Binding assay for the study of melanoma cell MSH receptors

Siegrist, Walter; Scimonelli, Teresa Nieves; Oestreicher, Marc; Stutz, Sibylla; Solca, Flavio; Girard, J.; Oberholzer, M.; Heitz, Philipp U.; Eberle, A.

doi:10.1016/0022-4731(87)91383-5

Cited by 4 publications

(10 citation statements)

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“…ACTH (4-10) (adrenocorticotropi¢ hormone) showed very low binding affinity (K~ = 22,400 + 7,200 pM), whereas the non-melanotropic POMC peptide, p-cndorphin, showed no affinity for the expressed MSH receptor. These data arc in close agreement with the affinities reported earlier for MSH receptors on several melanoma cell lines [3,20]. The high affinity of ACTH(1-39) for the MSH r~ptor can be attributed to the fact that the first 13 amino acids in the ACTH(l-39) molecule makes up the 0~-MSH molecule [21], as they are produced from the same POMC v,,,.,v,.v-,,,.-"' .... ,;.4,1 h,,,..., h,,.~ alternative cleavage [21].…”

supporting

confidence: 90%

“…The high affinity of ACTH(1-39) for the MSH r~ptor can be attributed to the fact that the first 13 amino acids in the ACTH(l-39) molecule makes up the 0~-MSH molecule [21], as they are produced from the same POMC v,,,.,v,.v-,,,.-"' .... ,;.4,1 h,,,..., h,,.~ alternative cleavage [21]. It has nlso been shown that the MSH receptor on melanoma cells recognizes different forms of the ACTH molecule with high affinity, in some cases an even higher affinity than ~z-MSH itself [20].…”

mentioning

confidence: 99%

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Molecular cloning and expression of the human melanocyte stimulating hormone receptor cDNA

1992

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Melanoeytes and melanoma cells are known to possess receptors for melanoeyte stimulating hormone (MSH). A eDNA clone, designated l ID, has b~.~n isolated from human melanoma cells and encodes a MSH receptor. The cloned eDNA encodes a 317 amino acid protein with transmembrane topography characteristics of a G-protein.coupled receptor, bat it does not show striking similarity to already pablish~ sequences of other G-protein-coupl~ receptors. When 11D eDNA is expressed in COS-7 cells, it binds an Z~l-labelled MSH analogue (NDP-MSH) in a Sl~Cifie manner. The bound ligand could be displaced by melanotropie peptides, a~-MSH, fl.MSH, 7-MSH and ACTH (adrenoeonieotropie hormone), but not by the non-melanotropie ~ptid¢,/3-endorphine. This is the first report of the cloning of a receptor geae of the melanotropin receptor family.

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confidence: 90%

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confidence: 99%

Molecular cloning and expression of the human melanocyte stimulating hormone receptor cDNA

1992

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“…The best example of such an approach was the successful somatostatin receptor–targeting with radiolabeled somatostatin analogs, now routinely used in the clinic 6. Concerning melanoma, it is also known that both melanotic and amelanotic murine and human melanomas overexpress the melanocortin type 1 receptor (MC1R), a member of the G protein‐coupled receptors family 7–9. Furthermore, more than 80% of human metastatic melanoma samples have also been identified to display MC1R receptors.…”

Section: Introductionmentioning

confidence: 99%

Melanocortin‐1 receptor‐targeting with radiolabeled cyclic α‐melanocyte‐stimulating hormone analogs for melanoma imaging

