Truncated FGFR is a clinically actionable oncogene in
Aug · Truncation of exon of FGFR (FGFRΔE) is a potent driver mutation in mice and humans and FGFR-targeted therapy should be considered for patients with cancer expressing stable FGFRΔE
FGFR Destabilizes PD-L via NEDD to Control T …
Jan · Bladder cancer is one of the most prevalent cancers with nearly new cases and deaths annually on a global scale () The relative -year overall survival rate of advanced-stage unresectable or metastatic urothelial carcinoma (UC) of the bladder is low () Using historical treatment with second-line chemotherapy the response rate is …
FGFR Inhibitors in Oncology Insight on the Management …
Jun · Abstract Fibroblast Growth Factor receptor (FGFR) pathway aberrations have been implicated in approximately of the malignancies As our knowledge of FGFR aberrations in cancer continues to evolve FGFR inhibitors emerged as potential targeted therapeutic agents The promising results of pemigatinib and infigratinib in advanced …
Signaling Pathway and Small-Molecule Drug …
Targeted therapy is a groundbreaking innovation for cancer treatment Among the receptor tyrosine kinases the fibroblast growth factor receptors (FGFRs) garnered substantial attention as promising therapeutic targets …
INCB (pemigatinib) a potent and selective inhibitor …
Introduction Deregulation of receptor tyrosine kinase (RTK) signaling has the potential to promote the acquisition of several hallmarks of cancer cells notably self-sustaining …
Fibroblast growth factor receptor fusions in cancer …
Nov · Abstract Fibroblast growth factors (FGFs) and their receptors (FGFRs) play critical roles in many biological processes and developmental functions Chromosomal translocation of FGFRs result in the formation of chimeric FGFR fusion proteins which often cause aberrant signaling leading to the development and progression of human cancer
Full article Futibatinib an investigational agent for the …
Introduction Biliary tract cancers (BTCs) including intrahepatic cholangiocarcinoma (iCCA) extrahepatic cholangiocarcinoma (eCCA) gallbladder cancer (GBC) and ampulla of Vater cancer (AVC) represent the most commonly diagnosed primary biliary malignancy accounting for approximately of all gastrointestinal cancers Citation Citation
FGF FGFR signaling in health and disease - Nature
Sep · FGF signaling plays critical roles in tissue organ development and homeostasis and dysregulated FGF signaling has been found in a variety of diseases and injuries (see above) It is a promising
Comprehensive functional evaluation of variants of …
Jul · Various genetic alterations of the fibroblast growth factor receptor (FGFR) family have been detected across a wide range of cancers However inhibition of FGFR signaling by kinase inhibitors
Preclinical Activity of ARQ a Novel Inhibitor Targeting …
Sep · Taken together these data suggest that ARQ inhibits the proliferation of FGFR amplified cells by inducing G cell cycle arrest and apoptosis ARQ arrests cells in the G cell cycle phase and induces apoptosis (A) NCI-H and SNU- cells were treated with μM of ARQ or vehicle for hours
Inhibition of fibroblast growth factor receptor attenuates
Jun · Pancreatic ductal adenocarcinoma (PDAC) is an aggressive human malignancy with an overall -year survival rate of At the molecular level a high percentage of PDACs overexpress a number of growth factors and their receptors including the epidermal growth factor epidermal growth factor receptor transforming growth factor …
Fibroblast growth factor receptors in cancer genetic - Nature
Fibroblast growth factor receptors (FGFRs) are aberrantly activated through single-nucleotide variants gene fusions and copy number amplifications in of all human …
Futibatinib Is a Novel Irreversible FGFR Inhibitor That …
Nov · The FGF FGFR signaling axis is involved in many cellular processes that include proliferation differentiation migration and survival () Deregulated FGFR signaling is associated with developmental disorders and several cancers () FGFR genomic aberrations such as gene amplifications fusions rearrangements activating mutations and altered …
Co-dependency for MET and FGFR in basal triple-negative …
Mar · Triple-negative breast cancer (TNBC) is a heterogeneous disease that lacks both effective patient stratification and therapeutic targets and where strategies to target TICs are still poorly
In vitro and in vivo evaluation of the radiosensitizing effect …
Background We examined the anti-tumor effect and radiosensitizing potential of a small molecule inhibitor of fibroblast growth factor receptor (FGFR) in colorectal cancer (CRC) …
Fibroblast Growth Factor Receptors (FGFRs) Structures …
Jun · Abstract Fibroblast growth factor receptors (FGFRs) are a family of receptor tyrosine kinases expressed on the cell membrane that play crucial roles in both developmental and adult cells Dysregulation of FGFRs has been implicated in a wide variety of cancers such as urothelial carcinoma hepatocellular carcinoma ovarian …
Signaling Pathway and Small-Molecule Drug Discovery of …
Targeted therapy is a groundbreaking innovation for cancer treatment Among the receptor tyrosine kinases the fibroblast growth factor receptors (FGFRs) garnered substantial attention as promising therapeutic targets due to their fundamental biological functions and frequently observed abnormality in tumors In the past decades several generations of …
