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BIOMARKER:

FGFR1 expression

i
Other names: FGFR1, BFGFR, CD331, CEK, FLG, FLT2, H2, H3, H4, H5, KAL2, N-SAM, Fibroblast growth factor receptor 1
Entrez ID:
15d
MiR-2110 induced by chemically synthesized cinobufagin functions as a tumor-metastatic suppressor via targeting FGFR1 to reduce PTEN ubiquitination degradation in nasopharyngeal carcinoma. (PubMed, Environ Toxicol)
Finally, a clinical sample assay indicated that reduced miR-2110 was negatively correlated with NPC lymph node metastasis and positively related to NPC patient survival prognosis. In summary, miR-2110 is a metastatic suppressor involving in CB-induced suppression of NPC metastasis.
Journal • Metastases
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PTEN (Phosphatase and tensin homolog) • FGFR1 (Fibroblast growth factor receptor 1) • JUN (Jun proto-oncogene) • PI3K (Phosphoinositide 3-kinases) • NEDD4 (NEDD4 E3 Ubiquitin Protein Ligase)
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FGFR1 expression • miR-211 expression
19d
Benzimidazole-oxindole hybrids as multi-kinase inhibitors targeting melanoma. (PubMed, Bioorg Chem)
Encouraged by its efficacy, it was further investigated for its antitumor activity and mechanism of action, using sorafenib as a reference standard...It also downregulated Notch1 protein expression and decreased TGF-β1 production. Molecular docking simulations suggest that 8e binds as a promising type II kinase inhibitor in the target kinases interacting with the key regions in their kinase domain.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • NOTCH1 (Notch 1) • KDR (Kinase insert domain receptor) • TGFB1 (Transforming Growth Factor Beta 1)
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BRAF V600E • BRAF V600 • BRAF wild-type • FGFR1 expression • KDR expression • NOTCH1 expression
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sorafenib
22d
Prevalence of fibroblast growth factor receptor (FGFR) alterations (alts) and programmed death-ligand 1 (PD-L1) expression (exp) in Chinese solid tumor patients (pts) (AACR 2024)
BALVERSA (erdafitinib), a selective pan-FGFR kinase inhibitor, has shown clinical activity against FGFR altered solid tumors in pts who exhausted standard treatment options... The large Chinese solid tumor cohort analysis showed comparable FGFR alts prevalence between Chinese and Western population. Differences in relationship between FGFR alts and PD-L1 expression across tumor types reflect the differential role of predominant FGFR types in each tumor type.
Clinical • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor)
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PD-L1 expression • PD-L1 overexpression • FGFR1 amplification • FGFR1 expression
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PD-L1 IHC 22C3 pharmDx • MSK-IMPACT
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Balversa (erdafitinib)
1m
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 expression
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gemcitabine • albumin-bound paclitaxel
2ms
Dual-hit strategy for therapeutic targeting of pancreatic cancer in patient-derived xenograft tumors. (PubMed, Clin Cancer Res)
This dual-hit strategy of SMO and FGFR inhibition provides a clinically-translatable approach to compromise the profound impermeability of PDAC tumors. Furthermore, clinical deployment of DW-MR imaging could fulfill the essential clinical-translational requirement for patient stratification.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 expression
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Truseltiq (infigratinib)
2ms
circNINL facilitates aerobic glycolysis, proliferation, invasion, and migration in lung cancer by sponging miR-3918 to mediate FGFR1 expression. (PubMed, Eur J Med Res)
Further, in vivo experiments using nude mouse xenograft models underscored that silencing circNINL substantially curtailed tumor growth in LC. Collectively, these findings illuminate that circNINL exacerbates LC malignancy via the miR-3918/FGFR1 axis, a process integrally linked with the activation of aerobic glycolysis.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • MIR3918 (MicroRNA 3918)
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FGFR1 expression
3ms
Fibroblast Growth Factor Receptors and Ligands in Context of Bevacizumab Response in Ovarian Carcinoma: An Exploratory Analysis of AGO-OVAR 11/ICON-7. (PubMed, Lab Invest)
All patients received carboplatin and paclitaxel given every three weeks for six cycles and were randomized to bevacizumab. An FGFR/FGF-based gene signature identified in our study appears to predict long-term benefit from bevacizumab. This observation is hypothesis-generating and requires validation on independent cohorts.
