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PDBsum entry 2fx6
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References listed in PDB file
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Key reference
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Title
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Structure-Guided design of peptide-Based tryptase inhibitors.
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Authors
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M.E.Mcgrath,
P.A.Sprengeler,
B.Hirschbein,
J.R.Somoza,
I.Lehoux,
J.W.Janc,
E.Gjerstad,
M.Graupe,
A.Estiarte,
C.Venkataramani,
Y.Liu,
R.Yee,
J.D.Ho,
M.J.Green,
C.S.Lee,
L.Liu,
V.Tai,
J.Spencer,
D.Sperandio,
B.A.Katz.
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Ref.
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Biochemistry, 2006,
45,
5964-5973.
[DOI no: ]
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PubMed id
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Abstract
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Improved peptide-based inhibitors of human beta tryptase were discovered using
information gleaned from tripeptide library screening and structure-guided
design methods, including fragment screening. Our efforts sought to improve this
class of inhibitors by replacing the traditional Lys or Arg P1 element. The
optimized compounds display low nanomolar potency against the mast cell target
and several hundred-fold selectivity with respect to serine protease off
targets. Thus, replacement of Lys/Arg at P1 in a peptide-like scaffold does not
need to be accompanied by a loss in target affinity.
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