Synthesis and characterisation of substrate-based peptides as inhibitors of histone demethylase KDM4C

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Synthesis and characterisation of substrate-based peptides as inhibitors of histone demethylase KDM4C. / Nielsen, Simon D; Leurs, Ulrike; Bergner, Magnus; Barris, Silvia Amor; Devkota, Kanchan; Meyer, Kamilla; Iaria, Daniella; McCaughan, Jack; Lohse, Brian; Kristensen, Jesper L; Clausen, Rasmus Prætorius.

In: Protein and Peptide Letters, Vol. 23, No. 9, 13.06.2016, p. 772 - 776.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Nielsen, SD, Leurs, U, Bergner, M, Barris, SA, Devkota, K, Meyer, K, Iaria, D, McCaughan, J, Lohse, B, Kristensen, JL & Clausen, RP 2016, 'Synthesis and characterisation of substrate-based peptides as inhibitors of histone demethylase KDM4C', Protein and Peptide Letters, vol. 23, no. 9, pp. 772 - 776. https://doi.org/10.2174/0929866523666160613210831

APA

Nielsen, S. D., Leurs, U., Bergner, M., Barris, S. A., Devkota, K., Meyer, K., ... Clausen, R. P. (2016). Synthesis and characterisation of substrate-based peptides as inhibitors of histone demethylase KDM4C. Protein and Peptide Letters, 23(9), 772 - 776. https://doi.org/10.2174/0929866523666160613210831

Vancouver

Nielsen SD, Leurs U, Bergner M, Barris SA, Devkota K, Meyer K et al. Synthesis and characterisation of substrate-based peptides as inhibitors of histone demethylase KDM4C. Protein and Peptide Letters. 2016 Jun 13;23(9):772 - 776. https://doi.org/10.2174/0929866523666160613210831

Author

Nielsen, Simon D ; Leurs, Ulrike ; Bergner, Magnus ; Barris, Silvia Amor ; Devkota, Kanchan ; Meyer, Kamilla ; Iaria, Daniella ; McCaughan, Jack ; Lohse, Brian ; Kristensen, Jesper L ; Clausen, Rasmus Prætorius. / Synthesis and characterisation of substrate-based peptides as inhibitors of histone demethylase KDM4C. In: Protein and Peptide Letters. 2016 ; Vol. 23, No. 9. pp. 772 - 776.

Bibtex

@article{481db8fd20e84fff84a3ab2265623255,
title = "Synthesis and characterisation of substrate-based peptides as inhibitors of histone demethylase KDM4C",
abstract = "The design and synthesis of modified pentapeptides based on a truncated version of the substrate for KDM4C, a histone lysine demethylase (KDM), and investigation of their inhibitory activity at KDM4C is reported. By modifying the lysine residue corresponding to lysine 9 at histone 3 (H3K9), three different series of peptides were designed and synthesized. One series contained N-acylated H3K9 and two series introduced triazoles in this position via click chemistry to enable facile variation of headgroups. As the click reaction is compatible with free amino acids this was performed on an azido containing deprotected pentapeptide, thus demonstrating a highly facile and convergent synthetic strategy for making substrate-based inhibitors. One of the 14 peptides showed inhibitory activity at KDM4C demonstrating the need for an iron chelator in the pentapeptide series.",
author = "Nielsen, {Simon D} and Ulrike Leurs and Magnus Bergner and Barris, {Silvia Amor} and Kanchan Devkota and Kamilla Meyer and Daniella Iaria and Jack McCaughan and Brian Lohse and Kristensen, {Jesper L} and Clausen, {Rasmus Pr{\ae}torius}",
year = "2016",
month = "6",
day = "13",
doi = "10.2174/0929866523666160613210831",
language = "English",
volume = "23",
pages = "772 -- 776",
journal = "Protein and Peptide Letters",
issn = "0929-8665",
publisher = "Bentham Science Publishers",
number = "9",

}

RIS

TY - JOUR

T1 - Synthesis and characterisation of substrate-based peptides as inhibitors of histone demethylase KDM4C

AU - Nielsen, Simon D

AU - Leurs, Ulrike

AU - Bergner, Magnus

AU - Barris, Silvia Amor

AU - Devkota, Kanchan

AU - Meyer, Kamilla

AU - Iaria, Daniella

AU - McCaughan, Jack

AU - Lohse, Brian

AU - Kristensen, Jesper L

AU - Clausen, Rasmus Prætorius

PY - 2016/6/13

Y1 - 2016/6/13

N2 - The design and synthesis of modified pentapeptides based on a truncated version of the substrate for KDM4C, a histone lysine demethylase (KDM), and investigation of their inhibitory activity at KDM4C is reported. By modifying the lysine residue corresponding to lysine 9 at histone 3 (H3K9), three different series of peptides were designed and synthesized. One series contained N-acylated H3K9 and two series introduced triazoles in this position via click chemistry to enable facile variation of headgroups. As the click reaction is compatible with free amino acids this was performed on an azido containing deprotected pentapeptide, thus demonstrating a highly facile and convergent synthetic strategy for making substrate-based inhibitors. One of the 14 peptides showed inhibitory activity at KDM4C demonstrating the need for an iron chelator in the pentapeptide series.

AB - The design and synthesis of modified pentapeptides based on a truncated version of the substrate for KDM4C, a histone lysine demethylase (KDM), and investigation of their inhibitory activity at KDM4C is reported. By modifying the lysine residue corresponding to lysine 9 at histone 3 (H3K9), three different series of peptides were designed and synthesized. One series contained N-acylated H3K9 and two series introduced triazoles in this position via click chemistry to enable facile variation of headgroups. As the click reaction is compatible with free amino acids this was performed on an azido containing deprotected pentapeptide, thus demonstrating a highly facile and convergent synthetic strategy for making substrate-based inhibitors. One of the 14 peptides showed inhibitory activity at KDM4C demonstrating the need for an iron chelator in the pentapeptide series.

U2 - 10.2174/0929866523666160613210831

DO - 10.2174/0929866523666160613210831

M3 - Journal article

VL - 23

SP - 772

EP - 776

JO - Protein and Peptide Letters

JF - Protein and Peptide Letters

SN - 0929-8665

IS - 9

ER -

ID: 162710545