neuromedin-c and Prostatic-Neoplasms

neuromedin-c has been researched along with Prostatic-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for neuromedin-c and Prostatic-Neoplasms

Article	Year
[(99m)Tc]Demomedin C, a radioligand based on human gastrin releasing peptide(18-27): synthesis and preclinical evaluation in gastrin releasing peptide receptor-expressing models. Journal of medicinal chemistry, 2012, Oct-11, Volume: 55, Issue:19 The synthesis and preclinical evaluation of [(99m)Tc]Demomedin C in GRPR-expressing models are reported. Demomedin C resulted by coupling a Boc-protected N(4)-chelator to neuromedin C (human GRP(18-27)), which, after (99m)Tc-labeling, afforded [(99m)Tc]Demomedin C. Demomedin C showed high affinity and selectivity for the GRPR during receptor autoradiography on human cancer samples (IC(50) in nM: GRPR, 1.4 ± 0.2; NMBR, 106 ± 18; and BB(3)R, >1000). It triggered GRPR internalization in HEK-GRPR cells and Ca(2+) release in PC-3 cells (EC(50) = 1.3 nM). [(99m)Tc]Demomedin C rapidly and specifically internalized at 37 °C in PC-3 cells and was stable in mouse plasma. [(99m)Tc]Demomedin C efficiently and specifically localized in human PC-3 implants in mice (9.84 ± 0.81%ID/g at 1 h pi; 6.36 ± 0.85%ID/g at 4 h pi, and 0.41 ± 0.07%ID/g at 4 h pi block). Thus, human GRP-based radioligands, such as [(99m)Tc]Demomedin C, can successfully target GRPR-expressing human tumors in vivo while displaying attractive biological features--e.g. higher GRPR-selectivity--vs their frog-homologues. Topics: Amino Acid Sequence; Animals; Anura; Autoradiography; Binding, Competitive; Bombesin; Bronchial Neoplasms; Calcium; Cell Line, Tumor; Cell Membrane; Drug Screening Assays, Antitumor; Humans; Ileal Neoplasms; Ligands; Male; Mice; Mice, SCID; Microscopy, Fluorescence; Neoplasm Transplantation; Oligopeptides; Organotechnetium Compounds; Peptide Fragments; Prostatic Neoplasms; Radionuclide Imaging; Radiopharmaceuticals; Receptors, Bombesin; Species Specificity; Structure-Activity Relationship; Technetium; Tissue Distribution; Transplantation, Heterologous	2012

Article

Year

[(99m)Tc]Demomedin C, a radioligand based on human gastrin releasing peptide(18-27): synthesis and preclinical evaluation in gastrin releasing peptide receptor-expressing models.

Journal of medicinal chemistry, 2012, Oct-11, Volume: 55, Issue:19

The synthesis and preclinical evaluation of [(99m)Tc]Demomedin C in GRPR-expressing models are reported. Demomedin C resulted by coupling a Boc-protected N(4)-chelator to neuromedin C (human GRP(18-27)), which, after (99m)Tc-labeling, afforded [(99m)Tc]Demomedin C. Demomedin C showed high affinity and selectivity for the GRPR during receptor autoradiography on human cancer samples (IC(50) in nM: GRPR, 1.4 ± 0.2; NMBR, 106 ± 18; and BB(3)R, >1000). It triggered GRPR internalization in HEK-GRPR cells and Ca(2+) release in PC-3 cells (EC(50) = 1.3 nM). [(99m)Tc]Demomedin C rapidly and specifically internalized at 37 °C in PC-3 cells and was stable in mouse plasma. [(99m)Tc]Demomedin C efficiently and specifically localized in human PC-3 implants in mice (9.84 ± 0.81%ID/g at 1 h pi; 6.36 ± 0.85%ID/g at 4 h pi, and 0.41 ± 0.07%ID/g at 4 h pi block). Thus, human GRP-based radioligands, such as [(99m)Tc]Demomedin C, can successfully target GRPR-expressing human tumors in vivo while displaying attractive biological features--e.g. higher GRPR-selectivity--vs their frog-homologues.

Topics: Amino Acid Sequence; Animals; Anura; Autoradiography; Binding, Competitive; Bombesin; Bronchial Neoplasms; Calcium; Cell Line, Tumor; Cell Membrane; Drug Screening Assays, Antitumor; Humans; Ileal Neoplasms; Ligands; Male; Mice; Mice, SCID; Microscopy, Fluorescence; Neoplasm Transplantation; Oligopeptides; Organotechnetium Compounds; Peptide Fragments; Prostatic Neoplasms; Radionuclide Imaging; Radiopharmaceuticals; Receptors, Bombesin; Species Specificity; Structure-Activity Relationship; Technetium; Tissue Distribution; Transplantation, Heterologous

2012