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CATH domain | Related DB codes (homologues) |
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2.40.10.10 : Thrombin, subunit H | M00139,D00214,M00167,D00426,M00133,D00428,D00429,D00430,D00431,D00432,D00434,D00435,M00227,M00209,D00194,D00197,D00211,D00212,D00216,M00212,D00224,D00497,M00217,M00216,D00528,D00848,D00850,D00851,D00852,D00855,M00152,M00155,M00157,M00181,M00315,M00316,M00317,M00348,M00349,T00074,T00410,T00411 |
Enzyme Name | UniProtKB | KEGG |
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| P24158 |
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Protein name | Myeloblastin | myeloblastinleukocyte proteinase 3leukocyte proteinase 4Wegener's granulomatosis autoantigenproteinase PR-3proteinase-3PMNL proteinase |
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Synonyms | EC 3.4.21.76Leukocyte proteinase 3PR-3PR3AGP7Wegener autoantigenP29C-ANCA antigenNeutrophil proteinase 4NP-4 |
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RefSeq | NP_002768.3 (Protein) NM_002777.3 (DNA/RNA sequence)
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MEROPS | S01.134 (Serine)
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Pfam | PF00089 (Trypsin) [Graphical view]
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UniProtKB:Accession Number | P24158 |
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Entry name | PRTN3_HUMAN |
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Activity | Hydrolysis of proteins, including elastin, by preferential cleavage: -Ala-|-Xaa- > -Val-|-Xaa-. |
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Subunit |
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Subcellular location |
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Cofactor |
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Compound table: links to PDB-related databases & PoSSuM |
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| Substrates | Products | intermediates |
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KEGG-id | C00012 | C00017 | C00001 | C00012 | C00017 | I00087 | I00085 | I00086 |
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Compound | Peptide | Protein | H2O | Peptide | Protein | Peptidyl-tetrahedral intermediate | Acyl-enzyme | Tetrahedral intermediate |
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Type | peptide/protein | peptide/protein | H2O | peptide/protein | peptide/protein |
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ChEBI |
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| 15377
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PubChem |
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| 22247451 962
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| | | | | | | | | | | | | | | |
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1fujA01 |  |  |  |  |  |  |  | Unbound | Unbound | | Unbound | Unbound | Unbound | Unbound | Unbound |
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1fujB01 |  |  |  |  |  |  |  | Unbound | Unbound | | Unbound | Unbound | Unbound | Unbound | Unbound |
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1fujC01 |  |  |  |  |  |  |  | Unbound | Unbound | | Unbound | Unbound | Unbound | Unbound | Unbound |
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1fujD01 |  |  |  |  |  |  |  | Unbound | Unbound | | Unbound | Unbound | Unbound | Unbound | Unbound |
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1fujA02 |  |  |  |  |  |  |  | Unbound | Unbound | | Unbound | Unbound | Unbound | Unbound | Unbound |
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1fujB02 |  |  |  |  |  |  |  | Unbound | Unbound | | Unbound | Unbound | Unbound | Unbound | Unbound |
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1fujC02 |  |  |  |  |  |  |  | Unbound | Unbound | | Unbound | Unbound | Unbound | Unbound | Unbound |
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1fujD02 |  |  |  |  |  |  |  | Unbound | Unbound | | Unbound | Unbound | Unbound | Unbound | Unbound |
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references | [1] |
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Comments | IDENTITY OF WEGENER'S AUTOANTIGEN WITH PROTEINASE 3. |
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Medline ID | 91055123 |
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PubMed ID | 2242436 |
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Journal | Blood |
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Year | 1990 |
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Volume | 76 |
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Pages | 2162 |
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Authors | Gupta SK, Niles JL, McCluskey RT, Arnaout MA |
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Title | Identity of Wegener's autoantigen (p29) with proteinase 3 and myeloblastin. |
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Related UniProtKB | P24158 |
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[2] |
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PubMed ID | 2258701 |
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Journal | J Exp Med |
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Year | 1990 |
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Volume | 172 |
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Pages | 1709-15 |
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Authors | Campanelli D, Melchior M, Fu Y, Nakata M, Shuman H, Nathan C, Gabay JE |
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Title | Cloning of cDNA for proteinase 3: a serine protease, antibiotic, and autoantigen from human neutrophils. |
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[3] |
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PubMed ID | 1459241 |
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Journal | FEBS Lett |
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Year | 1992 |
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Volume | 314 |
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Pages | 117-21 |
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Authors | Dolman KM, van de Wiel BA, Kam CM, Abbink JJ, Hack CE, Sonnenberg A, Powers JC, von dem Borne AE, Goldschmeding R |
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Title | Determination of proteinase 3-alpha 1-antitrypsin complexes in inflammatory fluids. |
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[4] |
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PubMed ID | 1380042 |
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Journal | J Immunol |
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Year | 1992 |
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Volume | 149 |
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Pages | 1409-15 |
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Authors | Bini P, Gabay JE, Teitel A, Melchior M, Zhou JL, Elkon KB |
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Title | Antineutrophil cytoplasmic autoantibodies in Wegener's granulomatosis recognize conformational epitope(s) on proteinase 3. |
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[5] |
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PubMed ID | 7925979 |
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Journal | FEBS Lett |
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Year | 1994 |
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Volume | 352 |
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Pages | 231-5 |
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Authors | Padrines M, Wolf M, Walz A, Baggiolini M |
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Title | Interleukin-8 processing by neutrophil elastase, cathepsin G and proteinase-3. |
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[6] |
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PubMed ID | 8157982 |
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Journal | J Immunol |
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Year | 1994 |
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Volume | 152 |
