Lestaurtinib – Knowledge and References

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The Advantages and Versatility of Carrier-Free Nanodrug and Nanoparticle Systems for Cancer Therapy

Published in Loutfy H. Madkour, Nanoparticle-Based Drug Delivery in Cancer Treatment, 2022

The low size of NPs allows them to cross cellular membranes and avoid detection by the RES, thus preventing their degradation. Their high surface area enhances the loading of therapeutic agents, making them ideal for medical purposes [215]. A wide range of anticancer drugs such as rituximab, lestaurtinib, carboplatin, PTX, DOX, and tyrosine kinase inhibitors have been loaded onto NPs with a potential effect against various cancers, and a superior therapeutic efficacy than free chemotherapeutics [216–220].

Residue-specific free energy analysis in ligand bindings to JAK2

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Journal Information

Published in Molecular Physics, 2018

Yifan Zhou, Xiao Liu, Youzhi Zhang, Long Peng, John Z. H. Zhang

Although it does not depend on the binding of cytokines and their cognate receptor, mutation of JAK2 can auto-phosphorylate and activate the downstream factors abnormally, resulting in uncontrollable cell proliferation and suppression of apoptosis [11–14]. Thus, inhibiting JAK2 is an effective treatment for cancer and related diseases. Ruxolitinib is the most studied JAK2 inhibitors in psoriasis since its approval by FDA in 2011 [15,16]. In the meantime, more small-molecule inhibitors of JAK2 have entered clinical trials. For example, Gandotinib (LY-2784 544) is used for the treatment of myeloproliferative neoplasms, and Lestaurtinib (CEP-701) is used in patients for acute myeloid leukemia (AML). More inhibitors of JAK2 are currently being discovered and studied [17–19].