X-ray Crystal Structure-Guided Design and Optimization of 7
Autor: | Younho, Lee, Hyunkyung, Kim, Haelee, Kim, Ha Yeon, Cho, Jun-Goo, Jee, Kyung-Ah, Seo, Jung Beom, Son, Eunhwa, Ko, Hwan Geun, Choi, Nam Doo, Kim, Ikyon, Kim |
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Rok vydání: | 2021 |
Předmět: |
Mice
Inbred ICR Binding Sites Transplantation Heterologous Administration Oral Breast Neoplasms Cell Cycle Proteins Protein Serine-Threonine Kinases Protein-Tyrosine Kinases Crystallography X-Ray Molecular Docking Simulation Mice Structure-Activity Relationship Pyrimidines Cell Line Tumor Drug Design Animals Humans Female Pyrroles Protein Kinase Inhibitors Half-Life |
Zdroj: | Journal of medicinal chemistry. 64(10) |
ISSN: | 1520-4804 |
Popis: | Triple-negative breast cancer (TNBC) is an aggressive breast-cancer subtype associated with poor prognosis and high relapse rates. Monopolar spindle 1 kinase (MPS1) is an apical dual-specificity protein kinase that is over-expressed in TNBC. We herein report a highly selective MPS1 inhibitor based on a 7 |
Databáze: | OpenAIRE |
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