Journal
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FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor) • FGF19 (Fibroblast growth factor 19) • FGFR4 (Fibroblast growth factor receptor 4) • PARP1 (Poly(ADP-Ribose) Polymerase 1)
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FGFR1 expression • FGF19 expression • FGFR2 expression
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Avastin (bevacizumab) • carboplatin • paclitaxel
4ms
CAV1 and KRT5 are potential targets for prostate cancer. (PubMed, Medicine (Baltimore))
CAV1 and KRT5 are highly expressed in prostate cancer. The higher expression of CAV1 and KRT5, the worse prognosis.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • CAV1 (Caveolin 1) • KRT5 (Keratin 5) • PRKCA (Protein Kinase C Alpha) • SNAI2 (Snail Family Transcriptional Repressor 2) • DLG4 (Discs Large MAGUK Scaffold Protein 4)
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FGFR1 expression • CAV1 expression
4ms
Targeting the fibroblast growth factor pathway in molecular subtypes of castration-resistant prostate cancer. (PubMed, Prostate)
Although FGFRi treatments suppressed tumor growth across CRPC phenotypes, our analyses did not identify a single pathway or biomarker that would identify tumor response to FGFRi. This is very likely due to the array of FGFR1-4 expression and tumor phenotypes present in CRPC. Nevertheless, our data nominate the FGFR pathway as a clinically actionable target that promotes tumor growth in diverse phenotypes of treatment-refractory metastatic CRPC.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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AR positive • MYC expression • AR amplification • FGFR1 expression
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enzalutamide capsule • Balversa (erdafitinib) • zoligratinib (Debio 1347)
4ms
FGF2 drives osteosarcoma metastasis through activating FGFR1-4 receptor pathway-mediated ICAM-1 expression. (PubMed, Biochem Pharmacol)
Moreover, the knockdown of endogenous FGF2 suppressed ICAM-1 expression and migration of osteosarcoma cells. These findings suggest that FGF2/FGFR1-4 signaling promotes metastasis via its direct downstream target gene ICAM-1, revealing a novel potential therapeutic target for osteosarcoma.
Journal
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FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1) • FGFR4 (Fibroblast growth factor receptor 4) • ICAM1 (Intercellular adhesion molecule 1) • FGF2 (Fibroblast Growth Factor 2) • JUN (Jun proto-oncogene)
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FGFR1 expression
4ms
Ex Vivo Drug Sensitivity Evaluation of a ZMYM2: : FGFR1 Fusion-Positive 8p11 Myeloproliferative Syndrome (EMS) Leukemia (ASH 2023)
Bortezomib and Axitinib exhibited high efficacy on the patient's sample...Other FGFR inhibitors, including Olverematinib, AZD4547, Axitinib, Cediranib, Dovitinib, and Lenvatinib, also demonstrated exquisite sensitivity. Despite extensive screening, no other single agents or drug combinations exhibited increased effectiveness in the ZMYM2: : FGFR1 transformed BaF3 cells except for Trametinib, a MEK inhibitor, and the combination of Belvarafenib (RAF inhibitor) and Gilteritinib (FLT3 inhibitor)... Ex vivo drug sensitivity assays demonstrated the highly selective efficacy of FGFR inhibitors in ZMYM2: : FGFR1 fusion-positive leukemia cells and a fusion-expressing BaF3 cell line. Mutations in the FGFR1 kinase domain (ZMYM2: : FGFR1 F1171L) could contribute to Ponatinib insensitivity. These ex vivo drug screening results provide further support for ongoing clinical trials which are investigating the use of single agent Pemigatinib and other FGFR1 inhibitors for the treatment of patients with FGFR1-fusion positive leukemias.
