title: Role of FGF receptors as an emerging therapeutic target in lung squamous cell carcinoma.
abstract: Recent advances in molecular medicine and high-throughput sequencing technologies have achieved major cancer strategies and therapeutics over the past decades. For example, identification of oncogenic EGF receptor mutations that are present in up to 20% of lung adenocarcinoma patients confer exquisite sensitivity to EGF receptor inhibitors. However, currently known 'druggable' targets are enriched in the subgroup of adenocarcinomas and individuals who have never smoked. We present an overview of FGFs and FGF receptor (FGFR) signaling in cancer, and the role of FGFR1 as a novel druggable target in lung squamous cell carcinoma. FGFR1 amplification in lung squamous cell carcinoma is required for the survival of FGFR1-amplified cell lines. Currently, clinical reagents that target the FGFs and FGFRs are being developed accordingly. This review focuses on the emerging role of FGFR1 as a therapeutic target in lung squamous cell carcinoma and reviews current agents that are in clinical development for the treatment of FGFR-dependent cancer.
authors.affiliation: Department of Internal Medicine, Division of Medical Oncology, Yonsei Cancer Center, Yonsei University College of Medicine, 50 Yonsei-ro, Seodaemun-Gu, Seoul 120-752, Korea.
authors.forename: Sun Min
authors.initials: SM
authors.lastname: Lim
authors.forename: Hye Ryun
authors.initials: HR
authors.lastname: Kim
authors.forename: Hyo Sup
authors.initials: HS
authors.lastname: Shim
authors.forename: Ross A
authors.initials: RA
authors.lastname: Soo
authors.forename: Byoung Chul
authors.initials: BC
authors.lastname: Cho
mesh_terms: D000409:Alanine / Q000031:analogs & derivatives / Q000494:pharmacology / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use; D001562:Benzimidazoles / Q000494:pharmacology / Q000627:therapeutic use; D002294:Carcinoma, Squamous Cell / Q000188:drug therapy* / Q000378:metabolism; D005784:Gene Amplification; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D058990:Molecular Targeted Therapy; D011799:Quinazolines / Q000494:pharmacology / Q000627:therapeutic use; D015363:Quinolones / Q000494:pharmacology / Q000627:therapeutic use; D017468:Receptors, Fibroblast Growth Factor / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism*; D015398:Signal Transduction; D014227:Triazines / Q000494:pharmacology / Q000627:therapeutic use; D007211:Indoles
chemical_list: D000409:Alanine; D000970:Antineoplastic Agents; D001562:Benzimidazoles; D011799:Quinazolines; D015363:Quinolones; D017468:Receptors, Fibroblast Growth Factor; D014227:Triazines; C500007:4-amino-5-fluoro-3-(5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl)quinolin-2(1H)-one; C509922:brivanib; C500926:cediranib; D007211:Indoles