Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-α converting enzyme (TACE)

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 12, 2003, Pages 2021-2024

  Sawa, Masaaki ^a,b   Kurokawa, Kiriko ^a   Inoue, Yoshimasa ^a   Kondo, Hirosato ^a,c   Yoshino, Kohichiro ^a  

^a Nippon Organon KK   (Japan)

^b DAINIPPON SUMITOMO PHARMA CO LTD   (Japan)

^c SHIONOGI AND CO LTD   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

GELATINASE B; INTERSTITIAL COLLAGENASE; PHOSPHORUS DERIVATIVE; STROMELYSIN; TETRAHYDROISOQUINOLINE DERIVATIVE; TUMOR NECROSIS FACTOR ALPHA CONVERTING ENZYME; TUMOR NECROSIS FACTOR ALPHA CONVERTING ENZYME INHIBITOR;

ARTICLE; DRUG ACTIVITY; DRUG POTENCY; DRUG SCREENING; DRUG SELECTIVITY; DRUG SYNTHESIS; ENZYME INHIBITION;

EID: 0038440615     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00292-0     Document Type: Article

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11. Recombinant human TACE, collagenase-1 (MMP-1), stromelysin 1 (MMP-3), and gelatinase B (MMP-9) were used in our studies (see ref 4 for assay conditions).
12. Models of TACE complexed with the phosphonamide inhibitors were constructed based on the crystal structure of a TACE/peptide-based inhibitor complex (PDB code, 1BKC). Docking and energy minimizations were performed with the TRIPOS force field within the SYBYL program. All computations were performed on an Silicon Graphics workstation.