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FGFR1 is a receptor tyrosine kinase, which participates in many physiological and pathological processes via regulating various signaling pathways. Clinical research suggested that the activation of FGFR1 is associated with many diseases. For example, the hereditary mutations of the FGFR1 gene have an impact on congenital malformations of the musculoskeletal system. It is often seen that somatic mutations and epigenetic changes of the expression of FGFR1 gene in various types of cancer, such as lung, breast, hematological cancers, which is thought to contribute to progression of cancer.
Fibroblast growth factor receptor 1 (FGFR1) is also called as basic fibroblast growth factor receptor 1, fms-related tyrosine kinase-2 / Pfeiffer syndrome, and CD331. As a receptor tyrosine kinase, it is a member of the fibroblast growth factor receptor (FGFR) family. FGFR1 is encoded by the FGFR1 gene in human. FGFR family has 4 members, FGFR1, FGFR2, FGFR3, FGFR4, they are activated by duplication, fusion with other genes, and point mutation of cancers in human, therefore, FGFR genes are called as proto-oncogenes.
On the one hand, cellular responses are initiated by signaling pathways activated by the binding of FGFR1 to proper FGF. The signaling pathways including phospholipase C/PI3K/AKT, ras subfamily/ERK, protein kinase C, IP3-induced raising of cytosolic Ca2+, and Ca2+/calmodulin-activated elements and pathways. On the other hand, FGFR1 activated by FGF promotes the activation of sprout proteins, which in turn interact with GRB2, SOS1, and/or c-Raf to reduce or inhibit further cell stimulation by activated FGFR1.
There are 3 main ways for FGFR1 to achieve constitutive activation, gene amplification, translocation, and activating mutations. The activation of FGFR1 has been seen in melanomas, breast cancer, squamous cell carcinomas of the head, neck, and esophagus, subsequently, also been seen in a subset of glioblastoma multiforme and in a rhabdomyosarcoma. Clinical results indicated that the activation of FGFR1 was associated with various malignancies, the alteration of FGF receptor activity contributes to cancer development by regulating different processes.
In addition, FGFR1 promotes phosphorylation of transforming growth factor β-activating kinase 1, which enhances NF-κB signaling. Ablation of FGFR1 decreased inflammatory reaction in TRAMP tumors, while in another study, continuous activation of FGFR1 increased inflammation in FOCK1 mouse model. It has been proved that promoting inflammation in the tumor microenvironment is one way for FGFR1 to promote tumor activity.
Approved Drugs
Palifermin, regorafenib, nintedanib, ponatinib, sorafenib, lenvatinib, heparin, etc.
Drugs in Development
3-(3-methoxybenzyl)-1H-pyrrolo[2,3-b]pyridine, (E)-[4-(3,5-Difluorophenyl)-3H-pyrrolo[2,3-b]pyridin-3-ylidene](3-methoxyphenyl)methanol, XL999, etc.
Multiple Receptor Tyrosine Kinases Inhibitor
Lenvatinib, sorafenib etc.
Transient tissue edema, hypertension, gastrointestinal bleeding, idiosyncratic reactions, fatigue, neutropenia and neuropathy.
Hypertension, bleeding, thrombosis, hematological toxicity with febrile neutropenia, cardiovascular system, and liver relative issues
FGFR1 TestingCD BioSciences provides FGFR1 testing services by ELISA, Flow, IHC, ICC, IF, or WB assay. The results of FGFR1 testing are used to evaluate the activities of candidates against FGFR1 or targeted diseases. You can choose one or more testing ways to detect the level of FGFR1 according to your experiment.
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 finding of targeted compounds more successful and faster.
Antibody Drugs Development Services (show more)Antibody drugs exhibit many incomparable advantages, such as high specificity, affinity, and efficiency, which is an emerging direction on targeted drug development. CD BioSciences provides comprehensive services on FGFR1-targeted antibody drug development with professional technology, extensive experience, and advanced equipment.
Pharmacological Experiments (show more)We will create a specific experimental plan according to your requirements, including but not limited to
Disease Model Screening (show more)We will create specific disease models to accelerate your targeted drug discovery project, including but not limited to
CD BioSciences will establish the specific disease models according to your requirements to evaluate the inhibitory activity of your candidates targeted FGFR1. We have various cell lines and the species of our animal models cover rats, mice, rabbits, dogs, and non-human primates.
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