Journal of enzyme inhibition最新文献_第4页

Carbonic Anhydrase Activity Modulators: Synthesis of Inhibitors and Activators Incorporating 2-substituted-thiazol-4-yl-methyl Scaffolds 碳酸酐酶活性调节剂:含2-取代噻唑-4-甲基支架的抑制剂和活化剂的合成

Journal of enzyme inhibition Pub Date : 2001-01-01 DOI: 10.1080/14756360109162383

A. Scozzafava, I. Şaramet, M. Banciu, C. Supuran

引用次数: 4

Glycosylasparaginase Inhibition Studies: Competitive Inhibitors, Transition State Mimics, Noncompetitive Inhibitors 糖基天冬酰胺酶抑制研究:竞争性抑制剂，过渡态模拟物，非竞争性抑制剂

Journal of enzyme inhibition Pub Date : 2001-01-01 DOI: 10.1080/14756360109162375

J. Risley, D. Huang, J. J. Kaylor, J. J. Malik, Yuan-qing Xia

{"title":"Glycosylasparaginase Inhibition Studies: Competitive Inhibitors, Transition State Mimics, Noncompetitive Inhibitors","authors":"J. Risley, D. Huang, J. J. Kaylor, J. J. Malik, Yuan-qing Xia","doi":"10.1080/14756360109162375","DOIUrl":"https://doi.org/10.1080/14756360109162375","url":null,"abstract":"Glycosylasparaginase catalyzes the hydrolysis of the N-glycosylic bond between asparagine and N-acetylglucosamine in the catabolism of N-linked glycoproteins. Previously only three competitive inhibitors, one noncompetitive inhibitor, and one irreversible inhibitor of glycosylasparaginase activity had been reported. Using human glycosylasparaginase from human amniotic fluid, L-aspartic acid and four of its analogues, where the a-amino group was substituted with a chloro, bromo, methyl or hydrogen, were competitive inhibitors having K, values between 0.6–7.7 mM. These results provide supporting evidence for a proposed intramolecular autoproteolytic activation reaction. A proposed phosphono transition state mimic and a sulfo transition state mimic were competitive inhibitors with Ki values 0.9 mM and 1.4 mM, respectively. These results support a mechanism for the enzyme-catalyzed reaction involving formation of a tetra-hedral high-energy intermediate. Three analogues of the natural substrate were noncompetitive inhibitors with Ki values between 0.56–0.75 mM, indicating the presence of a second binding site that may recognize (substituted)acetamido groups.","PeriodicalId":15776,"journal":{"name":"Journal of enzyme inhibition","volume":"40 1","pages":"269 - 274"},"PeriodicalIF":0.0,"publicationDate":"2001-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77548947","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 5

Carbonic Anhydrase Inhibitors: Metal Complexes of a Sulfanilamide Derived Schiff base and their Interaction with Isozymes I, II and IV 碳酸酐酶抑制剂:磺胺衍生席夫碱的金属配合物及其与同工酶I、II和IV的相互作用

Journal of enzyme inhibition Pub Date : 2001-01-01 DOI: 10.1080/14756360127571

M. ul-Hassan, A. Scozzafava, Z. Chohan, C. Supuran

引用次数: 22

An Invertase Inhibitory Protein From Pteris deflexa Link Fronds 一种从鹿角蝶连叶中提取的转化酶抑制蛋白

