摘要
磷脂酶a2(PLA2s)的酶,它裂开磷脂专门在sn-2位置解放自由脂肪酸,主要是花生四烯酸(AA)和溶血磷脂(lpl)。抑制PLA2防止AA和lpl的解放。因此,研究人员一直在考虑PLA2s可能是一个更好的比下游cyclooxygense酶和脂氧合酶的治疗目标。几个亚型的PLA2s存在,主要分为分泌PLA2s(sPLA2),胞质PLA2s(cPLA2)和钙独立PLA2s(iPLA2)、血小板激活因子-酰基水解酶(PAF-AH),溶酶体PLA2(LPLA2)adipose-specific PLA2(Ad - PLA)。每个同种型PLA2s不同的化学结构和生理功能。sPLA2s(团体活动花絮,V和X)描述为酶促炎调停,但他们的角色在癌症是有争议的。组IVA IVB和印度河流域文明司长委任cPLA2s存在于人类只有组IVA cPLA2在各种癌症和炎症的病理生理学中扮演关键角色。iPLA2在炎症和癌症的作用是有限的。脂蛋白相关PLA2(集团VIIA PLA2)PAF-AH同种型,在动脉粥样硬化的关键作用。数个同种型PLA2抑制剂已经被发达国家和一些特定的PLA2s抑制剂目前正在临床试验对各种炎症和肿瘤疾病。本文关注的是最近的实验证据支持这一概念,PLA2s是因果与癌症和炎症相关疾病的病理学和讨论具体同种型PLA2抑制剂的潜在效用作为预防和/或治疗药物。
关键词: 磷脂酶A2、炎症、癌症、PLA2同种型特定抑制剂。
图形摘要
Current Drug Targets
Title:Phospholipase A2 Isoforms as Novel Targets for Prevention and Treatment of Inflammatory and Oncologic Diseases
Volume: 17 Issue: 16
Author(s): Nagendra Sastry Yarla, Anupam Bishayee, Lakshmipathi Vadlakonda, Ramakrishna Chintala, Govinda Rao Duddukuri, Pallu Reddanna and Kaladhar S.V.G.K. Dowluru
Affiliation:
关键词: 磷脂酶A2、炎症、癌症、PLA2同种型特定抑制剂。
摘要: Phospholipase A2s (PLA2s) are group of enzymes, which cleave phospholipids specifically at sn-2 position to liberate free fatty acid, mostly arachidonic acid (AA) and lysophospholipids (LPLs). Inhibition of PLA2 prevents the liberation of AA and LPLs. Hence, researchers have been considering PLA2s could be a better therapeutic target than the downstream enzymes cyclooxygense and lipoxygenase. Several isoforms of PLA2s exist; they are mainly divided into secretory PLA2s (sPLA2), cytosolic PLA2s (cPLA2), and calcium independent PLA2s (iPLA2), platelet activating factor- acyl hydrolase (PAF-AH), lysosomal PLA2 (LPLA2), adipose-specific PLA2 (Ad- PLA). Each isoform of PLA2s is different in its chemical structure and physiological functions. sPLA2s (Groups IIA, V and X) are well characterized as proinflammatory mediating enzymes but their role in cancer is controversial. Groups IVA, IVB and IVC cPLA2s are present in humans but only Group IVA cPLA2 plays key role in pathophysiology of various cancers and inflammation. The role of iPLA2 in inflammation and cancer is limited. Lipoprotein associated PLA2 (Group VIIA PLA2), a PAF-AH isoform, has key role in atherosclerosis. Several isoform specific PLA2 inhibitors have been developed and some of the PLA2s inhibitors are currently under clinical trials for various inflammatory and oncologic diseases. This review focuses on the recent experimental evidences to support the notion that PLA2s are causally implicated in the pathobiology of cancer and inflammatory related disorders and discuss the potential utility of isoform specific PLA2 inhibitors as preventive and/or therapeutic agents.
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Nagendra Sastry Yarla, Anupam Bishayee, Lakshmipathi Vadlakonda, Ramakrishna Chintala, Govinda Rao Duddukuri, Pallu Reddanna and Kaladhar S.V.G.K. Dowluru , Phospholipase A2 Isoforms as Novel Targets for Prevention and Treatment of Inflammatory and Oncologic Diseases, Current Drug Targets 2016; 17 (16) . https://dx.doi.org/10.2174/1389450116666150727122501
DOI https://dx.doi.org/10.2174/1389450116666150727122501 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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