scholarly journals In vivo evaluation of188Re-labeled alpha-melanocyte stimulating hormone peptide analogs for melanoma therapy

2002 ◽  
Vol 101 (5) ◽  
pp. 480-487 ◽  
Author(s):  
Yubin Miao ◽  
Nellie K. Owen ◽  
Donna Whitener ◽  
Fabio Gallazzi ◽  
Timothy J. Hoffman ◽  
...  
Keyword(s):  
In Vivo Evaluation ◽  
Melanocyte Stimulating Hormone ◽  
Peptide Analogs ◽  
Melanoma Therapy ◽  
Stimulating Hormone

In vivo evaluation of 99mTc/188Re-labeled linear alpha-melanocyte stimulating hormone analogs for specific melanoma targeting

1999 ◽  
Vol 26 (6) ◽  
pp. 687-693 ◽  
Author(s):  
JianQing Chen ◽  
Michael F. Giblin ◽  
Nannan Wang ◽  
Silvia S. Jurisson ◽  
Thomas P. Quinn
Keyword(s):  
In Vivo Evaluation ◽  
Melanocyte Stimulating Hormone ◽  
Hormone Analogs ◽  
Stimulating Hormone

scholarly journals Synthesis of DOTA-pyridine chelates for 64Cu coordination and radiolabeling of αMSH peptide

2021 ◽  
Vol 6 (1) ◽  
Author(s):  
Hua Yang ◽  
Feng Gao ◽  
Brooke McNeil ◽  
Chengcheng Zhang ◽  
Zheliang Yuan ◽  
...  
Keyword(s):  
Full Potential ◽  
In Vivo Evaluation ◽  
Melanocortin 1 Receptor ◽  
Melanocyte Stimulating Hormone ◽  
Endogenous Copper ◽  
Coordination Ability ◽  
Copper Chelators ◽  
Cu Complexes ◽  
High Binding Affinity

Abstract Background 64Cu is one of the few radioisotopes that can be used for both imaging and therapy, enabling theranostics with identical chemical composition. Development of stable chelators is essential to harness the potential of this isotope, challenged by the presence of endogenous copper chelators. Pyridyl type chelators show good coordination ability with copper, prompting the present study of a series of chelates DOTA-xPy (x = 1–4) that sequentially substitute carboxyl moieties with pyridyl moieties on a DOTA backbone. Results We found that the presence of pyridyl groups significantly increases 64Cu labeling conversion yield, with DOTA-2Py, −3Py and -4Py quantitatively complexing 64Cu at room temperature within 5 min (1 × 10− 4 M). [64Cu]Cu-DOTA-xPy (x = 2–4) exhibited good stability in human serum up to 24 h. When challenged with 1000 eq. of NOTA, no transmetallation was observed for all three 64Cu complexes. DOTA-xPy (x = 1–3) were conjugated to a cyclized α-melanocyte-stimulating hormone (αMSH) peptide by using one of the pendant carboxyl groups as a bifunctional handle. [64Cu]Cu-DOTA-xPy-αMSH retained good serum stability (> 96% in 24 h) and showed high binding affinity (Ki = 2.1–3.7 nM) towards the melanocortin 1 receptor. Conclusion DOTA-xPy (x = 1–3) are promising chelators for 64Cu. Further in vivo evaluation is necessary to assess the full potential of these chelators as a tool to enable further theranostic radiopharmaceutical development.

Regulation of c-met expression in B16 murine melanoma cells by melanocyte stimulating hormone

1999 ◽  
Vol 112 (5) ◽  
pp. 623-630
Author(s):  
D. Rusciano ◽  
P. Lorenzoni ◽  
M.M. Burger
Keyword(s):  
Melanoma Cells ◽  
Parental Cell ◽  
Melanocortin Receptor ◽  
Parental Cell Line ◽  
Melanocyte Stimulating Hormone ◽  
Murine Melanoma ◽  
The One ◽  
Murine Melanoma Cells ◽  
Stimulating Hormone

B16 murine melanoma cells selected in vivo for enhanced liver metastatic ability (B16-LS9) show on the one hand an increased expression and constitutive activation of the proto-oncogene c-met (the receptor for hepatocyte growth factor/scatter factor), and on the other hand a more differentiated phenotype, when compared to the parental cell line, B16-F1. Following this observation, we have tried to establish whether there is a direct relationship between differentiation and c-met expression in B16 melanoma cells. Treatment of these cells with differentiating agents indicated that c-met expression was strongly induced by melanocyte stimulating hormone, while retinoic acid had almost no influence. c-met induction was triggered by engagement of the melanocortin receptor, cAMP elevation and PKA/PKC(α) activation, as respectively shown by the effects of ACTH, cAMP elevating agents and specific PK inhibitors. Regulation of c-met expression via the melanocortin receptor and cAMP raises the intriguing possibility that autocrine and/or paracrine mechanisms acting in vivo on this circuit might influence (through c-met expression and activation) the metastatic behavior of these tumor cells, which we have shown to be dependent on their c-met expression.

