Literature DB >> 19800228

Discovery of novel sphingosine kinase 1 inhibitors.

Yibin Xiang1, Gary Asmussen, Michael Booker, Bradford Hirth, John L Kane, Junkai Liao, Kevin D Noson, Christopher Yee.   

Abstract

Sphingosine kinase 1 (SK1) is an important enzyme that regulates the balance between ceramide and sphingosine-1-phosphate (S1P). Potent and novel SK1 inhibitors (6ag, 9ab and 12aa) have been discovered through a series of modifications of sphingosine (1), the substrate of this enzyme.

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Year:  2009        PMID： 19800228     DOI： 10.1016/j.bmcl.2009.09.022

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  16 in total

1.  Design, synthesis and biological activity of sphingosine kinase 2 selective inhibitors.

Authors:  Mithun R Raje; Kenneth Knott; Yugesh Kharel; Philippe Bissel; Kevin R Lynch; Webster L Santos
Journal:  Bioorg Med Chem       Date:  2011-11-15       Impact factor: 3.641

2.  Development of amidine-based sphingosine kinase 1 nanomolar inhibitors and reduction of sphingosine 1-phosphate in human leukemia cells.

Authors:  Andrew J Kennedy; Thomas P Mathews; Yugesh Kharel; Saundra D Field; Morgan L Moyer; James E East; Joseph D Houck; Kevin R Lynch; Timothy L Macdonald
Journal:  J Med Chem       Date:  2011-05-02       Impact factor: 7.446

3.  Analysis of selective target engagement by small-molecule sphingosine kinase inhibitors using the Cellular Thermal Shift Assay (CETSA).

Authors:  Jeremy A Hengst; Taryn E Dick; Charles D Smith; Jong K Yun
Journal:  Cancer Biol Ther       Date:  2020-08-23       Impact factor: 4.742

Review 4.  Sphingosine kinase inhibitors: a review of patent literature (2006-2015).

Authors:  Kevin R Lynch; S Brandon Thorpe; Webster L Santos
Journal:  Expert Opin Ther Pat       Date:  2016-08-30       Impact factor: 6.674

5.  A rapid assay for assessment of sphingosine kinase inhibitors and substrates.

Authors:  Yugesh Kharel; Thomas P Mathews; Andrew J Kennedy; Joseph D Houck; Timothy L Macdonald; Kevin R Lynch
Journal:  Anal Biochem       Date:  2011-01-07       Impact factor: 3.365

6.  Sphingosine kinase type 1 inhibition reveals rapid turnover of circulating sphingosine 1-phosphate.

Authors:  Yugesh Kharel; Thomas P Mathews; Amanda M Gellett; Jose L Tomsig; Perry C Kennedy; Morgan L Moyer; Timothy L Macdonald; Kevin R Lynch
Journal:  Biochem J       Date:  2011-12-15       Impact factor: 3.857

Review 7.  Sphingosine 1-phosphate and cancer.

Authors:  Nigel J Pyne; Susan Pyne
Journal:  Nat Rev Cancer       Date:  2010-06-17       Impact factor: 60.716

8.  Sphingosine kinase type 2 inhibition elevates circulating sphingosine 1-phosphate.

Authors:  Yugesh Kharel; Mithun Raje; Ming Gao; Amanda M Gellett; Jose L Tomsig; Kevin R Lynch; Webster L Santos
Journal:  Biochem J       Date:  2012-10-01       Impact factor: 3.857

9.  An electrophoretic mobility shift assay identifies a mechanistically unique inhibitor of protein sumoylation.

Authors:  Yeong Sang Kim; Katelyn Nagy; Samantha Keyser; John S Schneekloth
Journal:  Chem Biol       Date:  2013-04-18

10.  SKI-178: A Multitargeted Inhibitor of Sphingosine Kinase and Microtubule Dynamics Demonstrating Therapeutic Efficacy in Acute Myeloid Leukemia Models.

Authors:  Jeremy A Hengst; Taryn E Dick; Arati Sharma; Kenichiro Doi; Shailaja Hegde; Su-Fern Tan; Laura M Geffert; Todd E Fox; Arun K Sharma; Dhimant Desai; Shantu Amin; Mark Kester; Thomas P Loughran; Robert F Paulson; David F Claxton; Hong-Gang Wang; Jong K Yun
Journal:  Cancer Transl Med       Date:  2017-08-14
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