Biological evaluation of 177Lu-labeled DOTA-Ala(SO3H)-Aminooctanoyl-Gln-Trp-Ala-Val-N methyl Gly-His-Statine-Leu-NH2 for gastrin-releasing peptide receptor-positive prostate tumor targeting

Lim, Jae Cheong; Cho, Eun Ha; Kim, Jin Joo; Choi, Sang Mu; Lee, So young; Nam, Sung Soo; Park, Ul Jae; Park, Soo Hyun

doi:10.1016/j.nucmedbio.2014.10.007

Cited by 7 publications

(3 citation statements)

References 18 publications

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“…There is considerable interest in the possible treatment of prostate-cancer with BnR-ligands conjugated with cytotoxic-radiolabeled-Bn-analogues( 177 Lu, 90 Y, 213 Bi), as has been demonstrated so effectively using 177 Lu/ 90 Y-labeled-somatostatin-labeled-analogues to treat patients with malignant, neuroendocrine tumors[16•,50••,160]. Various 177 Lu/ 90 Y/ 213 Bi-coupled Bn-agonists/antagonists bind prostate-cells with high-affinity and can have cytotoxicity for prostate-cancer-cells in vitro / in vivo xenografts in nude-mice[77,157,160].…”

Section: Bn-peptides-bnr: Prostate-cancermentioning

confidence: 99%

“…Various 177 Lu/ 90 Y/ 213 Bi-coupled Bn-agonists/antagonists bind prostate-cells with high-affinity and can have cytotoxicity for prostate-cancer-cells in vitro / in vivo xenografts in nude-mice[77,157,160]. In one study the α–emitter, 213 Bi coupled to either of two different BnR-agonists, showed greater cytototoxicity to prostate-cancer-xenografts in mice that a β–emitting 177 Lu-BnR-agonist, with a good safety profile.…”

Section: Bn-peptides-bnr: Prostate-cancermentioning

confidence: 99%

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Bombesin related peptides/receptors and their promising therapeutic roles in cancer imaging, targeting and treatment

Moreno

Ramos-Álvarez

Moody

et al. 2016

Expert Opinion on Therapeutic Targets

102

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Introduction Despite remarkable advances in tumor treatment, many patients still die from common tumors (breast, prostate, lung, CNS, colon, and pancreas), and thus, new approaches are needed. Many of these tumors synthesize bombesin (Bn)-related peptides and over-express their receptors (BnRs), hence functioning as autocrine-growth-factors. Recent studies support the conclusion that Bn-peptides/BnRs are well-positioned for numerous novel antitumor treatments, including interrupting autocrine-growth via the use of over-expressed receptors for imaging and targeting cytotoxic-compounds, either by direct-coupling or combined with nanoparticle-technology. Areas covered The unique ability of common neoplasms to synthesize, secrete, and show a growth/proliferative/differentiating response due to BnR over-expression, is reviewed, both in general and with regard to the most frequently investigated neoplasms (breast, prostate, lung, and CNS). Particular attention is paid to advances in the recent years. Also considered are the possible therapeutic approaches to the growth/differentiation effect of Bn-peptides, as well as the therapeutic implication of the frequent BnR over-expression for tumor-imaging and/or targeted-delivery. Expert opinion Given that Bn-related-peptides/BnRs are so frequently ectopically-expressed by common tumors, which are often malignant and become refractory to conventional treatments, therapeutic interventions using novel approaches to Bn-peptides and receptors are being explored. Of particular interest is the potential of reproducing BnRs in common tumors, such as the recent success of utilizing overexpression of somatostatin-receptors by neuroendocrine-tumors to provide the most sensitive imaging methods and targeted delivery of cytotoxic-compounds.

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Section: Bn-peptides-bnr: Prostate-cancermentioning

confidence: 99%

Section: Bn-peptides-bnr: Prostate-cancermentioning

confidence: 99%

Bombesin related peptides/receptors and their promising therapeutic roles in cancer imaging, targeting and treatment

Moreno

Ramos-Álvarez

Moody

et al. 2016

Expert Opinion on Therapeutic Targets

102

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“…Since then, the use of radiolabeled BBN derivatives was investigated in various entities like gastrointestinal stromal tumors, glioma, optic pathway glioma, medullary thyroid, colorectal, breast, and prostate cancer [20,22,23,27,28,29,30,33,34,35,36,37,38,40,41,42,43,44,45,46,47,48,49,50,51,52,54,55,56,57,58,59,60,61,62,63,64,65,67,68,69,70,71,72,73,74,75,76,77,78,79,…”

Section: Introductionmentioning

confidence: 99%

GRPr Theranostics: Current Status of Imaging and Therapy using GRPr Targeting Radiopharmaceuticals

et al. 2022

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Addressing molecular targets, that are overexpressed by various tumor entities, using radiolabeled molecules for a combined diagnostic and therapeutic (theranostic) approach is of increasing interest in oncology. The gastrin-releasing peptide receptor (GRPr), which is part of the bombesin family, has shown to be overexpressed in a variety of tumors, therefore, serving as a promising target for those theranostic applications. A large amount of differently radiolabeled bombesin derivatives addressing the GRPr have been evaluated in the preclinical as well as clinical setting showing fast blood clearance and urinary excretion with selective GRPr-binding. Most of the available studies on GRPr-targeted imaging and therapy have evaluated the theranostic approach in prostate and breast cancer applying bombesin derivatives tagged with the predominantly used theranostic pair of 68Ga/177Lu which is the focus of this review.

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Radionuclide Therapy in Prostate Cancer

Acar

Bekiş

Polack

2022

Radionuclide Therapy

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Biological evaluation of 177Lu-labeled DOTA-Ala(SO3H)-Aminooctanoyl-Gln-Trp-Ala-Val-N methyl Gly-His-Statine-Leu-NH2 for gastrin-releasing peptide receptor-positive prostate tumor targeting

Cited by 7 publications

References 18 publications

Bombesin related peptides/receptors and their promising therapeutic roles in cancer imaging, targeting and treatment

Bombesin related peptides/receptors and their promising therapeutic roles in cancer imaging, targeting and treatment

GRPr Theranostics: Current Status of Imaging and Therapy using GRPr Targeting Radiopharmaceuticals

Radionuclide Therapy in Prostate Cancer

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