2foy: Difference between revisions

From Proteopedia
Jump to navigationJump to search
OCA (talk | contribs)
New page: left|200px<br /> <applet load="2foy" size="450" color="white" frame="true" align="right" spinBox="true" caption="2foy, resolution 1.55Å" /> '''Human Carbonic Anhy...
 
OCA (talk | contribs)
No edit summary
Line 1: Line 1:
[[Image:2foy.gif|left|200px]]<br />
[[Image:2foy.gif|left|200px]]<br /><applet load="2foy" size="350" color="white" frame="true" align="right" spinBox="true"  
<applet load="2foy" size="450" color="white" frame="true" align="right" spinBox="true"  
caption="2foy, resolution 1.55&Aring;" />
caption="2foy, resolution 1.55&Aring;" />
'''Human Carbonic Anhydrase I complexed with a two-prong inhibitor'''<br />
'''Human Carbonic Anhydrase I complexed with a two-prong inhibitor'''<br />


==Overview==
==Overview==
The atomic-resolution crystal structures of human carbonic anhydrases I, and II complexed with "two-prong" inhibitors are reported. Each inhibitor, contains a benzenesulfonamide prong and a cupric iminodiacetate, (IDA-Cu(2+)) prong separated by linkers of different lengths and, compositions. The ionized NH(-) group of each benzenesulfonamide, coordinates to the active site Zn(2+) ion; the IDA-Cu(2+) prong of the, tightest-binding inhibitor, BR30, binds to H64 of CAII and H200 of CAI., This work provides the first evidence verifying the structural basis of, nanomolar affinity measured for two-prong inhibitors targeting the, carbonic anhydrases.
The atomic-resolution crystal structures of human carbonic anhydrases I and II complexed with "two-prong" inhibitors are reported. Each inhibitor contains a benzenesulfonamide prong and a cupric iminodiacetate (IDA-Cu(2+)) prong separated by linkers of different lengths and compositions. The ionized NH(-) group of each benzenesulfonamide coordinates to the active site Zn(2+) ion; the IDA-Cu(2+) prong of the tightest-binding inhibitor, BR30, binds to H64 of CAII and H200 of CAI. This work provides the first evidence verifying the structural basis of nanomolar affinity measured for two-prong inhibitors targeting the carbonic anhydrases.


==About this Structure==
==About this Structure==
2FOY is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with ZN and B30 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Carbonate_dehydratase Carbonate dehydratase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=4.2.1.1 4.2.1.1] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2FOY OCA].  
2FOY is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=ZN:'>ZN</scene> and <scene name='pdbligand=B30:'>B30</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Carbonate_dehydratase Carbonate dehydratase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=4.2.1.1 4.2.1.1] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2FOY OCA].  


==Reference==
==Reference==
Line 15: Line 14:
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Banerjee, A.L.]]
[[Category: Banerjee, A L.]]
[[Category: Christianson, D.W.]]
[[Category: Christianson, D W.]]
[[Category: Haldar, M.K.]]
[[Category: Haldar, M K.]]
[[Category: Jude, K.M.]]
[[Category: Jude, K M.]]
[[Category: Mallik, S.]]
[[Category: Mallik, S.]]
[[Category: Manokaran, S.]]
[[Category: Manokaran, S.]]
[[Category: Roy, B.]]
[[Category: Roy, B.]]
[[Category: Srivastava, D.K.]]
[[Category: Srivastava, D K.]]
[[Category: B30]]
[[Category: B30]]
[[Category: ZN]]
[[Category: ZN]]
Line 30: Line 29:
[[Category: zinc]]
[[Category: zinc]]


''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 22:08:55 2007''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:23:41 2008''