1nl4: Difference between revisions

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[[Image:1nl4.jpg|left|200px]]<br /><applet load="1nl4" size="~~450~~" color="white" frame="true" align="right" spinBox="true"

[[Image:1nl4.jpg|left|200px]]<br /><applet load="1nl4" size="350" color="white" frame="true" align="right" spinBox="true"

caption="1nl4, resolution 2.7Å" />

'''Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor'''<br />

==Overview==

A series of imidazole-containing biphenyls was prepared and evaluated in, vitro for inhibition of FTase and cellular Ras processing. Several of, these analogues, such as 21, are potent inhibitors of FTase (<1nM), FTase/GGTase selective (>300-fold) and cellularly active (<or=80nM). An, X-ray crystal structure of inhibitor 21 bound to rat farnesyltransferase, is also presented.

A series of imidazole-containing biphenyls was prepared and evaluated in vitro for inhibition of FTase and cellular Ras processing. Several of these analogues, such as 21, are potent inhibitors of FTase (<1nM), FTase/GGTase selective (>300-fold) and cellularly active (<or=80nM). An X-ray crystal structure of inhibitor 21 bound to rat farnesyltransferase is also presented.

==About this Structure==

1NL4 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 FTL as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://~~ispc~~.weizmann.ac.il/oca-bin/ocashort?id=1NL4 OCA].

1NL4 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=FTL:'>FTL</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1NL4 OCA].

==Reference==

Line 14:

[[Category: Rattus norvegicus]]

[[Category: Cohen, J.]]

[[Category: Curtin, M.L.]]

[[Category: Curtin, M L.]]

[[Category: Florjancic, A.S.]]

[[Category: Florjancic, A S.]]

[[Category: Frost, D.J.]]

[[Category: Frost, D J.]]

[[Category: Gu, W.J.]]

[[Category: Gu, W J.]]

[[Category: Muchmore, S.W.]]

[[Category: Muchmore, S W.]]

[[Category: Sham, H.L.]]

[[Category: Sham, H L.]]

[[Category: FTL]]

[[Category: HFP]]

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[[Category: transferase]]

''Page seeded by [http://~~ispc~~.weizmann.ac.il/oca OCA ] on ~~Tue Nov 20 22~~:21:~~29 2007~~''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:07:14 2008''

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@@ Line 1: / Line 1: @@
-[[Image:1nl4.jpg|left|200px]]<br /><applet load="1nl4" size="450" color="white" frame="true" align="right" spinBox="true"
+[[Image:1nl4.jpg|left|200px]]<br /><applet load="1nl4" size="350" color="white" frame="true" align="right" spinBox="true"
 caption="1nl4, resolution 2.7&Aring;" />
 '''Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor'''<br />
 ==Overview==
-A series of imidazole-containing biphenyls was prepared and evaluated in, vitro for inhibition of FTase and cellular Ras processing. Several of, these analogues, such as 21, are potent inhibitors of FTase (&lt;1nM), FTase/GGTase selective (&gt;300-fold) and cellularly active (&lt;or=80nM). An, X-ray crystal structure of inhibitor 21 bound to rat farnesyltransferase, is also presented.
+A series of imidazole-containing biphenyls was prepared and evaluated in vitro for inhibition of FTase and cellular Ras processing. Several of these analogues, such as 21, are potent inhibitors of FTase (&lt;1nM), FTase/GGTase selective (&gt;300-fold) and cellularly active (&lt;or=80nM). An X-ray crystal structure of inhibitor 21 bound to rat farnesyltransferase is also presented.
 ==About this Structure==
-NL4 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 FTL as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1NL4 OCA].
+NL4 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=FTL:'>FTL</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1NL4 OCA].
 ==Reference==
@@ Line 14: / Line 14: @@
 [[Category: Rattus norvegicus]]
 [[Category: Cohen, J.]]
-[[Category: Curtin, M.L.]]
+[[Category: Curtin, M L.]]
-[[Category: Florjancic, A.S.]]
+[[Category: Florjancic, A S.]]
-[[Category: Frost, D.J.]]
+[[Category: Frost, D J.]]
-[[Category: Gu, W.J.]]
+[[Category: Gu, W J.]]
-[[Category: Muchmore, S.W.]]
+[[Category: Muchmore, S W.]]
-[[Category: Sham, H.L.]]
+[[Category: Sham, H L.]]
 [[Category: FTL]]
 [[Category: HFP]]
@@ Line 26: / Line 26: @@
 [[Category: transferase]]
-''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Nov 20 22:21:29 2007''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:07:14 2008''