View source for 2fww

[[Image:2fww.gif|left|200px]]

 {{Structure
|PDB= 2fww |SIZE=350|CAPTION= <scene name='initialview01'>2fww</scene>, resolution 2.25&Aring;
|SITE= 
|LIGAND= <scene name='pdbligand=C1R:4-PIPERIDINEBUTYRATE'>C1R</scene>
|ACTIVITY= [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] 
|GENE= TPSB2, TPS2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
}}

'''human beta-tryptase II complexed with 4-piperidinebutyrate to make acylenzyme'''


==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==
2FWW is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2FWW 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:[http://www.ncbi.nlm.nih.gov/pubmed/16681368 16681368]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Tryptase]]
[[Category: Katz, B A.]]
[[Category: C1R]]
[[Category: 29382]]
[[Category: proteinase]]
[[Category: serine protease]]

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