Total synthesis, NMR solution structure, and binding model of the potent histone deacetylase inhibitor FR235222.
نویسندگان
چکیده
منابع مشابه
Search for the Pharmacophore of Histone Deacetylase Inhibitors Using Pharmacophore Query and Docking Study
Histone deacetylase inhibitors have gained a great deal of attention recently for the treatment of cancers and inflammatory diseases. So design of new inhibitors is of great importance in pharmaceutical industries and labs. Creating pharmacophor models in order to design new molecules or search a library for finding lead compounds is of great interest. This approach reduces the overall cost ass...
متن کاملSearch for the Pharmacophore of Histone Deacetylase Inhibitors Using Pharmacophore Query and Docking Study
Histone deacetylase inhibitors have gained a great deal of attention recently for the treatment of cancers and inflammatory diseases. So design of new inhibitors is of great importance in pharmaceutical industries and labs. Creating pharmacophor models in order to design new molecules or search a library for finding lead compounds is of great interest. This approach reduces the overall cost ass...
متن کاملFR235222, a fungal metabolite, is a novel immunosuppressant that inhibits mammalian histone deacetylase III. Structure determination.
Cyclosporin A and tacrolimus dramatically changed the field of clinical transplantations, and they are also prescribed or currently developed for various autoimmune diseases. They suppress acute allograft rejection effectively, but chronic allograft rejection is a matter of issue on transplantations even when treated with these drugs1), and their dosages are restricted because of their toxiciti...
متن کاملDrug inhibition of HDAC3 and epigenetic control of differentiation in Apicomplexa parasites
Plasmodium and Toxoplasma are parasites of major medical importance that belong to the Apicomplexa phylum of protozoa. These parasites transform into various stages during their life cycle and express a specific set of proteins at each stage. Although little is yet known of how gene expression is controlled in Apicomplexa, histone modifications, particularly acetylation, are emerging as key reg...
متن کاملActivity of the histone deacetylase inhibitor FR235222 on Toxoplasma gondii: inhibition of stage conversion of the parasite cyst form and study of new derivative compounds.
Bradyzoite-to-tachyzoite conversion plays a role in the pathogenesis of recrudescence of ocular toxoplasmosis and disease in immunocompromised persons. The currently available medicines are ineffective on cysts and fail to prevent reactivation of latent toxoplasmosis. A previous study showed that the histone deacetylase inhibitor FR235222 has a dramatic effect on tachyzoite growth and induces t...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Angewandte Chemie
دوره 45 3 شماره
صفحات -
تاریخ انتشار 2006