These potent and specific inhibitors facilitate the study and treatment of leukemia, lymphoma, and other blood cancers, as well as cardiovascular and ophthalmic diseases. Scientists often rely on inhibitors to study the relationship between the enzyme Jak2 and a variety of diseases, including cancer, diabetes, and hypertension. A pharmacological Jak2 inhibitor commonly used in research is AG490. While AG490 inhibits Jak2, it also inhibits other tyrosine kinases, making Jak2 studies difficult. AG490’s broad inhibitory action presents a challenge for using AG490 as a therapeutic agent. Researchers at the University of Florida have identified compounds that function as effective and specific Jak2 inhibitors. These compounds will allow researchers specifically to inhibit Jak2, which in turn may provide a better understanding of how Jak2 correlates with these diseases and provide for a new class of drugs for those suffering from Jak2 related disorders.
Effective and specific inhibitors of Jak2 for the study and treatment of various diseases including Myeloproliferative Disorders (MPDs), such as leukemia, lymphoma, and other blood cancers, as well as cardiovascular and ophthalmic diseases
Jak2 plays an important role in cell development and growth by activating and deactivating other proteins. Jak2 functions as a non-receptor member of the Janus kinase (Jak) family of tyrosine kinases. It has been implicated in certain types of cancer, diabetes and Myeloproliferative Disorders (MPDs). Once activated, Jak2 phosphorylates its substrate proteins, which in turn induce gene transcription. These compounds developed at the University of Florida inhibit phosphorylation of Jak2 in both a time and dose-dependent fashion, including the disease associated Jak2-V617F mutant. Unlike currently available Jak2 pharmacological inhibitors such as AG490, these compounds potently and specifically inhibit Jak2, providing a therapeutic alternative for patients suffering from MPDs and other Jak2 related diseases.
