Data supporting a pilot high-throughput screen of a drug library for identification of DYRK1A inhibitors and high-content imaging analysis of identified harmine analogs
The data presented in this article support the accompanying research article “Identification of harmine and β-carboline analogs from a high-throughput screen of an approved drug collection; profiling as differential inhibitors of DYRK1A and monoamine oxidase A and for in vitro and in vivo anti-cance...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2021-08-01
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| Series: | Data in Brief |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S235234092100473X |
| _version_ | 1819130447100116992 |
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| author | Michael Tarpley Helen Oladapo Thomas B. Caligan Rob U. Onyenwoke Kevin P. Williams |
| author_facet | Michael Tarpley Helen Oladapo Thomas B. Caligan Rob U. Onyenwoke Kevin P. Williams |
| author_sort | Michael Tarpley |
| collection | DOAJ |
| description | The data presented in this article support the accompanying research article “Identification of harmine and β-carboline analogs from a high-throughput screen of an approved drug collection; profiling as differential inhibitors of DYRK1A and monoamine oxidase A and for in vitro and in vivo anti-cancer studies” [1]. As DYRK1A (dual-specificity tyrosine phosphorylation-regulated kinase 1a) plays a role in the pathophysiology of a number of diseases including diabetes, cancer and neurodegeneration [2–4], the identification of DYRK1A inhibitors is of significant interest. This data article details the hits identified from a DYRK1A high-throughput screen of a small molecule compound library containing over 95% approved drugs. Twenty-two compounds were identified with >50% inhibition, including harmine and four of its analogs. Subsequent profiling of these harmine analogs using glioma cancer cell lines and high-content image analysis identified those with effects on growth and cytotoxicity. |
| first_indexed | 2024-12-22T08:59:45Z |
| format | Article |
| id | doaj.art-af36df060592453a9272895bdc00d760 |
| institution | Directory Open Access Journal |
| issn | 2352-3409 |
| language | English |
| last_indexed | 2024-12-22T08:59:45Z |
| publishDate | 2021-08-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Data in Brief |
| spelling | doaj.art-af36df060592453a9272895bdc00d7602022-12-21T18:31:45ZengElsevierData in Brief2352-34092021-08-0137107189Data supporting a pilot high-throughput screen of a drug library for identification of DYRK1A inhibitors and high-content imaging analysis of identified harmine analogsMichael Tarpley0Helen Oladapo1Thomas B. Caligan2Rob U. Onyenwoke3Kevin P. Williams4Biomanufacturing Research Institute and Technology Enterprise, North Carolina Central University, Durham, NC 27707, USABiomanufacturing Research Institute and Technology Enterprise, North Carolina Central University, Durham, NC 27707, USA; INBS PhD Program, North Carolina Central University, Durham, NC 27707, USABiomanufacturing Research Institute and Technology Enterprise, North Carolina Central University, Durham, NC 27707, USABiomanufacturing Research Institute and Technology Enterprise, North Carolina Central University, Durham, NC 27707, USA; Department of Pharmaceutical Sciences, North Carolina Central University, Durham, NC 27707, USABiomanufacturing Research Institute and Technology Enterprise, North Carolina Central University, Durham, NC 27707, USA; Department of Pharmaceutical Sciences, North Carolina Central University, Durham, NC 27707, USA; Corresponding author.The data presented in this article support the accompanying research article “Identification of harmine and β-carboline analogs from a high-throughput screen of an approved drug collection; profiling as differential inhibitors of DYRK1A and monoamine oxidase A and for in vitro and in vivo anti-cancer studies” [1]. As DYRK1A (dual-specificity tyrosine phosphorylation-regulated kinase 1a) plays a role in the pathophysiology of a number of diseases including diabetes, cancer and neurodegeneration [2–4], the identification of DYRK1A inhibitors is of significant interest. This data article details the hits identified from a DYRK1A high-throughput screen of a small molecule compound library containing over 95% approved drugs. Twenty-two compounds were identified with >50% inhibition, including harmine and four of its analogs. Subsequent profiling of these harmine analogs using glioma cancer cell lines and high-content image analysis identified those with effects on growth and cytotoxicity.http://www.sciencedirect.com/science/article/pii/S235234092100473XDYRK1AHigh-throughput screeningHigh-content imagingHarmineCytotoxicityGlioma |
| spellingShingle | Michael Tarpley Helen Oladapo Thomas B. Caligan Rob U. Onyenwoke Kevin P. Williams Data supporting a pilot high-throughput screen of a drug library for identification of DYRK1A inhibitors and high-content imaging analysis of identified harmine analogs Data in Brief DYRK1A High-throughput screening High-content imaging Harmine Cytotoxicity Glioma |
| title | Data supporting a pilot high-throughput screen of a drug library for identification of DYRK1A inhibitors and high-content imaging analysis of identified harmine analogs |
| title_full | Data supporting a pilot high-throughput screen of a drug library for identification of DYRK1A inhibitors and high-content imaging analysis of identified harmine analogs |
| title_fullStr | Data supporting a pilot high-throughput screen of a drug library for identification of DYRK1A inhibitors and high-content imaging analysis of identified harmine analogs |
| title_full_unstemmed | Data supporting a pilot high-throughput screen of a drug library for identification of DYRK1A inhibitors and high-content imaging analysis of identified harmine analogs |
| title_short | Data supporting a pilot high-throughput screen of a drug library for identification of DYRK1A inhibitors and high-content imaging analysis of identified harmine analogs |
| title_sort | data supporting a pilot high throughput screen of a drug library for identification of dyrk1a inhibitors and high content imaging analysis of identified harmine analogs |
| topic | DYRK1A High-throughput screening High-content imaging Harmine Cytotoxicity Glioma |
| url | http://www.sciencedirect.com/science/article/pii/S235234092100473X |
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