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Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library
Published on: September 30, 2019
Fibroblast growth factor receptor inhibitors
Suneel B V S Kumar1, Lakshmi Narasu, Rambabu Gundla
1GVK Biosciences Pvt. Ltd., Phase-1, Technocrats Industrial Estate, Balanagar 500037, Andhra Pradesh, India. suneelkumar.bvs@gmail.com
Abstract:
Fibroblast growth factor receptors (FGFRs) play an important role in embryonic development, angiogenesis, wound healing, cell proliferation and differentiation. The fibroblast growth factor receptor (FGFR) isoforms have been under intense scrutiny for effective anticancer drug candidates. The fibroblast growth factor (FGF) and its receptor (FGFR) provide another pathway that seems critical to monitoring angiogenesis. Recent findings suggest that FGFR mediates signaling, regulates the PKM2 activity, and plays a crucial role in cancer metabolism. The current review also covers the recent findings on the role of FGFR1 in cancer metabolism. This paper reviews the progress, mechanism, and binding modes of recently known kinase inhibitors such as PD173074, SU series and other inhibitors still under clinical development. Some of the structural classes that will be highlighted in this review include Pyrido[2,3-d]pyrimidines, Indolin- 2-one, Pyrrolo[2,1-f][1,2,4]triazine, Pyrido[2,3-d]pyrimidin-7(8H)-one, and 1,6- Naphthyridin-2(1H)-ones.
Insights
Fibroblast growth factor receptors (FGFRs) are crucial in development and cancer. This review details FGFR1
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Fibroblast growth factor receptors (FGFRs) are vital in embryonic development, angiogenesis, and cell regulation.
- FGFR signaling is implicated in various cancers and tumor progression.
- FGFR1's role in cancer metabolism is an emerging area of research.
Purpose of the Study:
- To review recent advancements in understanding FGFR signaling in cancer metabolism.
- To explore the mechanisms and binding modes of FGFR kinase inhibitors.
- To highlight key structural classes of FGFR inhibitors for anticancer drug development.
Main Methods:
- Literature review of recent findings on FGFRs in cancer.
- Analysis of signaling pathways involving FGFR, PKM2, and cancer metabolism.
- Examination of structural classes and binding modes of FGFR kinase inhibitors.
Main Results:
- FGFRs mediate signaling pathways crucial for cancer metabolism.
- FGFR1 plays a significant role in regulating cancer cell metabolism.
- Various kinase inhibitors targeting FGFRs, including PD173074 and SU series, are under clinical investigation.
Conclusions:
- Targeting FGFR signaling presents a promising strategy for anticancer drug development.
- Understanding FGFR's role in cancer metabolism can lead to novel therapeutic approaches.
- Further research into FGFR inhibitors and their mechanisms is essential for clinical translation.
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