FGFR

HMGA1 induces FGF19 to drive pancreatic carcinogenesis and stroma formation

31 views | Jan 09 2024

The study unveils a novel relationship where HMGA1 upregulates FGF19, driving pancreatic cancer progression and stroma formation, establishing FGF19 as a potential therapeutic target for a distinct, highly aggressive subset of PDAC. [Read the Full Post]

Sertad1 Induces Neurological Injury after Ischemic Stroke via the CDK4/p-Rb Pathway

100 views | Jan 06 2024

Sertad1, upregulated in ischemic conditions, exacerbates neurological injury by activating the CDK4/p-Rb pathway, promoting cell cycle dysregulation and apoptotic cell death. [Read the Full Post]

Sulfatinib, a novel multi-targeted tyrosine kinase inhibitor of FGFR1, CSF1R, and VEGFR1-3, suppresses osteosarcoma proliferation and invasion via dual role in tumor cells and tumor microenvironment

46 views | Jan 05 2024

Sulfatinib demonstrates promise in inhibiting osteosarcoma growth while altering the tumor microenvironment towards an immune-activated state, offering potential for clinical translation. [Read the Full Post]

FGF2 positively regulates osteoclastogenesis via activating the ERK-CREB pathway

0 views | Jan 01 2024

FGF2 influences bone homeostasis by stimulating osteoclastogenesis via the ERK-CREB pathway, suggesting potential therapeutic avenues for bone-related disorders like osteoporosis through targeted inhibition of this signaling cascade. [Read the Full Post]

Discovery of ASP5878: Synthesis and structure-activity relationships of pyrimidine derivatives as pan-FGFRs inhibitors with improved metabolic stability and suppressed hERG channel inhibitory activity

34 views | Dec 26 2023

ASP5878 (27) exhibits promising potential as a therapeutic candidate for treating bladder cancer by targeting FGFR3, boasting improved metabolic stability, minimal hERG channel inhibition, potent FGFR3 inhibition in vitro and in vivo, and favorable safety and pharmacokinetic profiles in preclinical models. [Read the Full Post]

Combined inhibition of FGFR4 and VEGFR signaling enhances efficacy in FGF19 driven hepatocellular carcinoma

21 views | Dec 15 2023

The combination of Lenvatinib, a multi-kinase inhibitor, and FGFR4 inhibitor H3B-6527 demonstrates enhanced efficacy in treating FGF19-driven hepatocellular carcinoma by leveraging Lenvatinib's cell non-autonomous VEGFR activity, indicating a promising potential for clinical application. [Read the Full Post]

Lack of pharmacokinetic interaction between derazantinib and naringin in rats

29 views | Dec 14 2023

The study validated a sensitive UPLC-MS/MS method for measuring derazantinib concentration in rat plasma, revealing that co-administration of derazantinib with naringin did not significantly alter its pharmacokinetic parameters, suggesting a safe concomitant use without requiring dose adjustment. [Read the Full Post]

Combined inhibition of aurora kinases and Bcl-xL induces apoptosis through select BH3-only proteins

0 views | Nov 08 2023

The study demonstrates that combining small-molecule inhibitors of AURK with BH3-mimetic inhibitors targeting Bcl-xL potently induces apoptosis and may overcome resistance to AURK inhibitors in colon cancer cells. [Read the Full Post]

A phase 1b study of the allosteric extracellular FGFR2 inhibitor alofanib in patients with pretreated advanced gastric cancer

29 views | Oct 14 2023

Alofanib, a small-molecule allosteric extracellular FGFR2 inhibitor, showed acceptable tolerability and preliminary signs of clinical activity in heavily pretreated patients with advanced gastric cancer, with a recommended phase 2 dose of 350 mg/m2 administered 5 days on and 2 days off. [Read the Full Post]

ATF4 renders human T-cell acute lymphoblastic leukemia cell resistance to FGFR1 inhibitors through amino acid metabolic reprogramming

0 views | Oct 02 2023

This study reveals that targeting FGFR1 and mTOR in combination can overcome drug resistance in T-cell acute lymphoblastic leukemia (T-ALL) by inhibiting ATF4-mediated amino acid metabolic reprogramming. [Read the Full Post]