Design of a fluorescent ligand targeting the S-adenosylmethionine binding site of the histone methyltransferase MLL1.

Luan, Yepeng; Blazer, Levi L; Hu, Hao; Hajian, Taraneh; Zhang, Jing; Wu, Hong; Houliston, Scott; Arrowsmith, Cheryl H; Vedadi, Masoud; Zheng, Yujun George

Luan, Yepeng; Blazer, Levi L; Hu, Hao; Hajian, Taraneh; Zhang, Jing; Wu, Hong; Houliston, Scott; Arrowsmith, Cheryl H; Vedadi, Masoud; Zheng, Yujun George.

Affiliation

Luan Y; Department of Pharmaceutical and Biomedical Sciences, University of Georgia, Athens, Georgia 30602, USA. yzheng@uga.edu.

Org Biomol Chem ; 14(2): 631-638, 2016 Jan 14.

Article in En | MEDLINE | ID: mdl-26541578

Subject(s)

Drug Design; Drug Evaluation, Preclinical/methods; Enzyme Inhibitors/pharmacology; Fluorescence; Histone-Lysine N-Methyltransferase/chemistry; Histone-Lysine N-Methyltransferase/metabolism; Myeloid-Lymphoid Leukemia Protein/chemistry; Myeloid-Lymphoid Leukemia Protein/metabolism; S-Adenosylmethionine/metabolism; Small Molecule Libraries/pharmacology; Binding, Competitive/drug effects; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical/economics; Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/chemistry; Humans; Ligands; Molecular Structure; Protein Structure, Tertiary; Small Molecule Libraries/chemical synthesis; Small Molecule Libraries/chemistry; Structure-Activity Relationship; Time Factors

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: S-Adenosylmethionine / Drug Design / Histone-Lysine N-Methyltransferase / Drug Evaluation, Preclinical / Enzyme Inhibitors / Myeloid-Lymphoid Leukemia Protein / Small Molecule Libraries / Fluorescence Type of study: Prognostic_studies Limits: Humans Language: En Journal: Org Biomol Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2016 Type: Article Affiliation country: United States

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