Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.drudis.2013.07.021
Title: Current strategies for inhibiting FGFR activities in clinical applications: Opportunities, challenges and toxicological considerations
Authors: Ho, H.K. 
Yeo, A.H.L.
Kang, T.S. 
Chua, B.T.
Issue Date: Jan-2014
Citation: Ho, H.K., Yeo, A.H.L., Kang, T.S., Chua, B.T. (2014-01). Current strategies for inhibiting FGFR activities in clinical applications: Opportunities, challenges and toxicological considerations. Drug Discovery Today 19 (1) : 51-62. ScholarBank@NUS Repository. https://doi.org/10.1016/j.drudis.2013.07.021
Abstract: Aberrations in fibroblast growth factor receptor (FGFR) signaling are instrumental to the pathophysiology of several malignancies and disorders. Hence, FGFR inhibitors are explored in therapeutics with early candidates developed as competitors for the ATP-binding pocket in the kinase domain. More recent programs yielded compounds of diverse scaffolds with alternative binding modes. Concurrently, monoclonal antibodies and peptide-based agents provide independent options for clinical development. Notwithstanding this rapid progress, we contemplate the toxicological impact of FGFR inhibition based on the defined role of FGFR family members in physiology and homeostasis. The high homology among FGFR1-4 and also with other kinase subfamilies creates an additional challenge in developing selective inhibitors. It orchestrates an ongoing conundrum of moderating a balance between synergism through multitargeting kinase inhibition and minimizing off-target toxicities. © 2013 Elsevier Ltd. All rights reserved.
Source Title: Drug Discovery Today
URI: http://scholarbank.nus.edu.sg/handle/10635/106639
ISSN: 13596446
DOI: 10.1016/j.drudis.2013.07.021
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