Preclinical
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FLT3 (Fms-related tyrosine kinase 3) • FGFR1 (Fibroblast growth factor receptor 1) • RUNX1 (RUNX Family Transcription Factor 1)
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RUNX1 mutation • FGFR fusion • FGFR1 fusion • FGFR1 expression • FGFR1 rearrangement
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Mekinist (trametinib) • Iclusig (ponatinib) • Lenvima (lenvatinib) • bortezomib • Xospata (gilteritinib) • Pemazyre (pemigatinib) • Inlyta (axitinib) • fexagratinib (ABSK091) • belvarafenib (RG6185) • Recentin (cediranib) • dovitinib (TKI258)
4ms
NF-κB downstream miR-1262 disturbs colon cancer cell malignant behaviors by targeting FGFR1. (PubMed, Acta Biochim Biophys Sin (Shanghai))
Conclusively, miR-1262 serves as an antitumor miRNA in colon cancer by targeting FGFR1. The NF-κB/miR-1262/FGFR1 axis modulates colon cancer cell phenotypes, including proliferation, invasion, and migration.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • MIR1262 (MicroRNA 1262)
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FGFR1 overexpression • FGFR1 expression
4ms
A novel intronic circular RNA circFGFR1 up-regulates FGFR1 by recruiting transcriptional activators P65/FUS and suppressing miR-4687-5p to promote prostate cancer progression. (PubMed, J Transl Med)
Overexpression of circFGFR1 is significantly correlated with higher tumor grade, Gleason score, and PSA level, and is a significant unfavorable prognosticator for CRPC-free survival (CFS) (RR = 3.277, 95% confidence interval: 1.192-9.009; P = 0.021). These findings unravelled novel mechanisms controlling FGFR1 gene expression by intronic circRNA and its potential clinicopathological utility as a diagnostic or therapeutic target.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • FUS (FUS RNA Binding Protein)
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FGFR1 amplification • FGFR1 overexpression • FGFR1 expression
4ms
Unraveling the Mechanisms of Sensitivity to Anti-FGF Therapies in Imatinib-Resistant Gastrointestinal Stromal Tumors (GIST) Lacking Secondary KIT Mutations. (PubMed, Cancers (Basel))
This resulted in activation of both AKT- and MAPK-signaling pathways shown on mRNA and protein levels, and rendered cancer cells highly sensitive to pan-FGFR-inhibitors (BGJ 398, AZD 4547, and TAS-120). Collectively, our data illustrates that continuous inhibition of KIT signaling in IM-resistant GISTs lacking secondary KIT mutations induced clonal heterogeneity of GISTs and resulted in accumulation of cancer cells with overexpressed FGF-2 and FGFR1/2, thereby leading to activation of FGFR-signaling. This in turn rendered these cells extremely sensitive to the pan-FGFR inhibitors used in combination with IM, or even alone, and suggests a rationale to re-evaluate the effectiveness of FGFR-inhibitors in order to improve the second-line therapeutic strategies for selected subgroups of GIST patients (e.g., IM-resistant GISTs lacking secondary KIT mutations and exhibiting the activation of the FGFR-signaling pathway).
Journal • Stroma
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FGFR2 (Fibroblast growth factor receptor 2) • KIT (KIT proto-oncogene, receptor tyrosine kinase) • FGFR1 (Fibroblast growth factor receptor 1) • CASP3 (Caspase 3) • FGF2 (Fibroblast Growth Factor 2) • FGF (Fibroblast Growth Factor) • FRS2 (Fibroblast Growth Factor Receptor Substrate 2)
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KIT mutation • FGFR1 expression • KIT expression
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imatinib • Truseltiq (infigratinib) • Lytgobi (futibatinib) • fexagratinib (ABSK091)
4ms
Efficacy of futibatinib, an irreversible fibroblast growth factor receptor inhibitor, in FGFR-altered breast cancer. (PubMed, Sci Rep)
Per institutional and public databases, FGFR2 mutations and amplifications had a population frequency of 1.1%-2.6% and 1.5%-2.5%, respectively, in breast cancer patients. FGFR2 alterations in breast cancer may represent infrequent but highly promising targets for futibatinib.
