期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 6, 页码 1865-1869出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.01.002
关键词
Lysophosphatidic acid; sn-2 Radyl phosphorothioate; Agonist; Structure-activity relationship; Transforming growth factor-(TGF alpha) shedding assay
资金
- National Institute of Biomedical Innovation of Japan
- Ministry of Education, Science, Sports and Culture of Japan (MEXT) [KAKENHI 22116004]
- Core Research for Evolutional Sciences and Technology (CREST) from Japan Science and Technology Agency
- Schering-Plough
- University of Utah
- [KAKENHI 21790058]
- Grants-in-Aid for Scientific Research [24790064] Funding Source: KAKEN
We describe an efficient synthesis of metabolically stabilized sn-2 radyl phosphorothioate analogs of lysophosphatidic acid (LPA), and the determination of the agonist activity of each analog for the six LPA receptors (LPA(1-6)) using a recently developed TGF alpha shedding assay. In general, the sn-2 radyl OMPT analogs showed similar agonist activities to the previous 1-oleoyl-2-O-methyl-glycerophosphothioate (sn-1 OMPT) analogs for LPA(1-6) receptors. In most cases, the sn-2 radyl-OMPT analogs were more potent agonists than LPA itself. Most importantly, sn-2 alkyl OMPT analogs were very potent LPA(5) and LPA(6) agonists. The availability of sn-2 radyl OPMT analogs further refines the structure-activity relationships for ligand-receptor interactions for this class of GPCRs. (C) 2013 Elsevier Ltd. All rights reserved.
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