2015
DOI: 10.1016/j.nucmedbio.2015.07.010
|View full text |Cite
|
Sign up to set email alerts
|

Evaluation of DOTA-chelated neurotensin analogs with spacer-enhanced biological performance for neurotensin-receptor-1-positive tumor targeting

Abstract: Introduction Neurotensin receptor 1 (NTR1) is overexpressed in many cancers types. Neurotensin (NT), a 13 amino acid peptide, is the native ligand for NTR1 and exhibits high (nM) affinity to the receptor. Many laboratories have been investigating the development of diagnostic and therapeutic radiopharmaceuticals for NTR1-positive cancers based on the NT peptide. To improve the biological performance for targeting NTR1, we proposed NT analogs with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) … Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
2
2
1

Citation Types

1
31
1

Year Published

2016
2016
2024
2024

Publication Types

Select...
6
1

Relationship

1
6

Authors

Journals

citations
Cited by 24 publications
(36 citation statements)
references
References 36 publications
1
31
1
Order By: Relevance
“…The in vitro internalization and efflux studies were performed as stated previously 38, 39 . HT-29 cells (~1×10 6 ) were suspended in 100 μL of McCoy’s 5A medium (pH 7.4, 4.8 mg/mL HEPES, and 2 mg/mL BSA).…”
Section: Methodsmentioning
confidence: 99%
“…The in vitro internalization and efflux studies were performed as stated previously 38, 39 . HT-29 cells (~1×10 6 ) were suspended in 100 μL of McCoy’s 5A medium (pH 7.4, 4.8 mg/mL HEPES, and 2 mg/mL BSA).…”
Section: Methodsmentioning
confidence: 99%
“…Most importantly, the peptide with the PEG 4 ‐spacer linked to the DOTA chelator was found to have a more favorable receptor affinity by a factor of 4 compared with NT(8–13) without the spacer, and the presence of the spacer did not significantly affect the lipophilicity of the peptide. Similarly, the “spacer‐enhanced” in vivo performance of DOTA‐linked NT analogs has also been described by Jia et al, who found that a 4‐atom hydrocarbon spacer length was optimal for obtaining 177 Lu‐labeled DOTA NT peptides with adequate receptor binding affinity and tumor accumulation in vivo.…”
Section: Introductionmentioning
confidence: 99%
“…These NT receptors are over‐expressed in various tumors and cancerous cells/tissues . Therefore, various NT‐based radio‐labeled pharmaceutics using 188 Re, 177 Lu, 123/ 125 I, 111 In, 99m Tc, 64 Cu, and 18 F are being developed to target these cancer sites/tumors for diagnosis and therapy applications . The C‐terminal segment (NT8‐13) is more important for the receptor binding as compared to the N‐terminal.…”
Section: Discussionmentioning
confidence: 99%
“…[7,9,10] Therefore, various NT-based radio-labeled pharmaceutics using 188 Re, 177 Lu, 123/125 I, 111 In, 99m Tc, 64 Cu, and 18 F are being developed to target these cancer sites/tumors for diagnosis and therapy applications. [7,[78][79][80][81] The C-terminal segment (NT8-13) is more important for the receptor binding as compared to the N-terminal. Among them, Arg 8 , Tyr 11 , Leu 13 -COOH play a key role for its activity.…”
Section: Discussionmentioning
confidence: 99%