Journal
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FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3)
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FGFR2 mutation • FGFR2 amplification • FGFR2 overexpression • FGFR1 expression • FGFR2 expression • FGFR3 Y375C • FGFR2 Y375C
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Lytgobi (futibatinib)
4ms
FGFR1 expression correlates inversely with the efficacy of single-agent FGFR-specific inhibitors in pancreatic cancer. (PubMed, Br J Pharmacol)
Single-agent FGFRi's mediate selective, molecularly-targeted suppression of PDAC proliferation, and their effects are greatest in PDAC tumors expressing low- to-moderate FGFR1.
Journal
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FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 overexpression • FGFR1 expression
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gemcitabine • Truseltiq (infigratinib)
5ms
Phase classification • Combination therapy • Metastases
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FGFR1 expression
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Tecentriq (atezolizumab) • rogaratinib (BAY 1163877)
5ms
LncRNA VPS9D1-AS1 regulates miR-187-3p/fibroblast growth factor receptor-like 1 axis to promote proliferation, migration, and invasion of prostate cancer cells. (PubMed, Chin J Physiol)
Moreover, combined with the results of the rescue experiment, VPS9D1-AS1 was found to upregulate FGFRL1 by competitively sponging miR-187-3p to accelerate the malignant behaviors of prostate cancer cells. In conclusion, VPS9D1-AS1 could promote the phenotype progression of prostate cancer cells through targeting the miR-187-3p/FGFRL1 axis, and it has the potential to be a target for prostate cancer patients.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor) • FGFRL1 (Fibroblast Growth Factor Receptor Like 1) • MIR187 (MicroRNA 187)
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FGFR1 expression
5ms
Multi-kinase compensation rescues EGFR knockout in a cell line model of head and neck squamous cell carcinoma. (PubMed, Arch Oral Biol)
These data offer insights into EGFR inhibitor resistance and show that resistance to EGFR knockout likely occurs through a complex network of kinases. Future studies of cetuximab-resistant HNSCC tumors are warranted to determine if this EMT phenotype and/or multi-kinase resistance is observed in patients.
Preclinical • Journal
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EGFR (Epidermal growth factor receptor) • FGFR1 (Fibroblast growth factor receptor 1) • TWIST1 (Twist Family BHLH Transcription Factor 1) • XIAP (X-Linked Inhibitor Of Apoptosis) • ITK (IL2 Inducible T Cell Kinase) • SNAI1 (Snail Family Transcriptional Repressor 1) • ZEB1 (Zinc Finger E-box Binding Homeobox 1)
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FGFR1 expression • ZEB1 expression
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Erbitux (cetuximab)
5ms
The D647N mutation of FGFR1 induces ligand-independent receptor activation. (PubMed, Biochim Biophys Acta Gen Subj)
Remarkably, the D647N mutation significantly increases the sensitivity of FGFR1 to the ATP-competitive inhibitor Erdafitinib suggesting the possibility that this mutation could become a specific target for the development of new inhibitors. Although further efforts are warranted for an exhaustive description of the activation mechanisms, for the identification of more specific inhibitors and for confirming the clinical significance of mutated FGFR1, overall our data demonstrate that the D647N substitution of FGFR1 is a novel pro-oncogenic activating mutation of the receptor that, when found in cancer patients, may anticipate good response to erdafitinib treatment.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 mutation • FGFR1 expression
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Balversa (erdafitinib)
5ms
Receptor tyrosine kinase gene expression profiling of orbital rhabdomyosarcoma unveils MET as a potential biomarker and therapeutic target. (PubMed, Hum Cell)
Well-separated tumor clusters confirmed the association between MET gene and collective expression of RTK genes. Therefore, the therapeutic potential of multi-kinase inhibitors targeting MET and the 9 other significant RTKs needs to be explored.
