Synthesis and in Vitro Evaluation of Stabilized and Selective Neuromedin U-1 Receptor Agonists

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Synthesis and in Vitro Evaluation of Stabilized and Selective Neuromedin U-1 Receptor Agonists. / De Prins, An; Martin, Charlotte; Van Wanseele, Yannick; Tömböly, Csaba; Tourwé, Dirk; Caveliers, Vicky; Holst, Birgitte; Van Eeckhaut, Ann; Rosenkilde, Mette M; Smolders, Ilse; Ballet, Steven.

In: ACS Medicinal Chemistry Letters, Vol. 9, No. 5, 10.05.2018, p. 496-501.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

De Prins, A, Martin, C, Van Wanseele, Y, Tömböly, C, Tourwé, D, Caveliers, V, Holst, B, Van Eeckhaut, A, Rosenkilde, MM, Smolders, I & Ballet, S 2018, 'Synthesis and in Vitro Evaluation of Stabilized and Selective Neuromedin U-1 Receptor Agonists', ACS Medicinal Chemistry Letters, vol. 9, no. 5, pp. 496-501. https://doi.org/10.1021/acsmedchemlett.8b00105

APA

De Prins, A., Martin, C., Van Wanseele, Y., Tömböly, C., Tourwé, D., Caveliers, V., Holst, B., Van Eeckhaut, A., Rosenkilde, M. M., Smolders, I., & Ballet, S. (2018). Synthesis and in Vitro Evaluation of Stabilized and Selective Neuromedin U-1 Receptor Agonists. ACS Medicinal Chemistry Letters, 9(5), 496-501. https://doi.org/10.1021/acsmedchemlett.8b00105

Vancouver

De Prins A, Martin C, Van Wanseele Y, Tömböly C, Tourwé D, Caveliers V et al. Synthesis and in Vitro Evaluation of Stabilized and Selective Neuromedin U-1 Receptor Agonists. ACS Medicinal Chemistry Letters. 2018 May 10;9(5):496-501. https://doi.org/10.1021/acsmedchemlett.8b00105

Author

De Prins, An ; Martin, Charlotte ; Van Wanseele, Yannick ; Tömböly, Csaba ; Tourwé, Dirk ; Caveliers, Vicky ; Holst, Birgitte ; Van Eeckhaut, Ann ; Rosenkilde, Mette M ; Smolders, Ilse ; Ballet, Steven. / Synthesis and in Vitro Evaluation of Stabilized and Selective Neuromedin U-1 Receptor Agonists. In: ACS Medicinal Chemistry Letters. 2018 ; Vol. 9, No. 5. pp. 496-501.

Bibtex

@article{b08d948300fe4373a426edb97fe6bef8,
title = "Synthesis and in Vitro Evaluation of Stabilized and Selective Neuromedin U-1 Receptor Agonists",
abstract = "Neuromedin U (NMU) is a multifunctional neuropeptide which is characterized by a high conservation through all species. Herein, we describe the synthesis of a novel set of NMU-analogs based on the truncated NMU-8. Through combination of previously reported modifications, an elaborate structure-activity relationship study was performed aiming for the development of peptides with an increased selectivity toward NMU receptor 1 (NMUR1). Compound 7 possessed the highest NMUR1 selectivity (IC50 = 0.54 nM, selectivity ratio = 5313) together with an increased potency (EC50 = 3.7 nM), an 18% increase of the maximal effect at NMUR1, and a higher resistance against enzymatic degradation as compared to the native NMU-8. The development of a potent NMUR1 agonist with extended half-life could represent an attractive tool to further unveil the role of NMUR1 in NMU signaling.",
author = "{De Prins}, An and Charlotte Martin and {Van Wanseele}, Yannick and Csaba T{\"o}mb{\"o}ly and Dirk Tourw{\'e} and Vicky Caveliers and Birgitte Holst and {Van Eeckhaut}, Ann and Rosenkilde, {Mette M} and Ilse Smolders and Steven Ballet",
year = "2018",
month = may,
day = "10",
doi = "10.1021/acsmedchemlett.8b00105",
language = "English",
volume = "9",
pages = "496--501",
journal = "ACS Medicinal Chemistry Letters",
issn = "1948-5875",
publisher = "American Chemical Society",
number = "5",

}

RIS

TY - JOUR

T1 - Synthesis and in Vitro Evaluation of Stabilized and Selective Neuromedin U-1 Receptor Agonists

AU - De Prins, An

AU - Martin, Charlotte

AU - Van Wanseele, Yannick

AU - Tömböly, Csaba

AU - Tourwé, Dirk

AU - Caveliers, Vicky

AU - Holst, Birgitte

AU - Van Eeckhaut, Ann

AU - Rosenkilde, Mette M

AU - Smolders, Ilse

AU - Ballet, Steven

PY - 2018/5/10

Y1 - 2018/5/10

N2 - Neuromedin U (NMU) is a multifunctional neuropeptide which is characterized by a high conservation through all species. Herein, we describe the synthesis of a novel set of NMU-analogs based on the truncated NMU-8. Through combination of previously reported modifications, an elaborate structure-activity relationship study was performed aiming for the development of peptides with an increased selectivity toward NMU receptor 1 (NMUR1). Compound 7 possessed the highest NMUR1 selectivity (IC50 = 0.54 nM, selectivity ratio = 5313) together with an increased potency (EC50 = 3.7 nM), an 18% increase of the maximal effect at NMUR1, and a higher resistance against enzymatic degradation as compared to the native NMU-8. The development of a potent NMUR1 agonist with extended half-life could represent an attractive tool to further unveil the role of NMUR1 in NMU signaling.

AB - Neuromedin U (NMU) is a multifunctional neuropeptide which is characterized by a high conservation through all species. Herein, we describe the synthesis of a novel set of NMU-analogs based on the truncated NMU-8. Through combination of previously reported modifications, an elaborate structure-activity relationship study was performed aiming for the development of peptides with an increased selectivity toward NMU receptor 1 (NMUR1). Compound 7 possessed the highest NMUR1 selectivity (IC50 = 0.54 nM, selectivity ratio = 5313) together with an increased potency (EC50 = 3.7 nM), an 18% increase of the maximal effect at NMUR1, and a higher resistance against enzymatic degradation as compared to the native NMU-8. The development of a potent NMUR1 agonist with extended half-life could represent an attractive tool to further unveil the role of NMUR1 in NMU signaling.

U2 - 10.1021/acsmedchemlett.8b00105

DO - 10.1021/acsmedchemlett.8b00105

M3 - Journal article

C2 - 29795766

VL - 9

SP - 496

EP - 501

JO - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

SN - 1948-5875

IS - 5

ER -

ID: 209112675