title: Synthesis of selective inhibitors of sphingosine kinase 1.
abstract: 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: Department of Chemistry and Biochemistry, Queens College of the City University of New York, Flushing, New York 11367-1597, USA.
authors: Dong Jae
authors: DJ
authors: Baek
authors: Neil
authors: N
authors: MacRitchie
authors: Nigel J
authors: NJ
authors: Pyne
authors: Susan
authors: S
authors: Pyne
authors: Robert
authors: R
authors: Bittman
mesh_terms: D002460:Cell Line; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D000068876:Fingolimod Hydrochloride; D057809:HEK293 Cells; D006801:Humans; D017853:Phosphotransferases (Alcohol Group Acceptor) / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry; D011409:Propylene Glycols / Q000737:chemistry*; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism; D013110:Sphingosine / Q000031:analogs & derivatives* / Q000737:chemistry; D000099157:Sphingosine Kinase
chemical_list: D004791:Enzyme Inhibitors; D000068876:Fingolimod Hydrochloride; D017853:Phosphotransferases (Alcohol Group Acceptor); D010880:Piperidines; D011409:Propylene Glycols; D046988:Proteasome Endopeptidase Complex; D013110:Sphingosine; D000099157:Sphingosine Kinase; C583391:1-(4-octylphenethyl)piperidin-4-ol
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