Small-molecule CSF1R kinase inhibitors; review of patents 2015-present.

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dc.contributor.author Denny, William A
dc.contributor.author Flanagan, Jack U
dc.coverage.spatial England
dc.date.accessioned 2022-02-20T22:02:53Z
dc.date.available 2022-02-20T22:02:53Z
dc.date.issued 2021-2
dc.identifier.issn 1354-3776
dc.identifier.uri https://hdl.handle.net/2292/58276
dc.description.abstract <h4>Introduction</h4>Colony stimulating factor 1 receptor (CSF-1R, also known as c-FMS kinase) is in the class III receptor tyrosine kinase family, along with c-Kit, Flt3 and PDGFRα. CSF-1/CSF-1R signaling promotes the differentiation and survival of myeloid progenitors into populations of monocytes, macrophages, dendritic cells and osteoclasts, as well as microglial cells and also recruits host macrophages to develop into tumor-associated macrophages (TAMs), which promote tumor progression and metastasis.<h4>Areas covered</h4>In the last 5 years, and recently stimulated by the approval of pexidartinib (Turalio™, Daiichi Sankyo) in 2019 for the treatment of tenosynovial giant cell tumors, there has been a large increase in activity (both journal articles and patent applications) around small molecule inhibitors of CSF1R. Features of this work have been the surprising diversity of chemical classes shown to be potent and selective inhibitors, and the breadth of disease states (cancer, arthritis, and 'cytokine storm' syndromes) covered by CSF1R inhibitors. All these aspects are covered in the following sections.<h4>Expert opinion</h4>The field has developed rapidly from 2014 to the present, with many different chemotypes proving to be potent inhibitors. The range of potential utilities of CSF1R inhibitors has also expanded to include dementia, ulcerative colitis/Crohn's disease, rheumatoid arthritis inflammation, and fibrosis.
dc.format.medium Print-Electronic
dc.language eng
dc.publisher Informa UK Limited
dc.relation.ispartofseries Expert opinion on therapeutic patents
dc.rights Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher.
dc.rights.uri https://researchspace.auckland.ac.nz/docs/uoa-docs/rights.htm
dc.subject Animals
dc.subject Humans
dc.subject Neoplasms
dc.subject Neoplasm Metastasis
dc.subject Disease Progression
dc.subject Receptor, Macrophage Colony-Stimulating Factor
dc.subject Protein Kinase Inhibitors
dc.subject Patents as Topic
dc.subject Tumor-Associated Macrophages
dc.subject Alzheimers
dc.subject CSF1R
dc.subject Colony-stimulating factor-1 receptor
dc.subject cancer
dc.subject inflammation
dc.subject Animals
dc.subject Disease Progression
dc.subject Humans
dc.subject Neoplasm Metastasis
dc.subject Neoplasms
dc.subject Patents as Topic
dc.subject Protein Kinase Inhibitors
dc.subject Receptor, Macrophage Colony-Stimulating Factor
dc.subject Tumor-Associated Macrophages
dc.subject Science & Technology
dc.subject Life Sciences & Biomedicine
dc.subject Chemistry, Medicinal
dc.subject Pharmacology & Pharmacy
dc.subject Colony-stimulating factor-1 receptor
dc.subject CSF1R
dc.subject cancer
dc.subject Alzheimers
dc.subject inflammation
dc.subject FMS TYROSINE KINASE
dc.subject MICROGLIAL PROLIFERATION
dc.subject CSF-1R INHIBITOR
dc.subject RECEPTOR
dc.subject JNJ-40346527
dc.subject 0903 Biomedical Engineering
dc.subject 1115 Pharmacology and Pharmaceutical Sciences
dc.title Small-molecule CSF1R kinase inhibitors; review of patents 2015-present.
dc.type Journal Article
dc.identifier.doi 10.1080/13543776.2021.1839414
pubs.issue 2
pubs.begin-page 107
pubs.volume 31
dc.date.updated 2022-01-10T00:58:11Z
dc.rights.holder Copyright: The author en
pubs.author-url https://www.ncbi.nlm.nih.gov/pubmed/33108917
pubs.end-page 117
pubs.publication-status Published
dc.rights.accessrights http://purl.org/eprint/accessRights/RetrictedAccess en
pubs.subtype Review
pubs.subtype Journal Article
pubs.elements-id 823476
dc.identifier.eissn 1744-7674
pubs.online-publication-date 2020-10-28


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