一系列凝血酶亲和标记物的抑制剂常数和烷基化速率评估
Evaluation of inhibitor constants and alkylation rates for a series of thrombin affinity labels.
作者信息
Walker B, Wikstrom P, Shaw E
出版信息
Biochem J. 1985 Sep 15;230(3):645-50. doi: 10.1042/bj2300645.
Abstract
The kinetics for the inactivation of thrombin (EC 3.4.21.5) by a series of peptides containing C-terminal arginyl chloromethane in the presence of substrate were determined. The inhibitor effectiveness was analysed so as to allow for both the evaluation of the affinity with which the enzyme binds the inhibitor before irreversible modification and also the rate of covalent-bond formation between enzyme and inhibitor. The results obtained show that the observed large range in inhibitor effectiveness can be accounted for almost entirely by marked differences in affinity, with only small variations in rates of formation of covalent complex.
摘要
在底物存在的情况下，测定了一系列含有C端精氨酰氯甲烷的肽对凝血酶（EC 3.4.21.5）的失活动力学。分析了抑制剂的有效性，以便评估酶在不可逆修饰之前与抑制剂结合的亲和力，以及酶与抑制剂之间共价键形成的速率。所得结果表明，观察到的抑制剂有效性的大范围差异几乎完全可以由亲和力的显著差异来解释，而共价复合物形成速率的变化很小。
相似文献
1
Evaluation of inhibitor constants and alkylation rates for a series of thrombin affinity labels.一系列凝血酶亲和标记物的抑制剂常数和烷基化速率评估
Biochem J. 1985 Sep 15;230(3):645-50. doi: 10.1042/bj2300645.
2
Inactivation of boar acrosin by peptidyl-arginyl-chloromethanes. Comparison of the reactivity of acrosin, trypsin and thrombin.肽基 - 精氨酰 - 氯甲烷对猪顶体蛋白酶的失活作用。顶体蛋白酶、胰蛋白酶和凝血酶反应活性的比较。
Hoppe Seylers Z Physiol Chem. 1978 Sep;359(9):1183-91. doi: 10.1515/bchm2.1978.359.2.1183.
3
4
Inactivation of trypsin-like enzymes with peptides of arginine chloromethyl ketone.用精氨酸氯甲基酮肽使类胰蛋白酶失活。
Methods Enzymol. 1981;80 Pt C:826-42. doi: 10.1016/s0076-6879(81)80065-1.
5
The inhibition of crotalase, a thrombin-like snake venom enzyme, by several peptide chloromethyl ketone derivatives.几种肽氯甲基酮衍生物对凝血酶样蛇毒酶——响尾蛇酶的抑制作用。
Biochem Biophys Res Commun. 1981 Oct 30;102(4):1302-9. doi: 10.1016/s0006-291x(81)80153-2.
6
Inactivation of pyroglutamyl aminopeptidase by N alpha-carbobenzoxy-L-pyroglutamyl chloromethyl ketone.Nα-苄氧羰基-L-焦谷氨酰氯甲基酮对焦谷氨酰氨基肽酶的失活作用。
J Biochem. 1981 Aug;90(2):433-7. doi: 10.1093/oxfordjournals.jbchem.a133490.
7
Synthesis of peptides of arginine chloromethyl ketone. Selective inactivation of human plasma kallikrein.
Biochemistry. 1978 Oct 31;17(22):4778-84. doi: 10.1021/bi00615a027.
8
The susceptibility of urokinase to affinity labeling by peptides of arginine chloromethyl ketone.尿激酶对精氨酸氯甲基酮肽亲和标记的敏感性。
Biochim Biophys Acta. 1979 Jul 11;569(1):31-40. doi: 10.1016/0005-2744(79)90078-0.
9
Effect of thrombomodulin on the kinetics of the interaction of thrombin with substrates and inhibitors.血栓调节蛋白对凝血酶与底物及抑制剂相互作用动力学的影响。
Biochem J. 1986 Jul 1;237(1):243-51. doi: 10.1042/bj2370243.
10
Haloketones as affinity labeling reagents.
Methods Enzymol. 1977;46:130-53. doi: 10.1016/s0076-6879(77)46014-2.
引用本文的文献
1
Novel inhibitors and activity-based probes targeting serine proteases.靶向丝氨酸蛋白酶的新型抑制剂及基于活性的探针
Front Chem. 2022 Sep 28;10:1006618. doi: 10.3389/fchem.2022.1006618. eCollection 2022.