Journal of enzyme inhibition Pub Date : 2001-01-01 DOI: 10.1080/14756360127573

J. Sayago, M. A. Vattuone, A. Sampietro, M. Isla

{"title":"An Invertase Inhibitory Protein From Pteris deflexa Link Fronds","authors":"J. Sayago, M. A. Vattuone, A. Sampietro, M. Isla","doi":"10.1080/14756360127573","DOIUrl":"https://doi.org/10.1080/14756360127573","url":null,"abstract":"Plant invertases play important roles in sucrose metabolism. Cell wall invertase was reported to participate in phloem loading and unloading. Soluble invertases would be involved in hexose level regulation in mature tissues and in stored sucrose utilization within vacuoles. Invertase inhibitory proteins were described as one of the possible mechanisms for invertase activity regulation in some plant species; nevertheless, these proteins were found only in sink tissues, suggesting that this mechanism would not be relevant in the sucrose turnover of leaves. This report describes the purification of invertase from Pteris deflexa fronds and the occurrence of an invertase inhibitory protein in this fern organ, as well as its purification and invertase-inhibitor interactions. The Mr of the invertase and of its inhibitory protein were 90,000 and 18,000, respectively. SDS-PAGE in the presence of 2-mercaptoetanol gave two subunits for the enzyme (Mr=66,000 and 30,000) and only one for the inhibitor. The inhibitor protein is a glycoprotein (12% w/w of neutral sugars) that did not show agglutinating activity like some others, and also showed a high heat stability at pH 5.0. The optimum pH of invertase activity is 5.0, while invertase inhibitory protein caused maximal inhibition at the same pH value. Invertase-inhibitor complex formation occurs in an immediate manner and a protease activity was discarded. The inhibition is non-competitive (Ki=1.5 × 10 −6 M) without interactions among the binding sites. The complex is slightly dissociable and sucrose was able to partially reduce the inhibitory effect. Up to the present, invertase inhibitory proteins have been found solely in heterotrophic tissues. In this work we demonstrate that this protein is also present in an autotrophic tissue of a lower vascular plant.","PeriodicalId":15776,"journal":{"name":"Journal of enzyme inhibition","volume":"43 1","pages":"517 - 525"},"PeriodicalIF":0.0,"publicationDate":"2001-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85804011","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 6

Quantitative Structure-Activity Relationships (QSARs) Within Series of Inhibitors for Mammalian Cytochromes P450 (CYPs) 哺乳动物细胞色素P450 (CYPs)抑制剂系列的定量构效关系(QSARs)

Journal of enzyme inhibition Pub Date : 2001-01-01 DOI: 10.1080/14756360109162380

D. Lewis, M. Dickins

引用次数: 19

Inhibition of Saccharomyces cerevisiae Phosphomannose Isomerase by the NO-donor S-nitroso-acetyl-penicillamine no供体s -亚硝基乙酰青霉胺对酿酒酵母菌磷酸甘菊糖异构酶的抑制作用

Journal of enzyme inhibition Pub Date : 2001-01-01 DOI: 10.1080/14756360109162377

L. Salvati, M. Mattu, F. Tiberi, F. Polticelli, P. Ascenzi

引用次数: 1

Inhibition of Potato Polyphenol Oxidase by Anions and Activity in Various Carboxylate Buffers (pH 4.8) at Constant Ionic Strength 阴离子对马铃薯多酚氧化酶的抑制作用及其在不同羧酸缓冲液(pH 4.8)中的活性

Journal of enzyme inhibition Pub Date : 2001-01-01 DOI: 10.1080/14756360109162363

Benjamin D. Malkin, Karen R. Thickman, C. Markworth, D. Wilcox, F. Kull

引用次数: 0

Evidence for an Essential Arginine in the Flavoprotein Nitroalkane Oxidase 黄蛋白硝基烷烃氧化酶中存在必需精氨酸的证据

Journal of enzyme inhibition Pub Date : 2001-01-01 DOI: 10.1080/14756360109162365

G. Gadda, A. Banerjee, Gaylon S. Fleming, P. Fitzpatrick

引用次数: 4

Inhibition of Glutamate Carboxypeptidase II by Phosphonamidothionate Derivatives of Glutamic Acid 谷氨酸氨基膦酸衍生物对谷氨酸羧肽酶II的抑制作用

Journal of enzyme inhibition Pub Date : 2001-01-01 DOI: 10.1080/14756360109162384

C. E. Rodríguez, Haiyan Lu, Alicia R. Martinez, Yingying Hu, A. Brunelle, C. Berkman

引用次数: 12

Phospholipase A2 from Trypanosoma brucei gambiense and Trypanosoma brucei brucei: Inhibition by Organotins 冈比亚布氏锥虫和布氏锥虫的磷脂酶A2:有机肽的抑制作用

Journal of enzyme inhibition Pub Date : 2001-01-01 DOI: 10.1080/14756360109162392

M. Shuaibu, H. Kanbara, T. Yanagi, D. Ameh, J. J. Bonire, A. Nok

引用次数: 15