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. 2021 Apr 22;11:650453. doi: 10.3389/fonc.2021.650453

Table 1.

Examples of potential therapeutic targets in the ECM of breast cancer.

Target Therapeutic agent Type Effects on breast cancer Ref.
HAS2, CD44 4-MU Small molecule inhibitor Inhibiting hyaluronic acid synthesis, regulating HAS2, CD44, matrix degrading enzymes, and inflammatory mediators (93)
Robo1 R5 Neutralizing antibody Significantly inhibited BC growth and metastasis MMTV-PyMT transgenic mouse model and xenografted breast cancer model (91)
EphA2 CD44 exon V10 DNA aptamers Significantly inhibited BC cell migration (92)
MMP-2 MMPIs Remodeling enzyme inhibitor Specifically inhibited MMP-2 and prevent breast tumor growth and associated bone destruction (94)
Heparanase 9E8, H1023 Monoclonal antibody Significantly inhibited cell invasion and tumor metastasis, no significant cytotoxicity to BC cells (95)
Zinc transporter LIV-1 SGM-LIV1A Blocking antibody SGN-LIV1A displays specific in vitro cytotoxic activity against LIV-1-expressing cancer cells; in vitro results are recapitulated in vivo with antitumor activity in animal models (96)
(VCP)/p97 NPD8733 Small molecule inhibitor NPD8733 silenced VCP expression in NIH3T3 fibroblasts and reduced the migration of the co-cultured NIH3T3 fibroblasts (97)
Src/FAK Lycorine Small molecule inhibitor Inhibited tumor growth in a breast cancer xenograft model and inhibited breast cancer metastasis in the MDA-MB-231 caudal vein model (98)
TAMs Endostatin Recombinant peptide Indicate the mouse breast cancer growth in vivo by regulating the polarization of tumor-associated macrophages (99)
Endostatin rh-Endostatin Recombinant peptide Chemotherapy combined with rh-endostatin is more effective than chemotherapy alone and is considered a promising breast cancer treatment strategy (100)

HAS2, Hyaluronan synthase 2; 4-MU: 4-methylumbelliferone; EphA2, Erythrogenic human hepatocytes A; MMP-2, matrix metalloproteinase-2; MMPIs, MMP inhibitors; VCP, valosin-containing protein; Src/FAK, Src-focal adhesion kinase; TAM, tumor-associated macrophage; BC, breast cancer.