2024
DOI: 10.1021/acs.jmedchem.4c02051
|View full text |Cite
|
Sign up to set email alerts
|

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

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...

Citation Types

0
0
0

Publication Types

Select...

Relationship

0
0

Authors

Journals

citations
Cited by 0 publications
references
References 51 publications
0
0
0
Order By: Relevance

No citations

Set email alert for when this publication receives citations?