Repurposing the Kinase Inhibitor Mavelertinib for Giardiasis Therapy
| العنوان: | Repurposing the Kinase Inhibitor Mavelertinib for Giardiasis Therapy |
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| المؤلفون: | Samantha A. Michaels, Matthew A. Hulverson, Grant R. Whitman, Linh T. Tran, Ryan Choi, Erkang Fan, Case W. McNamara, Melissa S. Love, Kayode K. Ojo |
| المصدر: | Antimicrobial Agents and Chemotherapy. 66 |
| بيانات النشر: | American Society for Microbiology, 2022. |
| سنة النشر: | 2022 |
| مصطلحات موضوعية: | ErbB Receptors, Giardiasis, Pharmacology, Mice, HEK293 Cells, Infectious Diseases, Animals, Humans, Pharmacology (medical), Giardia lamblia, Protein Kinase Inhibitors |
| الوصف: | A phenotypic screen of the ReFRAME compound library was performed to identify cell-active inhibitors that could be developed as therapeutics for giardiasis. A primary screen against Giardia lamblia GS clone H7 identified 85 cell-active compounds at a hit rate of 0.72%. A cytotoxicity counterscreen against HEK293T cells was carried out to assess hit compound selectivity for further prioritization. Mavelertinib (PF-06747775), a third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI), was identified as a potential new therapeutic based on indication, activity, and availability after reconfirmation. Mavelertinib has |
| تدمد: | 1098-6596 0066-4804 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f49b5e244e7e31e1804db574cf430baTest https://doi.org/10.1128/aac.00017-22Test |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....7f49b5e244e7e31e1804db574cf430ba |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 10986596 00664804 |
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