竞争性抑制剂

作为体内半乳糖凝集素-3（galectin-3）配体的竞争性抑制剂，它能够封闭肿瘤细胞表面的galectin-3位点，阻止肿瘤细胞的形成与发展。

As the competitive inhibitor of Galectin - 3 ' ligand , it can close the Galectin-3 site of tumor cells surface and prevent the formation and development of tumor cells .

Ca2+通道阻断剂Verapamil、Ca2+通道竞争性抑制剂LaCl3和钙调素拮抗剂TFP、CPZ可明显抑制KT诱导的原生质体膨大。

The swelling of protoplasts induced by KT could be significantly inhibited by Verapamil ( Ca 2 + channel blocker ) or LaCl 3 ( Ca 2 + channel competitive inhibitor ) respectively . Calmodulin antagonists TFP , CPZ and W 7 could obviously inhibit protoplasts swelling induced by KT .

表皮生长因子受体的ATP竞争性抑制剂

ATP Competitive Inhibitors of Epidermal Growth Factor Receptor

竞争性抑制剂对NOS的抑制可减少胶原沉积，加重切割伤的严重程度，并且使伤口的愈合功能受损。

Inhibition of NOS by competitive inhibitors decreases collagen deposition and braking strength of incisional wounds and impairs the healing of other wound models .

结论龙葵碱是NAT酶2-AF底物的非竞争性抑制剂。

CONCLUSION Solanine is a non-competitive inhibitor of NATs .

导致内皮功能紊乱的机制之一即内源性eNOS竞争性抑制剂不对称二甲基精氨酸（ADMA）的积聚。

One of the mechanisms leading to endothelial dysfunction is the accumulation of an endogenous inhibitor of eNOS , asymmetric dimethylarginine ( ADMA ) .

动力学研究（Lineweaver-Burk作图法）发现，GLPIA1是蛋白酶A的非竞争性抑制剂。

Kinetic studies ( Lineweaver-Burk method ) showed GLPIA_1 is a kind of noncompetitive inhibitor to yeast proteinase A .

洛伐他汀是一种有效的降胆固醇药物，这种真菌次生代谢产物及其衍生物是胆固醇生物合成限速酶&HMGCoA还原酶的竞争性抑制剂。

Lovastatin is a potent cholesterol-lowering drug . This fungal secondary metabolite and its derivatives act as competitive inhibitors of HMG-CoA reductase , the rate limiting enzyme in the biosynthesis of cholesterol .

综述了表皮生长因子受体酪氨酸激酶的ATP竞争性抑制剂的研究进展，介绍了抑制剂结合受体蛋白的方式及其作用机理，重点介绍了可逆抑制剂和不可逆抑制剂的作用机理及其构效关系。

This article reviews the recent research progress in ATP competitive inhibitors of epidermal growth factor receptor . The binding manner and inhibiting mechanism are introduced , with an emphasis on the mechanism and structure-activity relationship of both reversible and irreversible inhibitors .

染料木素是表皮生长因子受体酪氨酸激酶结构域（EGFR-TK）高度特异的非竞争性抑制剂。

Genistein is a high specific and noncompetitive inhibitor of epidermal growth factor receptor tyramine kinase domain ( EGFR-TK ) .

非对称性二甲基精氨酸（ADMA）是内皮型一氧化氮合酶的内源性竞争性抑制剂，它使内皮一氧化氮合成减少，造成内皮功能紊乱。

Asymmetric dimethylarginine ( ADMA ) is an endogenous competitive inhibitor of endothelial nitric oxide synthase and an important cause of endothelial dysfunction . Its elevated plasma concentration is associated with a variety of traditional cardiovascular risk factors , and may mediate their effects on vascular endothelium dysfunction .

上述结果初步表明三尖杉酯碱可能是酶的竞争性抑制剂。

These data showed that harringtonine may be a competitive inhibitor of DNA polymerase α .

一个非竞争性抑制剂的净结果相当于转化某些酶成为钝化形式。

The net result of a non-competitive inhibitor is equivalent to converting some of the enzyme present to an inactive form .

美伐他汀是3羟甲基戊二酰辅酶A还原酶的有效的竞争性抑制剂，它是一种胆固醇生物合成调解酶。

Mevastatin is a potent competitive inhibitor of3-hydroxy-3-methyl-glutaryl ( HMG ) - CoA reductase , a regulatory enzyme for cholesterol biosynthesis .

研究了竞争性抑制剂苯基硼酸对α胰凝乳蛋白酶反胶团萃取过程的影响及对酶活力的稳定作用。

The effect of phenylboronic acid , a competitive inhibitor , on the extraction process and activity recovery of α - chymotrypsin by AOT [ sodium 1,4-bis ( 2-ethylhexyl ) sulfusuccinate ] reverse micelles was studied .

非竞争性抑制剂箭毒，在酶的外周阴离子部位有表现不同亲和力的两种结合作用，只有其中高亲和力的抑制作用为钙离子解除。

There were two kinds of association of different affinities between the peripheral anionic sites of the enzyme and the non-competitive inhibitor curare . Only the inhibition with the higher affinity was eliminated by calcium ions .

由甲基化引起基因沉默而出现的肿瘤，可通过DNA甲基转移酶非竞争性或竞争性抑制剂抑制甲基化的发生，活化沉默的抑癌基因，从而达到治疗肿瘤的目的。

Caused by the methylation of gene silencing the tumor , available through DNA methyltransferase non-competitive or competitive inhibitors methylation occurs , activating the silence of the tumor suppressor gene , so as to achieve the aim of the treatment of tumors .

目的探讨新型非竞争性5α还原酶抑制剂爱普列特（epristeride）治疗良性前列腺增生（BPH）的有效性及安全性。

Objective Study the efficacy and safety of epristeride , a new uncompetitive 5 α - reductase inhibitor , in the treatment of benign prostatic hyperplasia ( BPH ) .