Novel TNF-α converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 24, 2010, Pages 7283-7287

  Girijavallabhan, Vinay M ^a   Chen, Lei ^a   Dai, Chaoyang ^a   Feltz, Robert J ^a   Firmansjah, Luke ^a   Li, Dansu ^a   Kim, Seong Heon ^a   Kozlowski, Joseph A ^a   Lavey, Brian J ^a   Kosinski, Aneta ^a   Piwinski, John J ^a   Popovici Muller, Janeta ^a   Rizvi, Razia ^a   Rosner, Kristin E ^a   Shankar, Banderpalle B ^a   Shih, Neng Yang ^a   Siddiqui, M Arshad ^a   Tong, Ling ^a   Wong, Michael K C ^a   Yang, De Yi ^a   Yang, Liping ^a   Yu, Wensheng ^a   Zhou, Guowei ^a   Guo, Zhuyan ^a   Orth, Peter ^a   Madison, Vincent ^a   Bian, Hong ^a   Lundell, Daniel ^a   Niu, Xiaoda ^a   Shah, Himanshu ^a   Sun, Jing ^a   Umland, Shelby ^a   more..

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Hydantoin; Rheumatoid arthritis; TACE inhibitor

Indexed keywords

TUMOR NECROSIS FACTOR ALPHA CONVERTING ENZYME INHIBITOR;

ARTICLE; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; INFLAMMATORY DISEASE;

ACETYLENE; ADAM PROTEINS; ANIMALS; ANTI-INFLAMMATORY AGENTS; ARTHRITIS, RHEUMATOID; DOGS; HAPLORHINI; HUMANS; PROTEASE INHIBITORS; RATS;

EID: 78449287666     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.10.081     Document Type: Article

References (23)

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18. Human whole blood procedure: Human whole blood is diluted 1:1 with serum free medium (RPMI, l-glutamine, Pen-Strep, HEPES) and incubated with a compound in a final volume of 360 L for 1 h at 37 °C. Forty microliters of LPS (10 μg/mL) is then added. Supernatant is collected after 3.5 h incubation and the concentration of TNF-α is determined by ELISA (R&D Systems).
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23. Attempts were made to make correlations between hWBA and protein binding but no trends were apparent. It became clear through our studies that hWBA optimization was empirical.