Journal: Molecular Cancer

Article Title: Clinical advances and challenges in targeting FGF/FGFR signaling in lung cancer

doi: 10.1186/s12943-024-02167-9

Figure Lengend Snippet: FGFR genomic alterations in lung cancer

Article Snippet: These approaches include small-molecule FGFR inhibitors that target the ATP-binding site of the tyrosine kinase domain of various growth factor receptors (multitarget TKIs), selective TKIs that specifically target the kinase domain of FGFRs, and biological agents (Fig. ).

Techniques: Mutagenesis

Journal: Molecular Cancer

Article Title: Clinical advances and challenges in targeting FGF/FGFR signaling in lung cancer

doi: 10.1186/s12943-024-02167-9

Figure Lengend Snippet: Targeting FGF/FGFR signaling in lung cancer. Drugs targeting FGFR that are at the clinical stage include multitarget TKIs (nintedanib, dovitinib, pazopanib, and ponatinib) and selective TKIs (pan-FGFR inhibitors such as erdafitinib and rogaratinib; FGFR1/2/3 inhibitors such as pemigatinib, infigratinib and fexagratinib). FP-1039, which targets FGF, has also been investigated in clinical trials. New strategies for targeting FGF/FGFR include the use of FGFR degraders (DGY-09-192 and LC-MB12), specific FGFR inhibitors and anti-FGF2 aptamers

Article Snippet: These approaches include small-molecule FGFR inhibitors that target the ATP-binding site of the tyrosine kinase domain of various growth factor receptors (multitarget TKIs), selective TKIs that specifically target the kinase domain of FGFRs, and biological agents (Fig. ).

Techniques: Clinical Proteomics

Journal: Molecular Cancer

Article Title: Clinical advances and challenges in targeting FGF/FGFR signaling in lung cancer

doi: 10.1186/s12943-024-02167-9

Figure Lengend Snippet: Clinical trials of multitarget TKIs in lung cancer

Article Snippet: These approaches include small-molecule FGFR inhibitors that target the ATP-binding site of the tyrosine kinase domain of various growth factor receptors (multitarget TKIs), selective TKIs that specifically target the kinase domain of FGFRs, and biological agents (Fig. ).

Techniques: Clinical Proteomics, Control, Amplification, Adjuvant

Journal: Molecular Cancer

Article Title: Clinical advances and challenges in targeting FGF/FGFR signaling in lung cancer

doi: 10.1186/s12943-024-02167-9

Figure Lengend Snippet: Clinical trials of selective FGFR inhibitors in lung cancer

Article Snippet: These approaches include small-molecule FGFR inhibitors that target the ATP-binding site of the tyrosine kinase domain of various growth factor receptors (multitarget TKIs), selective TKIs that specifically target the kinase domain of FGFRs, and biological agents (Fig. ).

Techniques: Clinical Proteomics

Journal: Molecular Cancer

Article Title: Clinical advances and challenges in targeting FGF/FGFR signaling in lung cancer

doi: 10.1186/s12943-024-02167-9

Figure Lengend Snippet: Resistance mechanisms of targeted FGFR therapies in lung cancer. In addition to FGFR mutations, changes in signaling pathways and the tumor microenvironment confer resistance to targeted FGFR therapies in lung cancer. ( A ) Bypass and downstream pathway activation. ( B ) Multidrug resistance pathway activation and DNA damage inhibition. ( C ) Cytokine reprogramming in the tumor microenvironment

Article Snippet: These approaches include small-molecule FGFR inhibitors that target the ATP-binding site of the tyrosine kinase domain of various growth factor receptors (multitarget TKIs), selective TKIs that specifically target the kinase domain of FGFRs, and biological agents (Fig. ).

Techniques: Protein-Protein interactions, Activation Assay, Inhibition

Journal: Cancer Medicine

Article Title: Fibroblast growth factor signaling and inhibition in non-small cell lung cancer and their role in squamous cell tumors

doi: 10.1002/cam4.238

Figure Lengend Snippet: Ongoing trials 1 of multitargeted antiangiogenic tyrosine kinase inhibitors in squamous NSCLC

Article Snippet: Additional preclinical data have described the antiangiogenic and antitumor activities of individual multitargeted small molecule inhibitors—specifically those for which the targets include FGF/FGFRs—against NSCLC; these include cediranib (RecentinTM, AstraZeneca; Wilmington, DE) , nintedanib (BIBF 1120, Boehringer Ingelheim; Ingelheim, Germany) , pazopanib (VotrientTM, GlaxoSmithKline; London, UK) , ponatinib (Iclusig®, ARIAD Pharmaceuticals, Inc, Cambridge, MA) , and a number of other investigational agents , – .

Techniques: