Incorporation of fluorinated phenylalanine generates highly specific inhibitor of proteasome's chymotrypsin-like sites.

Geurink, Paul P; Liu, Nora; Spaans, Michiel P; Downey, Sondra L; van den Nieuwendijk, Adrianus M C H; van der Marel, Gijsbert A; Kisselev, Alexei F; Florea, Bogdan I; Overkleeft, Herman S

Geurink, Paul P; Liu, Nora; Spaans, Michiel P; Downey, Sondra L; van den Nieuwendijk, Adrianus M C H; van der Marel, Gijsbert A; Kisselev, Alexei F; Florea, Bogdan I; Overkleeft, Herman S.

Affiliation

Geurink PP; Leiden Institute of Chemistry and Netherlands Proteomics Centre, Gorlaeus Laboratories, Einsteinweg 55, 2333 CC Leiden, The Netherlands.

J Med Chem ; 53(5): 2319-23, 2010 Mar 11.

Article in En | MEDLINE | ID: mdl-20131905

Subject(s)

Catalytic Domain/drug effects; Chymotrypsin/metabolism; Cysteine Proteinase Inhibitors/chemical synthesis; Phenylalanine/analogs & derivatives; Proteasome Endopeptidase Complex/metabolism; Chymotrypsin/antagonists & inhibitors; Cysteine Proteinase Inhibitors/chemistry; Cysteine Proteinase Inhibitors/pharmacology; Inhibitory Concentration 50; Phenylalanine/chemical synthesis; Phenylalanine/chemistry; Phenylalanine/pharmacology; Proteasome Inhibitors; Structure-Activity Relationship

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Phenylalanine / Chymotrypsin / Cysteine Proteinase Inhibitors / Catalytic Domain / Proteasome Endopeptidase Complex Language: En Journal: J Med Chem Journal subject: QUIMICA Year: 2010 Document type: Article Affiliation country: Netherlands Country of publication: United States

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