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 journal › Journal article › Research › peer-review
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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
C2 - 22917519
VL - 22
SP - 5811
EP - 5813
JO - Bioorganic & Medicinal Chemistry Letters
JF - Bioorganic & Medicinal Chemistry Letters
SN - 0960-894X
IS - 18
ER -
ID: 45967576