer","role":"aut"},{"family":"Leotta","role":"aut","given":"Karin","display":"Leotta, Karin"},{"role":"aut","family":"Haberkorn","display":"Haberkorn, Uwe","given":"Uwe"},{"role":"aut","family":"Eder","given":"Matthias","display":"Eder, Matthias"},{"given":"Klaus","display":"Kopka, Klaus","role":"aut","family":"Kopka"}],"note":["Im Titel ist \"68\" in 68Ga-labeled hochgestellt","Gesehen am 25.02.2020"]} | ||
| SRT | |a LIOLIOSCHRMONOMERICA1220 | ||