scholarly journals ?-melanocyte-stimulating hormone peptide analogs labeled with technetium-99m and indium-111 for malignant melanoma targeting

Cancer ◽  
2002 ◽  
Vol 94 (S4) ◽  
pp. 1196-1201 ◽  
Author(s):  
JianQing Chen ◽  
Zhen Cheng ◽  
Yubin Miao ◽  
Silvia S. Jurisson ◽  
Thomas P. Quinn
Keyword(s):  
Malignant Melanoma ◽  
Technetium 99M ◽  
Melanocyte Stimulating Hormone ◽  
Peptide Analogs ◽  
Indium 111 ◽  
Stimulating Hormone

scholarly journals Synthesis of DOTA-Pyridine Chelates for 64Cu Coordination and Radiolabeling of αMSH Peptide

2020 ◽  
Author(s):  
Hua Yang ◽  
Feng Gao ◽  
Brooke McNeil ◽  
Chengcheng Zhang ◽  
Stefan Zeisler ◽  
...  
Keyword(s):  
Full Potential ◽  
In Vivo Evaluation ◽  
Melanocortin 1 Receptor ◽  
Melanocyte Stimulating Hormone ◽  
Endogenous Copper ◽  
Coordination Ability ◽  
Copper Chelators ◽  
Cu Complexes ◽  
High Binding Affinity

Abstract Background : 64Cu is one of the few radioisotopes that can be used for both imaging and therapy, enabling theranostics with identical chemical composition. Development of stable chelators is essential to harness the potential of this isotope, challenged by the presence of endogenous copper chelators. Pyridyl type chelators show good coordination ability with copper, prompting the present study of a series of chelates DOTA-xPy (x=1-4) that sequentially substitute carboxyl moieties with pyridyl moieties on a DOTA backbone. Results: We found that the presence of pyridyl groups significantly increases 64 Cu labeling yield, with DOTA-2Py, -3Py and -4Py quantitatively complexing 64 Cu at room temperature within 5 min (10 -4 M). [ 64 Cu]Cu-DOTA-xPy (x=2-4) exhibited good stability in human serum up to 24 hours. When challenged with 1000 eq. of NOTA, no transmetallation was observed for all three 64 Cu complexes. DOTA-xPy (x=1-3) were conjugated to a cyclized α-melanocyte-stimulating hormone (αMSH) peptide by using one of the pendant carboxyl groups as a bifunctional handle. [ 64 Cu]Cu-DOTA-xPy-αMSH retained good serum stability (>96% in 24 hours) and showed high binding affinity (Ki=2.1-3.7 nM) towards the melanocortin 1 receptor. Conclusion : DOTA-xPy (x=1-3) are promising chelators for 64 Cu. Further in vivo evaluation is necessary to assess the full potential of these chelators as a tool to enable further theranostic radiopharmaceutical development.

Des-acetylated variants of α-melanocyte-stimulating hormone and β-endorphin can antagonize the mammotrope-recruiting activity of their acetylated forms

1993 ◽  
Vol 139 (2) ◽  
pp. 295-300 ◽  
Author(s):  
E. Ellerkmann ◽  
R. D. Kineman ◽  
T. E. Porter ◽  
L. S. Frawley
Keyword(s):  
Cell Cultures ◽  
Anterior Pituitary ◽  
Relative Number ◽  
Pituitary Cell ◽  
Ovariectomized Rats ◽  
Anterior Pituitary Cell ◽  
Melanocyte Stimulating Hormone ◽  
Absolute Requirement ◽  
Stimulating Hormone

ABSTRACT We have previously reported that hypophysial neurointermediate lobe peptides, di-acetylated α-melanocyte-stimulating hormone (di-ac-α-MSH) and N-acetylated β-endorphin (N-ac-β-END), can acutely increase the relative number of prolactin-secreting cells in anterior pituitary cell cultures from ovariectomized rats. Inasmuch as the des-acetylated forms of these peptides (des-ac-α-MSH and β-END) were not effective in this regard, we concluded that acetylation was an absolute requirement for manifestation of the recruitment response. The aim of the present study was to determine whether these des-acetylated variants could antagonize the mammotrope-recruiting activity of their acetylated congeners. Treatment of anterior pituitary cell cultures with di-ac-α-MSH and N-ac-β-END increased the relative amount of prolactin secretors above control values. Interestingly, des-acetylated variants of α-MSH and β-END blocked the mammotrope-recruitment activity of their respective acetylated forms. In addition, β-END antagonized the mammotrope-recruitment activity of di-ac-α-MSH while des-ac-α-MSH did not attenuate the stimulatory effect of N-ac-β-END. Given that mammotropes maintained in vivo are exposed to all these peptides, it is possible that these acetylated and non-acetylated congeners may act in an opposing manner to regulate dynamic prolactin release. Journal of Endocrinology (1993) 139, 295–300

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