fgf receptors (FGFRs) - Cancer Science

Introduction to FGFRs

FGF receptors (FGFRs) are a family of receptor tyrosine kinases that play crucial roles in developmental processes and tissue homeostasis. Dysregulation of FGFR signaling is implicated in various cancers, making them significant targets for therapeutic interventions.

What are FGFRs?

FGFRs are transmembrane proteins that bind to fibroblast growth factors (FGFs) to initiate a signaling cascade. There are four main types of FGFRs: FGFR1, FGFR2, FGFR3, and FGFR4. Each receptor type can bind to different FGFs, leading to diverse biological outcomes.

How do FGFRs contribute to cancer?

Alterations in FGFRs such as mutations, amplifications, and fusions can result in uncontrolled cell proliferation, survival, and angiogenesis, contributing to cancer development and progression. For instance, FGFR1 amplification has been observed in breast cancer, while FGFR2 mutations are common in endometrial cancer.

What types of cancers are associated with FGFR alterations?

FGFR alterations have been identified in a variety of cancers, including but not limited to:

Breast cancer
Bladder cancer
Lung cancer
Gastric cancer
Multiple myeloma

What are the therapeutic strategies targeting FGFRs?

Therapeutic strategies targeting FGFRs include small molecule inhibitors, monoclonal antibodies, and ligand traps. Small molecule inhibitors like Erdafitinib and Pemigatinib have shown efficacy in treating cancers with FGFR alterations.

What are the challenges in targeting FGFRs?

Challenges in targeting FGFRs include the development of resistance to FGFR inhibitors, toxicity due to off-target effects, and the complexity of FGFR signaling pathways. Combination therapies and personalized medicine approaches are being explored to overcome these challenges.

Conclusion

FGFRs play a pivotal role in cancer biology, and targeting them offers promising therapeutic potential. Ongoing research and clinical trials continue to enhance our understanding and ability to effectively target FGFRs in various cancers.

Relevant Publications

Diverse Responses of Oligodendrocytes to Different FGF-Family Members: Uncoupling Structure-Function Relationship Within FGF Subfamilies.

Issue Release: 2024

Quantitative and qualitative differences in the activation of a fibroblast growth factor receptor by different FGF ligands.

Issue Release: 2024

STAT3 inhibitor Stattic Exhibits the Synergistic Effect with FGFRs Inhibitor Erdafitinib in FGFR1-positive Lung Squamous Cell Carcinoma.

Issue Release: 2024

Overcoming drug resistance of cancer cells by targeting the FGF1/FGFR1 axis with honokiol or FGF ligand trap.

Issue Release: 2024

Neuropeptides regulate embryonic salivary gland branching through the FGF/FGFR pathway in aging klotho-deficient mice.

Issue Release: 2024

The endocrine FGFs axis: A systemic anti-fibrotic response that could prevent pulmonary fibrogenesis?

Issue Release: 2024

Glycosylation of FGF/FGFR: An underrated sweet code regulating cellular signaling programs.

Issue Release: 2024

Exploring endocrine FGFs - structures, functions and biomedical applications.

Issue Release: 2024

Fgf17: A regulator of the mid/hind brain boundary in mammals.

Issue Release: 2024

The Caenorhabditis elegans protein SOC-3 permits an alternative mode of signal transduction by the EGL-15 FGF receptor.

Issue Release: 2024

Fibroblast Growth Factor Receptors and Ligands in Context of Bevacizumab Response in Ovarian Carcinoma: An Exploratory Analysis of AGO-OVAR 11/ICON-7.

Issue Release: 2023

[Fibroblast growth factor (FGF) endocrines and pulmonary fibrogenesis].

Issue Release: 2023

Short report galectins use N-glycans of FGFs to capture growth factors at the cell surface and fine-tune their signaling.

Issue Release: 2023

FGF2 drives osteosarcoma metastasis through activating FGFR1-4 receptor pathway-mediated ICAM-1 expression.

Issue Release: 2023

FGFR families: biological functions and therapeutic interventions in tumors.

Issue Release: 2023

The fibroblast growth factor-Klotho axis at molecular level.

Issue Release: 2023

Intracellular FGF1 promotes invasion and migration in thyroid carcinoma via HMGA1 independent of FGF receptors.

Issue Release: 2023

FGF homologous factors are secreted from cells to induce FGFR-mediated anti-apoptotic response.

Issue Release: 2023

The small molecule FGFR inhibitor infigratinib exerts anti-inflammatory effects and remyelination in a model of multiple sclerosis.

Issue Release: 2023

The FGF/FGFR system in the microglial neuroinflammation with Borrelia burgdorferi: likely intersectionality with other neurological conditions.

Issue Release: 2023

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