Journal
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EGFR (Epidermal growth factor receptor) • MET (MET proto-oncogene, receptor tyrosine kinase) • FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • AXL (AXL Receptor Tyrosine Kinase) • KDR (Kinase insert domain receptor) • PDGFRB (Platelet Derived Growth Factor Receptor Beta) • FLT1 (Fms-related tyrosine kinase 1) • FLT4 (Fms-related tyrosine kinase 4) • IGF1 (Insulin-like growth factor 1) • IGF2 (Insulin-like growth factor 2) • FCGR2A (Fc fragment of IgG receptor IIa) • PDGFA (Platelet Derived Growth Factor Subunit A) • PDGFB (Platelet Derived Growth Factor Subunit B) • FCGR2B (Fc Fragment Of IgG Receptor IIb)
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MET overexpression • MET expression • AXL overexpression • FGFR1 expression • FLT1 expression • RET expression
5ms
Targeting fibroblast growth factor receptor (FGFR1) expression through G-quadruplex stabilization inhibits metastatic breast cancer (SABCS 2023)
Importantly, use of the G4-binding compound CX-5461 stabilized the FGFR1 G4 structure, blocked the transcriptional activity of the FGFR1 proximal promoter and decreased FGFR1 expression...In conclusion, consistent with the clinical observations our evaluation of FGFR kinase inhibitors validates the resistance to FGFR kinase inhibitors in MBC. Our findings indicate that targeting FGFR1 expression through G4 stabilization may be a potential strategy for MBC.
Metastases
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FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 amplification • FGFR1 expression
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pidnarulex (CX-5461)
5ms
Unravelling the role of FGFR1 in innate immune sensing and endocrine resistance in breast cancer (SABCS 2023)
Furthermore, we found that the inhibition of FGFR kinase enhances the expression of IFN-alpha, IFN-beta, TLR7, and TLR9 in T47D cells when stimulated with the TLR7 agonist loxoribine. These results strongly suggest that FGFR1 functions as an innate checkpoint and may be exploited by tumor cells to dampen Type 1 interferon responses, thereby inhibiting antitumor immunity in hormone receptor-positive breast cancer.
IO biomarker
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ER (Estrogen receptor) • FGFR1 (Fibroblast growth factor receptor 1) • TLR9 (Toll Like Receptor 9) • IFNA1 (Interferon Alpha 1)
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HR positive • FGFR1 amplification • FGFR1 expression
5ms
Somatic rearrangements causing oncogenic ectodomain deletions of FGFR1 in squamous cell lung cancer. (PubMed, J Clin Invest)
Thus, the genomic events shaping the architecture of the 8p11-p12 amplicon provide a mechanistic explanation for the emergence of FGFR1-driven squamous cell lung cancer. Specifically, FGFR1 ectodomain deficient and FGFR1-centered amplifications caused by tail-to-tail rearrangements are novel somatic genomic event, which might be predictive of therapeutically relevant FGFR1 dependency.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 amplification • FGFR1 expression
5ms
Molecular Analysis of Biliary Tract Cancers with the Custom 3' RACE-Based NGS Panel. (PubMed, Diagnostics (Basel))
Parallel analysis of 47 iCCA samples with the Illumina TruSight Tumor 170 kit confirmed good performance of our NGS panel. In conclusion, targeted RNA sequencing coupled with the 3' RACE technology is an efficient tool for the molecular diagnostics of BTCs.
