Pharmacological and Biological Targeting of FGFR1 in Cancer

  • Curr Issues Mol Biol. 2024 Nov 18;46(11):13131-13150. doi: 10.3390/cimb46110783.
Shuai Fan  1 Yuxin Chen  1 Wenyu Wang  1 Wanting Xu  1 Mei Tian  1 Yuetong Liu  1 Yutong Zhou  1 Dan Liu  1 Qin Xia  1 Lei Dong  1
Affiliations
  • 1. State Key Laboratory of Molecular Medicine and Biological Diagnosis and Treatment (Ministry of Industry and Information Technology), School of Life Science, Beijing Institute of Technology, Beijing 100081, China.
Abstract

FGFR1 is a key member of the Fibroblast Growth Factor receptor family, mediating critical signaling pathways such as RAS-MAPK and PI3K-AKT. which are integral to regulating essential cellular processes, including proliferation, differentiation, and survival. Alterations in FGFR1 can lead to constitutive activation of signaling pathways that drive oncogenesis by promoting uncontrolled cell division, inhibiting Apoptosis, and enhancing the metastatic potential of Cancer cells. This article reviews the activation mechanisms and signaling pathways of FGFR1 and provides a detailed exposition of the types of FGFR1 aberration. Furthermore, we have compiled a comprehensive overview of current therapies targeting FGFR1 aberration in Cancer, aiming to offer new perspectives for future Cancer treatments by focusing on drugs that address specific FGFR1 alterations.

Keywords
FGFR1; TKI; aberration; antibody drugs; ligand traps; targeted therapeutics.
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