1tvk: Difference between revisions

Line 1:

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

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

caption="1tvk, resolution 2.89Å" />

'''The binding mode of epothilone A on a,b-tubulin by electron crystallography'''<br />

==Overview==

The structure of epothilone A, bound to alpha,beta-tubulin in, zinc-stabilized sheets, was determined by a combination of electron, crystallography at 2.89 angstrom resolution and nuclear magnetic, resonance-based conformational analysis. The complex explains both the, broad-based epothilone structure-activity relationship and the known, mutational resistance profile. Comparison with Taxol shows that the, longstanding expectation of a common pharmacophore is not met, because, each ligand exploits the tubulin-binding pocket in a unique and, independent manner.

The structure of epothilone A, bound to alpha,beta-tubulin in zinc-stabilized sheets, was determined by a combination of electron crystallography at 2.89 angstrom resolution and nuclear magnetic resonance-based conformational analysis. The complex explains both the broad-based epothilone structure-activity relationship and the known mutational resistance profile. Comparison with Taxol shows that the longstanding expectation of a common pharmacophore is not met, because each ligand exploits the tubulin-binding pocket in a unique and independent manner.

==About this Structure==

1TVK is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] with GDP, GTP and EP as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://~~ispc~~.weizmann.ac.il/oca-bin/ocashort?id=1TVK OCA].

1TVK is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] with <scene name='pdbligand=GDP:'>GDP</scene>, <scene name='pdbligand=GTP:'>GTP</scene> and <scene name='pdbligand=EP:'>EP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1TVK OCA].

==Reference==

Line 14:

[[Category: Protein complex]]

[[Category: Cornett, B.]]

[[Category: Downing, K.H.]]

[[Category: Downing, K H.]]

[[Category: Krahn, J.M.]]

[[Category: Krahn, J M.]]

[[Category: Li, H.]]

[[Category: Nettles, J.H.]]

[[Category: Nettles, J H.]]

[[Category: Snyder, J.P.]]

[[Category: Snyder, J P.]]

[[Category: EP]]

[[Category: GDP]]

Line 24:

[[Category: epothilone; taxol; ligand interactions]]

''Page seeded by [http://~~ispc~~.weizmann.ac.il/oca OCA ] on ~~Wed Nov~~ 21 03:37:~~43 2007~~''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:17:49 2008''

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@@ Line 1: / Line 1: @@
-[[Image:1tvk.gif|left|200px]]<br /><applet load="1tvk" size="450" color="white" frame="true" align="right" spinBox="true"
+[[Image:1tvk.gif|left|200px]]<br /><applet load="1tvk" size="350" color="white" frame="true" align="right" spinBox="true"
 caption="1tvk, resolution 2.89&Aring;" />
 '''The binding mode of epothilone A on a,b-tubulin by electron crystallography'''<br />
 ==Overview==
-The structure of epothilone A, bound to alpha,beta-tubulin in, zinc-stabilized sheets, was determined by a combination of electron, crystallography at 2.89 angstrom resolution and nuclear magnetic, resonance-based conformational analysis. The complex explains both the, broad-based epothilone structure-activity relationship and the known, mutational resistance profile. Comparison with Taxol shows that the, longstanding expectation of a common pharmacophore is not met, because, each ligand exploits the tubulin-binding pocket in a unique and, independent manner.
+The structure of epothilone A, bound to alpha,beta-tubulin in zinc-stabilized sheets, was determined by a combination of electron crystallography at 2.89 angstrom resolution and nuclear magnetic resonance-based conformational analysis. The complex explains both the broad-based epothilone structure-activity relationship and the known mutational resistance profile. Comparison with Taxol shows that the longstanding expectation of a common pharmacophore is not met, because each ligand exploits the tubulin-binding pocket in a unique and independent manner.
 ==About this Structure==
-TVK is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] with GDP, GTP and EP as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1TVK OCA].
+TVK is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] with <scene name='pdbligand=GDP:'>GDP</scene>, <scene name='pdbligand=GTP:'>GTP</scene> and <scene name='pdbligand=EP:'>EP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1TVK OCA].
 ==Reference==
@@ Line 14: / Line 14: @@
 [[Category: Protein complex]]
 [[Category: Cornett, B.]]
-[[Category: Downing, K.H.]]
+[[Category: Downing, K H.]]
-[[Category: Krahn, J.M.]]
+[[Category: Krahn, J M.]]
 [[Category: Li, H.]]
-[[Category: Nettles, J.H.]]
+[[Category: Nettles, J H.]]
-[[Category: Snyder, J.P.]]
+[[Category: Snyder, J P.]]
 [[Category: EP]]
 [[Category: GDP]]
@@ Line 24: / Line 24: @@
 [[Category: epothilone; taxol; ligand interactions]]
-''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Wed Nov 21 03:37:43 2007''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:17:49 2008''