1ni1

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(New page: 200px<br /><applet load="1ni1" size="450" color="white" frame="true" align="right" spinBox="true" caption="1ni1, resolution 2.30&Aring;" /> '''Imidazole and cyanop...)
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[[Image:1ni1.gif|left|200px]]<br /><applet load="1ni1" size="450" color="white" frame="true" align="right" spinBox="true"
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[[Image:1ni1.gif|left|200px]]<br /><applet load="1ni1" size="350" color="white" frame="true" align="right" spinBox="true"
caption="1ni1, resolution 2.30&Aring;" />
caption="1ni1, resolution 2.30&Aring;" />
'''Imidazole and cyanophenyl farnesyl transferase inhibitors'''<br />
'''Imidazole and cyanophenyl farnesyl transferase inhibitors'''<br />
==Overview==
==Overview==
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A pyridyl moiety was introduced into a previously developed series of, farnesyltransferase inhibitors containing imidazole and cyanophenyl (such, as 4), resulting in potent inhibitors with improved pharmacokinetics.
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A pyridyl moiety was introduced into a previously developed series of farnesyltransferase inhibitors containing imidazole and cyanophenyl (such as 4), resulting in potent inhibitors with improved pharmacokinetics.
==About this Structure==
==About this Structure==
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1NI1 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with ZN, HFP and 2C5 as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1NI1 OCA].
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1NI1 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with <scene name='pdbligand=ZN:'>ZN</scene>, <scene name='pdbligand=HFP:'>HFP</scene> and <scene name='pdbligand=2C5:'>2C5</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1NI1 OCA].
==Reference==
==Reference==
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[[Category: Bauch, J.]]
[[Category: Bauch, J.]]
[[Category: Cohen, J.]]
[[Category: Cohen, J.]]
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[[Category: Gu, W.Z.]]
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[[Category: Gu, W Z.]]
[[Category: Hasvold, L.]]
[[Category: Hasvold, L.]]
[[Category: Leonard, N.]]
[[Category: Leonard, N.]]
[[Category: Li, Q.]]
[[Category: Li, Q.]]
[[Category: Li, T.]]
[[Category: Li, T.]]
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[[Category: Lin, N.H.]]
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[[Category: Lin, N H.]]
[[Category: Marsh, K.]]
[[Category: Marsh, K.]]
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[[Category: Rosenberg, S.H.]]
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[[Category: Rosenberg, S H.]]
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[[Category: Sham, H.L.]]
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[[Category: Sham, H L.]]
[[Category: Stoll, V.]]
[[Category: Stoll, V.]]
[[Category: Tong, Y.]]
[[Category: Tong, Y.]]
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Nov 20 22:16:36 2007''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:06:18 2008''

Revision as of 12:06, 21 February 2008


1ni1, resolution 2.30Å

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Imidazole and cyanophenyl farnesyl transferase inhibitors

Overview

A pyridyl moiety was introduced into a previously developed series of farnesyltransferase inhibitors containing imidazole and cyanophenyl (such as 4), resulting in potent inhibitors with improved pharmacokinetics.

About this Structure

1NI1 is a Protein complex structure of sequences from Rattus norvegicus with , and as ligands. Full crystallographic information is available from OCA.

Reference

Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability., Tong Y, Lin NH, Wang L, Hasvold L, Wang W, Leonard N, Li T, Li Q, Cohen J, Gu WZ, Zhang H, Stoll V, Bauch J, Marsh K, Rosenberg SH, Sham HL, Bioorg Med Chem Lett. 2003 May 5;13(9):1571-4. PMID:12699757

Page seeded by OCA on Thu Feb 21 14:06:18 2008

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