Raposinho¹,

Correia²,

Oliveira³

et al. 2010

Biopolymers

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Melanoma is a type of skin cancer known for its high aggressiveness, early dissemination of metastases, and poor prognosis once metastasized. Thus, early diagnosis of melanoma is a key issue for increasing patient survival. The overexpression of melanocortin-1 receptors (MC1R) in isolated melanoma cells and melanoma tissues led to the radiolabeling of several linear and cyclic MC analogs for melanoma imaging or therapy. Cyclization of α-melanocyte stimulating hormone (α-MSH) peptides has been successfully used to improve binding affinity and in vivo stability of peptides. Herein, we describe the different peptide cyclization strategies recently reported for radiolabeled α-MSH analogs and discuss how such strategies affect MC1R binding affinity, pharmacokinetic profile, and MC1R-melanoma imaging. This review also highlights how the nature of the radiometal and labeling approach influence those properties. Among the cyclized α-MSH peptides reported, (99m)Tc/(111)In-labeled metal-cyclized and lactam bridge-cyclized peptides displayed the highest melanoma and lowest renal uptake values in B16/F1 melanoma-bearing mice and became the most promising tools to be further explored as potential melanoma imaging probes.

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“…It is primarily responsible for the regulation of skin pigmentation [97]. As these receptors are over-expressed on the surface of human malignant melanomas [99,100], these tumors were proposed as potential targets for the application of radiolabeled -MSH peptides [101,102]. As these receptors are over-expressed on the surface of human malignant melanomas [99,100], these tumors were proposed as potential targets for the application of radiolabeled -MSH peptides [101,102].…”

Section: Alpha-melanocyte Stimulating Hormone ( -Msh)mentioning

confidence: 99%

“…99m Tc is readily available at low costs from its parent nuclide 99 Mo (t 0.5 = 66 h) from a 99 Mo/ 99m Tc generator. 99m Tc is used in about 85 % of all diagnostic applications.…”

Section: Technetium ( 99m Tc)mentioning

confidence: 99%

Targeted Tumor Diagnosis and Therapy with Peptide Hormones as Radiopharmaceuticals

Khan¹,

Beck‐Sickinger

2008

ACAMC

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Regulatory, receptor-binding peptides could be considered as future agents of choice for diagnostic imaging and therapy of cancers because their receptors are overexpressed in various human cancer cells. Peptides exhibit several advantages over classical macromolecules or drugs, e.g., from the chemical point of view: they are easy to synthesize and can withstand harsh chemical conditions which are required for chelation and radiolabeling. From the biological point of view, peptides exhibit fast blood clearance and high target-to-background ratios through receptor-mediated internalization. Furthermore, they are effective carriers for the delivery of cytotoxic drugs to target the affected tissues, thus avoiding normal cells from non-specific toxicity of anticancer agents. Owing to these features, radiolabeled receptor-binding peptides have emerged as a new class of radiopharmaceuticals for tumor scintigraphy and, more recently, to treat cancers by using peptide receptor radiation therapy (PRRT). The challenge in this scenario is to modify bioactive peptide hormones and to synthesize new sequences with improved metabolic stability without affecting the receptor binding properties after labeling with a chelator for incorporation of a radiometal. At the present time, however, the radiolabeled cholecystokinin-2 (CCK2)- and octreotide somatostatin-receptor selective analogs are the only examples that are being used in clinical practice. Other peptides such as neurotensin-, substance P-, gastrin-releasing peptide-, glucagons-like peptide 1 and neuropeptide Y (NPY) are under investigation to target breast, prostate, ovary, pancreas and brain tumors, in which overexpression of these peptide receptors has been reported. Among these peptides, neuropeptide Y (NPY) seems to be a very promising candidate because the change in its subtype receptor expression correlates with neoplastic changes. Here, we summarize the variety of experiences gained in the development of various peptide analogs, chelator/radiolabeling techniques for applications in tumor imaging and therapy.

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Binding assay for the study of melanoma cell MSH receptors

Cited by 4 publications

References 0 publications

Molecular cloning and expression of the human melanocyte stimulating hormone receptor cDNA

Molecular cloning and expression of the human melanocyte stimulating hormone receptor cDNA

Melanocortin‐1 receptor‐targeting with radiolabeled cyclic α‐melanocyte‐stimulating hormone analogs for melanoma imaging

Targeted Tumor Diagnosis and Therapy with Peptide Hormones as Radiopharmaceuticals

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