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High throughput in silico screening and in vitro testing of polypharmacological bromodomain 4 and cancer associated kinase inhibitors
Dissertation (MSc (Physiology))--University of Pretoria, 2022.
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| Format: | Thesis |
| Language: | English |
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University of Pretoria
2023
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| _version_ | 1867613722466320384 |
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| access_status_str | Open Access |
| author2 | Phulukdaree, Alisa |
| author_browse | Phulukdaree, Alisa |
| author_facet | Phulukdaree, Alisa |
| collection | Thesis |
| dc_rights_str_mv | © 2022 University of Pretoria. All rights reserved. The copyright in this work vests in the University of Pretoria. No part of this work may be reproduced or transmitted in any form or by any means, without the prior written permission of the University of Pretoria. |
| description | Dissertation (MSc (Physiology))--University of Pretoria, 2022. |
| format | Thesis |
| id | oai:repository.up.ac.za:2263/89836 |
| institution | University of Pretoria (South Africa) |
| language | English |
| last_indexed | 2026-06-10T12:40:40.078Z |
| license_str | Other — see source repository |
| provenance_str_mv | Harvested via OAI-PMH from UPSpace — University of Pretoria Institutional Repository |
| publishDate | 2023 |
| publishDateRange | 2023 |
| publishDateSort | 2023 |
| publisher | University of Pretoria |
| publisherStr | University of Pretoria |
| record_format | dspace |
| source_str | UPSpace — University of Pretoria Institutional Repository |
| spelling | oai:repository.up.ac.za:2263/89836 High throughput in silico screening and in vitro testing of polypharmacological bromodomain 4 and cancer associated kinase inhibitors Phulukdaree, Alisa danieljoubertdf@gmail.com Nortje, Evangeline Joubert, Daniel Francois In Silico Poly-inhibitor BRD4 inhibitor AURKA inhibitor AURKB inhibitor EGFR inhibitor Biofocus library High Throughput virtual screening UCTD Dissertation (MSc (Physiology))--University of Pretoria, 2022. Polypharmacology has recently become an intense subject of research, specifically in the development and design of anti-cancer compounds. Drugs that have more than one target, potentially have higher efficacy in the treatment of triple negative breast cancer and prevent the development of drug resistance. Bromodomain containing protein 4 (BRD4) is a known dysregulated enzyme in triple negative breast cancer, together with other kinases such as aurora kinase A and B (AURKA and AURKB), cyclin dependant kinases 4 and 6 (CDK4/6), polo-like kinase (PLK1) and epidermal growth factor receptor (EGFR). The research set out to identify a poly-inhibitors of BRD4 and cancer associated kinases, using virtual high throughput screening. The 10 promising compounds have either imidazo[1,2-b]pyridazine or 1H-imidazo[4,5-c]pyridine backbones in their chemical structure. The 10 poly-inhibitors underwent in vitro screening from which one compound was identified as being active. Further in vitro assays were performed to elucidate its effect on TNBCs in vitro. RESCOM SoM Physiology MSc (Physiology) Unrestricted 2023-02-27T08:51:50Z 2023-02-27T08:51:50Z 2023-04 2022 Dissertation * A2023 https://repository.up.ac.za/handle/2263/89836 10.25403/UPresearchdata.22133912 en © 2022 University of Pretoria. All rights reserved. The copyright in this work vests in the University of Pretoria. No part of this work may be reproduced or transmitted in any form or by any means, without the prior written permission of the University of Pretoria. application/pdf University of Pretoria |
| spellingShingle | In Silico Poly-inhibitor BRD4 inhibitor AURKA inhibitor AURKB inhibitor EGFR inhibitor Biofocus library High Throughput virtual screening UCTD High throughput in silico screening and in vitro testing of polypharmacological bromodomain 4 and cancer associated kinase inhibitors |
| title | High throughput in silico screening and in vitro testing of polypharmacological bromodomain 4 and cancer associated kinase inhibitors |
| title_full | High throughput in silico screening and in vitro testing of polypharmacological bromodomain 4 and cancer associated kinase inhibitors |
| title_fullStr | High throughput in silico screening and in vitro testing of polypharmacological bromodomain 4 and cancer associated kinase inhibitors |
| title_full_unstemmed | High throughput in silico screening and in vitro testing of polypharmacological bromodomain 4 and cancer associated kinase inhibitors |
| title_short | High throughput in silico screening and in vitro testing of polypharmacological bromodomain 4 and cancer associated kinase inhibitors |
| title_sort | high throughput in silico screening and in vitro testing of polypharmacological bromodomain 4 and cancer associated kinase inhibitors |
| topic | In Silico Poly-inhibitor BRD4 inhibitor AURKA inhibitor AURKB inhibitor EGFR inhibitor Biofocus library High Throughput virtual screening UCTD |
| url | https://repository.up.ac.za/handle/2263/89836 |