Combining elements from two antagonists of formyl peptide receptor 2 generates more potent peptidomimetic antagonists

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

Standard

Combining elements from two antagonists of formyl peptide receptor 2 generates more potent peptidomimetic antagonists. / Skovbakke, Sarah Line; Holdfeldt, Andre; Nielsen, Christina; Hansen, Anna Mette; Perez-Gassol, Iris; Dahlgren, Claes; Forsman, Huamei; Franzyk, Henrik.

In: Journal of Medicinal Chemistry, Vol. 60, No. 16, 2017, p. 6991-6997.

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

Harvard

Skovbakke, SL, Holdfeldt, A, Nielsen, C, Hansen, AM, Perez-Gassol, I, Dahlgren, C, Forsman, H & Franzyk, H 2017, 'Combining elements from two antagonists of formyl peptide receptor 2 generates more potent peptidomimetic antagonists', Journal of Medicinal Chemistry, vol. 60, no. 16, pp. 6991-6997. https://doi.org/10.1021/acs.jmedchem.7b00489

APA

Skovbakke, S. L., Holdfeldt, A., Nielsen, C., Hansen, A. M., Perez-Gassol, I., Dahlgren, C., Forsman, H., & Franzyk, H. (2017). Combining elements from two antagonists of formyl peptide receptor 2 generates more potent peptidomimetic antagonists. Journal of Medicinal Chemistry, 60(16), 6991-6997. https://doi.org/10.1021/acs.jmedchem.7b00489

Vancouver

Skovbakke SL, Holdfeldt A, Nielsen C, Hansen AM, Perez-Gassol I, Dahlgren C et al. Combining elements from two antagonists of formyl peptide receptor 2 generates more potent peptidomimetic antagonists. Journal of Medicinal Chemistry. 2017;60(16):6991-6997. https://doi.org/10.1021/acs.jmedchem.7b00489

Author

Skovbakke, Sarah Line ; Holdfeldt, Andre ; Nielsen, Christina ; Hansen, Anna Mette ; Perez-Gassol, Iris ; Dahlgren, Claes ; Forsman, Huamei ; Franzyk, Henrik. / Combining elements from two antagonists of formyl peptide receptor 2 generates more potent peptidomimetic antagonists. In: Journal of Medicinal Chemistry. 2017 ; Vol. 60, No. 16. pp. 6991-6997.

Bibtex

@article{8dc3b13b974444e9b45a103b47d040f9,
title = "Combining elements from two antagonists of formyl peptide receptor 2 generates more potent peptidomimetic antagonists",
abstract = "Structural optimization of a peptidomimetic antagonist of formyl peptide receptor 2 (FPR2) was explored by an approach involving combination of elements from the two most potent FPR2 antagonists described: a Rhodamine B-conjugated 10-residue gelsonin-derived peptide (i.e., PBP10, RhB-QRLFQVKGRR-OH) and the palmitoylated α-peptide/β-peptoid hybrid Pam-(Lys-βNspe)6-NH2. This generated an array of hybrid compounds from which a new subclass of receptor-selective antagonists was identified. The most potent representatives displayed activity in the low nanomolar range. The resulting stable and potent FPR2-selective antagonists (i.e., RhB-(Lys-βNphe)n-NH2; n = 4–6) are expected to become valuable tools in further elucidation of the physiological role of FPR2 in health and disease.",
author = "Skovbakke, {Sarah Line} and Andre Holdfeldt and Christina Nielsen and Hansen, {Anna Mette} and Iris Perez-Gassol and Claes Dahlgren and Huamei Forsman and Henrik Franzyk",
year = "2017",
doi = "10.1021/acs.jmedchem.7b00489",
language = "English",
volume = "60",
pages = "6991--6997",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "16",

}

RIS

TY - JOUR

T1 - Combining elements from two antagonists of formyl peptide receptor 2 generates more potent peptidomimetic antagonists

AU - Skovbakke, Sarah Line

AU - Holdfeldt, Andre

AU - Nielsen, Christina

AU - Hansen, Anna Mette

AU - Perez-Gassol, Iris

AU - Dahlgren, Claes

AU - Forsman, Huamei

AU - Franzyk, Henrik

PY - 2017

Y1 - 2017

N2 - Structural optimization of a peptidomimetic antagonist of formyl peptide receptor 2 (FPR2) was explored by an approach involving combination of elements from the two most potent FPR2 antagonists described: a Rhodamine B-conjugated 10-residue gelsonin-derived peptide (i.e., PBP10, RhB-QRLFQVKGRR-OH) and the palmitoylated α-peptide/β-peptoid hybrid Pam-(Lys-βNspe)6-NH2. This generated an array of hybrid compounds from which a new subclass of receptor-selective antagonists was identified. The most potent representatives displayed activity in the low nanomolar range. The resulting stable and potent FPR2-selective antagonists (i.e., RhB-(Lys-βNphe)n-NH2; n = 4–6) are expected to become valuable tools in further elucidation of the physiological role of FPR2 in health and disease.

AB - Structural optimization of a peptidomimetic antagonist of formyl peptide receptor 2 (FPR2) was explored by an approach involving combination of elements from the two most potent FPR2 antagonists described: a Rhodamine B-conjugated 10-residue gelsonin-derived peptide (i.e., PBP10, RhB-QRLFQVKGRR-OH) and the palmitoylated α-peptide/β-peptoid hybrid Pam-(Lys-βNspe)6-NH2. This generated an array of hybrid compounds from which a new subclass of receptor-selective antagonists was identified. The most potent representatives displayed activity in the low nanomolar range. The resulting stable and potent FPR2-selective antagonists (i.e., RhB-(Lys-βNphe)n-NH2; n = 4–6) are expected to become valuable tools in further elucidation of the physiological role of FPR2 in health and disease.

U2 - 10.1021/acs.jmedchem.7b00489

DO - 10.1021/acs.jmedchem.7b00489

M3 - Journal article

C2 - 28700225

VL - 60

SP - 6991

EP - 6997

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

SN - 0022-2623

IS - 16

ER -

ID: 182521174