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Identification of Novel Small Molecule Ligands for JAK2 Pseudokinase Domain

Hyperactive mutation V617F in the JAK2 regulatory pseudokinase domain (JH2) is prevalent in patients with myeloproliferative neoplasms. Here, we identified novel small molecules that target JH2 of JAK2 V617F and characterized binding via biochemical and structural approaches. Screening of 107,600 sm...

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Principais autores: Anniina T. Virtanen, Teemu Haikarainen, Parthasarathy Sampathkumar, Maaria Palmroth, Sanna Liukkonen, Jianping Liu, Natalia Nekhotiaeva, Stevan R. Hubbard, Olli Silvennoinen
Formato: Artigo
Idioma:Inglês
Publicado em: MDPI AG 2023-01-01
coleção:Pharmaceuticals
Assuntos:
JAK inhibitor
JAK2 V617F
myeloproliferative neoplasm
cytokine signaling
pseudokinase
Acesso em linha:https://www.mdpi.com/1424-8247/16/1/75
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