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Derazantinib (formerly ARQ 087) is an investigational orally administered small molecule panFGFR kinase inhibitor with strong activity against FGFR1, 2, and 3.
On the left is the FGFR1 gene in its natural state.
By selectively inhibiting FGFR1, 2 and 3, and blocking those signals, E7090 has the potential to become a new molecular targeted therapy for cancers with FGFR genetic aberrations.
Recurrent somatic alterations of FGFR1 and NTRK2 in pilocytic astrocytoma.
However, the underlying molecular mechanism of miR-497 in gastric cancer progression by targeting FGFR1 is rarely investigated.
The FGFR1 gene on chromosome 8 is one of the most common genes that are amplified in human cancers.
(3) Lung SCCs are characterized by complex genomic alterations with recurrent mutations in several genes, including TP53, NFE2L2, KEAP1, BAI3, FBXW7, GRM8, MUC16, RUNX1T1, STK11, ERBB4, DDR2, and FGFR1 amplification.
Figure S2: expression of bFGF, FGFR1, FGFR2, FGFR3, and FGFR4 for feeder cells and cESCs, respectively, using RT-PCR.
It suppresses lung cancer progression by targeting FOXM1 ; inhibits hepatocellular carcinoma cell growth by targeting CXCR6 ; decreases glycolytic metabolism, proliferation, and invasion of breast cancer by targeting FGFR1 and MMP1 ; and prevents the malignant progression of prostate cancer cells by targeting STAT6 .
The patient had negative fluorescence in situ hybridization (FISH) results using a panel for hypereosinophilia containing probes for 4q12 (SCFD2, LNX, and PDGFRA) rearrangement, 5q32 (PDGFRB) rearrangement, 8p11.2 (FGFR1) rearrangement, and 9q34 and 22q11.2 (BCR/ABL1) rearrangement on a bone marrow specimen.
Separate from this classification, pathological conditions based on four molecular abnormalities, namely, PDGFRA, PDGFRbeta (PDGFRB), fibroblast growth factor receptor 1 (FGFR1), and PCM1JAK2 (fusion gene resulting from a t(8;9)(p22;p24) chromosomal translocation), are classified as myeloid/ lymphoid tumors, all of which belong to the HESN variant.
Se ha encontrado que el heteroreceptor FGFR1/5-HT1AR esta involucrado en la regulacion de la neuroplasticidad del hipocampo de ratas (23) y que la administracion aguda de los agonistas FGF-2 y 8-OH-DPAT de los receptores de FGFR1 y 5-HT1A respectivamente, producen un efecto antidepresivo sinergico en animales de experimentacion (23).
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- FGFR signalling adaptor
- FGFR substrate 2
- FGFR-signalling adaptor SNT