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FGFR4-Targeted Drug Discovery Services

FGFRs are hot targets due to their function on cell survival, proliferation, migration, and angiogenesis, while most of these studies focus on FGFR1, FGFR2 and FGFR3. There is growing evidence suggested that FGFR4 plays an important and unique role in oncogenesis, tumor progression and anti-tumor therapy in many types of cancer. Abnormal expression of FGFR4, including, FGFR4 overexpression, FGF ligand overexpression, FGFR4 somatic hotspot mutations, and the FGFR4 G388R single nucleotide polymorphism, play different roles in development of cancer.

Whatever information you want about FGFR4 targeted drug discovery, you can find it here. For more details or related services, please feel free to contact us.

What is FGFR4?

What is FGFR4?

Fibroblast growth factor receptor 4 (FGFR4), also known as cluster of differentiation 334 (CD334), is one of a family of highly conserved tyrosine kinase receptors, which consists of a cellular ligand domain, a single transmembrane helixdomain, and a cytoplasmic domain with tyrosine kinase activity. FGFR4 is a protein encoded by the FGFR4 gene, which contains a unique amino acid in the kinase domain, the C552 residue.

FGFR4 is widely expressed in the embryonic stage, participating in tissue differentiation and organogenesis. After birth,the function of FGFR4 is restrained to actively growing tissue, including liver, lung and bone, to regulate bile acid production, metabolism, muscle differentiation, and tissue repair.

The structure of FGFR4
How FGFR4 Work?

How FGFR4 Work?

FGFR4 participates in the regulation of many signaling pathways. Canonical FGFR4 signaling pathways is dependent on FGF ligand binding, which causes tyrosine phosphorylation in the intracellular domain of FGFRs. A pro-growth and anti-apoptotic state are achieved through canonical FGFR4 activation. Besides, there are several non-canonical ways to activate FGFR4, thereby regulate cell proliferation, migration, morphological changes and even the invasion and metastasis of tumor cells.

How FGFR4 Work
How FGFR4 Work

FGFR4 is reportedly overexpressed in various cancers, such as breast, prostate, hepatocellular, ovarian, gastric, colorectal, and pancreatic cancer, where it may contribute to tumor progression. Inhibition of FGFR4 suppresses the aggressiveness of gastric, colorectal, and serous ovarian cancers that are high grade.

Direction of Drug Discovery Based on FGFR4

Direction of Drug Discovery Based on FGFR4

  • Preparation of Anti-FGFR4 Monoclonal Antibody
  • Protein Tyrosine Kinase Activity
  • 2-aminopyriminide Derivative
  • Binding to The C552 Residue
  • Developing New Clinical Effects on FGFR4 from Existing Drugs
The Drugs Targeting FGFR4

The Drugs Targeting FGFR4

Classification of Drug Status

Approved Drugs
Ponatinib, lenvatinib, heparin, erdafitinib, pemigatinib, etc.
Drugs in Development
FGF401, BLU-554, H3B-6527, NCT02325739, etc.

Classification of Mechanism of Action

Protein Tyrosine Kinase Activity
Ponatinib, lenvatinib, heparin, etc.
Compound Binding to The C552 Residue
FGF401, BLU-554, H3B-6527, NCT02325739, etc.
Anti-FGFR4 Monoclonal Antibody
U3–1784, LD1, etc.

The Most Common Side Effects

The Most Common Side Effects

Hypertension, rash, abdominal pain, fatigue, headache, dry skin, constipation, arthralgia, nausea, pyrexia, thrombocytopenia, anemia, neutropenia, lymphopenia, leukopenia, stomatitis, palmar-plantar erythrodysethesia syndrome and proteinuria.

Drug Combination

Drug Combination

Lenvatinib plus everolimus treats advanced renal cell carcinoma.

Drug Combination

What We Offer

FGFR4 Testing FGFR4 Testing

CD BioSciences provides FGFR4 testing services by Elisa, WB, IP, or IF assay. The results of FGFR4 testing are used to evaluate the activities of candidates against FGFR4 or targeted diseases. You can choose one or more testing ways to detect the level of FGFR4 according to your experiment.

Hit Identification Hit Identification (show more)

The goal of early drug discovery is to find novel lead compounds that have the desired potency, selectivity, and ADMET properties for pre-clinical evaluation.

CD BioSciences offers hit identification services to make your find targeted compounds more successful and faster.

  • High-Throughput Screening
  • FGFR4-Targeted in Silico Virtual Screening
  • Fragment-Based Drug Discovery
  • High-Content Screening

Antibody Drugs Development Services Antibody Drugs Development Services (show more)

Antibody drugs exhibit many incomparable advantages, such as the high specificity, affinity, and efficiency, which is an emerging direction on targeted drug development.

CD BioSciences provides comprehensive services on FGFR4-targeted antibody drugs development with professional technology, extensive experience, and advanced equipment.

  • Antibody Preparation Services
  • Phage Display Services
  • Antibody-Drug Conjugates
  • Antibody Humanization Services

Pharmacological Experiment Pharmacological Experiments (show more)

We will make a specific experimental plan according to your requirements, including but not limited to

  • Pharmacokinetics / Pharmacodynamics
  • Pharmacodynamics
  • Pharmacokinetics
  • Safety Pharmacology

Cancer Models Screening Cancer Models Screening (show more)

We will make specific disease models to accelerate your targeted drug discovery project, including but not limited to

  • Cancers—Breast cancer, prostate cancer, hepatocellular cancer, ovarian cancer, gastric cancer, colorectal cancer, and pancreatic cancer, etc.

CD BioSciences will establish the specific disease model according to your requirements to evaluate the inhibitory activity of your candidates targeted FGFR4. We have various cell lines and the species of our animal models cover rats, mice, rabbits, dogs, and non-human primates.

Inquire Us Inquire Us

References

  1. Levine, K.M.; et al. Fgfr4: A promising therapeutic target for breast cancer and other solid tumors. Pharmacol Ther. 2020, 214(p.107590.
  2. Xin, Z.; et al. Blocking fgfr4 exerts distinct anti-tumorigenic effects in esophageal squamous cell carcinoma. Thorac Cancer. 2018, 9(12): p.1687-1698.
  3. Sasaki, N.; et al. Fgfr4 inhibitor blu9931 attenuates pancreatic cancer cell proliferation and invasion while inducing senescence: Evidence for senolytic therapy potential in pancreatic cancer. Cancers (Basel). 2020, 12(10):
  4. Prieto-Dominguez, N.; et al. Making way for suppressing the fgf19/fgfr4 axis in cancer. Future Med Chem. 2018, 10(20): p.2457-2470.
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