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PDBsum entry 2w3l
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References listed in PDB file
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Key reference
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Title
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Tetrahydroisoquinoline amide substituted phenyl pyrazoles as selective bcl-2 inhibitors.
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Authors
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J.Porter,
A.Payne,
B.De candole,
D.Ford,
B.Hutchinson,
G.Trevitt,
J.Turner,
C.Edwards,
C.Watkins,
I.Whitcombe,
J.Davis,
C.Stubberfield.
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Ref.
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Bioorg Med Chem Lett, 2009,
19,
230-233.
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PubMed id
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Abstract
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Anti-apoptotic Bcl-2 protects cells from apoptosis by binding to pro-apoptotic
members of the Bcl-2 family thereby playing a role in tumour survival in
response to chemo- or radiation therapy. We describe a series of phenyl
pyrazoles that have high affinity for Bcl-2 and rationalise the observed SAR by
means of an X-ray crystal structure.
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