Discovery of (2
| Autor: | Qibin, Su, Erica, Banks, Geraldine, Bebernitz, Kirsten, Bell, Cassandra F, Borenstein, Huawei, Chen, Claudio E, Chuaqui, Nanhua, Deng, Andrew D, Ferguson, Sameer, Kawatkar, Neil P, Grimster, Linette, Ruston, Paul D, Lyne, Jon A, Read, Xianyou, Peng, Xiaohui, Pei, Stephen, Fawell, Zhanlei, Tang, Scott, Throner, Melissa M, Vasbinder, Haoyu, Wang, Jon, Winter-Holt, Richard, Woessner, Allan, Wu, Wenzhan, Yang, Michael, Zinda, Jason G, Kettle |
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| Rok vydání: | 2020 |
| Předmět: |
Acrylamides
Aniline Compounds Indoles Molecular Structure Mice Nude Drug Synergism Janus Kinase 1 Xenograft Model Antitumor Assays ErbB Receptors Structure-Activity Relationship Cell Line Tumor Drug Design Drug Discovery Animals Humans Female Drug Screening Assays Antitumor Protein Kinase Inhibitors |
| Zdroj: | Journal of medicinal chemistry. 63(9) |
| ISSN: | 1520-4804 |
| Popis: | JAK1, JAK2, JAK3, and TYK2 belong to the JAK (Janus kinase) family. They play critical roles in cytokine signaling. Constitutive activation of JAK/STAT pathways is associated with a wide variety of diseases. Particularly, pSTAT3 is observed in response to the treatment with inhibitors of oncogenic signaling pathways such as EGFR, MAPK, and AKT and is associated with resistance or poorer response to agents targeting these pathways. Among the JAK family kinases, JAK1 has been shown to be the primary driver of STAT3 phosphorylation and signaling; therefore, selective JAK1 inhibition can be a viable means to overcome such treatment resistances. Herein, an account of the medicinal chemistry optimization from the promiscuous kinase screening hit |
| Databáze: | OpenAIRE |
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