Structure-activity relationship studies on 1-(2-oxopropyl)indole-5-carboxylic acids acting as inhibitors of cytosolic phospholipase A2α: Effect of substituents at the indole 3-position on activity, solubility, and metabolic stability.
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DOI: 10.1016/j.ejmech.2016.10.039
Abstract: Cytosolic phospholipase A2α (cPLA2α) is a key enzyme in the biosynthesis of pro-inflammatory lipid mediators and therefore represents an attractive target for the development of new anti-inflammatory drugs. Recently, we have found that 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid… read more here.
Keywords: cytosolic phospholipase; indole carboxylic; oxopropyl indole; effect ... See more keywords
Highly Potent 2-Oxoester Inhibitors of Cytosolic Phospholipase A2 (GIVA cPLA2)
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DOI: 10.1021/acsomega.8b01214
Abstract: Cytosolic phospholipase A2 (GIVA cPLA2) has attracted great interest as a medicinal target because it initiates the eicosanoid cascade and is involved in a number of inflammatory diseases. As a consequence, the development of potent… read more here.
Keywords: highly potent; oxoester; cytosolic phospholipase; giva cpla2 ... See more keywords
A New Generation of Arachidonic Acid Analogues as Potential Neurological Agent Targeting Cytosolic Phospholipase A2
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DOI: 10.1038/s41598-017-13996-8
Abstract: Cytosolic phospholipase A2 (cPLA2) is an enzyme that releases arachidonic acid (AA) for the synthesis of eicosanoids and lysophospholipids which play critical roles in the initiation and modulation of oxidative stress and neuroinflammation. In the… read more here.
Keywords: new generation; arachidonic acid; cytosolic phospholipase; acid analogues ... See more keywords
A randomized, double‐blind, placebo‐controlled, dose‐escalation first‐in‐man study (phase 0) to assess the safety and efficacy of topical cytosolic phospholipase A2 inhibitor, AVX001, in patients with mild to moderate plaque psoriasis
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DOI: 10.1111/jdv.14128
Abstract: Cytosolic phospholipase A2 (cPLA2α) is an enzyme suggested as a therapeutic target in inflammatory skin diseases. AVX001, a cPLA2α inhibitor, was investigated in a randomized, double‐blind, placebo‐controlled, split‐design, first‐in‐man study in patients with mild to… read more here.
Keywords: randomized double; cytosolic phospholipase; placebo controlled; first man ... See more keywords
Targeting Cytosolic Phospholipase A2α for Novel Anti-Inflammatory Agents.
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DOI: 10.2174/0929867325666180117103919
Abstract: Group IV cytosolic phospholipase A2 (cPLA2α) plays a critical role in inflammatory processes. It produces arachidonic acid which is the main source of the pro-inflammatory eicosanoids mediators that are important in innate immune system. In… read more here.
Keywords: cytosolic phospholipase; inflammatory; targeting cytosolic; novel anti ... See more keywords
Calcium-Dependent Cytosolic Phospholipase A2α as Key Factor in Calcification of Subdermally Implanted Aortic Valve Leaflets
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DOI: 10.3390/ijms23041988
Abstract: Calcium-dependent cytosolic phospholipase A2α (cPLA2α) had been previously found to be overexpressed by aortic valve interstitial cells (AVICs) subjected to in vitro calcific induction. Here, cPLA2α expression was immunohistochemically assayed in porcine aortic valve leaflets… read more here.
Keywords: aortic valve; dependent cytosolic; cytosolic phospholipase; calcium dependent ... See more keywords
Functions and mechanisms of cytosolic phospholipase A2 in central nervous system trauma
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DOI: 10.4103/1673-5374.346460
Abstract: Central nervous system (CNS) trauma, including traumatic brain injury and spinal cord injury, has a high rate of disability and mortality, and effective treatment is currently lacking. Previous studies have revealed that neural inflammation plays… read more here.
Keywords: cpla2; cytosolic phospholipase; cns trauma; central nervous ... See more keywords