scholarly journals Research Progress of Small Molecule VEGFR/c-Met Inhibitors as Anticancer Agents (2016–Present)

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2666 ◽  
Author(s):  
Qian Zhang ◽  
Pengwu Zheng ◽  
Wufu Zhu
Keyword(s):  
Growth Factor ◽  
Small Molecule ◽  
Anticancer Agents ◽  
Small Molecule Inhibitors ◽  
Growth Factor Receptor ◽  
New Drugs ◽  
Research Progress ◽  
Chemical Structures ◽  
High Affinity Receptor ◽  
Dual Target

Vascular endothelial growth factor receptor 2 (VEGFR-2) binds to VEGFR-A, VEGFR-C and VEGFR-D and participates in the formation of tumor blood vessels, mediates the proliferation of endothelial cells, enhances microvascular permeability, and blocks apoptosis. Blocking or downregulating the signal transduction of VEGFR is the main way to discover new drugs for many human angiogenesis-dependent malignancies. Mesenchymal epithelial transfer factor tyrosine kinase (c-Met) is a high affinity receptor for hepatocyte growth factor (HGF). Abnormal c-Met signaling plays an important role in the formation, invasion and metastasis of human tumors. Therefore, the HGF/c-Met signaling pathway has become a significant target for cancer treatment. Related studies have shown that the conduction of the VEGFR and c-Met signaling pathways has a synergistic effect in inducing angiogenesis and inhibiting tumor growth. In recent years, multi-target small molecule inhibitors have become a research hotspot, among which the research of VEGFR and c-Met dual-target small molecule inhibitors has become more and more extensive. In this review, we comprehensively summarize the chemical structures and biological characteristics of novel VEGFR/c-Met dual-target small-molecule inhibitors in the past five years.

scholarly journals The same site on the integrase-binding domain of lens epithelium–derived growth factor is a therapeutic target for MLL leukemia and HIV

Blood ◽  
2014 ◽  
Vol 124 (25) ◽  
pp. 3730-3737 ◽  
Author(s):  
Marcelo J. Murai ◽  
Jonathan Pollock ◽  
Shihan He ◽  
Hongzhi Miao ◽  
Trupta Purohit ◽  
...  
Keyword(s):  
Growth Factor ◽  
Small Molecule ◽  
Therapeutic Target ◽  
Small Molecule Inhibitors ◽  
Binding Domain ◽  
Lens Epithelium ◽  
New Drugs ◽  
Structural Studies ◽  
Key Points

Key Points Inhibiting LEDGF interaction with a novel fragment of MLL represents an attractive approach to develop new drugs for MLL leukemias. Structural studies reveal a new pocket on the LEDGF IBD suitable for targeting by small-molecule inhibitors.

Monoclonal antibodies, small molecule inhibitors and antibody-drug conjugates as HER2 inhibitors

2020 ◽  
Vol 27 ◽  
Author(s):  
Xiu-Fang Li ◽  
Chen-Fu Liu ◽  
Guo-Wu Rao
Keyword(s):  
Monoclonal Antibodies ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Growth Factor Receptor ◽  
Research Progress ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Her 2 ◽  
Epidermal Growth ◽  
Antibody Drug

: Overexpression of human epidermal growth factor receptor (HER)-2 is found in a variety of cancers, often portending poor clinical outcomes. Therefore, HER2 is an attractive target for treatment. This review describes the research progress of HER2 targeted inhibitors in recent years. Excellent reviews are available, so we focus on the development, mechanisms of action, and structure-activity relationships of different types of inhibitors, including monoclonal antibodies, small molecule inhibitors, and antibody-drug conjugates (ADCs). In addition, the differences among them are compared.

Sign in / Sign up

Export Citation Format

Share Document