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. 2023 Mar 24;12(7):1002. doi: 10.3390/cells12071002

Table 1.

The table summarizes all the bFGF/FGFR axis targeting therapies described in this review.

Cancer Type First Author Title Therapeutic Treatment References
Brain Meric-Bernstam et al.
(2022)
“Futibatinib, an Irreversible FGFR1–4 Inhibitor, in Patients with Advanced Solid Tumors Harboring FGF/FGFR Aberrations: A Phase I Dose-Expansion Study.” Fisogatinib and Futibatinib could be two effective and safe compounds capable of improving the CNS neoplastic conditions. [74]
Khabibov et al. (2022) “Signaling pathways and therapeutic approaches in glioblastoma multiforme.” [75]
Esophageal Shi et al. (2016) “FGF2 regulates proliferation, migration, and invasion of ECA109 cells through PI3K/Akt signalling pathway in vitro.” LY294002, a PI3K inhibitor, as a therapeutic strategy for alleviating the tumorigenic effects of bFGF. [77]
Gastrointestinal Fan et al. (2015) “A peptide derivative serves as a fibroblast growth factor 2 antagonist in human gastric cancer.” P29 and P32 suppressed the bFGF-induced proliferation of GC cells and inhibited the activation of AKT and Erk1/2 cascades. [85]
Li et al. (2016) “Peptidomimetic suppresses proliferation and invasion of gastric cancer cells by fibroblast growth factor 2 signaling cascade blockage.” [86]
Gao et al. (2022) “miRNA-381-3p Functions as a Tumor Suppressor to Inhibit Gastric Cancer by Targeting Fibroblast Growth Factor Receptor-2.” MiR-381-3p and miR-195 target bFGF, decreasing tumorigenesis of GC. [87]
Wang et al. (2020) “MicroRNA-195 inhibits human gastric cancer by directly targeting basic fibroblast growth factor.” [88]
Guo et al. (2012) “Toxicarioside A inhibits SGC-7901 proliferation, migration and invasion via NF-kappaB/bFGF signaling.” Toxicarioside A reduced cell viability, cell growth, cell migration, and invasion in SGC-7901 GC cells by NF-κB/bFGF/FGFR1 signaling. [89]
Zhu et. al. (2017) “Catalpol suppressed proliferation, growth and invasion of CT26 colon cancer by inhibiting inflammation and tumor angiogenesis.” Catalpol blocked cell proliferation, growth, and invasion of CT26 lines. [97]
Zhou et al. (2021) “Oridonin inhibits tumor angiogenesis and induces vessel normalization in experimental colon cancer.” Oridonin controlled JAK2/STAT3 signaling and angiogenesis-related factors, including bFGF. [98]
CRC Sudha et al. (2021) “Pomegranate (Punica granatum) Fruit Extract Suppresses Cancer Progression and Tumor Angiogenesis of Pancreatic and Colon Cancer in Chick Chorioallantoic Membrane Model.” Morin and pomegranate, respectively, decreased bFGF levels in vivo and in colo205 cell lines. [99]
Sharma et al. (2020) “Morin supplementation modulates PERK branch of UPR and mitigates 1,2-dimethylhydrazine-induced angiogenesis and oxidative stress in the colon of experimental rats.” [100]
Liver Wei et al.
(2017)
“Plumbagin restrains hepatocellular carcinoma angiogenesis by suppressing the migration and invasion of tumor-derived vascular endothelial cells.” Plumbagin suppresses angiogenesis pathways such as PI3K-Akt, VEGF/KDR, and Angiopoietins/Tie2, as well as angiogenic factors such as bFGF. [110]
Liu et al.
(2020)
“Sorafenib combined with transarterial chemoembolization prolongs survival of patients with advanced hepatocellular carcinoma.” Sorafenib-treated HCC patients evidently revealed lower levels of VEGF, bFGF, and AFP in serum. [111]
Tong et al. (2021) “The effect of TACE in combination with thalidomide-mediated adjuvant therapy on the levels of VEGF and bFGF in patients with hepatocellular carcinoma.” Combined therapies of TACE with thalidomide downregulated VEGF and bFGF levels. [114]
