2za5

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{{STRUCTURE_2za5| PDB=2za5 | SCENE= }}
{{STRUCTURE_2za5| PDB=2za5 | SCENE= }}
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'''Crystal Structure of human tryptase with potent non-peptide inhibitor'''
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===Crystal Structure of human tryptase with potent non-peptide inhibitor===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 18272363 is the PubMed ID number.
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{{ABSTRACT_PUBMED_18272363}}
==About this Structure==
==About this Structure==
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==Reference==
==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:[http://www.ncbi.nlm.nih.gov/pubmed/18272363 18272363]
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:[http://www.ncbi.nlm.nih.gov/pubmed/18272363 18272363]
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Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone., Costanzo MJ, Yabut SC, Almond HR Jr, Andrade-Gordon P, Corcoran TW, De Garavilla L, Kauffman JA, Abraham WM, Recacha R, Chattopadhyay D, Maryanoff BE, J Med Chem. 2003 Aug 28;46(18):3865-76. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12930148 12930148]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: Tetramer]]
[[Category: Tetramer]]
[[Category: Tryptase]]
[[Category: Tryptase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 18:03:21 2008''

Revision as of 15:03, 27 July 2008

Template:STRUCTURE 2za5

Crystal Structure of human tryptase with potent non-peptide inhibitor

Template:ABSTRACT PUBMED 18272363

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

Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone., Costanzo MJ, Yabut SC, Almond HR Jr, Andrade-Gordon P, Corcoran TW, De Garavilla L, Kauffman JA, Abraham WM, Recacha R, Chattopadhyay D, Maryanoff BE, J Med Chem. 2003 Aug 28;46(18):3865-76. PMID:12930148

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