2
Non-canonical proteolytic activation of human prothrombin by subtilisin from may shift the procoagulant-anticoagulant equilibrium toward thrombosis.来自[具体来源未提及]的枯草杆菌蛋白酶对人凝血酶原的非经典蛋白水解激活可能会使促凝血-抗凝血平衡向血栓形成方向转变。
J Biol Chem. 2017 Sep 15;292(37):15161-15179. doi: 10.1074/jbc.M117.795245. Epub 2017 Jul 6.
3
Site-specific Labeling of a Protein Lysine Residue By Novel Kinetic Labeling Combinatorial Libraries.通过新型动力学标记组合文库对蛋白质赖氨酸残基进行位点特异性标记。
Comput Struct Biotechnol J. 2014 Mar 26;9:e201403001. doi: 10.5936/csbj.201403001. eCollection 2014.
4
Synthesis and properties of peptidyl derivatives of arginylfluoromethanes.精氨酰氟甲烷的肽基衍生物的合成与性质
Biochem J. 1988 Dec 1;256(2):481-6. doi: 10.1042/bj2560481.
本文引用的文献
1
The availability of the acetyl derivatives of lysine for growth.赖氨酸乙酰衍生物对生长的可用性。
Biochem J. 1943 Oct;37(4):515-8. doi: 10.1042/bj0370515.
2
Esters of methanesulfonic acid as irreversible inhibitors of acetylcholinesterase.甲磺酸酯作为乙酰胆碱酯酶的不可逆抑制剂
J Biol Chem. 1962 Oct;237:3245-9.
3
Synthesis of p-amino-L-phenylalanine derivatives with protected p-amino group for preparation of p-azido-L-phenylalanine peptides.用于制备对叠氮基-L-苯丙氨酸肽的具有保护的对氨基的对氨基-L-苯丙氨酸衍生物的合成。
Int J Pept Protein Res. 1980 Apr;15(4):323-30. doi: 10.1111/j.1399-3011.1980.tb02908.x.
4
The selective affinity labeling of factor Xa by peptides of arginine chloromethyl ketone.精氨酸氯甲基酮肽对凝血因子Xa的选择性亲和标记
Thromb Res. 1981;22(5-6):645-52. doi: 10.1016/0049-3848(81)90062-1.
5
Determination of the rate constant of enzyme modification by measuring the substrate reaction in the presence of the modifier.通过在修饰剂存在的情况下测量底物反应来测定酶修饰的速率常数。
Biochemistry. 1982 Mar 2;21(5):1028-32. doi: 10.1021/bi00534a031.
6
Proflavin binding within the fibrinopeptide groove adjacent to the catalytic site of human alpha-thrombin.原黄素与人α-凝血酶催化位点相邻的纤维蛋白肽凹槽内的结合。
Biochemistry. 1984 Apr 10;23(8):1818-23. doi: 10.1021/bi00303a037.
7
The irreversible inhibition of urokinase, kidney-cell plasminogen activator, plasmin and beta-trypsin by 1-(N-6-amino-n-hexyl)carbamoylimidazole.1-(N-6-氨基正己基)氨基甲酰咪唑对尿激酶、肾细胞纤溶酶原激活物、纤溶酶和β-胰蛋白酶的不可逆抑制作用
Biochem J. 1984 Jul 1;221(1):277-80. doi: 10.1042/bj2210277.
8
Inhibition of trypsin-like serine proteinases by tripeptide arginyl and lysyl chloromethylketones.三肽精氨酰氯甲基酮和赖氨酰氯甲基酮对类胰蛋白酶丝氨酸蛋白酶的抑制作用。
Thromb Res. 1984 Jun 1;34(5):431-7. doi: 10.1016/0049-3848(84)90247-0.
9
Inactivation of trypsin-like enzymes with peptides of arginine chloromethyl ketone.用精氨酸氯甲基酮肽使类胰蛋白酶失活。
Methods Enzymol. 1981;80 Pt C:826-42. doi: 10.1016/s0076-6879(81)80065-1.
10
Assay of coagulation proteases using peptide chromogenic and fluorogenic substrates.使用肽发色底物和荧光底物测定凝血蛋白酶。
Methods Enzymol. 1981;80 Pt C:341-61. doi: 10.1016/s0076-6879(81)80030-4.
Zotero 插件