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Article

Targeting substrate-site in Jak2 kinase prevents emergence of genetic resistance.

Scientific reports - 30 Sept 2015

Kesarwani Meenu, Huber Erika, Kincaid Zachary, Evelyn Chris R, Biesiada Jacek, Rance Mark, Thapa Mahendra B, Shah Neil P, Meller Jarek, Zheng Yi, Azam Mohammad

Abstract excerpt

Emergence of genetic resistance against kinase inhibitors poses a great challenge for durable therapeutic response. Here, we report a novel mechanism of JAK2 kinase inhibition by fedratinib (TG101348) that prevents emergence of genetic resistance. Using in vitro drug screening, we identified 211 amino-acid substitutions conferring resistance to ruxolitinib (INCB018424) and cross-resistance to the JAK2 inhibitors...

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Source

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Identifiers

PMID: 26419724
DOI: 10.1038/srep14538
PMCID: PMC4588578

Genes

JAK2

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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