The open enzyme inhibition journal最新文献_第3页

Allosteric Cooperativity in Inhibition of Protein Kinase a Catalytic Subunit 抑制蛋白激酶催化亚基的变构协同性

The open enzyme inhibition journal Pub Date : 2008-06-27 DOI: 10.2174/1874940200801010042

A. Kuznetsov, J. Järv

引用次数: 5

Homocysteine inhibits hydrogen peroxide breakdown by catalase 同型半胱氨酸通过过氧化氢酶抑制过氧化氢分解

The open enzyme inhibition journal Pub Date : 2008-05-27 DOI: 10.2174/1874940200801010034

N. Milton

引用次数: 28

Folate Biosynthesis – Reappraisal of Old and Novel Targets in the Search for New Antimicrobials 叶酸生物合成-在寻找新的抗菌剂中对新旧靶点的重新评价

The open enzyme inhibition journal Pub Date : 2008-05-20 DOI: 10.2174/1874940200801010012

J. Swarbrick, P. Iliades, J. Simpson, I. Macreadie

{"title":"Folate Biosynthesis – Reappraisal of Old and Novel Targets in the Search for New Antimicrobials","authors":"J. Swarbrick, P. Iliades, J. Simpson, I. Macreadie","doi":"10.2174/1874940200801010012","DOIUrl":"https://doi.org/10.2174/1874940200801010012","url":null,"abstract":"Folate biosynthesis remains a key target for antimicrobial therapy. Folate is an essential vitamin (vitamin B9) that is required for many one-carbon transfer reactions and is a critical precursor for the biosynthesis of purines, pyrimidi- nes, and amino acids. Unlike higher eukaryotes that scavenge preformed folates, prokaryotic and lower eukaryotic micro- organisms are dependent on several enzymes for the de novo biosynthesis of folate. One of these enzymes, dihydropte- roate synthase (DHPS), is the target of the first chemically-synthesized antimicrobial agents, the sulfadrugs, which date back to the 1940s. Others are essential enzymes that remain to be explored as drug targets. Resistance to the sulfadrugs rapidly emerges due to the ability of the microbe to alter its susceptibility to the drug by various means. Recently a num- ber of new structures of the enzymes in the pathway has become available. We review the recent literature relating to these targets (the enzymes: GTP cyclohydrolase (GTP-CH); 7,8-dihydroneopterin aldolase (DHNA), 6-hydroxymethyl- 7,8-dihydropterin pyrophosphokinase (HPPK), dihydropteroate synthase (DHPS), dihydrofolate synthase (DHFS)), their mode of action and how current drugs may modulate this on a structural level. Furthermore, these data advance our un- derstanding of the emergence of drug resistance and may aid efforts and play a major role in the design of new, more ef- fective compounds as antimicrobial agents. To this end we also review the recent literature in the development of inhibi- tors of these enzymes. Future progress in this key area has the potential to benefit the war against devastating organisms such as drug-resistant Staphylococcus aureus and Plasmodium falciparum.","PeriodicalId":89033,"journal":{"name":"The open enzyme inhibition journal","volume":"1 1","pages":"12-33"},"PeriodicalIF":0.0,"publicationDate":"2008-05-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68095266","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: 38

Lithium Promotes Adult Neural Progenitor Differentiation Via GSK3β- Dependent Signaling Pathways 锂通过依赖GSK3β的信号通路促进成体神经祖细胞分化

The open enzyme inhibition journal Pub Date : 2008-04-18 DOI: 10.2174/1874940200801010005

Heinrich F. Bürgers, Dominik W. Schelshorn, W. Kuschinsky, M. Maurer

{"title":"Lithium Promotes Adult Neural Progenitor Differentiation Via GSK3β- Dependent Signaling Pathways","authors":"Heinrich F. Bürgers, Dominik W. Schelshorn, W. Kuschinsky, M. Maurer","doi":"10.2174/1874940200801010005","DOIUrl":"https://doi.org/10.2174/1874940200801010005","url":null,"abstract":"Lithium is one of the standard drugs in the treatment of bipolar disorder, although its molecular modes of ac- tion are not well understood. It is a potent inhibitor of the multifunctional enzyme Glycogen Synthase Kinase 3s (GSK3s), which also plays a central role in neurogenesis via the developmental Wnt signaling pathway. In the present study, we analyzed the influence of lithium on GSK3s signaling in adult neural progenitor cells (NPCs) from the rat sub- ventricular zone. Protein expression patterns of NPCs cultured in the presence of 20 mM lithium chloride were compared to those of untreated cells. A proteomic approach based on two-dimensional gel electrophoresis and mass spectrometry showed changes in several GSK3s-related proteins. We demonstrate the inhibition of GSK3s by stabilization and nuclear transfer of its downstream target, s-catenin. Moreover, the phosphorylated (=inhibited) GSK3s protein was strongly enri- ched in the nuclear fraction of lithium-treated cells. The fraction of cells differentiated into astroglia increased moderately, and the fraction of cells differentiated into neurons increased strongly, as shown by immunostaining. In conclusion, li- thium promotes NPC differentiation, mainly to neurons, via GSK3s-related pathways.","PeriodicalId":89033,"journal":{"name":"The open enzyme inhibition journal","volume":"1 1","pages":"5-11"},"PeriodicalIF":0.0,"publicationDate":"2008-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68095252","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: 0

Ca Chelators and Membrane Transport: “Geometric” Considerations 钙螯合剂和膜运输:“几何”考虑

The open enzyme inhibition journal Pub Date : 2008-04-04 DOI: 10.2174/1874940200801010001

Ronald F. Abercrombiea, James E. Moore

引用次数: 0