Unleashing the potential of combining FGFR inhibitor and …
Mar · Conclusion Here we review the role of FGF FGFR signaling in TME regulation and the potential mechanisms of FGFR-TKI in combination with ICB In addition we review clinical data surrounding ICB alone or in combination with FGFR-TKI for the treatment of FGFR-dysregulated tumors highlighting that FGFR inhibitors may sensitize …
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Fibroblast Growth Factor Receptor (FGFR) Inhibitors in …
Sep · The structure of FGFR is composed of three distinct domains an extracellular domain a single‐pass transmembrane domain and an intracellular tyrosine kinase domain The extracellular domain contains the FGF‐binding site and has three immunoglobulin (Ig)‐like domains designated D D (D D forms the ligand‐binding …
Characteristics of three human gastric cancer cell lines NU …
Electron microscopy revealed epithelial characteristics in all cell lines The average doubling time of NU-GC- was hours that of NU-GC- was hours and that of …
Negative Regulation of FGFR (Fibroblast Growth Factor …
May · FGFR (fibroblast growth factor receptor) signaling controls fundamental processes in embryonic fetal and adult human life The magnitude duration and location of FGFR signaling must be strictly controlled in order to induce the correct biological response
Inhibition of the FGF FGFR System Induces Apoptosis in …
Dec · Introduction Lung tumors are the leading cause of cancer-related mortality worldwide making up almost of all cancer deaths and giving rise to more than million deaths annually () Non-small-cell lung cancer (NSCLC) accounts for of cases and is divided roughly equally into two main histological types adenocarcinomas …
Targeting of FGF-Signaling Re-Sensitizes Gastrointestinal Stromal
Oct · Dysregulation of the fibroblast growth factor (FGF) fibroblast growth factor receptor (FGFR) signaling pathway is frequently observed in multiple human malignancies and thus therapeutic strategies targeting FGFs and FGFRs in human cancer are being extensively explored We observed the activation o …
Fibroblast growth factor receptors as treatment targets in …
Oct · FGFRs are receptor tyrosine kinases with a role in several biological processes such as the regulation of development and tissue repair However alterations in FGFRs such as
- Gene ResultFGFR fibroblast growth factor receptor …
The protein encoded by this gene is a member of the fibroblast growth factor receptor (FGFR) family where amino acid sequence is highly conserved between members and throughout evolution FGFR family members differ from one another in their ligand affinities and tissue distribution A full-length representative protein consists of an extracellular …
Some typical staining results a) FGFR staining in NU
A panel of markers selected for the suspected bladder cancer relevance of their corresponding genes were explored for their expression and subcellular location in urinary bladder tissue
What is FGFR BALVERSA (erdafitinib)
FGFR stands for fibroblast growth factor receptor FGFR helps cells grow survive and multiply In certain types of cancer like in some cases of bladder cancer the gene that controls FGFR can change or mutate (known as an FGFR alteration) The FGFR alteration may cause cancer cells to develop leading to growth and spread
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FGFR-TKI resistance in cancer current status and perspectives
Feb · Fibroblast growth factor receptors (FGFRs) play key roles in promoting the proliferation differentiation and migration of cancer cell Inactivation of FGFRs by tyrosine kinase inhibitors (TKI) has achieved great success in tumor-targeted therapy However resistance to FGFR-TKI has become a concern Here we review the mechanisms of …
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F-FDG PET as an imaging biomarker for the response to …
Rationale The overall clinical response to FGFR inhibitor (FGFRi) is far from satisfactory in cancer patients stratified by FGFR aberration the current biomarker in clinical practice A …
RAS-MAPK reactivation facilitates acquired resistance in
The Fibroblast Growth Factor Receptor (FGFR) kinases are promising therapeutic targets in multiple cancer types including lung and head and neck squamous cell carcinoma cholangiocarcinoma and bladder cancer Although several FGFR kinase inhibitors have
Fibroblast growth factor receptor fusions in cancer …
Nov · Fibroblast growth factors (FGFs) and their receptors (FGFRs) play critical roles in many biological processes and developmental functions Chromosomal translocation of FGFRs result in the formation of chimeric FGFR fusion proteins which often cause aberrant signaling leading to the development and progression of human cancer Due to …
mTOR inhibition improves fibroblast growth factor receptor …
Feb · Systemic therapy has proven only marginal effects in hepatocellular carcinoma (HCC) so far The aim of this study was to evaluate the effect of targeting fibroblast growth factor receptor (FGFR
INCB (pemigatinib) a potent and selective inhibitor …
Apr · Alterations in fibroblast growth factor receptor (FGFR) genes have been identified as potential driver oncogenes Pharmacological targeting of FGFRs may therefore provide therapeutic benefit to selected cancer patients and proof-of-concept has been established in early clinical trials of FGFR inhibitors Here we present the molecular …