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VPR-254: an inhibitor of ROR-gamma T with potential utility for the treatment of inflammatory bowel disease.

Abstract：

INTRODUCTION:Retinoic Acid Related Orphan Nuclear Receptor gamma T (RORγT) is a lineage specifying transcription factor for IL-17 expressing cells, which may contribute to the pathogenesis of Inflammatory Bowel Disease (IBD). VPR-254 is a selective in vitro inhibitor of RORγT. AIMS:The main goals of our study were twofold: (1) To determine if ex vivo treatment with VPR-254 reduced relevant cytokine (IL-17 and IL-21) secretion from colonic strips of mice with colitis; (2) To determine if treatment of mice with VPR-254 attenuated parameters of colitis, using three murine IBD models. METHODS:VPR-254 was evaluated ex vivo in a colonic strip assay, using tissue from mice with Dextran sulfate sodium (DSS)-induced colitis. In vivo, VPR-254 was evaluated for efficacy in DSS, Trintirobenzenesulfonic acid (TNBS) and Anti-CD40 antibody-induced murine models of colitis. RESULTS:VPR-254 reduced the production of key pro-inflammatory cytokines (e.g., IL-17) in ex vivo and in vivo models of colitis. This small molecule inhibitor of RORγT also improved various morphometric and histological parameters associated with three diverse murine models of IBD. CONCLUSION:Our results support the concept that an inhibitor of ROR-gamma T may have potential utility for the treatment of IBD.

journal_name

Inflammopharmacology

journal_title

Inflammopharmacology

authors

Fitzpatrick LR,Small J,O'Connell R,Talbott G,Alton G,Zapf J

doi

10.1007/s10787-019-00643-z

subject

Has Abstract

pub_date

2020-04-01 00:00:00

pages

499-511

issue

2

eissn

0925-4692

issn

1568-5608

pii

10.1007/s10787-019-00643-z

journal_volume

28

pub_type

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