Covalent inhibitors of human monoacylglycerol lipase: ligand-assisted characterization of the catalytic site by mass spectrometry and mutational analysis [0.03%]
用于表征人类单酰基甘油脂肪酶催化位点的配体辅助串联质谱和突变分析的共价抑制剂
Nikolai Zvonok,Lakshmipathi Pandarinathan,John Williams et al.
Nikolai Zvonok et al.
The active site of recombinant hexa-histidine-tagged human monoacylglycerol lipase (hMGL) is characterized by mass spectrometry using the inhibitors 5-((biphenyl-4-yl)methyl)-N,N-dimethyl-2H-tetrazole-2-carboxamide (AM6701), and N-arachidon...
Biochemical and structural insights of the early glycosylation steps in calicheamicin biosynthesis [0.03%]
有关抗-calicheamicins糖基化生物合成早期阶段的生化和结构见解
Changsheng Zhang,Eduard Bitto,Randal D Goff et al.
Changsheng Zhang et al.
The enediyne antibiotic calicheamicin (CLM) gamma(1)(I) is a prominent antitumor agent that is targeted to DNA by a novel aryltetrasaccharide comprised of an aromatic unit and four unusual carbohydrates. Herein we report the heterologous ex...
Development of pyrrole-imidazole polyamide for specific regulation of human aurora kinase-A and -B gene expression [0.03%]
开发针对人类aurora激酶-A和-B基因表达的特异性调节的吡咯-咪唑多胺
Teruyuki Takahashi,Yukihiro Asami,Eiko Kitamura et al.
Teruyuki Takahashi et al.
Pyrrole-imidazole polyamide (PIP) is a nuclease-resistant novel compound that inhibits gene expression through binding to the minor groove of DNA. Human aurora kinase-A (AURKA) and -B (AURKB) are important regulators in mitosis during the c...
Enzymatic macrolactonization in the presence of DNA leading to triostin A analogs [0.03%]
DNA存在下的酶促内酯化反应得到Triostin A类似物
Kento Koketsu,Hiroki Oguri,Kenji Watanabe et al.
Kento Koketsu et al.
Excised thioesterase domains are versatile catalysts for macrocyclization. However, thioesterase-catalyzed cyclization is often precluded due to the occurrence of hydrolysis and product inhibition. To circumvent these obstacles, we devised ...
System-wide investigation of ErbB4 reveals 19 sites of Tyr phosphorylation that are unusually selective in their recruitment properties [0.03%]
针对ErbB4开展的系统性研究发现其具有19个酪氨酸磷酸化位点，并且这些位点在募集能力方面表现得极为特异
Alexis Kaushansky,Andrew Gordus,Bogdan A Budnik et al.
Alexis Kaushansky et al.
The first three members of the ErbB family of receptor tyrosine kinases activate a wide variety of signaling pathways and are frequently misregulated in cancer. Much less is known about ErbB4. Here we use tandem mass spectrometry to identif...
Chemical dissection of the link between streptozotocin, O-GlcNAc, and pancreatic cell death [0.03%]
链脲佐菌素、O-GlcNAc和胰腺细胞死亡之间关系的化学解析
Shalini Pathak,Helge C Dorfmueller,Vladimir S Borodkin et al.
Shalini Pathak et al.
Streptozotocin is a natural product that selectively kills insulin-secreting beta cells, and is widely used to generate mouse models of diabetes or treat pancreatic tumors. Several studies suggest that streptozotocin toxicity stems from its...
Deciphering deazapurine biosynthesis: pathway for pyrrolopyrimidine nucleosides toyocamycin and sangivamycin [0.03%]
去嘌呤生物合成揭秘：toyocamycin和sangivamycin吡咯嘧啶核苷途径
Reid M McCarty,Vahe Bandarian
Reid M McCarty
Pyrrolopyrimidine nucleosides analogs, collectively referred to as deazapurines, are an important class of structurally diverse compounds found in a wide variety of biological niches. In this report, a cluster of genes from Streptomyces rim...
Loop grafting of Bacillus subtilis lipase A: inversion of enantioselectivity [0.03%]
芽孢杆菌脂酶A的环状嫁接：手性选择性转换
Ykelien L Boersma,Tjaard Pijning,Margriet S Bosma et al.
Ykelien L Boersma et al.
Lipases are successfully applied in enantioselective biocatalysis. Most lipases contain a lid domain controlling access to the active site, but Bacillus subtilis Lipase A (LipA) is a notable exception: its active site is solvent exposed. To...
DKxanthene biosynthesis--understanding the basis for diversity-oriented synthesis in myxobacterial secondary metabolism [0.03%]
大黄酮生物合成-理解放线菌次级代谢中导向多样性的合成机制
Peter Meiser,Kira J Weissman,Helge B Bode et al.
Peter Meiser et al.
The DKxanthenes are a family of yellow pigments which play a critical role in myxobacterial development. Thirteen unique structures from Myxococcus xanthus DK1622 differ in the length of their characteristic polyene functionality, as well a...
Cloning, expression, and biochemical characterization of Streptomyces rubellomurinus genes required for biosynthesis of antimalarial compound FR900098 [0.03%]
红斑链霉菌抗疟化合物FR900098生物合成所需的基因克隆、表达及生化特征分析
Andrew C Eliot,Benjamin M Griffin,Paul M Thomas et al.
Andrew C Eliot et al.
The antibiotics fosmidomycin and FR900098 are members of a unique class of phosphonic acid natural products that inhibit the nonmevalonate pathway for isoprenoid biosynthesis. Both are potent antibacterial and antimalarial compounds, but de...