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Article

New scaffolds for type II JAK2 inhibitors overcome the acquired G993A resistance mutation.

Cell chemical biology - 15 Jun 2023

Arwood Matthew L, Liu Yao, Harkins Shannon K, Weinstock David M, Yang Lei, Stevenson Kristen E, Plana Olivia D, Dong Jingyun, Cirka Haley, Jones Kristen L, Virtanen Anniina T, Gupta Dikshat G, Ceas Amanda, Lawney Brian, Yoda Akinori, Leahy Catharine, Hao Mingfeng, He Zhixiang, Choi Hwan Geun, Wang Yaning, Silvennoinen Olli, Hubbard Stevan R, Zhang Tinghu, Gray Nathanael S, Li Loretta S

Abstract excerpt

Recurrent JAK2 alterations are observed in myeloproliferative neoplasms, B-cell acute lymphoblastic leukemia, and other hematologic malignancies. Currently available type I JAK2 inhibitors have limited activity in these diseases. Preclinical data support the improved efficacy of type II JAK2 inhibitors, which lock the kinase in the inactive conformation. By screening small molecule libraries, we identified a lead...

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Identifiers

PMID: 37290440
DOI: 10.1016/j.chembiol.2023.05.007
PMCID: PMC10495080

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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