Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation

Search Page

Filters

My NCBI Filters

Results by year

Table representation of search results timeline featuring number of search results per year.

Year Number of Results
2008 1
2009 1
2010 2
2011 1
2013 1
2014 1
2015 1
2024 0

Text availability

Article attribute

Article type

Publication date

Search Results

7 results

Results by year

Filters applied: . Clear all
Page 1
The cPLA2alpha inhibitor efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid.
Nickerson-Nutter CL, Goodwin D, Shen MW, Damphousse C, Duan W, Samad TA, McKew JC, Lee KL, Zaleska MM, Mollova N, Clark JD. Nickerson-Nutter CL, et al. Neuropharmacology. 2011 Mar;60(4):633-41. doi: 10.1016/j.neuropharm.2010.11.025. Epub 2010 Dec 10. Neuropharmacology. 2011. PMID: 21146550
The nociceptive response was significantly inhibited by orally administered efipladib, yet spinal fluid levels of PGE(2) and temperature measurements were unaffected compared to vehicle-treated animals. Conversely, intrathecal (IT) administration of efipladib reduce …
The nociceptive response was significantly inhibited by orally administered efipladib, yet spinal fluid levels of PGE(2) and temperat …
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
McKew JC, Lee KL, Shen MW, Thakker P, Foley MA, Behnke ML, Hu B, Sum FW, Tam S, Hu Y, Chen L, Kirincich SJ, Michalak R, Thomason J, Ipek M, Wu K, Wooder L, Ramarao MK, Murphy EA, Goodwin DG, Albert L, Xu X, Donahue F, Ku MS, Keith J, Nickerson-Nutter CL, Abraham WM, Williams C, Hegen M, Clark JD. McKew JC, et al. J Med Chem. 2008 Jun 26;51(12):3388-413. doi: 10.1021/jm701467e. Epub 2008 May 23. J Med Chem. 2008. PMID: 18498150
Optimization of these regions led to the discovery of 111 (efipladib) and 121 (WAY-196025), which are shown to be potent, selective inhibitors of cPLA 2 alpha in a variety of isolated enzyme assays, cell based assays, and rat and human whole blood assays. ...
Optimization of these regions led to the discovery of 111 (efipladib) and 121 (WAY-196025), which are shown to be potent, selective i …
Decrease in expression or activity of cytosolic phospholipase A2alpha increases cyclooxygenase-1 action: A cross-talk between key enzymes in arachidonic acid pathway in prostate cancer cells.
Niknami M, Vignarajan S, Yao M, Hua S, Witting PK, Kita Y, Shimizu T, Sved P, Patel MI, Dong Q. Niknami M, et al. Biochim Biophys Acta. 2010 Jul;1801(7):731-7. doi: 10.1016/j.bbalip.2010.03.003. Epub 2010 Mar 20. Biochim Biophys Acta. 2010. PMID: 20227521
Treatment with Efipladib also led to a decrease in most LOX products (HETEs) as measured by LC/MS/MS. Replenishing 5- and 12-HETEs abolished Efipladib-induced COX-1 and PGE(2) levels. Decreasing 5- and 12-HETE production, as a result of treating cells with inhibitor …
Treatment with Efipladib also led to a decrease in most LOX products (HETEs) as measured by LC/MS/MS. Replenishing 5- and 12-HETEs ab …
Targeting of cytosolic phospholipase A2α impedes cell cycle re-entry of quiescent prostate cancer cells.
Yao M, Xie C, Kiang MY, Teng Y, Harman D, Tiffen J, Wang Q, Sved P, Bao S, Witting P, Holst J, Dong Q. Yao M, et al. Oncotarget. 2015 Oct 27;6(33):34458-74. doi: 10.18632/oncotarget.5277. Oncotarget. 2015. PMID: 26416244 Free PMC article.
Simultaneously, Efipladib prohibited the emergence of Skp2 while maintained p27 at a high level in the nuclear compartment during cell cycle re-entry. ...Moreover, a pre-treatment of the prostate cancer cells with Efipladib during induction of cell cycle re-entry su …
Simultaneously, Efipladib prohibited the emergence of Skp2 while maintained p27 at a high level in the nuclear compartment during cel …
Cytosolic phospholipase A2α sustains pAKT, pERK and AR levels in PTEN-null/mutated prostate cancer cells.
Hua S, Yao M, Vignarajan S, Witting P, Hejazi L, Gong Z, Teng Y, Niknami M, Assinder S, Richardson D, Dong Q. Hua S, et al. Biochim Biophys Acta. 2013 Jun;1831(6):1146-57. doi: 10.1016/j.bbalip.2013.02.011. Epub 2013 Mar 14. Biochim Biophys Acta. 2013. PMID: 23500889
The inhibitory effect of cPLA2alpha siRNA on pAKT and AR protein levels was reduced by the addition of arachidonic acid (AA), whereas the stimulatory effect of AA on pAKT, pERK and AR levels was decreased by an inhibitor of 5-hydroxyeicosatetraenoic acid production. Pharmacologic …
The inhibitory effect of cPLA2alpha siRNA on pAKT and AR protein levels was reduced by the addition of arachidonic acid (AA), whereas the st …
Targeting cytosolic phospholipase A2 α in colorectal cancer cells inhibits constitutively activated protein kinase B (AKT) and cell proliferation.
Zheng Z, He X, Xie C, Hua S, Li J, Wang T, Yao M, Vignarajan S, Teng Y, Hejazi L, Liu B, Dong Q. Zheng Z, et al. Oncotarget. 2014 Dec 15;5(23):12304-16. doi: 10.18632/oncotarget.2639. Oncotarget. 2014. PMID: 25365190 Free PMC article.
In contrast, silencing of cPLA2alpha with siRNA or inhibition with Efipladib decreased basal and EGF-stimulated AKT phosphorylation and proliferation in HT-29. Treating animals transplanted with DLD-1 with Efipladib (10 mg/kg, i.p. daily) over 14 days reduced xenogr …
In contrast, silencing of cPLA2alpha with siRNA or inhibition with Efipladib decreased basal and EGF-stimulated AKT phosphorylation a …