Chemical Screening of Nuclear Receptor Modulators
Nuclear receptors are ligand-inducible transcriptional factors that control multiple biological phenomena, including proliferation, differentiation, reproduction, metabolism, and the maintenance of homeostasis. Members of the nuclear receptor superfamily have marked structural and functional similar...
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doaj-950f7a8d0d1e4d16b704b97edf9064ac2020-11-25T02:53:50ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672020-07-01215512551210.3390/ijms21155512Chemical Screening of Nuclear Receptor ModulatorsMari Ishigami-Yuasa0Hiroyuki Kagechika1Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University (TMDU), 2-3-10 Kanda-Surugadai, Chiyoda-ku, Tokyo 101-0062, JapanInstitute of Biomaterials and Bioengineering, Tokyo Medical and Dental University (TMDU), 2-3-10 Kanda-Surugadai, Chiyoda-ku, Tokyo 101-0062, JapanNuclear receptors are ligand-inducible transcriptional factors that control multiple biological phenomena, including proliferation, differentiation, reproduction, metabolism, and the maintenance of homeostasis. Members of the nuclear receptor superfamily have marked structural and functional similarities, and their domain functionalities and regulatory mechanisms have been well studied. Various modulators of nuclear receptors, including agonists and antagonists, have been developed as tools for elucidating nuclear receptor functions and also as drug candidates or lead compounds. Many assay systems are currently available to evaluate the modulation of nuclear receptor functions, and are useful as screening tools in the discovery and development of new modulators. In this review, we cover the chemical screening methods for nuclear receptor modulators, focusing on assay methods and chemical libraries for screening. We include some recent examples of the discovery of nuclear receptor modulators.https://www.mdpi.com/1422-0067/21/15/5512chemical screeningnuclear receptor modulatorshigh-throughput screeningchemical library |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Mari Ishigami-Yuasa Hiroyuki Kagechika |
spellingShingle |
Mari Ishigami-Yuasa Hiroyuki Kagechika Chemical Screening of Nuclear Receptor Modulators International Journal of Molecular Sciences chemical screening nuclear receptor modulators high-throughput screening chemical library |
author_facet |
Mari Ishigami-Yuasa Hiroyuki Kagechika |
author_sort |
Mari Ishigami-Yuasa |
title |
Chemical Screening of Nuclear Receptor Modulators |
title_short |
Chemical Screening of Nuclear Receptor Modulators |
title_full |
Chemical Screening of Nuclear Receptor Modulators |
title_fullStr |
Chemical Screening of Nuclear Receptor Modulators |
title_full_unstemmed |
Chemical Screening of Nuclear Receptor Modulators |
title_sort |
chemical screening of nuclear receptor modulators |
publisher |
MDPI AG |
series |
International Journal of Molecular Sciences |
issn |
1661-6596 1422-0067 |
publishDate |
2020-07-01 |
description |
Nuclear receptors are ligand-inducible transcriptional factors that control multiple biological phenomena, including proliferation, differentiation, reproduction, metabolism, and the maintenance of homeostasis. Members of the nuclear receptor superfamily have marked structural and functional similarities, and their domain functionalities and regulatory mechanisms have been well studied. Various modulators of nuclear receptors, including agonists and antagonists, have been developed as tools for elucidating nuclear receptor functions and also as drug candidates or lead compounds. Many assay systems are currently available to evaluate the modulation of nuclear receptor functions, and are useful as screening tools in the discovery and development of new modulators. In this review, we cover the chemical screening methods for nuclear receptor modulators, focusing on assay methods and chemical libraries for screening. We include some recent examples of the discovery of nuclear receptor modulators. |
topic |
chemical screening nuclear receptor modulators high-throughput screening chemical library |
url |
https://www.mdpi.com/1422-0067/21/15/5512 |
work_keys_str_mv |
AT mariishigamiyuasa chemicalscreeningofnuclearreceptormodulators AT hiroyukikagechika chemicalscreeningofnuclearreceptormodulators |
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1724724114110808064 |