2za5

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
[[Image:2za5.jpg|left|200px]]
[[Image:2za5.jpg|left|200px]]
-
{{Structure
+
<!--
-
|PDB= 2za5 |SIZE=350|CAPTION= <scene name='initialview01'>2za5</scene>, resolution 2.300&Aring;
+
The line below this paragraph, containing "STRUCTURE_2za5", creates the "Structure Box" on the page.
-
|SITE= <scene name='pdbsite=AC1:2ff+Binding+Site+For+Residue+B+1'>AC1</scene>, <scene name='pdbsite=AC2:2ff+Binding+Site+For+Residue+A+4'>AC2</scene>, <scene name='pdbsite=AC3:2ff+Binding+Site+For+Residue+D+3'>AC3</scene> and <scene name='pdbsite=AC4:2ff+Binding+Site+For+Residue+C+2'>AC4</scene>
+
You may change the PDB parameter (which sets the PDB file loaded into the applet)
-
|LIGAND= <scene name='pdbligand=2FF:(5-(AMINOMETHYL)-2H-SPIRO[BENZOFURAN-3,4&#39;-PIPERIDINE]-1&#39;-YL)(5-(PHENYLETHYNYL)FURAN-2-YL)METHANONE'>2FF</scene>
+
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-
|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Tryptase Tryptase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.59 3.4.21.59] </span>
+
or leave the SCENE parameter empty for the default display.
-
|GENE=
+
-->
-
|DOMAIN=<span class='plainlinks'>[http://www.ncbi.nlm.nih.gov/Structure/cdd/cddsrv.cgi?uid=cd00190 Tryp_SPc]</span>
+
{{STRUCTURE_2za5| PDB=2za5 | SCENE= }}
-
|RELATEDENTRY=
+
-
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2za5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2za5 OCA], [http://www.ebi.ac.uk/pdbsum/2za5 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2za5 RCSB]</span>
+
-
}}
+
'''Crystal Structure of human tryptase with potent non-peptide inhibitor'''
'''Crystal Structure of human tryptase with potent non-peptide inhibitor'''
Line 30: Line 27:
[[Category: Milligan, C.]]
[[Category: Milligan, C.]]
[[Category: Spurlino, J C.]]
[[Category: Spurlino, J C.]]
-
[[Category: hydrolase]]
+
[[Category: Hydrolase]]
-
[[Category: serine protease]]
+
[[Category: Serine protease]]
-
[[Category: tetramer]]
+
[[Category: Tetramer]]
-
[[Category: tryptase]]
+
[[Category: Tryptase]]
-
 
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 20:05:13 2008''
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Apr 2 11:32:34 2008''
+

Revision as of 17:05, 4 May 2008

Image:2za5.jpg

Template:STRUCTURE 2za5

Crystal Structure of human tryptase with potent non-peptide inhibitor


Overview

We have explored a series of spirocyclic piperidine amide derivatives (5) as tryptase inhibitors. Thus, 4 (JNJ-27390467) was identified as a potent, selective tryptase inhibitor with oral efficacy in two animal models of airway inflammation (sheep and guinea pig asthma models). An X-ray co-crystal structure of 4.tryptase revealed a hydrophobic pocket in the enzyme's active site, which is induced by the phenylethynyl group and is comprised of amino acid residues from two different monomers of the tetrameric protein.

About this Structure

2ZA5 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives., Costanzo MJ, Yabut SC, Zhang HC, White KB, de Garavilla L, Wang Y, Minor LK, Tounge BA, Barnakov AN, Lewandowski F, Milligan C, Spurlino JC, Abraham WM, Boswell-Smith V, Page CP, Maryanoff BE, Bioorg Med Chem Lett. 2008 Jan 30;. PMID:18272363 Page seeded by OCA on Sun May 4 20:05:13 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2za5"
Personal tools