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PDBsum entry 4py1
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References listed in PDB file
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Key reference
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Title
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Kinase domain inhibition of leucine rich repeat kinase 2 (lrrk2) using a [1,2,4]triazolo[4,3-B]pyridazine scaffold.
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Authors
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P.Galatsis,
J.L.Henderson,
B.L.Kormos,
S.Han,
R.G.Kurumbail,
T.T.Wager,
P.R.Verhoest,
G.S.Noell,
Y.Chen,
E.Needle,
Z.Berger,
S.J.Steyn,
C.Houle,
W.D.Hirst.
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Ref.
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Bioorg Med Chem Lett, 2014,
24,
4132-4140.
[DOI no: ]
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PubMed id
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Abstract
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Leucine rich repeat kinase 2 (LRRK2) has been genetically linked to Parkinson's
disease (PD). The most common mutant, G2019S, increases kinase activity, thus
LRRK2 kinase inhibitors are potentially useful in the treatment of PD. We herein
disclose the structure, potential ligand-protein binding interactions, and
pharmacological profiling of potent and highly selective kinase inhibitors based
on a triazolopyridazine chemical scaffold.
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