Phospholipase A2 structure/function, mechanism, and signaling
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Tremendous advances in understanding the structure and function of the superfamily of phospholipase A2 (PLA2) enzymes has occurred in the twenty-first century. The superfamily includes 15 groups comprising four main types including the secreted sPLA2, cytosolic cPLA2, calcium-independent iPLA2, and platelet activating factor (PAF) acetyl hydrolase/oxidized lipid lipoprotein associated (Lp)PLA2. We review herein our current understanding of the structure and interaction with substrate phospholipids, which resides in membranes for a representative of each of these main types of PLA2. We will also briefly review the development of inhibitors of these enzymes and their roles in lipid signaling.
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Darapladib (which targeted Lp-PLA2) failed in SOLID-TIMI 52 and STABILITY trials.
“Darapladib (which targeted Lp-PLA 2 ) failed in SOLID-TIMI 52 128 and STABILITY 129 trials”
From Integrating genomics with biomarkers and therapeutic targets to invigorate cardiovascular drug development (2021) · cites this paper as [129]
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- Authors
- Burke, J. E., & Dennis, E. A.
- Affiliations
- University of California San Diego (US)
- Venue
- Journal of Lipid Research
- Publisher
- Elsevier BV
- Published
- 2009-04
- Volume
- 50
- Pages
- S237-S242
- ISSN
- 0022-2275 (ISSN-L)
- PMC
- PMC2674709
- OpenAlex
- W2083681924
- Cited by
- 933
- References
- 66
- Citations by year
- 2026: 33 · 2025: 35 · 2024: 28 · 2023: 68 · 2022: 47 · 2021: 75 · 2020: 38 · 2019: 67 · 2018: 52 · 2017: 50 · 2016: 56 · 2015: 49 · 2014: 46 · 2013: 54 · 2012: 75
- FWCI
- 3.70
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Journal of Lipid Research (publishedVersion, cc-by)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- eScholarship (California Digital Library) (submittedVersion)
- Funders
- National Institutes of Health (GM 20,501)
- National Institute of General Medical Sciences (R01GM020501, GM20501)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Biochemistry › Lipid metabolism and biosynthesis
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Sphingolipid Metabolism and Signaling
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Kinase Regulation and GTPase Signaling
- Keywords
- phospholipase A2, secretory phospholipase A2, cytosolic phospholipase A2, calcium-independent phospholipase A2, lipoprotein-associated phospholipase A2, enzyme structure, membrane-bound enzyme, enzyme inhibitors, lipid signaling
- MeSH terms
- Animals, Calcium, Cytosol, Humans, Signal Transduction, 1-Alkyl-2-acetylglycerophosphocholine Esterase, Lipid Metabolism, Phospholipases A2
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