Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C)

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Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C). / Leurs, Ulrike; Clausen, Rasmus P; Kristensen, Jesper L; Lohse, Brian.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 22, No. 18, 15.09.2012, p. 5811-3.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Leurs, U, Clausen, RP, Kristensen, JL & Lohse, B 2012, 'Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C)', Bioorganic & Medicinal Chemistry Letters, vol. 22, no. 18, pp. 5811-3. https://doi.org/10.1016/j.bmcl.2012.07.091

APA

Leurs, U., Clausen, R. P., Kristensen, J. L., & Lohse, B. (2012). Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C). Bioorganic & Medicinal Chemistry Letters, 22(18), 5811-3. https://doi.org/10.1016/j.bmcl.2012.07.091

Vancouver

Leurs U, Clausen RP, Kristensen JL, Lohse B. Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C). Bioorganic & Medicinal Chemistry Letters. 2012 Sep 15;22(18):5811-3. https://doi.org/10.1016/j.bmcl.2012.07.091

Author

Leurs, Ulrike ; Clausen, Rasmus P ; Kristensen, Jesper L ; Lohse, Brian. / Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C). In: Bioorganic & Medicinal Chemistry Letters. 2012 ; Vol. 22, No. 18. pp. 5811-3.

Bibtex

@article{808a051a931e40aa9b4a773083258fa6,
title = "Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C)",
abstract = "The human histone demethylases of the KDM4 (JMJD2) family have been associated to diseases such as prostate and breast cancer, as well as X-linked mental retardation. Therefore, these enzymes are considered oncogenes and their selective inhibition might be a possible therapeutic approach to treat cancer. Here we describe a heterocyclic ring system library screened against the histone demethylase KDM4C (JMJD2C) in the search for novel inhibitory scaffolds. A 4-hydroxypyrazole scaffold was identified as an inhibitor of KDM4C; this scaffold could be employed in the further development of novel therapeutics, as well as for the elucidation of the biological roles of KDM4C on epigenetic regulation.",
keywords = "Dose-Response Relationship, Drug, Drug Design, Enzyme Inhibitors, Humans, Jumonji Domain-Containing Histone Demethylases, Molecular Structure, Pyrazoles, Small Molecule Libraries, Structure-Activity Relationship",
author = "Ulrike Leurs and Clausen, {Rasmus P} and Kristensen, {Jesper L} and Brian Lohse",
note = "Copyright {\circledC} 2012 Elsevier Ltd. All rights reserved.",
year = "2012",
month = "9",
day = "15",
doi = "10.1016/j.bmcl.2012.07.091",
language = "English",
volume = "22",
pages = "5811--3",
journal = "Bioorganic & Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Pergamon Press",
number = "18",

}

RIS

TY - JOUR

T1 - Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C)

AU - Leurs, Ulrike

AU - Clausen, Rasmus P

AU - Kristensen, Jesper L

AU - Lohse, Brian

N1 - Copyright © 2012 Elsevier Ltd. All rights reserved.

PY - 2012/9/15

Y1 - 2012/9/15

N2 - The human histone demethylases of the KDM4 (JMJD2) family have been associated to diseases such as prostate and breast cancer, as well as X-linked mental retardation. Therefore, these enzymes are considered oncogenes and their selective inhibition might be a possible therapeutic approach to treat cancer. Here we describe a heterocyclic ring system library screened against the histone demethylase KDM4C (JMJD2C) in the search for novel inhibitory scaffolds. A 4-hydroxypyrazole scaffold was identified as an inhibitor of KDM4C; this scaffold could be employed in the further development of novel therapeutics, as well as for the elucidation of the biological roles of KDM4C on epigenetic regulation.

AB - The human histone demethylases of the KDM4 (JMJD2) family have been associated to diseases such as prostate and breast cancer, as well as X-linked mental retardation. Therefore, these enzymes are considered oncogenes and their selective inhibition might be a possible therapeutic approach to treat cancer. Here we describe a heterocyclic ring system library screened against the histone demethylase KDM4C (JMJD2C) in the search for novel inhibitory scaffolds. A 4-hydroxypyrazole scaffold was identified as an inhibitor of KDM4C; this scaffold could be employed in the further development of novel therapeutics, as well as for the elucidation of the biological roles of KDM4C on epigenetic regulation.

KW - Dose-Response Relationship, Drug

KW - Drug Design

KW - Enzyme Inhibitors

KW - Humans

KW - Jumonji Domain-Containing Histone Demethylases

KW - Molecular Structure

KW - Pyrazoles

KW - Small Molecule Libraries

KW - Structure-Activity Relationship

U2 - 10.1016/j.bmcl.2012.07.091

DO - 10.1016/j.bmcl.2012.07.091

M3 - Journal article

VL - 22

SP - 5811

EP - 5813

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

IS - 18

ER -

ID: 45967576