Loading
GRPR is a hormone receptor abundant in early and hormone-sensitive prostate cancer, imaged and treated with bombesin-like radioligands.
The gastrin-releasing peptide receptor (GRPR) is a G-protein-coupled receptor for bombesin and GRP whose expression is high in hormone-sensitive prostate cancer and falls with castration resistance. It is overexpressed in primary and hormone-naive prostate cancer, often in PSMA-negative tumours, as well as in ER-positive breast cancer and GIST, which makes it a complementary theranostic target to PSMA. Bombesin-like radioligands exploit it: 68Ga-RM2 PET for imaging and 177Lu-NeoB (Novartis) for therapy are in clinical trials. Because expression declines as disease becomes castration-resistant, GRPR agents may suit earlier disease or PSMA-negative patients rather than replacing PSMA therapy. A newcomer can think of GRPR as a second radioactive address on prostate cancer, useful where PSMA is dim.
In plain words · GRPR is a hormone receptor abundant in early and hormone-sensitive prostate cancer, imaged and treated with bombesin-like radioligands.
GRPR is a hormone receptor abundant in early and hormone-sensitive prostate cancer, imaged and treated with bombesin-like radioligands.
G-protein-coupled receptor for bombesin/GRP; expression falls with castration resistance.
No product in this corpus aims at GRPR (gastrin-releasing peptide receptor) yet. Because it sits on the outside of the cell, it can be reached from the bloodstream: antibodies flag the cell, ADCs deliver a toxin, radioligands deliver radiation, and CAR-T or bispecifics bring a T cell.
First described 1991. Earliest sequence paper UniProt cites for the protein: Corjay M.H. et al, J. Biol. Chem, 1991, "Two distinct bombesin receptor subtypes are expressed and functional in human lung carcinoma cells". Source.
G-protein-coupled receptor for bombesin/GRP; expression falls with castration resistance.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Prostate cancer | 100% | Receptor autoradiography, GRPR in 30 of 30 invasive prostate carcinomas | Markwalder and Reubi 1999 (Cancer Res); receptor density was high in carcinoma and PIN and low or absent in normal and hyperplastic prostate | PMC |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Query for this target: (TITLE:"GRPR" OR ABSTRACT:"GRPR" OR TITLE:"gastrin-releasing peptide receptor" OR ABSTRACT:"gastrin-releasing peptide receptor") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about GRPR (gastrin-releasing peptide receptor), not a curated reading list.
Shares Radioligand therapy (beta emitters) and the tag theranostic.
Shares PET (positron emission tomography), Radioligand therapy (beta emitters), Prostate cancer.
Shares PET (positron emission tomography), Radioligand therapy (beta emitters).
Shares PET (positron emission tomography), Radioligand therapy (beta emitters), Prostate cancer.