Ranatensin

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Philippe Fernandez - One of the best experts on this subject based on the ideXlab platform.

  • a new class of radiopeptides for pet imaging of neuromedin b receptor 68ga Ranatensin analogs
    MedChemComm, 2016
    Co-Authors: Clément Morgat, Raunak Varshney, Delphine Vimont, C. Riès, C. Chanseau, Sandrine S. Bertrand, Anil K. Mishra, Elif Hindié, C Savonabaron, Philippe Fernandez
    Abstract:

    The neuromedin B receptor (NMB-R) is a promising target in several human processes, for instance thymic carcinoma, intestinal carcinoids, pruritus, etc. NMB-R Positron Emission Tomography (PET) molecular imaging may be of great value. We here report on the development of the first 68Ga-Ranatensin analog. The Ranatensin derivative (Aib-Gln-Trp-Ala-Val-Gly-His-Phe-Met-CONH2, RV_15) was synthesized and conjugated to the DOTA macrocycle with good yield. This chelator is particularly suitable for 68Ga (T1/2 = 67.71 min, β+ branching = 89.14%) radiolabeling. Radiochemical purity, hydrophilicity, stability, pharmacological properties, inhibitory concentrations (IC50) and biodistribution in normal strain-A mice were investigated. Radiochemical purity of the 68Ga-Ranatensin analog was always >97%. The non-radioactive analog, natGa-DOTA–RV_15, was found to be hydrophilic and behaves like an agonist to NMB-R and GRP-R (gastrin-releasing-peptide receptor which is another subtype of bombesin receptor) (EC50 values of 5.6 ± 0.1 × 10−9 M and 2.1 ± 0.1 × 10−9 M, respectively). Moreover, it showed nanomolar binding inhibitory concentrations for human NMB-R (IC50 = 3.0 ± 1.1 × 10−8 M) and somewhat less for human GRP-R (IC50 = 3.2 ± 1.2 × 10−7 M) in a competitive binding assay. 68Ga-DOTA–RV_15 is stable in plasma up to 45 minutes. Finally, this 68Ga-Ranatensin agonist demonstrated rapid blood and urinary clearances and uptake in the pancreas and kidneys in normal mice. In conclusion, we have developed a novel class of radiopeptide analogue which potentially could be used for NMB-R molecular imaging.

  • Correction: A new class of radiopeptides for PET imaging of neuromedin-B receptor: 68Ga-Ranatensin analogs
    MedChemComm, 2016
    Co-Authors: Clément Morgat, Raunak Varshney, Delphine Vimont, C. Savona-baron, C. Riès, C. Chanseau, Sandrine S. Bertrand, Anil K. Mishra, Elif Hindié, Philippe Fernandez
    Abstract:

    Correction for ‘A new class of radiopeptides for PET imaging of neuromedin-B receptor: 68Ga-Ranatensin analogs’ by C. Morgat et al., Med. Chem. Commun., 2016, 7, 1217–1223.

Clément Morgat - One of the best experts on this subject based on the ideXlab platform.

  • a new class of radiopeptides for pet imaging of neuromedin b receptor 68ga Ranatensin analogs
    MedChemComm, 2016
    Co-Authors: Clément Morgat, Raunak Varshney, Delphine Vimont, C. Riès, C. Chanseau, Sandrine S. Bertrand, Anil K. Mishra, Elif Hindié, C Savonabaron, Philippe Fernandez
    Abstract:

    The neuromedin B receptor (NMB-R) is a promising target in several human processes, for instance thymic carcinoma, intestinal carcinoids, pruritus, etc. NMB-R Positron Emission Tomography (PET) molecular imaging may be of great value. We here report on the development of the first 68Ga-Ranatensin analog. The Ranatensin derivative (Aib-Gln-Trp-Ala-Val-Gly-His-Phe-Met-CONH2, RV_15) was synthesized and conjugated to the DOTA macrocycle with good yield. This chelator is particularly suitable for 68Ga (T1/2 = 67.71 min, β+ branching = 89.14%) radiolabeling. Radiochemical purity, hydrophilicity, stability, pharmacological properties, inhibitory concentrations (IC50) and biodistribution in normal strain-A mice were investigated. Radiochemical purity of the 68Ga-Ranatensin analog was always >97%. The non-radioactive analog, natGa-DOTA–RV_15, was found to be hydrophilic and behaves like an agonist to NMB-R and GRP-R (gastrin-releasing-peptide receptor which is another subtype of bombesin receptor) (EC50 values of 5.6 ± 0.1 × 10−9 M and 2.1 ± 0.1 × 10−9 M, respectively). Moreover, it showed nanomolar binding inhibitory concentrations for human NMB-R (IC50 = 3.0 ± 1.1 × 10−8 M) and somewhat less for human GRP-R (IC50 = 3.2 ± 1.2 × 10−7 M) in a competitive binding assay. 68Ga-DOTA–RV_15 is stable in plasma up to 45 minutes. Finally, this 68Ga-Ranatensin agonist demonstrated rapid blood and urinary clearances and uptake in the pancreas and kidneys in normal mice. In conclusion, we have developed a novel class of radiopeptide analogue which potentially could be used for NMB-R molecular imaging.

