
Insights on JAK2 Modulation by Potent, Selective, and Cell …
2022年6月2日 · JAK2 is a non-receptor tyrosine kinase that regulates hematopoiesis through the JAK-STAT pathway. The pseudokinase domain (JH2) is an important regulator of the activity …
简洁优雅中蕴含着深度—JAK-STAT信号通路 - 知乎
哺乳动物有4个jak同源基因,包括jak1、jak2、jak3和tyk2 四个成员。 JAKs的分子量在120-140kDa之间,每个JAKs成员具有7个保守的JH结构域,无跨膜结构域 。 JAK的特征是双激酶 …
Molecular basis of JAK2 activation in erythropoietin receptor and ...
2024年3月8日 · JH2 was originally identified in JAK2 as a key regulator of activation that functions in a dualistic fashion; JH2 maintains JAKs in an inactive state in the absence of cytokine …
JAK2 JH2 Pseudokinase Domain Inhibitor Screening Assay Kit
The JAK2 JH2 Pseudokinase Domain Inhibitor Screening Assay Kit is designed for screening and profiling small molecules that displace the fluorescently labeled probe (JH2 probe 1) from the …
Crystal structures of the Jak2 pseudokinase domain and the …
Jak2 possesses a pseudokinase domain (JH2) and a tyrosine kinase domain (JH1). Through unknown mechanisms, JH2 regulates the catalytic activity of JH1, and hyperactivating …
Crystal structures of the JAK2 pseudokinase domain and the ... - PubMed
JAK2 possesses a pseudokinase domain (JH2) and a tyrosine kinase domain (JH1). Through unknown mechanisms, JH2 regulates the catalytic activity of JH1, and hyperactivating …
Selective Janus Kinase 2 (JAK2) Pseudokinase Ligands with a ...
2020年5月28日 · The present focus is on the discovery of molecules that may regulate the activity of JAK2 by selective binding to the JAK2 pseudokinase domain, JH2. Specifically, the …
Covalent Modification of the JH2 Domain of Janus Kinase 2
Probe molecules that covalently modify the JAK2 pseudokinase domain (JH2) are reported. Selective targeting of JH2 domains over the kinase (JH1) domains is a necessary feature for …
SAR317461 Inhibit JAK2/STAT3 Phosphorylation for Enhanced
6 天之前 · It downregulated JAK2 and STAT3 phosphorylation and stimulated autophagy in leukemic cells. In vivo, SAR317461 reduced peripheral blood leukocyte counts and prolonged …
The pseudokinase domain of JAK2 is a dual-specificity protein …
Mutations in JH2 lead to increased JAK2 activity contributing to myeloproliferative neoplasms (MPNs). Here, we show that JH2 is a dual-specificity protein kinase that phosphorylates two …