Title : FOLH1/GCPII is elevated in IBD patients, and its inhibition ameliorates murine IBD abnormalities.

Pub. Date : 2016 Aug 4

PMID : 27536732






4 Functional Relationships(s)
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1 Using a human-to-mouse approach, we next showed a similar enzymatic increase in two well-validated IBD murine models and evaluated the therapeutic effect of the potent FOLH1/ GCPII inhibitor 2-phosphonomethyl pentanedioic acid (2-PMPA) (IC50 = 300 pM). 2-(phosphonomethyl)pentanedioic acid folate hydrolase 1 Mus musculus
2 Using a human-to-mouse approach, we next showed a similar enzymatic increase in two well-validated IBD murine models and evaluated the therapeutic effect of the potent FOLH1/ GCPII inhibitor 2-phosphonomethyl pentanedioic acid (2-PMPA) (IC50 = 300 pM). 2-(phosphonomethyl)pentanedioic acid folate hydrolase 1 Mus musculus
3 In the dextran sodium sulfate (DSS) colitis model, 2-PMPA inhibited the GCPII activity in the colonic mucosa by over 90% and substantially reduced the disease activity. 2-(phosphonomethyl)pentanedioic acid folate hydrolase 1 Homo sapiens
4 In the murine IL-10-/- model of spontaneous colitis, daily 2-PMPA treatment also significantly reduced both macroscopic and microscopic disease severity. 2-(phosphonomethyl)pentanedioic acid interleukin 10 Mus musculus