  • Correction: A new class of radiopeptides for PET imaging of neuromedin-B receptor: 68Ga-Ranatensin analogs
    MedChemComm, 2016
    Co-Authors: Clément Morgat, Raunak Varshney, Delphine Vimont, C. Savona-baron, C. Riès, C. Chanseau, Sandrine S. Bertrand, Anil K. Mishra, Elif Hindié, Philippe Fernandez
    Abstract:

    Correction for ‘A new class of radiopeptides for PET imaging of neuromedin-B receptor: 68Ga-Ranatensin analogs’ by C. Morgat et al., Med. Chem. Commun., 2016, 7, 1217–1223.

Elif Hindié - One of the best experts on this subject based on the ideXlab platform.

  • a new class of radiopeptides for pet imaging of neuromedin b receptor 68ga Ranatensin analogs
    MedChemComm, 2016
    Co-Authors: Clément Morgat, Raunak Varshney, Delphine Vimont, C. Riès, C. Chanseau, Sandrine S. Bertrand, Anil K. Mishra, Elif Hindié, C Savonabaron, Philippe Fernandez
    Abstract:

    The neuromedin B receptor (NMB-R) is a promising target in several human processes, for instance thymic carcinoma, intestinal carcinoids, pruritus, etc. NMB-R Positron Emission Tomography (PET) molecular imaging may be of great value. We here report on the development of the first 68Ga-Ranatensin analog. The Ranatensin derivative (Aib-Gln-Trp-Ala-Val-Gly-His-Phe-Met-CONH2, RV_15) was synthesized and conjugated to the DOTA macrocycle with good yield. This chelator is particularly suitable for 68Ga (T1/2 = 67.71 min, β+ branching = 89.14%) radiolabeling. Radiochemical purity, hydrophilicity, stability, pharmacological properties, inhibitory concentrations (IC50) and biodistribution in normal strain-A mice were investigated. Radiochemical purity of the 68Ga-Ranatensin analog was always >97%. The non-radioactive analog, natGa-DOTA–RV_15, was found to be hydrophilic and behaves like an agonist to NMB-R and GRP-R (gastrin-releasing-peptide receptor which is another subtype of bombesin receptor) (EC50 values of 5.6 ± 0.1 × 10−9 M and 2.1 ± 0.1 × 10−9 M, respectively). Moreover, it showed nanomolar binding inhibitory concentrations for human NMB-R (IC50 = 3.0 ± 1.1 × 10−8 M) and somewhat less for human GRP-R (IC50 = 3.2 ± 1.2 × 10−7 M) in a competitive binding assay. 68Ga-DOTA–RV_15 is stable in plasma up to 45 minutes. Finally, this 68Ga-Ranatensin agonist demonstrated rapid blood and urinary clearances and uptake in the pancreas and kidneys in normal mice. In conclusion, we have developed a novel class of radiopeptide analogue which potentially could be used for NMB-R molecular imaging.

  • Correction: A new class of radiopeptides for PET imaging of neuromedin-B receptor: 68Ga-Ranatensin analogs
    MedChemComm, 2016
    Co-Authors: Clément Morgat, Raunak Varshney, Delphine Vimont, C. Savona-baron, C. Riès, C. Chanseau, Sandrine S. Bertrand, Anil K. Mishra, Elif Hindié, Philippe Fernandez
    Abstract:

    Correction for ‘A new class of radiopeptides for PET imaging of neuromedin-B receptor: 68Ga-Ranatensin analogs’ by C. Morgat et al., Med. Chem. Commun., 2016, 7, 1217–1223.

Anil K. Mishra - One of the best experts on this subject based on the ideXlab platform.

  • a new class of radiopeptides for pet imaging of neuromedin b receptor 68ga Ranatensin analogs
    MedChemComm, 2016
    Co-Authors: Clément Morgat, Raunak Varshney, Delphine Vimont, C. Riès, C. Chanseau, Sandrine S. Bertrand, Anil K. Mishra, Elif Hindié, C Savonabaron, Philippe Fernandez
    Abstract:

