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Identification of fenoldopam as a novel LSD1 inhibitor to abrogate the proliferation of renal cell carcinoma using drug repurposing strategy.
Zheng, Yan; Ma, Yuan; Cao, Huixia; Yan, Lei; Gu, Yue; Ren, Xuejing; Jiao, Xiaojing; Wan, Shengfeng; Shao, Fengmin.
Afiliação
  • Zheng Y; Key Laboratory of Immunization of Kidney Disease, People's Hospital of Henan Province, China.
  • Ma Y; Institute of Clinical Medicine, Urodynamic Center and Department of Urology, The First Affiliated Hospital of Zhengzhou University, China.
  • Cao H; Key Laboratory of Immunization of Kidney Disease, People's Hospital of Henan Province, China.
  • Yan L; Key Laboratory of Immunization of Kidney Disease, People's Hospital of Henan Province, China.
  • Gu Y; Key Laboratory of Immunization of Kidney Disease, People's Hospital of Henan Province, China.
  • Ren X; Key Laboratory of Immunization of Kidney Disease, People's Hospital of Henan Province, China.
  • Jiao X; Key Laboratory of Immunization of Kidney Disease, People's Hospital of Henan Province, China.
  • Wan S; Key Laboratory of Immunization of Kidney Disease, People's Hospital of Henan Province, China.
  • Shao F; Key Laboratory of Immunization of Kidney Disease, People's Hospital of Henan Province, Zhengzhou University, China. Electronic address: fengminshao01@163.com.
Bioorg Chem ; : 104561, 2020 Dec 16.
Artigo em Inglês | MEDLINE | ID: mdl-33349457
ABSTRACT
Although targeted therapy for renal cell carcinoma (RCC) has achieved good therapeutic effects in clinic, a considerable number of patients develop drug resistance over time. So, there is still an urgent need to develop new drugs for RCC treatment. As LSD1 is considered as a promising drug target in diverse cancers, including RCC, we tried to find new LSD1 inhibitor using drug repurposing strategy from a compound library, and fenoldopam, an FDA-approved drug, was identified as a potent LSD1 inhibitor with IC50 = 0.8974 µM in a reversible manner. Molecular docking predicted that fenoldopam occupied the FAD cavity of LSD1, forming hydrogen bonds with surrounding residues. Moreover, fenoldopam inactivated LSD1 and performed antiproliferative activity against ACHN cells and promoted cells apoptosis in vitro. Taken together, fenoldopam was identified as a novel LSD1 inhibitor firstly, and may serve as a new skeleton for RCC therapy.
Texto completo: Disponível Coleções: Bases de dados internacionais Base de dados: MEDLINE Tipo de estudo: Estudo diagnóstico Idioma: Inglês Revista: Bioorg Chem Ano de publicação: 2020 Tipo de documento: Artigo País de afiliação: China

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Texto completo: Disponível Coleções: Bases de dados internacionais Base de dados: MEDLINE Tipo de estudo: Estudo diagnóstico Idioma: Inglês Revista: Bioorg Chem Ano de publicação: 2020 Tipo de documento: Artigo País de afiliação: China