Small molecule recognition of c-Src via the Imatinib-binding conformation [0.03%]
伊马替尼结合构象的小分子c-Src识别
Arvin C Dar,Michael S Lopez,Kevan M Shokat
Arvin C Dar
The cancer drug, Imatinib, is a selective Abl kinase inhibitor that does not inhibit the closely related kinase c-Src. This one drug and its ability to selectively inhibit Abl over c-Src has been a guiding principle in virtually all kinase ...
Brian C Smith,William C Hallows,John M Denu
Brian C Smith
Sirtuins are critical regulators of many cellular processes, including insulin secretion, the cell cycle, and apoptosis. Sirtuins are associated with a variety of age-associated diseases such as type II diabetes, obesity, and Alzheimer's di...
Sabesan Yoganathan,John C Vederas
Sabesan Yoganathan
Haloduracin is a bacterially produced antibiotic system of two alkali-stable peptides (Halalpha and Halbeta) that have extensive posttranslational modifications, including lanthionine rings. Now, Cooper et al. (2008) revise the structure of...
Divergence of catalytic mechanism within a glycosidase family provides insight into evolution of carbohydrate metabolism by human gut flora [0.03%]
糖苷酶家族催化机制的分歧为肠道菌群碳水化合物代谢进化提供了见解
Tracey M Gloster,Johan P Turkenburg,Jennifer R Potts et al.
Tracey M Gloster et al.
Enzymatic cleavage of the glycosidic bond yields products in which the anomeric configuration is either retained or inverted. Each mechanism reflects the dispositions of the enzyme functional groups; a facet of which is essentially conserve...
Structure-guided development of efficacious antifungal agents targeting Candida glabrata dihydrofolate reductase [0.03%]
基于结构的开发有效的针对光滑假丝酵母二氢叶酸还原酶的抗真菌剂
Jieying Liu,David B Bolstad,Adrienne E Smith et al.
Jieying Liu et al.
Candida glabrata is a lethal fungal pathogen resistant to many antifungal agents and has emerged as a critical target for drug discovery. Over the past several years, we have been developing a class of propargyl-linked antifolates as antimi...
Directed evolution of streptavidin variants using in vitro compartmentalization [0.03%]
应用体外间隔室法对链霉抗生物素蛋白变异体进行定向进化
Matthew Levy,Andrew D Ellington
Matthew Levy
We have developed and implemented an in vitro compartmentalization (IVC) selection scheme for the identification of streptavidin (SA) variants with altered specificities for the biotin analog desthiobiotin. Wild-type SA and selected variant...
Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries [0.03%]
通过筛选现有的药物库鉴定人组织.transglutaminase的化学抑制剂
Thung-S Lai,Yusha Liu,Tim Tucker et al.
Thung-S Lai et al.
Human tissue transglutaminase (TGM2) is a calcium-dependent crosslinking enzyme involved in the posttranslational modification of intra- and extracellular proteins and implicated in several neurodegenerative diseases. To find specific inhib...
The human protease inhibitor cystatin C is an activating cofactor for the streptococcal cysteine protease IdeS [0.03%]
人蛋白酶抑制剂胱抑素C是链球菌半胱氨酸蛋白酶IdeS的激活辅助因子
Bjarne Vincents,Reine Vindebro,Magnus Abrahamson et al.
Bjarne Vincents et al.
Human cystatin C is considered the physiologically most important inhibitor of endogenous papain-like cysteine proteases. We present here an unexpected function of cystatin C. Instead of acting as an inhibitor, cystatin C acts as a facultat...
Functional analysis of MycCI and MycG, cytochrome P450 enzymes involved in biosynthesis of mycinamicin macrolide antibiotics [0.03%]
MycCI和MycG的功能分析，它们是合成mycinamicin大环内酯类抗生素的细胞色素P450酶
Yojiro Anzai,Shengying Li,Mani Raj Chaulagain et al.
Yojiro Anzai et al.
Macrolides are a class of valuable antibiotics that include a macrolactone ring, at least one appended sugar unit, and, in most cases, additional hydroxyl or epoxide groups installed by cytochrome P450 enzymes. These functional groups contr...