Journal • PD(L)-1 Biomarker • IO biomarker • Next-generation sequencing
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HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • MET (MET proto-oncogene, receptor tyrosine kinase) • NRAS (Neuroblastoma RAS viral oncogene homolog) • MSI (Microsatellite instability) • FGFR2 (Fibroblast growth factor receptor 2) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • NTRK1 (Neurotrophic tyrosine kinase, receptor, type 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2) • NTRK3 (Neurotrophic tyrosine kinase, receptor, type 3) • FGFR1 (Fibroblast growth factor receptor 1) • NTRK2 (Neurotrophic tyrosine kinase, receptor, type 2)
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PD-L1 expression • BRAF V600E • KRAS mutation • HER-2 amplification • PIK3CA mutation • BRAF V600 • HER-2 mutation • HER-2 expression • MET exon 14 mutation • FGFR2 mutation • FGFR1 expression • PIK3CA expression
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TruSight Tumor 170 Assay
5ms
FGFR blockade inhibits targeted therapy-tolerant persister in basal FGFR1- and FGF2-high cancers with driver oncogenes. (PubMed, NPJ Precis Oncol)
We screened an anti-cancer compound library and identified fibroblast growth factor receptor 1 (FGFR1) promoting alectinib-induced anaplastic lymphoma kinase (ALK) fusion-positive DTP cell's survival...The combination of FGFR and targeted TKIs enhanced cell growth inhibition and apoptosis induction in basal FGFR1- and FGF2-high protein expressing cells with ALK-rearranged and epidermal growth factor receptor (EGFR)-mutated NSCLC, human epidermal growth factor receptor 2 (HER2)-amplified breast cancer, or v-raf murine sarcoma viral oncogene homolog B1 (BRAF)-mutated melanoma by preventing compensatory extracellular signal-regulated kinase (ERK) reactivation. These results suggest that a targeted TKI-induced DTP state results from an oncogenic switch from activated oncogenic driver signaling to the FGFR1 pathway in basal FGFR1- and FGF2-high expressing cancers and initial dual blockade of FGFR and driver oncogenes based on FGFR1 and FGF2 expression levels at baseline is a potent treatment strategy to prevent acquired drug resistance to targeted TKIs through DTP cells regardless of types of driver oncogenes.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • FGFR1 (Fibroblast growth factor receptor 1) • FGF2 (Fibroblast Growth Factor 2)
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EGFR mutation • BRAF mutation • HER-2 amplification • ALK positive • ALK rearrangement • ALK fusion • FGFR1 fusion • FGFR1 expression
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Alecensa (alectinib)
6ms
Exploiting the fibroblast growth factor receptor-1 vulnerability to therapeutically restrict the MYC-EZH2-CDKN1C axis-driven proliferation in Mantle cell lymphoma. (PubMed, Leukemia)
Further, pharmacological targeting with erdafitinib, a selective small molecule targeting FGFRs, induced cell-cycle arrest and cell death in-vitro, inhibited tumor progression, and improved overall survival in-vivo. We performed extensive pre-clinical assessments in multiple in-vivo model systems to confirm the therapeutic potential of erdafitinib in MCL and demonstrated FGFR1 as a viable therapeutic target in MCL.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • CDKN1C (Cyclin Dependent Kinase Inhibitor 1C)
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FGFR1 expression
|
Balversa (erdafitinib)
7ms
Spatial distribution and functional relevance of FGFR1 and FGFR2 expression for glioblastoma tumor invasion. (PubMed, Cancer Lett)
Comparative analysis of RNA-sequencing data of FGFR1 and FGFR2 knockdown glioblastoma cells revealed a FGFR1-specific gene regulatory network associated with tumor invasion. Our study reveals new gene candidates linked to FGFR1-mediated glioblastoma invasion.
