121st General Meeting of the KCS

Type Poster Presentation
Area Medicinal Chemistry
Room No. Event Hall
Time 4월 19일 (목요일) 11:00~12:30
Code MEDI.P-635
Subject Potent New scaffold Inhibitor of Fibroblast Growth Factor Receptors
Authors SeongShick Ryu, Yunju Nam, Taebo Sim1,*
Korea University, Korea
1Chemical Kinomics Research Center, Korea Institute of Science and Technology, Korea
Abstract Fibroblast growth factor receptors (FGFRs) are a family of four receptor tyrosine kinases and each of the four FGFRs (FGFR1−4) consists of three extracellular immunoglobulin domains, a single transmembrane domain, and a cytoplasmic tyrosine kinase domain. Fibroblast growth factors (FGF) and their receptors (FGFR) tightly regulate key cell proliferation, differentiation, migration and survival. Dysregulation of the FGF/FGFR signaling pathway has been related with many cancers. Genetic alterations that constitutively activate FGFR including amplification and mutation drive activation of the FGFR and the downstream pathway in various malignant tumors and are reported to be related with cancer cell growth, angiogenesis, cell migration, invasion and metastasis. FGFR1 amplification is reported squamous non-small cell lung carcinoma and hormone receptor-positive breast cancers. FGFR2 is amplified and mutated in about 10% gastric cancer, 4% triple-negative breast cancers and 10% of endometrial cancer. Moreover, mutations of FGFR3 are found in about half of bladder cancers, which are strongly associated to low-grade tumors. Therefore, the inhibition of FGFR signaling is could be a good therapeutic option for cancer.
E-mail ssryu129@gmail.com