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Pages | 4722-37 |
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Authors | Williams RC Jr, Staud R, Malone CC, Payabyab J, Byres L, Underwood D |
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Title | Epitopes on proteinase-3 recognized by antibodies from patients with Wegener's granulomatosis. |
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[7] |
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PubMed ID | 8581420 |
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Journal | Bioorg Med Chem |
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Year | 1995 |
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Volume | 3 |
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Pages | 375-81 |
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Authors | Groutas WC, Brubaker MJ, Chong LS, Venkataraman R, Huang H, Epp JB, Kuang R, Hoidal JR |
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Title | Design, synthesis and biological evaluation of succinimide derivatives as potential mechanism-based inhibitors of human leukocyte elastase, cathepsin G and proteinase 3. |
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[8] |
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PubMed ID | 7796053 |
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Journal | Bioorg Med Chem |
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Year | 1995 |
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Volume | 3 |
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Pages | 187-93 |
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Authors | Groutas WC, Chong LS, Venkataraman R, Epp JB, Kuang R, Houser-Archield N, Hoidal JR |
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Title | The Gabriel-Colman rearrangement in biological systems: design, synthesis and biological evaluation of phthalimide and saccharin derivatives as potential mechanism-based inhibitors of human leukocyte elastase, cathepsin G and proteinase 3. |
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[9] |
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PubMed ID | 7796046 |
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Journal | Bioorg Med Chem |
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Year | 1995 |
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Volume | 3 |
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Pages | 125-8 |
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Authors | Groutas WC, Venkataraman R, Chong LS, Yoder JE, Epp JB, Stanga MA, Kim EH |
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Title | Isoxazoline derivatives as potential inhibitors of the proteolytic enzymes human leukocyte elastase, cathepsin G and proteinase 3: a structure-activity relationship study. |
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[10] |
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PubMed ID | 8806743 |
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Journal | Arch Biochem Biophys |
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Year | 1996 |
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Volume | 332 |
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Pages | 335-40 |
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Authors | Groutas WC, Chong LS, Venkataraman R, Kuang R, Epp JB, Houser-Archield N, Huang H, Hoidal JR |
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Title | Amino acid-derived phthalimide and saccharin derivatives as inhibitors of human leukocyte elastase, cathepsin G, and proteinase 3. |
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[11] |
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PubMed ID | 8894097 |
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Journal | Bioorg Med Chem |
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Year | 1996 |
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Volume | 4 |
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Pages | 1393-400 |
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Authors | Groutas WC, Epp JB, Venkataraman R, Kuang R, Truong TM, McClenahan JJ, Prakash O |
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Title | Design, synthesis, and in vitro inhibitory activity toward human leukocyte elastase, cathepsin G, and proteinase 3 of saccharin-derived sulfones and congeners. |
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[12] |
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Comments | X-RAY CRYSTALLOGRAPHY (2.2 ANGSTROMS). |
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Medline ID | 96346178 |
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PubMed ID | 8757293 |
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Journal | J Mol Biol |
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Year | 1996 |
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Volume | 261 |
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Pages | 267-78 |
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Authors | Fujinaga M, Chernaia MM, Halenbeck R, Koths K, James MN |
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Title | The crystal structure of PR3, a neutrophil serine proteinase antigen of Wegener's granulomatosis antibodies. |
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Related PDB | 1fuj |
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Related UniProtKB | P24158 |
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[13] |
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PubMed ID | 9125494 |
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Journal | Biochemistry |
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Year | 1997 |
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Volume | 36 |
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Pages | 4739-50 |
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Authors | Groutas WC, Kuang R, Venkataraman R, Epp JB, Ruan S, Prakash O |
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Title | Structure-based design of a general class of mechanism-based inhibitors of the serine proteinases employing a novel amino acid-derived heterocyclic scaffold. |
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[14] |
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PubMed ID | 9058715 |
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Journal | Blood |
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Year | 1997 |
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Volume | 89 |
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Pages | 1944-53 |
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Authors | Renesto P, Si-Tahar M, Moniatte M, Balloy V, Van Dorsselaer A, Pidard D, Chignard M |
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Title | Specific inhibition of thrombin-induced cell activation by the neutrophil proteinases elastase, cathepsin G, and proteinase 3: evidence for distinct cleavage sites within the aminoterminal domain of the thrombin receptor. |
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[15] |
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PubMed ID | 9092534 |
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Journal | J Biol Chem |
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Year | 1997 |
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Volume | 272 |
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Pages | 9950-5 |
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Authors | Cadene M, Duranton J, North A, Si-Tahar M, Chignard M, Bieth JG |
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Title | Inhibition of neutrophil serine proteinases by suramin. |
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[16] |
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PubMed ID | 9681132 |
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Journal | Bioorg Med Chem |
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Year | 1998 |
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Volume | 6 |
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Pages | 661-71 |
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Authors | Groutas WC, Kuang R, Ruan S, Epp JB, Venkataraman R, Truong TM |
