Sarah H Lawrence,Ursula D Ramirez,Lei Tang et al.
Sarah H Lawrence et al.
Enzymes that regulate their activity by modulating an equilibrium of alternate, nonadditive, functionally distinct oligomeric assemblies (morpheeins) constitute a recently described mode of allostery. The oligomeric equilibrium for porphobi...
Optimization of taxane binding to microtubules: binding affinity dissection and incremental construction of a high-affinity analog of paclitaxel [0.03%]
紫杉烷与微管结合的优化：亲和力分析及高亲和力紫杉醇类似物的构建
Ruth Matesanz,Isabel Barasoain,Chun-Gang Yang et al.
Ruth Matesanz et al.
The microtubule binding affinities of a series of synthetic taxanes have been measured with the aims of dissecting individual group contributions and obtaining a rationale for the design of novel compounds with the ability to overcome drug ...
Characterization of orphan monooxygenases by rapid substrate screening using FT-ICR mass spectrometry [0.03%]
运用傅里叶变换回旋共振质谱技术快速筛选底物表征孤儿单氧酶
Toshiki Furuya,Tatsunari Nishi,Daisuke Shibata et al.
Toshiki Furuya et al.
Characterization of orphan enzymes, for which the catalytic functions and actual substrates are still not elucidated, is a significant challenge in the postgenomic era. Here, we describe a general strategy for exploring the catalytic potent...
Fiona Girdler,Fabio Sessa,Simona Patercoli et al.
Fiona Girdler et al.
Aurora kinases have emerged as potential targets in cancer therapy, and several drugs are currently undergoing preclinical and clinical validation. Whether clinical resistance to these drugs can arise is unclear. We exploited a hypermutagen...
A universal screening assay for glycosynthases: directed evolution of glycosynthase XynB2(E335G) suggests a general path to enhance activity [0.03%]
甘露糖基转移酶甘酰化酶的通用筛选试验：XynB2（E335G）甘酰化酶的定向进化为其活性增强提出了一种普遍途径
Alon Ben-David,Gil Shoham,Yuval Shoham
Alon Ben-David
Glycosynthases are catalytic mutants of mainly retaining glycoside hydrolases that catalyze the synthesis of oligosaccharides from their corresponding glycosyl-fluoride donors and suitable acceptors. Here we describe the development of a ge...
Crystal structures of lipoglycopeptide antibiotic deacetylases: implications for the biosynthesis of A40926 and teicoplanin [0.03%]
脂糖肽类抗生素脱乙酰酶的晶体结构及对A40926和替考拉宁生物合成的意义
Yaozhong Zou,Joseph S Brunzelle,Satish K Nair
Yaozhong Zou
The lipoglycopeptide antibiotics teicoplanin and A40926 have proven efficacy against Gram-positive pathogens. These drugs are distinguished from glycopeptide antibiotics by N-linked long chain acyl-D-glucosamine decorations that contribute ...
Molecular genetic mining of the Aspergillus secondary metabolome: discovery of the emericellamide biosynthetic pathway [0.03%]
曲霉属次级代谢组的分子遗传挖掘——emericellamide生物合成途径的研究
Yi-Ming Chiang,Edyta Szewczyk,Tania Nayak et al.
Yi-Ming Chiang et al.
The recently sequenced genomes of several Aspergillus species have revealed that these organisms have the potential to produce a surprisingly large range of natural products, many of which are currently unknown. We have found that A. nidula...
Andrea G Cochran
Andrea G Cochran
Aurora kinases are important mitotic regulators, and Aurora kinase inhibitors are under investigation as treatments for cancer. An ongoing debate in the field is which Aurora kinase is the better drug target. A new study (Girdler et al., 20...
Raquell M Holmes,Leslie M Loew
Raquell M Holmes
Through live cell imaging and computational modeling, Neves et al. (2008) demonstrate that molecular interactions alone are insufficient to explain the patterns of MAPK activation: a model must include the cell morphology and spatial distri...
Wendy Wolfson
Wendy Wolfson