SAR studies of 2-methoxyestradiol and development of its analogs as probes of anti-tumor mechanisms

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 13, 2006, Pages 3383-3387

  Ho, Abby ^a   Kim, Yang eon ^a   Lee, Hyo Sung ^a   Cyrus, Kedra ^a   Baek, Sun Hee ^a   Kim, Kyung Bo ^a  

^a University of Kentucky   (United States)

Author keywords

2 Methoxyestradiol; Affinity matrix; Anti tumor estrogen metabolites; Biotinylation

Indexed keywords

2 METHOXYESTRADIOL; ESTRADIOL DERIVATIVE;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CANCER CLASSIFICATION; DRUG MECHANISM; DRUG SYNTHESIS; HUMAN; HUMAN CELL; STRUCTURE ACTIVITY RELATION; TUMOR CELL;

ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; CELL PROLIFERATION; DRUG SCREENING ASSAYS, ANTITUMOR; ESTRADIOL; HUMANS; MOLECULAR CONFORMATION; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 33646838414     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.04.030     Document Type: Article

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35. 2 (8) overnight at 4 °C on rocking shaker. Affigel-10 was washed with DMSO, 1 N acetic acid, and distilled water sequentially and stored in 0.05% sodium azide in distilled water before needed.
36. Purification of 2ME binding protein (MBP): purification. Cytosolic and nucleic lysates were precleaned with protein A/G agarose (Santa Cruz Biotechnology). After centrifugation, lysates containing equal amounts of total protein were incubated with 2ME-linked Affigel-10 with and without a 1-fold and 5-fold excess of 2ME on rocking shaker for 30 min at 4 °C. Unbounded proteins were extensively washed with 50 mM Tris and bound proteins were eluted. After SDS-PAGE, the 2ME binding proteins were silver-stained and dried.