Antitumor activity and structure-activity relationship of heparanase inhibitors: Recent advances.
作者： Kaishuo Fu , Zhifeng Bai , Lanlan Chen , Wenchong Ye , Meizhu Wang
DOI: 10.1016/J.EJMECH.2020.112221
关键词: Tumor progression 、 Crosstalk (biology) 、 Heparan sulfate 、 Metastasis 、 Cancer research 、 Heparanase 、 Autophagy 、 Tumor microenvironment 、 Extracellular matrix 、 Chemistry
摘要: Heparanase (HPSE)-directed tumor progression plays a crucial role in mediating tumor-host crosstalk and priming the microenvironment, leading to growth, metastasis chemo-resistance. HPSE-mediated breakdown of structural heparan sulfate (HS) networks extracellular matrix (ECM) basement membranes (BM) directly facilitates growth metastasis. Lysosome HPSE also induces multi-drug resistance via enhanced autophagy. Therefore, inhibitors development has become an attractive topic block or eliminate drug resistance. In this review, we summarize applied experimentally clinically according interaction with binding sites participation factors. The antitumor activity structure-activity relationship (SAR) are emphasized.
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