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Targeting Upstream Janus Kinases

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posted on 2023-02-15, 03:03 authored by Parisa Rasighaemi, Alister WardAlister Ward
Janus kinases (JAKs) are the tyrosine kinases that are the principal activators of STAT proteins – particularly downstream of cytokine receptors – during normal development and homeostasis. The JAKs also make a major contribution to the hyperactivation of STATs observed in various malignancies, including through mutation of the JAKs themselves in several neoplastic conditions. These properties have made JAKs attractive targets for the development of small molecule inhibitors based on similar approaches used for other tyrosine kinases. This chapter details the lead JAK inhibitors, which show variable specificity, including multi-kinase inhibitors that have demonstrated excellent clinical efficacy.

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Pagination

163-175

ISSN

2196-9906

eISSN

2196-9914

Title of book

Cancer Drug Discovery and Development

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