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Title | Potent and specific inhibition of human leukocyte elastase, cathepsin G and proteinase 3 by sulfone derivatives employing the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold. |
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[17] |
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PubMed ID | 9756722 |
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Journal | Clin Immunol Immunopathol |
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Year | 1998 |
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Volume | 89 |
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Pages | 35-43 |
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Authors | Davis JA, Peen E, Williams RC, Perkins S, Malone CC, McCormack WT, Csernok E, Gross WL, Kolaskar AS, Kulkarni-Kale U |
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Title | Determination of primary amino acid sequence and unique three-dimensional structure of WGH1, a monoclonal human IgM antibody with anti-PR3 specificity. |
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[18] |
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PubMed ID | 10103046 |
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Journal | Eur J Biochem |
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Year | 1999 |
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Volume | 261 |
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Pages | 155-62 |
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Authors | Goldmann WH, Niles JL, Arnaout MA |
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Title | Interaction of purified human proteinase 3 (PR3) with reconstituted lipid bilayers. |
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[19] |
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PubMed ID | 11094439 |
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Journal | Arthritis Res |
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Year | 2000 |
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Volume | 2 |
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Pages | 263-7 |
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Authors | Specks U |
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Title | What you should know about PR3-ANCA. Conformational requirements of proteinase 3 (PR3) for enzymatic activity and recognition by PR3-ANCA. |
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[20] |
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PubMed ID | 10976518 |
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Journal | Bioorg Med Chem |
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Year | 2000 |
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Volume | 8 |
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Pages | 1713-7 |
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Authors | He S, Kuang R, Venkataraman R, Tu J, Truong TM, Chan HK, Groutas WC |
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Title | Potent inhibition of serine proteases by heterocyclic sulfide derivatives of 1,2,5-thiadiazolidin-3-one 1,1 dioxide. |
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[21] |
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PubMed ID | 10975855 |
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Journal | J Immunol |
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Year | 2000 |
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Volume | 165 |
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Pages | 3366-74 |
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Authors | Campbell EJ, Campbell MA, Owen CA |
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Title | Bioactive proteinase 3 on the cell surface of human neutrophils: quantification, catalytic activity, and susceptibility to inhibition. |
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[22] |
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PubMed ID | 11159195 |
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Journal | Am J Pathol |
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Year | 2001 |
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Volume | 158 |
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Pages | 581-92 |
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Authors | Yang JJ, Preston GA, Pendergraft WF, Segelmark M, Heeringa P, Hogan SL, Jennette JC, Falk RJ |
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Title | Internalization of proteinase 3 is concomitant with endothelial cell apoptosis and internalization of myeloperoxidase with generation of intracellular oxidants. |
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[23] |
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PubMed ID | 11747453 |
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Journal | Biochemistry |
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Year | 2001 |
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Volume | 40 |
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Pages | 15762-70 |
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Authors | Cooley J, Takayama TK, Shapiro SD, Schechter NM, Remold-O'Donnell E |
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Title | The serpin MNEI inhibits elastase-like and chymotrypsin-like serine proteases through efficient reactions at two active sites. |
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[24] |
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PubMed ID | 11408173 |
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Journal | Bioorg Med Chem |
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Year | 2001 |
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Volume | 9 |
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Pages | 1543-8 |
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Authors | Groutas WC, He S, Kuang R, Ruan S, Tu J, Chan HK |
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Title | Inhibition of serine proteases by functionalized sulfonamides coupled to the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold. |
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[25] |
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PubMed ID | 11168015 |
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Journal | Clin Exp Immunol |
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Year | 2001 |
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Volume | 123 |
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Pages | 170-7 |
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Authors | Griffith ME, Coulthart A, Pemberton S, George AJ, Pusey CD |
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Title | Anti-neutrophil cytoplasmic antibodies (ANCA) from patients with systemic vasculitis recognize restricted epitopes of proteinase 3 involving the catalytic site. |
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[26] |
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PubMed ID | 12135665 |
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Journal | Exp Hematol |
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Year | 2002 |
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Volume | 30 |
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Pages | 689-96 |
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Authors | Skold S, Zeberg L, Gullberg U, Olofsson T |
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Title | Functional dissociation between proforms and mature forms of proteinase 3, azurocidin, and granzyme B in regulation of granulopoiesis. |
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comments | This enzyme belongs to the peptidase family-S1. This enzyme has got a classical catalytic triad, composed of Ser/His/Asp, which is the same as that of trypsin (D00197 in EzCatDB). It suggests that it may have a similar catalytic mechanism to that of trypsin.
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created | updated |
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2004-10-29 | 2011-02-21 |
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