PGE synthase
Prostaglandin E (PGE) is the most common prostanoid with a variety of bioactivities and has been implicated in various pathologies. PGE is produced via three sequential enzymatic reactions: release of arachidonic acid (AA) from membrane glycerophospholipids by phospholipase A2 (PLA2), conversion of AA to the unstable intermediate prostanoid PGH2 by cyclooxygenase (COX), and isomerization of PGH2 to PGE by prostaglandin E synthase (PGES). Despite a rapidly expanding body of information on the structures, expression and regulatory functions of various eicosanoidbiosyntheticenzymes during the last decade, little has been learned about the molecular identity of PGES until very recently. The membrane-bound and cytosolic forms of PGES are now designated as mPGES-1 and cPGES, respectively. The primary structures of mPGES-1 proteins from several species show a high degree of sequence homology. mPGES-1 also shows significant homology with other MAPEG superfamily proteins, including MGST-1, MGST-2, MGST-3, 5-lipoxygenase-activating protein (FLAP) and leukotriene C4 synthase (LTCS), with the highest homology being found with MGST-1 (~40%).
In the immediate response elicited by Ca2+ agonists, AA rapidly released by cPLA2a is metabolized to PGE2 via the constitutive enzymes COX-1 and cPGES, which forms a tertiary complex with Hsp90 and CK2. In the delayed response induced by proinflammatory stimuli (plain arrows), AA slowly and continuously released by cPLA2a is metabolized to PGE2 via the two inducible enzymes COX-2 and mPGES-1. mPGES-1 is capable of producing PGE2 via COX-1 when explosive activation of cPLA2a occurs (i.e. large amounts of AA are released). mPGES-2, a constitutive enzyme that is initially associated with the Golgi membrane and is released into the cytoplasm after N-terminal proteolysis, is coupled with both COX-1 and COX-2. mPGES-1 play important roles in the febrile and pain responses in the CNS, inflammatory arthritis, granulation, angiogenesis and edema, and the development of cancer. In addition, spatiotemporal expression of mPGES-1 supports the involvement of this enzyme in the reproduction, gastrointestinal and renal homeostasis, and DA closure. Transcript for mPGES-2 is more abundantly distributed in the brain, heart, skeletal muscle, kidney and liver than in other tissues, which differs from the expression profile of that for mPGES-1. In contrast to the marked inducibility of mPGES-1 (see above), mPGES-2 is constitutively expressed in various cells and tissues and is not increased appreciably during tissue inflammation or damage.
References
1.Murakami M, Kudo I. Curr Pharm Des. 2006;12(8):943–954.
In the immediate response elicited by Ca2+ agonists, AA rapidly released by cPLA2a is metabolized to PGE2 via the constitutive enzymes COX-1 and cPGES, which forms a tertiary complex with Hsp90 and CK2. In the delayed response induced by proinflammatory stimuli (plain arrows), AA slowly and continuously released by cPLA2a is metabolized to PGE2 via the two inducible enzymes COX-2 and mPGES-1. mPGES-1 is capable of producing PGE2 via COX-1 when explosive activation of cPLA2a occurs (i.e. large amounts of AA are released). mPGES-2, a constitutive enzyme that is initially associated with the Golgi membrane and is released into the cytoplasm after N-terminal proteolysis, is coupled with both COX-1 and COX-2. mPGES-1 play important roles in the febrile and pain responses in the CNS, inflammatory arthritis, granulation, angiogenesis and edema, and the development of cancer. In addition, spatiotemporal expression of mPGES-1 supports the involvement of this enzyme in the reproduction, gastrointestinal and renal homeostasis, and DA closure. Transcript for mPGES-2 is more abundantly distributed in the brain, heart, skeletal muscle, kidney and liver than in other tissues, which differs from the expression profile of that for mPGES-1. In contrast to the marked inducibility of mPGES-1 (see above), mPGES-2 is constitutively expressed in various cells and tissues and is not increased appreciably during tissue inflammation or damage.
References
1.Murakami M, Kudo I. Curr Pharm Des. 2006;12(8):943–954.
Immunology/Inflammation
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PGE synthase
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F092
产品货号 : M36304
cas no: 2250261-59-5
F092 is a potent inhibitor of hematopoietic prostaglandin D synthetase (H-PGDS), which can be used to study allergic inflammation and vascular-related diseases. -
GSK-2894631A
产品货号 : M23952
cas no: 2101626-26-8
HPGDS抑制剂2是一种有效的、选择性造血前列腺素D合酶(h-pgds)抑制剂。 -
Limaprost
产品货号 : M22940
cas no: 74397-12-9
利马前列素是 PGE1 的类似物,经过结构修饰,旨在延长其半衰期并增强效力。它是一种有效的口服活性血管扩张剂。利马前列素增加血流量并抑制血小板聚集。利马前列素可用于缓解疼痛,具有抗心绞痛作用,并具有治疗缺血症状的潜力。 -
ALPHA-PINENE
产品货号 : M18295
cas no: 2437-95-8
ALPHA-PINENE 是一种双环单萜,存在于松树和其他植物中,包括具有多种生物活性的大麻。它减少了 7 种革兰氏阳性菌、7 种革兰氏阴性菌和 8 种酵母菌株的生长,MIC 值分别为 0.75-1.29、1.05-1.59 和 0.7-1.17%。它对 C. molestus 幼虫具有杀虫活性,LC50 值范围为 47 至 49 mg/L。它 (100 μg/ml) 可诱导细胞凋亡,增加阴离子超氧化物的产生和 DNA 片段化,并激活 B16/ 中的 Caspase-3 F10 黑色素瘤细胞 。 -
Crisdesalazine
产品货号 : M16640
cas no: 927685-43-6
Crisdesalazine (AAD-2004、AAD2004) 是阿司匹林的衍生物,可抑制微粒体 PGE(2) 合酶-1 (mPGES-1) 活性,以响应 LPS 处理的 BV2 细胞(IC50 为 230 nM)和重组人 mPGES-1 蛋白体外 IC50 为 249 nM。