[99mTc]Demomedin C, a Radioligand Based on Human Gastrin Releasing Peptide(18-27): Synthesis and Preclinical Evaluation in Gastrin Releasing Peptide Receptor-Expressing Models

2012 ◽  
Vol 55 (19) ◽  
pp. 8364-8374 ◽  
Author(s):  
Berthold A. Nock ◽  
Renzo Cescato ◽  
Eleni Ketani ◽  
Beatrice Waser ◽  
Jean Claude Reubi ◽  
...  
Keyword(s):  
Preclinical Evaluation ◽  
Peptide Receptor ◽  
Gastrin Releasing Peptide ◽  
Human Gastrin

scholarly journals [99mTc]Tc-DB15 in GRPR-Targeted Tumor Imaging with SPECT: From Preclinical Evaluation to the First Clinical Outcomes

Cancers ◽  
2021 ◽  
Vol 13 (20) ◽  
pp. 5093
Author(s):  
Berthold A. Nock ◽  
Aikaterini Kaloudi ◽  
Panagiotis Kanellopoulos ◽  
Barbara Janota ◽  
Barbara Bromińska ◽  
...  
Keyword(s):  
Tumor Imaging ◽  
Pharmacokinetic Profile ◽  
Diglycolic Acid ◽  
Preclinical Evaluation ◽  
Peptide Receptor ◽  
Gastrin Releasing Peptide ◽  
Specific Uptake ◽  
Grpr Antagonist

Diagnostic imaging and radionuclide therapy of prostate (PC) and breast cancer (BC) using radiolabeled gastrin-releasing peptide receptor (GRPR)-antagonists represents a promising approach. We herein propose the GRPR-antagonist based radiotracer [99mTc]Tc-DB15 ([99mTc]Tc-N4-AMA-DGA-DPhe6,Sar11,LeuNHEt13]BBN(6-13); N4: 6-carboxy-1,4,8,11-tetraazaundecane, AMA: aminomethyl-aniline, DGA: diglycolic acid) as a new diagnostic tool for GRPR-positive tumors applying SPECT/CT. The uptake of [99mTc]Tc-DB15 was tested in vitro in mammary (T-47D) and prostate cancer (PC-3) cells and in vivo in T-47D or PC-3 xenograft-bearing mice as well as in BC patients. DB15 showed high GRPR-affinity (IC50 = 0.37 ± 0.03 nM) and [99mTc]Tc-DB15 strongly bound to the cell-membrane of T-47D and PC-3 cells, according to a radiolabeled antagonist profile. In mice, the radiotracer showed high and prolonged GRPR-specific uptake in PC-3 (e.g., 25.56 ± 2.78 %IA/g vs. 0.72 ± 0.12 %IA/g in block; 4 h pi) and T-47D (e.g., 15.82 ± 3.20 %IA/g vs. 3.82 ± 0.30 %IA/g in block; 4 h pi) tumors, while rapidly clearing from background. In patients with advanced BC, the tracer could reveal several bone and soft tissue metastases on SPECT/CT. The attractive pharmacokinetic profile of [99mTc]DB15 in mice and its capability to target GRPR-positive BC lesions in patients highlight its prospects for a broader clinical use, an option currently being explored by ongoing clinical studies.

Preclinical Evaluation of Novel 64Cu-Labeled Gastrin-Releasing Peptide Receptor Bioconjugates for PET Imaging of Prostate Cancer

2021 ◽  
Author(s):  
George Makris ◽  
Antonio Shegani ◽  
Pavithra H. A. Kankanamalage ◽  
Marina Kuchuk ◽  
Rajendra P. Bandari ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Pet Imaging ◽  
Preclinical Evaluation ◽  
Peptide Receptor ◽  
Gastrin Releasing Peptide

The human gastrin-releasing peptide receptor gene structure, its tissue expression and promoter

Gene ◽  
2001 ◽  
Vol 264 (1) ◽  
pp. 95-103 ◽  
Author(s):  
Dongmei Xiao ◽  
Junning Wang ◽  
Lori L. Hampton ◽  
H.Christian Weber
Keyword(s):  
Gene Structure ◽  
Receptor Gene ◽  
Tissue Expression ◽  
Peptide Receptor ◽  
Gastrin Releasing Peptide ◽  
Human Gastrin
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