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.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
El-Gamal MI,Al-Ameen SK,Al-Koumi DM,Hamad MG,Jalal NA,Oh CHdoi
10.1021/acs.jmedchem.7b00873subject
Has Abstractpub_date
2018-07-12 00:00:00pages
5450-5466issue
13eissn
0022-2623issn
1520-4804journal_volume
61pub_type
杂志文章,评审abstract：:The objective of this study is the measurement of the rates of hydrolysis of a series of chloroethyl sulfide derivatives, under stimulated physiological conditions. Interferences encountered with the conventional spectrophotometric method prompted the use of a rapid-response, chloride selective electrode. This probe w...
journal_title：Journal of medicinal chemistry
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doi：10.1021/jm00222a037
更新日期：1977-12-01 00:00:00
abstract：:A number of bis(diazeniumdiolates) that we designed to release up to 4 mol of nitric oxide (NO) and that are structural analogues of the NO prodrug and anticancer lead compound O(2)-{2,4-dinitro-5-[4-(N-methylamino)benzoyloxy]phenyl} 1-(N,N-dimethylamino)diazen-1-ium-1,2- diolate (PABA/NO) were synthesized and studied...
journal_title：Journal of medicinal chemistry
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更新日期：2008-12-25 00:00:00
abstract：:The synthesis of 5-(arylacetyl)-4-[(alkylamino)methyl]furo[3,2-c] pyridines (16-23, 26, 27) and their activities as kappa-opioid receptor agonists are described. kappa-Agonist potency was particularly sensitive to the nature of the basic moiety. In particular, in the rabbit vas deferens (kappa-specific tissue), the 3-...
journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm00040a004
更新日期：1994-07-08 00:00:00
abstract：:An essential step in the HIV life cycle is integration of the viral DNA into the host chromosome. This step is catalyzed by a 32-kDa viral enzyme HIV integrase (IN). HIV-1 IN is an important and validated target, and the drugs that selectively inhibit this enzyme, when used in combination with reverse transcriptase (R...
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doi：10.1021/jm960666x
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journal_title：Journal of medicinal chemistry
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更新日期：2013-04-25 00:00:00
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更新日期：2005-02-10 00:00:00
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doi：10.1021/jm9605851
更新日期：1996-12-20 00:00:00
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更新日期：2013-02-28 00:00:00
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journal_title：Journal of medicinal chemistry
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doi：10.1021/jm00375a017
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
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更新日期：2004-05-06 00:00:00
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journal_title：Journal of medicinal chemistry
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更新日期：2012-08-09 00:00:00
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journal_title：Journal of medicinal chemistry
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doi：10.1021/jm801389m
更新日期：2009-02-26 00:00:00
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm00239a004
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abstract：:Molecular docking studies of carbohydrate derivatives in protein binding sites are often challenging because of water-mediated interactions and the inherent flexibility of the many terminal hydroxyl groups. Using the recognition process between heat-labile enterotoxin from Escherichia coli and ganglioside GM1 as a par...
journal_title：Journal of medicinal chemistry
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pub_type： 杂志文章
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更新日期：2019-11-14 00:00:00
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journal_title：Journal of medicinal chemistry
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abstract：:Dual-acting kappa opioid receptor (KOR) agonist and mu opioid receptor (MOR) partial agonist ligands have been put forward as potential treatment agents for cocaine and other psychostimulant abuse. Members of the orvinol series of ligands are known for their high binding affinity to both KOR and MOR, but efficacy at t...
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
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journal_title：Journal of medicinal chemistry
pub_type： 杂志文章
doi：10.1021/jm0301787
更新日期：2003-10-23 00:00:00