Pancreatic Li et al.
(2016)
“Celecoxib suppresses fibroblast growth factor-2 expression in pancreatic ductal adenocarcinoma PANC-1 cells.” Quercetin-3-O-glucoside and Celecoxib acted as bFGF inhibitors, avoiding the expansion of local metastasis. [119]
Lee et al.
(2016)
“Quercetin-3-O-glucoside suppresses pancreatic cancer cell migration induced by tumor-deteriorated growth factors in vitro.” [120]
Oral cavity Khandelwal et al. (2018) “Local and systemic Curcumin C3 complex inhibits 4NQO-induced oral tumorigenesis via modulating FGF-2/FGFR-2 activation.” Curcumin inhibited 4NQO-induced tumorigenesis via modulation of the bFGF/FGFR-2 axis. [131]
Aytatli et al. (2022) “AZD4547 targets the FGFR/Akt/SOX2 axis to overcome paclitaxel resistance in head and neck cancer.” AZD4547 targeted the FGFR/Akt/SOX2 axis to overcome paclitaxel resistance in HNSCC. [132]
Lung Yang et al.
(2017)
“Production of bFGF monoclonal antibody and its inhibition of metastasis in Lewis lung carcinoma.” mAb-E12 inhibited CLL metastasis spreading. [134]
Kidney Zhang et al. (2018) “MiR-148b-3p inhibits renal carcinoma cell growth and pro-angiogenic phenotype of endothelial cell potentially by modulating FGF2.” miR-148b-3p stimulated renal carcinoma cell apoptosis and migration growth via the FGF2-FGFR2 pathway. [144]
Xu et al.
(2015)
“miR-203 inhibition of renal cancer cell proliferation, migration and invasion by targeting of FGF2.” miR-203 targeted bFGF, limiting renal cancer cell growth and metastases. [145]
Bone Tsubaki et al.
(2011)
“Blockade of the Ras/MEK/ERK and Ras/PI3K/Akt pathways by statins reduces the expression of bFGF, HGF, and TGF-beta as angiogenic factors in mouse osteosarcoma.” Inhibition of growth factors such as bFGF, HGF, and TGF- β with Statins. [154]
Thyroid Xu et al. (2017) “miR-27b-3p is Involved in Doxorubicin Resistance of Human Anaplastic Thyroid Cancer Cells via Targeting Peroxisome Proliferator-Activated Receptor Gamma.” miR-195 overexpression limited bFGF and, consequently, the proliferation, migration, and invasion of PTC cell lines. [159]
Wu et al. (2019) “Peptide P11 suppresses the growth of human thyroid carcinoma by inhibiting the PI3K/AKT/mTOR signaling pathway.” P11 peptide inhibited the PI3K/Akt/mTOR signaling pathway.
Bladder Chen et al. (2016) “FGF2-mediated reciprocal tumor cell-endothelial cell interplay contributes to the growth of chemoresistant cells: a potential mechanism for superficial bladder cancer recurrence.” Evaluation of the antagonism against bFGF using the neutralizing antibody, which, however, did not affect the growth of 253J/DOX cells. [167]
Prostate Hotchkiss et al. (2002) “Inhibition of endothelial cell function in vitro and angiogenesis in vivo by docetaxel (Taxotere): association with impaired repositioning of the microtubule organizing center.” Taxane and Docetaxel effectively downregulated bFGF expression. [191]
Cenni et al. (2007) “Inhibition of angiogenesis via FGF-2 blockage in primitive and bone metastatic renal cell carcinoma.” Antisense bFGF oligonucleotide blocked the production of FGF by both tumor and endothelial cells. [194]
Breast Shee et al. (2018) “Therapeutically targeting tumor microenvironment-mediated drug resistance in estrogen receptor-positive breast cancer.” PD170374 inhibiting bFGF stopped ECM/FGF-mediated regulation of ER breast cancer. [203]
Ovarian Wang et al. (2021) “Cancer-associated fibroblasts secrete FGF-1 to promote ovarian proliferation, migration, and invasion through the activation of FGF-1/FGFR4 signaling.” PD173074 terminated cellular proliferation, migration, and invasion. [209]