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Inhibitors of the Fibroblast Growth Factor Receptor [PDF]

Topics in Medicinal Chemistry, 2017
Signaling through the fibroblast growth factor receptor (FGFR) tyrosine kinase is crucial to a number of key pharmacological processes; however, dysregulation of this signaling is observed with a number of different cancers suggesting that inhibition of FGFR may provide an important therapeutic agent in the treatment of cancers.
Kurt G Pike
exaly   +5 more sources

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Fibroblast Growth Factor Receptor Inhibitors

Current Pharmaceutical Design, 2012
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.
Suneel B V S, Kumar, Lakshmi, Narasu, Rambabu, Gundla, Raveendra, Dayam, Sarma, J A R P   +4 more
openaire   +2 more sources

Pan fibroblast growth factor receptor inhibitor associated retinopathy

European Journal of Ophthalmology, 2023
Purpose To report a case of Fibroblast Growth Factor Receptor inhibitor (FGFRi) associated retinopathy in a patient treated with Erdafitinib. Case report A patient with a history of non-muscle invasive urothelial carcinoma treated with
Arianna Paris, Bahram Bodaghi, Sara Touhami   +2 more
openaire   +2 more sources

Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors [PDF]

Cells, 2019
Fibroblast growth factor receptors (FGFRs) are a family of receptor tyrosine kinases expressed on the cell membrane that play crucial roles in both developmental and adult cells. Dysregulation of FGFRs has been implicated in a wide variety of cancers, such as urothelial carcinoma, hepatocellular carcinoma, ovarian cancer and lung adenocarcinoma. Due to
Yongheng Chen, Shuyan Dai, Guangyu Xu
exaly   +4 more sources

Novel inhibitor for fibroblast growth factor receptor tyrosine kinase

Bioorganic & Medicinal Chemistry Letters, 2007
NP603, the 6-dimethoxy phenyl indolin-2-one, was designed as FGF receptor 1 inhibitor by computational study. NP603 was synthesized and found to be more active against endothelial proliferation of HUVEC after the rhFGF-2 stimulation than SU6668 with minimum effective dose of 0.4 microM but with similar potency as SU16g.
Naparat, Kammasud, Chantana, Boonyarat, Satoshi, Tsunoda, Hiroaki, Sakurai, Ikuo, Saiki, David S, Grierson, Opa, Vajragupta   +6 more
openaire   +2 more sources

Fibroblast Growth Factor Receptor Inhibitors: Patent Review (2015–2019)

Expert Opinion on Therapeutic Patents, 2019
Introduction: fibroblast growth factor receptors (FGFRs) are a family of tyrosine-kinase receptors whose signaling cascade regulates cellular proliferation, differentiation, and survival. Deregulation of the FGFR pathway is recognized as a driving factor in tumor development.
Riccardo Castelli, Alessio Lodola, Marco Mor   +2 more
exaly   +5 more sources

Ocular Toxicities of Fibroblast Growth Factor Receptor Inhibitors: A Review

Survey of Ophthalmology
Fibroblast growth factor receptor (FGFR) inhibitors are an emerging class of small molecule targeted cancer drugs with promising therapeutic possibilities for a wide variety of malignancies. While ocular adverse events from FGFR inhibitors are reported in clinical trials, subsequent case studies continue to reveal new toxicities.
Jerry Hsu, Jasmine Francis, Sumayya Ahmad   +2 more
exaly   +3 more sources

Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor

Journal of Medicinal Chemistry, 2021
Aberrant activation of FGFR has been linked to the pathogenesis of many tumor types. Selective inhibition of FGFR has emerged as a promising approach for cancer treatment. Herein, we describe the discovery of compound 38 (INCB054828, pemigatinib), a highly potent and selective inhibitor of FGFR1, FGFR2, and FGFR3 with excellent physiochemical ...
Liangxing Wu, Colin Zhang, Chunhong He, Dingquan Qian, Liang Lu, Yaping Sun, Meizhong Xu, Jincong Zhuo, Phillip C. C. Liu, Ronald Klabe, Richard Wynn, Maryanne Covington, Karen Gallagher, Lynn Leffet, Kevin Bowman, Sharon Diamond, Holly Koblish, Yue Zhang, Maxim Soloviev, Gregory Hollis, Timothy C. Burn, Peggy Scherle, Swamy Yeleswaram, Reid Huber, Wenqing Yao   +24 more
openaire   +2 more sources