Prometic's differentiated research involves the study of two G-protein-coupled-receptors, GPR40 and GPR84
. These drug candidates have a dual mode-of-action as agonists ('stimulators') of GPR40 and antagonists ('inhibitors') of GPR84
Galapagos NV (EPA: GLPG) announced on Monday its PINTA Phase 2 trial design with its GPR84 inhibitor GLPG1205 in patients with idiopathic pulmonary fibrosis (IPF).
GLPG1205 is a GPR84 inhibitor that has shown a reduction in signs and symptoms of IPF in animal models, with favourable tolerability in healthy volunteers and ulcerative colitis patients in previous trials.
The paper entitled "A Newly Discovered Antifibrotic Pathway Regulated by Two Fatty Acid Receptors: GPR40 and GPR84
" documents the discovery of an antifibrotic pathway involving these two receptors.
In the last decades, several G-protein coupled receptors (GPCRs), i.e., GPR40, GPR41, GPR43, GPR84
, and GPR120, were deorphaned as free fatty acids (FFAs) receptors [1-5].
Dumas et al., "GPR84
deficiency reduces microgliosis, but accelerates dendritic degeneration and cognitive decline in a mouse model of Alzheimer's disease," Brain, Behavior, and Immunity, vol.
GLPG1205, which isA is fully proprietary to Galapagos, inhibits GPR84
and forms a potential novel treatment for inflammatory bowel diseases.
DEGs Accession number Signal of control Signal of d Score experimental Cd3 NM-011337 5.37 8.81 10.04 Atf3 NM.007498 6.12 9.18 10.10 Plek NM_019549 6.67 9.20 8.10 Ctla2b NM_001145801 5.45 7.90 8.08 Bcl2ala NM.007534 7.23 9.59 8.37 Ch25h NM_009890 6.82 9.13 8.27 Plek NM.019549 5.87 8.12 7.58 TnfaipS NM_001166402 5.75 7.45 8.12 Tgifl NM.001164074 6.05 7.59 8.52 Gpr84
NM.030720 6.31 7.83 7.92 DEGs Fold change P value q-value Expression Rank change Cd3 10.91 2.20E-05 0 Up 1 Atf3 8.37 2.20E-05 0 Up 2 Plek 5.77 2.20E-05 0 Up 3 Ctla2b 5.45 2.20E-05 0 Up 4 Bcl2ala 5.14 2.20E-05 0 Up 5 Ch25h 4.95 2.20E-05 0 Up 6 Plek 4.76 2.20E-05 0 Up 7 TnfaipS 3.24 2.20E-05 0 Up 8 Tgifl 2.91 2.20E-05 0 Up 9 Gpr84
2.86 2.20E-05 0 Up 10 Table 2: Top 10 GO terms and KEGG pathways enrichment results of DEGs.
(SeeNews) - Dec 16, 2014 - Belgian biotechnology firm Galapagos (AMS:GLPG) said Tuesday it had signed an agreement with Janssen Pharmaceutica to regain full rights to the entire GPR84
programme, including the inhibitor GLPG1205 and the backup compound GLPG2196.