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| Content Provider | PubMed Central |
|---|---|
| Author | Ganesan, Ramya Mahankali, Madhu Alter, Gerald Gomez Cambronero, Julian |
| Copyright Year | 2014 |
| Abstract | PLD has been implicated in many physiological functions, such aschemotaxis and phagocytosis, as well as pathological functions, such as cancercell invasion and metastasis. New inhibitors have been described that hamper therole of PLD in those pathologies but their site of action is not known. We havecharacterized the biochemical and biological behavior of the PLD1/2 dualinhibitor 5-Fluoro-2-indolyl des-chlorohalopemide (FIPI), and the specific PLD2inhibitor,N-[2-[1-(3-Fluorophenyl)-4-oxo-1,3,-8-triazaspiro[4.5]dec-8-yl]ethyl]-2-naphthalenecarboxamide(NFOT), and found that both FIPI and NFOT are mixed-kinetics inhibitors.Mutagenesis studies indicate that FIPI binds at S757 of PLD2, which is withinthe HKD2 catalytic site of the enzyme, whereas NFOT binds to PLD2 at twodifferent sites, one being at S757/S648 and another to an allosteric site thatis a natural site occupied by PIP2 (R210/R212). This latter site,along with F244/L245/L246, forms a hydrophobic pocket in the PH domain. Themechanism of action of FIPI is a direct effect on the catalytic site (and assuch inhibits both PLD1 and PLD2 isoforms) whereas PLD2 affects both thecatalytic site (orthosteric) and blocks PIP2 binding to PLD2(allosteric), which negates the natural enhancing role of PIP2.Moreover, NFOT prevents cell invasion of cancer cells, which does not occur incells overexpressing PLD2-F244A/L245A/L246A, or PLD2-R210A/R212A, orPLD2-S757/S648 mutants. This study provides new specific knowledge of enzymeregulation and mechanisms of activation and inhibition of PLD2 that arenecessary to understand its role in cell signaling and to develop new inhibitorsfor cancer cell invasion and metastasis. |
| Related Links | http://dx.doi.org/10.1016/j.bbalip.2014.12.007 |
| Ending Page | 272 |
| Page Count | 12 |
| Starting Page | 261 |
| File Format | |
| ISSN | 00063002 |
| Journal | Biochimica et biophysica acta |
| Issue Number | 3 |
| Volume Number | 1851 |
| Language | English |
| Publisher Date | 2015-03-01 |
| Access Restriction | Open |
| Subject Keyword | Research in Higher Education |
| Content Type | Text |
| Resource Type | Article |
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