2fx6
From Proteopedia
(New page: 200px<br /><applet load="2fx6" size="450" color="white" frame="true" align="right" spinBox="true" caption="2fx6, resolution 1.57Å" /> '''bovine trypsin compl...) |
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| - | [[Image:2fx6.gif|left|200px]]<br /><applet load="2fx6" size=" | + | [[Image:2fx6.gif|left|200px]]<br /><applet load="2fx6" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="2fx6, resolution 1.57Å" /> | caption="2fx6, resolution 1.57Å" /> | ||
'''bovine trypsin complexed with 2-aminobenzamidazole'''<br /> | '''bovine trypsin complexed with 2-aminobenzamidazole'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Improved peptide-based inhibitors of human beta tryptase were discovered | + | Improved peptide-based inhibitors of human beta tryptase were discovered using information gleaned from tripeptide library screening and structure-guided design methods, including fragment screening. Our efforts sought to improve this class of inhibitors by replacing the traditional Lys or Arg P1 element. The optimized compounds display low nanomolar potency against the mast cell target and several hundred-fold selectivity with respect to serine protease off targets. Thus, replacement of Lys/Arg at P1 in a peptide-like scaffold does not need to be accompanied by a loss in target affinity. |
==About this Structure== | ==About this Structure== | ||
| - | 2FX6 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 and 270 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:// | + | 2FX6 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> and <scene name='pdbligand=270:'>270</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=2FX6 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Trypsin]] | [[Category: Trypsin]] | ||
| - | [[Category: Katz, B | + | [[Category: Katz, B A.]] |
[[Category: 270]] | [[Category: 270]] | ||
[[Category: CA]] | [[Category: CA]] | ||
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[[Category: serine protease]] | [[Category: serine protease]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:25:59 2008'' |
Revision as of 15:25, 21 February 2008
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bovine trypsin complexed with 2-aminobenzamidazole
Overview
Improved peptide-based inhibitors of human beta tryptase were discovered using information gleaned from tripeptide library screening and structure-guided design methods, including fragment screening. Our efforts sought to improve this class of inhibitors by replacing the traditional Lys or Arg P1 element. The optimized compounds display low nanomolar potency against the mast cell target and several hundred-fold selectivity with respect to serine protease off targets. Thus, replacement of Lys/Arg at P1 in a peptide-like scaffold does not need to be accompanied by a loss in target affinity.
About this Structure
2FX6 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
Structure-guided design of peptide-based tryptase inhibitors., McGrath ME, Sprengeler PA, Hirschbein B, Somoza JR, Lehoux I, Janc JW, Gjerstad E, Graupe M, Estiarte A, Venkataramani C, Liu Y, Yee R, Ho JD, Green MJ, Lee CS, Liu L, Tai V, Spencer J, Sperandio D, Katz BA, Biochemistry. 2006 May 16;45(19):5964-73. PMID:16681368
Page seeded by OCA on Thu Feb 21 17:25:59 2008
Categories: Bos taurus | Single protein | Trypsin | Katz, B A. | 270 | CA | Fragment screening | S1 site | Serine protease
