Identification of a Potent Inhibitor of CREB-Mediated Gene Transcription with Efficacious in Vivo Anticancer Activity

• Published in: Journal of medicinal chemistry Vol. 58; no. 12; pp. 5075 - 5087
• Main Authors: Xie, Fuchun, Li, Bingbing X, Kassenbrock, Alina, Xue, Changhui, Wang, Xiaoyan, Qian, David Z, Sears, Rosalie C, Xiao, Xiangshu
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 25.06.2015; Amer Chemical Soc
• Subjects: Animals; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antineoplastic Agents - therapeutic use; Breast - drug effects; Breast - metabolism; Breast - pathology; Breast Neoplasms - drug therapy; Breast Neoplasms - genetics; Breast Neoplasms - metabolism; Breast Neoplasms - pathology; Cell Line, Tumor; Cell Proliferation - drug effects; Chemistry, Medicinal; Cyclic AMP Response Element-Binding Protein - antagonists & inhibitors; Cyclic AMP Response Element-Binding Protein - metabolism; Female; Gene Expression Regulation, Neoplastic - drug effects; HEK293 Cells; Humans; Life Sciences & Biomedicine; Mice, Inbred BALB C; Mice, Nude; Naphthalenes - chemistry; Naphthalenes - pharmacology; Naphthalenes - therapeutic use; Pharmacology & Pharmacy; Science & Technology; Transcriptional Activation - drug effects; NAPHTHOL AS-E; DESIGN; ACTIVATOR; ELEMENT-BINDING-PROTEIN; BIOLOGICAL EVALUATION; CANCER; EXPRESSION; PROMOTES; DISCOVERY; FAMILY

Recent studies have shown that nuclear transcription factor cyclic adenosine monophosphate response element binding protein (CREB) is overexpressed in many different types of cancers. Therefore, CREB has been pursued as a novel cancer therapeutic target. Naphthol AS-E and its closely related derivat...