    The neuromedin B receptor (NMB-R) is a promising target in several human processes, for instance thymic carcinoma, intestinal carcinoids, pruritus, etc. NMB-R Positron Emission Tomography (PET) molecular imaging may be of great value. We here report on the development of the first 68Ga-Ranatensin analog. The Ranatensin derivative (Aib-Gln-Trp-Ala-Val-Gly-His-Phe-Met-CONH2, RV_15) was synthesized and conjugated to the DOTA macrocycle with good yield. This chelator is particularly suitable for 68Ga (T1/2 = 67.71 min, β+ branching = 89.14%) radiolabeling. Radiochemical purity, hydrophilicity, stability, pharmacological properties, inhibitory concentrations (IC50) and biodistribution in normal strain-A mice were investigated. Radiochemical purity of the 68Ga-Ranatensin analog was always >97%. The non-radioactive analog, natGa-DOTA–RV_15, was found to be hydrophilic and behaves like an agonist to NMB-R and GRP-R (gastrin-releasing-peptide receptor which is another subtype of bombesin receptor) (EC50 values of 5.6 ± 0.1 × 10−9 M and 2.1 ± 0.1 × 10−9 M, respectively). Moreover, it showed nanomolar binding inhibitory concentrations for human NMB-R (IC50 = 3.0 ± 1.1 × 10−8 M) and somewhat less for human GRP-R (IC50 = 3.2 ± 1.2 × 10−7 M) in a competitive binding assay. 68Ga-DOTA–RV_15 is stable in plasma up to 45 minutes. Finally, this 68Ga-Ranatensin agonist demonstrated rapid blood and urinary clearances and uptake in the pancreas and kidneys in normal mice. In conclusion, we have developed a novel class of radiopeptide analogue which potentially could be used for NMB-R molecular imaging.

  • Correction: A new class of radiopeptides for PET imaging of neuromedin-B receptor: 68Ga-Ranatensin analogs
    MedChemComm, 2016
    Co-Authors: Clément Morgat, Raunak Varshney, Delphine Vimont, C. Savona-baron, C. Riès, C. Chanseau, Sandrine S. Bertrand, Anil K. Mishra, Elif Hindié, Philippe Fernandez
    Abstract:

    Correction for ‘A new class of radiopeptides for PET imaging of neuromedin-B receptor: 68Ga-Ranatensin analogs’ by C. Morgat et al., Med. Chem. Commun., 2016, 7, 1217–1223.

Sandrine S. Bertrand - One of the best experts on this subject based on the ideXlab platform.

  • a new class of radiopeptides for pet imaging of neuromedin b receptor 68ga Ranatensin analogs
    MedChemComm, 2016
    Co-Authors: Clément Morgat, Raunak Varshney, Delphine Vimont, C. Riès, C. Chanseau, Sandrine S. Bertrand, Anil K. Mishra, Elif Hindié, C Savonabaron, Philippe Fernandez
    Abstract:

    The neuromedin B receptor (NMB-R) is a promising target in several human processes, for instance thymic carcinoma, intestinal carcinoids, pruritus, etc. NMB-R Positron Emission Tomography (PET) molecular imaging may be of great value. We here report on the development of the first 68Ga-Ranatensin analog. The Ranatensin derivative (Aib-Gln-Trp-Ala-Val-Gly-His-Phe-Met-CONH2, RV_15) was synthesized and conjugated to the DOTA macrocycle with good yield. This chelator is particularly suitable for 68Ga (T1/2 = 67.71 min, β+ branching = 89.14%) radiolabeling. Radiochemical purity, hydrophilicity, stability, pharmacological properties, inhibitory concentrations (IC50) and biodistribution in normal strain-A mice were investigated. Radiochemical purity of the 68Ga-Ranatensin analog was always >97%. The non-radioactive analog, natGa-DOTA–RV_15, was found to be hydrophilic and behaves like an agonist to NMB-R and GRP-R (gastrin-releasing-peptide receptor which is another subtype of bombesin receptor) (EC50 values of 5.6 ± 0.1 × 10−9 M and 2.1 ± 0.1 × 10−9 M, respectively). Moreover, it showed nanomolar binding inhibitory concentrations for human NMB-R (IC50 = 3.0 ± 1.1 × 10−8 M) and somewhat less for human GRP-R (IC50 = 3.2 ± 1.2 × 10−7 M) in a competitive binding assay. 68Ga-DOTA–RV_15 is stable in plasma up to 45 minutes. Finally, this 68Ga-Ranatensin agonist demonstrated rapid blood and urinary clearances and uptake in the pancreas and kidneys in normal mice. In conclusion, we have developed a novel class of radiopeptide analogue which potentially could be used for NMB-R molecular imaging.

  • Correction: A new class of radiopeptides for PET imaging of neuromedin-B receptor: 68Ga-Ranatensin analogs
    MedChemComm, 2016
    Co-Authors: Clément Morgat, Raunak Varshney, Delphine Vimont, C. Savona-baron, C. Riès, C. Chanseau, Sandrine S. Bertrand, Anil K. Mishra, Elif Hindié, Philippe Fernandez
    Abstract:

    Correction for ‘A new class of radiopeptides for PET imaging of neuromedin-B receptor: 68Ga-Ranatensin analogs’ by C. Morgat et al., Med. Chem. Commun., 2016, 7, 1217–1223.