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PDBsum entry 4p7e
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References listed in PDB file
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Key reference
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Title
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Triazolopyridines as selective jak1 inhibitors: from hit identification to glpg0634.
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Authors
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C.J.Menet,
S.R.Fletcher,
G.Van lommen,
R.Geney,
J.Blanc,
K.Smits,
N.Jouannigot,
P.Deprez,
E.M.Van der aar,
P.Clement-Lacroix,
L.Lepescheux,
R.Galien,
B.Vayssiere,
L.Nelles,
T.Christophe,
R.Brys,
M.Uhring,
F.Ciesielski,
L.Van rompaey.
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Ref.
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J Med Chem, 2014,
57,
9323-9342.
[DOI no: ]
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PubMed id
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Abstract
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Janus kinases (JAK1, JAK2, JAK3, and TYK2) are involved in the signaling of
multiple cytokines important in cellular function. Blockade of the JAK-STAT
pathway with a small molecule has been shown to provide therapeutic
immunomodulation. Having identified JAK1 as a possible new target for arthritis
at Galapagos, the compound library was screened against JAK1, resulting in the
identification of a triazolopyridine-based series of inhibitors represented by
3. Optimization within this chemical series led to identification of GLPG0634
(65, filgotinib), a selective JAK1 inhibitor currently in phase 2B development
for RA and phase 2A development for Crohn's disease (CD).
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