2. Academic Validation
  3. Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors

Recent Advances of Colony-Stimulating Factor-1 Receptor (CSF-1R) Kinase and Its Inhibitors

  • J Med Chem. 2018 Jul 12;61(13):5450-5466. doi: 10.1021/acs.jmedchem.7b00873.
Mohammed I El-Gamal 1 2,  Shahad K Al-Ameen 1,  Dania M Al-Koumi 1,  Mawadda G Hamad 1,  Nouran A Jalal 1,  Chang-Hyun Oh 3 4
Affiliations

Affiliations

  • 1 College of Pharmacy , University of Sharjah , Sharjah 27272 , United Arab Emirates.
  • 2 Department of Medicinal Chemistry, Faculty of Pharmacy , University of Mansoura , Mansoura 35516 , Egypt.
  • 3 Center for Biomaterials , Korea Institute of Science and Technology , P.O. Box 131, Cheongryang , Seoul 130-650 , Republic of Korea.
  • 4 Department of Biomolecular Science , University of Science and Technology , 113 Gwahangno, Yuseong-gu , Daejeon 305-333 , Republic of Korea.
PMID: 29293000 DOI: 10.1021/acs.jmedchem.7b00873
Abstract

Colony stimulation factor-1 receptor (CSF-1R), which is also known as FMS kinase, plays an important role in initiating inflammatory, Cancer, and bone disorders when it is overstimulated by its ligand, CSF-1. Innate immunity, as well as macrophage differentiation and survival, are regulated by the stimulation of the CSF-1R. Another ligand, interlukin-34 (IL-34), was recently reported to activate the CSF-1R receptor in a different manner. The relationship between CSF-1R and microglia has been reviewed. Both CSF-1 antibodies and small molecule CSF-1R kinase inhibitors have now been tested in animal models and in humans. In this Perspective, we discuss the role of CSF-1 and IL-34 in producing Cancer, bone disorders, and inflammation. We also review the newly discovered and improved small molecule kinase inhibitors and monoclonal antibodies that have shown potent activity toward CSF-1R, reported from 2012 until 2017.

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