Journal
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FGFR2 (Fibroblast growth factor receptor 2) • FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 expression • FGFR2 expression • FGFR2b expression
7ms
A novel FGFR1 inhibitor CYY292 suppresses tumor progression, invasion, and metastasis of glioblastoma by inhibiting the Akt/GSK3β/snail signaling axis. (PubMed, Genes Dis)
In vivo experiments revealed that CYY292 inhibited U87MG tumor growth more effectively than AZD4547. CYY292 also efficiently reduced GBM cell proliferation and increased survival in orthotopic GBM models. This study further elucidates the function of FGFR1 in the GBM and reveals the effect of CYY292, which targets FGFR1, on downstream signaling pathways directly reducing GBM cell growth, invasion, and metastasis and thus impairing the recruitment, activation, and function of immune cells.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
|
FGFR1 expression
|
fexagratinib (ABSK091)
8ms
FGFR1Pred: an artificial intelligence-based model for predicting fibroblast growth factor receptor 1 inhibitor. (PubMed, Mol Divers)
The developed inhibitor prediction model (FGFR1Pred) provides a valuable tool for identifying potential FGFR1 inhibitors, expediting the drug discovery process and ultimately facilitating the development of new therapeutics. The model is made available at https://github.com/PGlab-NIPER/FGFR1Pred.git.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 expression
8ms
FGF/FGFR1 system in paired breast tumor-adjacent and tumor tissues, associations with mammographic breast density and tumor characteristics. (PubMed, Front Oncol)
While no clear association between FGFR1 expression and MBD was found, FGF ligand (FGF1, FGF11, FGF18) expression was positively correlated with MBD. Taken together, these findings support a role of the FGF/FGFR1 system in early breast cancer which warrants further investigation in the MBD-breast cancer context.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • FGF18 (Fibroblast Growth Factor 18)
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FGFR1 amplification • FGFR1 expression
8ms
Fibroblast growth factor 3 promotes spontaneous mammary tumorigenesis in Tientsin albino 2 mice via the FGF3/FGFR1/STAT3 pathway. (PubMed, Front Oncol)
Inhibition of STAT3 or Akt phosphorylation promoted the expression of FGFR1. Validating the conclusions obtained in this study in human breast cancer (HBC) may contribute to targeted therapy and it is worth exploring whether the homologous sequences of MMTV in HBC have a similar oncogenic effect.
Preclinical • Journal
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FGFR1 (Fibroblast growth factor receptor 1) • FGF3 (Fibroblast growth factor 3)
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FGFR1 expression
8ms
THSD7A Positivity Predicts Poor Survival and Is Linked to High FAK Expression and FGFR1-Wildtype in Female Patients with Squamous Cell Carcinoma of the Lung. (PubMed, Int J Mol Sci)
To our knowledge, we are the first to report these correlations in lung cancer. The results might be proof of the assumed activation of FAK-dependent signaling pathways by THSD7A and that as a membrane-associated protein, THSD7A might serve as a putative therapeutic target in LSCC.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • PTK2 (Protein Tyrosine Kinase 2)
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FGFR1 expression • FGFR wild-type
10ms
Long noncoding RNA CCDC183-AS1 depletion represses breast cancer cell proliferation, colony formation, and motility by sponging microRNA-3918. (PubMed, Oncol Res)
In summary, CCDC183-AS1 deteriorates the malignancy of BC cells by controlling miR-3918/FGFR1 regulatory axis. We believe that our study can deepen our understanding of BC etiology and contribute to an improvement in treatment choices.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
|
FGFR1 overexpression • FGFR1 expression
10ms
ATF4 renders human T-cell acute lymphoblastic leukemia cell resistance to FGFR1 inhibitors through amino acid metabolic reprogramming. (PubMed, Acta Pharmacol Sin)
However, the T-ALL cells were resistant to FGFR1 inhibitors AZD4547 and PD-166866 even though FGFR1 signaling was specifically inhibited in the early stage...These results reveal that FGFR1 is a potential therapeutic target in human T-ALL, and ATF4-mediated amino acid metabolic reprogramming contributes to the FGFR1 inhibitor resistance. Synergistically inhibiting FGFR1 and mTOR can overcome this obstacle in T-ALL therapy.
