1rxp
From Proteopedia
(New page: 200px<br /><applet load="1rxp" size="450" color="white" frame="true" align="right" spinBox="true" caption="1rxp, resolution 1.70Å" /> '''STRUCTURE OF TRYPSIN...) |
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| - | [[Image:1rxp.gif|left|200px]]<br /><applet load="1rxp" size=" | + | [[Image:1rxp.gif|left|200px]]<br /><applet load="1rxp" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1rxp, resolution 1.70Å" /> | caption="1rxp, resolution 1.70Å" /> | ||
'''STRUCTURE OF TRYPSIN (ORTHORHOMBIC) WITH 1-(4-TERT-BUTYLCARBAMOYL- PIPERAZINE-1-CARBONYL)-3-(3-GUANIDINO-PROPYL)-4-OXO-AZETIDINE-2-CARBOXYLIC ACID'''<br /> | '''STRUCTURE OF TRYPSIN (ORTHORHOMBIC) WITH 1-(4-TERT-BUTYLCARBAMOYL- PIPERAZINE-1-CARBONYL)-3-(3-GUANIDINO-PROPYL)-4-OXO-AZETIDINE-2-CARBOXYLIC ACID'''<br /> | ||
==Overview== | ==Overview== | ||
| - | A series of nonguanidine N1-activated C4-carboxy azetidinone tryptase | + | A series of nonguanidine N1-activated C4-carboxy azetidinone tryptase inhibitors was prepared by solid-phase methodology to quickly assess the SAR associated with distal functionality on the N1-activating group. From these studies, potent inhibitors with improved specificity were discovered. |
==About this Structure== | ==About this Structure== | ||
| - | 1RXP is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] with CA, SO4 and 169 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Trypsin Trypsin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.4 3.4.21.4] Full crystallographic information is available from [http:// | + | 1RXP is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] with <scene name='pdbligand=CA:'>CA</scene>, <scene name='pdbligand=SO4:'>SO4</scene> and <scene name='pdbligand=169:'>169</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Trypsin Trypsin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.4 3.4.21.4] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1RXP OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Trypsin]] | [[Category: Trypsin]] | ||
| - | [[Category: Bisacchi, G | + | [[Category: Bisacchi, G S.]] |
[[Category: Jacobson, B.]] | [[Category: Jacobson, B.]] | ||
[[Category: 169]] | [[Category: 169]] | ||
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[[Category: tryptase inhibitor; serine protease; azetidinone]] | [[Category: tryptase inhibitor; serine protease; azetidinone]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:55:38 2008'' |
Revision as of 12:55, 21 February 2008
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STRUCTURE OF TRYPSIN (ORTHORHOMBIC) WITH 1-(4-TERT-BUTYLCARBAMOYL- PIPERAZINE-1-CARBONYL)-3-(3-GUANIDINO-PROPYL)-4-OXO-AZETIDINE-2-CARBOXYLIC ACID
Overview
A series of nonguanidine N1-activated C4-carboxy azetidinone tryptase inhibitors was prepared by solid-phase methodology to quickly assess the SAR associated with distal functionality on the N1-activating group. From these studies, potent inhibitors with improved specificity were discovered.
About this Structure
1RXP is a Single protein structure of sequence from Bos taurus with , and as ligands. Active as Trypsin, with EC number 3.4.21.4 Full crystallographic information is available from OCA.
Reference
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors., Sutton JC, Bolton SA, Davis ME, Hartl KS, Jacobson B, Mathur A, Ogletree ML, Slusarchyk WA, Zahler R, Seiler SM, Bisacchi GS, Bioorg Med Chem Lett. 2004 May 3;14(9):2233-9. PMID:15081015
Page seeded by OCA on Thu Feb 21 14:55:38 2008
