Potent and selective peptidyl boronic acid inhibitors of the serine protease prostate-specific antigen [0.03%]
Aaron M LeBeau,Pratap Singh,John T Isaacs et al.
Aaron M LeBeau et al.
Prostate cancer cells produce high (microgram to milligram/milliliter) levels of the serine protease Prostate-Specific Antigen (PSA). PSA is enzymatically active in the extracellular fluid surrounding prostate cancers but is found at 1,000-...
Natural Sphingomonas glycolipids vary greatly in their ability to activate natural killer T cells [0.03%]
Yuki Kinjo,Bo Pei,Simone Bufali et al.
Yuki Kinjo et al.
Mouse natural killer T (NKT) cells expressing an invariant T cell antigen receptor (TCR) recognize glycosphingolipids (GSLs) from Sphingomonas bacteria. The synthetic antigens previously tested, however, were designed to closely resemble th...
The small-molecule iron transport inhibitor ferristatin/NSC306711 promotes degradation of the transferrin receptor [0.03%]
Lior Horonchik,Marianne Wessling-Resnick
Lior Horonchik
Iron delivery by transferrin (Tf) is accomplished through clathrin-mediated endocytosis of Tf receptors. The small molecule NSC306711 inhibits iron uptake from the Tf-TfR pathway. Here we show that the drug's mechanism of action is to induc...
Jiehua Zhou,John J Rossi
Jiehua Zhou
Aptamers, sometimes termed "chemical antibodies," have been engineered into multimerized versions for therapeutic application. The groups of Gilboa and Sullenger now report the development of a bivalent aptamer-molecular device as a recepto...
Pooja Arora,Steven A Porcelli
Pooja Arora
In this issue of Chemistry & Biology, Kinjo et al. (2008) propose that the addition of oligosaccharides to the core outer membrane glycosphingolipid in Sphingomonas spp. may be an adaptation that allows bacteria to evade recognition by Natu...
Leslie Pray
Leslie Pray
Incomplete beta-ketone processing as a mechanism for polyene structural variation in the FR-008/candicidin complex [0.03%]
FR-008/ candicidin 复合聚烯类化合物的结构多态性及其β-酮基不完全加工机制研究
Yongjun Zhou,Jialiang Li,Jing Zhu et al.
Yongjun Zhou et al.
FR-008/candicidin is a heptaene macrolide with established antifungal activity, produced by Streptomyces sp. FR-008 as a complex mixture of compounds. Here, six components (FR-008-I to -VI) of the FR-008/candicidin complex were determined; ...
Quantification of real-time Salmonella effector type III secretion kinetics reveals differential secretion rates for SopE2 and SptP [0.03%]
量化沙门氏菌效应蛋白III型分泌动力学的速率发现SopE2和SptP的分泌速率不同
Schuyler B Van Engelenburg,Amy E Palmer
Schuyler B Van Engelenburg
Gram-negative pathogenic bacteria such as Salmonella utilize the type III secretion system to inject bacterial effector proteins into a host cell. Upon entry, these effectors bind mammalian cell proteins, hijack cellular signaling pathways,...
Redesigning enzymes based on adaptive evolution for optimal function in synthetic metabolic pathways [0.03%]
基于适应性进化优化酶在合成代谢途径中功能的从头设计
Yasuo Yoshikuni,Jeffrey A Dietrich,Farnaz F Nowroozi et al.
Yasuo Yoshikuni et al.
Nature has balanced most metabolic pathways such that no one enzyme in the pathway controls the flux through that pathway. However, unnatural or nonnative, constructed metabolic pathways may have limited product flux due to unfavorable in v...
A structural view of the inactivation of the SARS coronavirus main proteinase by benzotriazole esters [0.03%]
苯并三唑酯类化合物灭活冠状病毒主要蛋白酶的结构观点
Koen H G Verschueren,Ksenia Pumpor,Stefan Anemüller et al.
Koen H G Verschueren et al.
The main proteinase (M(pro)) of the severe acute respiratory syndrome (SARS) coronavirus is a principal target for the design of anticoronaviral compounds. Benzotriazole esters have been reported as potent nonpeptidic inhibitors of the enzy...