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Recent development of multi-target VEGFR-2 inhibitors for the cancer therapy.
Liu, Xiu-Juan; Zhao, Hong-Cheng; Hou, Su-Juan; Zhang, Hao-Jie; Cheng, Lei; Yuan, Shuo; Zhang, Li-Rong; Song, Jian; Zhang, Sai-Yang; Chen, Shi-Wu.
Afiliación
  • Liu XJ; School of Pharmacy, Lanzhou University, Lanzhou 730000, China.
  • Zhao HC; Hubei Key Laboratory of Tumor Microenvironment and Immunotherapy, Medical College of China Three Gorges University, Yichang 443003, China.
  • Hou SJ; School of Pharmacy, Lanzhou University, Lanzhou 730000, China.
  • Zhang HJ; School of Pharmacy, Lanzhou University, Lanzhou 730000, China.
  • Cheng L; School of Pharmacy, Lanzhou University, Lanzhou 730000, China.
  • Yuan S; Children's Hospital Affiliated to Zhengzhou University, Henan Children's Hospital, Zhengzhou Children's Hospital, Zhengzhou 450018, China.
  • Zhang LR; Department of Pharmacology, School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China.
  • Song J; Department of Pharmacology, School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China. Electronic address: mumuandzz@163.com.
  • Zhang SY; Department of Pharmacology, School of Basic Medical Sciences, Zhengzhou University, Zhengzhou 450001, China. Electronic address: saiyangz@zzu.edu.cn.
  • Chen SW; School of Pharmacy, Lanzhou University, Lanzhou 730000, China. Electronic address: chenshw@lzu.edu.cn.
Bioorg Chem ; 133: 106425, 2023 04.
Article en En | MEDLINE | ID: mdl-36801788
Vascular epidermal growth factor receptor-2 (VEGFR-2), as an important tyrosine transmembrane protein, plays an important role in regulating endothelial cell proliferation and migration, regulating angiogenesis and other biological functions. VEGFR-2 is aberrantly expressed in many malignant tumors, and it is also related to the occurrence, development, and growth of tumors and drug resistance. Currently, there are nine VEGFR-2 targeted inhibitors approved by US.FDA for clinical use as anticancer drugs. Due to the limited clinical efficacy and potential toxicity of VEGFR inhibitors, it is necessary to develop new strategies to improve the clinical efficacy of VEGFR inhibitors. The development of multitarget therapy, especially dual-target therapy, has become a hot research field of cancer therapy, which may provide an effective strategy with higher therapeutic efficacy, pharmacokinetic advantages and low toxicity. Many groups have reported that the therapeutic effects could be improved by simultaneously inhibiting VEGFR-2 and other targets, such as EGFR, c-Met, BRAF, HDAC, etc. Therefore, VEGFR-2 inhibitors with multi-targeting capabilities have been considered to be promising and effective anticancer agents for cancer therapy. In this work, we reviewed the structure and biological functions of VEGFR-2, and summarized the drug discovery strategies, and inhibitory activities of VEGFR-2 inhibitors with multi-targeting capabilities reported in recent years. This work might provide the reference for the development of VEGFR-2 inhibitors with multi-targeting capabilities as novel anticancer agents.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptor 2 de Factores de Crecimiento Endotelial Vascular / Neoplasias / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2023 Tipo del documento: Article País de afiliación: China Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Receptor 2 de Factores de Crecimiento Endotelial Vascular / Neoplasias / Antineoplásicos Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2023 Tipo del documento: Article País de afiliación: China Pais de publicación: Estados Unidos