 |
PDBsum entry 3io7
|
|
|
|
References listed in PDB file
|
 |
|
Key reference
|
|
|
Title
|
|
2-Aminopyrazolo[1,5-A]pyrimidines as potent and selective inhibitors of jak2.
|
|
|
Authors
|
|
M.W.Ledeboer,
A.C.Pierce,
J.P.Duffy,
H.Gao,
D.Messersmith,
F.G.Salituro,
S.Nanthakumar,
J.Come,
H.J.Zuccola,
L.Swenson,
D.Shlyakter,
S.Mahajan,
T.Hoock,
B.Fan,
W.J.Tsai,
E.Kolaczkowski,
S.Carrier,
J.K.Hogan,
R.Zessis,
S.Pazhanisamy,
Y.L.Bennani.
|
|
|
Ref.
|
|
Bioorg Med Chem Lett, 2009,
19,
6529-6533.
|
|
|
PubMed id
|
|
|
|
|
|
Abstract
|
|
|
Constitutive activation of the EPO/JAK2 signaling cascade has recently been
implicated in a variety of myeloproliferative disorders including polycythemia
vera, essential thrombocythemia and myelofibrosis. In an effort to uncover
therapeutic potential of blocking the EPO/JAK2 signaling cascade, we sought to
discover selective inhibitors that block the kinase activity of JAK2. Herein, we
describe the discovery and structure based optimization of a novel series of
2-amino-pyrazolo[1,5-a]pyrimidines that exhibit potent inhibition of JAK2.
|
|
|
|
|
|
|
