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 supporting a pilot high-throughput screen of a drug library for identification of DYRK1A inhibitors and high-content imaging analysis of identified harmine analogs.
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DOI：
10.1016/j.dib.2021.107189
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发表时间：
2021-08
期刊：
影响因子：
1.2
通讯作者：
Williams KP
中科院分区：
文献类型：
--
作者：
Tarpley M;Oladapo H;Caligan TB;Onyenwoke RU;Williams KP
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”. 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, 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.
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影响因子：
9.7
作者：
Oladapo HO;Tarpley M;Sauer SJ;Addo KA;Ingram SM;Strepay D;Ehe BK;Chdid L;Trinkler M;Roques JR;Darr DB;Fleming JM;Devi GR;Williams KP
通讯作者：
Williams KP
影响因子：
8.2
作者：
Rachdi, Latif;Kariyawasam, Dulanjalee;Scharfmann, Raphael
通讯作者：
Scharfmann, Raphael
DOI：
10.1016/j.ejps.2021.105821
发表时间：
2021-07-01
期刊：
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
影响因子：
--
作者：
Tarpley M;Oladapo HO;Strepay D;Caligan TB;Chdid L;Shehata H;Roques JR;Thomas R;Laudeman CP;Onyenwoke RU;Darr DB;Williams KP
通讯作者：
Williams KP
影响因子：
--
作者：
Abraham, Vivek C.;Towne, Danli L.;Burns, David J.
通讯作者：
Burns, David J.
影响因子：
1.9
作者：
Tarpley M;Caligan TB;Onyenwoke RU;Williams KP
通讯作者：
Williams KP