Document Detail


Synthesis of selective inhibitors of sphingosine kinase 1.
MedLine Citation:
PMID:  23388656     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Sphingosine kinase isoform 1 (SK1) inhibitors may serve as therapeutic agents for proliferative diseases, including hypertension. We synthesized a series of sphingosine-based SK1-selective inhibitors, the most potent of which is RB-005 (IC(50) = 3.6 μM), which also induced proteasomal degradation of SK1 in human pulmonary arterial smooth muscle cells.
Authors:
Dong Jae Baek; Neil MacRitchie; Nigel J Pyne; Susan Pyne; Robert Bittman
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't     Date:  2013-02-07
Journal Detail:
Title:  Chemical communications (Cambridge, England)     Volume:  49     ISSN:  1364-548X     ISO Abbreviation:  Chem. Commun. (Camb.)     Publication Date:  2013 Mar 
Date Detail:
Created Date:  2013-02-15     Completed Date:  2013-09-12     Revised Date:  2014-03-17    
Medline Journal Info:
Nlm Unique ID:  9610838     Medline TA:  Chem Commun (Camb)     Country:  England    
Other Details:
Languages:  eng     Pagination:  2136-8     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Cell Line
Enzyme Inhibitors / chemical synthesis*,  chemistry
HEK293 Cells
Humans
Phosphotransferases (Alcohol Group Acceptor) / antagonists & inhibitors*,  genetics,  metabolism
Piperidines / chemical synthesis*,  chemistry
Propylene Glycols / chemistry*
Proteasome Endopeptidase Complex / metabolism
Sphingosine / analogs & derivatives*,  chemistry
Grant Support
ID/Acronym/Agency:
29476//British Heart Foundation; HL-083187/HL/NHLBI NIH HHS; R24 HL083187/HL/NHLBI NIH HHS
Chemical
Reg. No./Substance:
0/1-(4-octylphenethyl)piperidin-4-ol; 0/Enzyme Inhibitors; 0/Piperidines; 0/Propylene Glycols; 3QN8BYN5QF/fingolimod; EC 2.7.1.-/Phosphotransferases (Alcohol Group Acceptor); EC 2.7.1.-/sphingosine kinase; EC 3.4.25.1/Proteasome Endopeptidase Complex; NGZ37HRE42/Sphingosine
Comments/Corrections

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