Core Modifications of GSK3335103 toward Orally Bioavailable αvβ6 Inhibitors with Improved Synthetic Tractability
Heather F. Hryczanek,
John Barrett,
Tim N. Barrett
et al.
Abstract:The α v β 6 integrin has been identified as a target for the treatment of fibrotic diseases, based on the role it has in activating TGF-β 1 , a protein implicated in the pathogenesis of fibrosis. However, the development of orally bioavailable α v β 6 inhibitors has proven challenging due to the zwitterionic pharmacophore required to bind to the RGD binding site. This work describes the design and development of a novel, orally bioavailable series of α v β 6 inhibitors, developing on two previously published α… Show more
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