Journal
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SLC1A5 (Solute Carrier Family 1 Member 5) • ASS1 (Argininosuccinate synthase 1) • ATF4 (Activating Transcription Factor 4) • PHGDH (Phosphoglycerate Dehydrogenase)
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FGFR1 expression
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fexagratinib (ABSK091)
10ms
Whole exome and transcriptome analysis revealed the activation of ERK and Akt signaling pathway in canine histiocytic sarcoma. (PubMed, Sci Rep)
The findings obtained in the present study indicated that ERK and Akt signaling were activated in canine HS and drugs targeting FGFR1 might be effective in part of the cases. The present study provides translational evidence that leads to establishment of novel therapeutic strategies targeting ERK and Akt signaling in HS patients.
Journal
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FGFR1 expression
11ms
F-labeled FGFR1 peptide: a new PET probe for subtype FGFR1 receptor imaging. (PubMed, Front Oncol)
Micro-PET/CT imaging revealed a significant concentration of [18F]F-FGFR1 in RT-112 xenografts with no or very low uptake in nontargeted organs and tissues, which demonstrated that [18F]F-FGFR1 was selectively taken up by FGFR1-positive tumors. [18F]F-FGFR1 showed high stability, affinity, specificity and good imaging capacity for FGFR1-overexpressing tumors in vivo, which provides new application potential in the visualization of FGFR1 expression in solid tumors.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
|
FGFR1 overexpression • FGFR1 expression
11ms
Expression and Purification of FGFR1-Fc Fusion Protein and Its Effects on Human Lung Squamous Carcinoma. (PubMed, Appl Biochem Biotechnol)
In addition, the FGFR1-Fc fusion protein significantly inhibited angiogenesis in an embryonic chorioallantoic membrane model. The FGFR1-Fc fusion protein may be an effective therapeutic candidate for LSCC.
Journal
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FGFR1 (Fibroblast growth factor receptor 1) • FGF2 (Fibroblast Growth Factor 2) • FRS2 (Fibroblast Growth Factor Receptor Substrate 2)
|
FGFR1 overexpression • FGFR1 fusion • FGFR1 expression
11ms
Molecular Pathology of Micropapillary Carcinomas: Is Characteristic Morphology Related to Molecular Mechanisms? (PubMed, Appl Immunohistochem Mol Morphol)
Prediction of prognosis and targeted therapy may benefit from the understanding of molecular mechanisms of micropapillary morphology. This review describes the molecular pathologic mechanisms underlying the micropapillary changes of cancers in various organs in a cell polarity-related dimension.
Journal
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • FGFR1 (Fibroblast growth factor receptor 1) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • CCND1 (Cyclin D1) • APC (APC Regulator Of WNT Signaling Pathway) • CDH1 (Cadherin 1) • RAC1 (Rac Family Small GTPase 1) • RHOA (Ras homolog family member A) • FOXO3 (Forkhead box O3) • JAG1 (Jagged Canonical Notch Ligand 1) • SNAI2 (Snail Family Transcriptional Repressor 2) • ZEB1 (Zinc Finger E-box Binding Homeobox 1) • DNAH9 (Dynein Axonemal Heavy Chain 9) • ITGA1 (Integrin Subunit Alpha 1) • ITGB1 (Integrin Subunit Beta 1) • OCLN (Occludin)
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TP53 mutation • BRAF mutation • PIK3CA mutation • HER-2 mutation • APC mutation • MYC expression • FGFR1 expression • TP53 expression
11ms
Presence of PD-1 similarity genes in monocytes may promote the development of type 1 diabetes mellitus and poor prognosis of pancreatic cancer. (PubMed, BMJ Open Diabetes Res Care)
Genes encoding immunoglobulin V-set domain similar to PD-1 may contribute to the occurrence of T1DM. Of these genes, MYOM3 and SPEG may serve as potential biomarkers for the prognosis of pancreatic cancer.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • FGFR1 (Fibroblast growth factor receptor 1) • PD-1 (Programmed cell death 1) • CD14 (CD14 Molecule) • HHLA2 (HERV-H LTR-Associating 2)
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FGFR1 overexpression • FGFR1 expression