Identification of Compounds That Decrease Glioblastoma Growth and Glucose Uptake in Vitro.

abstract：:Enzymatic plasticity, as a modern term referring to the functional conversion of an enzyme, is significant for enzymatic activity redesign. The bacterial diterpene cyclase CotB2 is a typical plastic enzyme by which its native form precisely conducts a chemical reaction while its mutants diversify the catalytic functio...

journal_title：ACS chemical biology

authors： Tang X,Zhang F,Zeng T,Li W,Yin S,Wu R

更新日期：2020-10-16 00:00:00

abstract：:Histo-blood group epitopes are fucosylated branched oligosaccharides with well-defined conformations in solution that are recognized by receptors, such as lectins from pathogens. We report here the results of a series of experimental and computational endeavors revealing the unusual distortion of histo-blood group ant...

journal_title：ACS chemical biology

authors： Topin J,Lelimousin M,Arnaud J,Audfray A,Pérez S,Varrot A,Imberty A

更新日期：2016-07-15 00:00:00

abstract：:Cocaine esterase (CocE) is known as the most efficient natural enzyme for cocaine hydrolysis. The major obstacle to the clinical application of wild-type CocE is the thermoinstability with a half-life of only ∼12 min at 37 °C. The previously designed T172R/G173Q mutant (denoted as enzyme E172-173) with an improved in ...

journal_title：ACS chemical biology

authors： Fang L,Chow KM,Hou S,Xue L,Chen X,Rodgers DW,Zheng F,Zhan CG

更新日期：2014-08-15 00:00:00

abstract：:Transcriptomes provide a myriad of potential RNAs that could be the targets of therapeutics or chemical genetic probes of function. Cell-permeable small molecules, however, generally do not exploit these targets, owing to the difficulty in the design of high affinity, specific small molecules targeting RNA. As part of...

journal_title：ACS chemical biology

authors： Rzuczek SG,Gao Y,Tang ZZ,Thornton CA,Kodadek T,Disney MD

更新日期：2013-10-18 00:00:00

abstract：:Pathogenic Yersinia spp. secrete the effector YopJ (YopP) into host cells to counteract cytokine production and to induce programmed cell death (apoptosis). YopJ achieves these aims by inactivating mitogen-activated protein kinase (MAPK) and nuclear factor kappaB signaling pathways. YopJ was shown to bind to members o...

journal_title：ACS chemical biology

authors： Bliska JB

更新日期：2006-07-21 00:00:00

abstract：:Targeting native progenitors with small molecule pharmaceuticals that direct cell fate decisions is an attractive approach for regenerative medicine. Here, we show that 3,5-disubstituted isoxazoles (Isx), stem cell-modulator small molecules originally recovered in a P19 embryonal carcinoma cell-based screen, directed ...

journal_title：ACS chemical biology

authors： Russell JL,Goetsch SC,Aguilar HR,Frantz DE,Schneider JW

更新日期：2012-06-15 00:00:00

abstract：:Originally discovered as part of an adaptive bacterial defense system against the invasion of foreign phages, programmable CRISPR-Cas nucleases have emerged as remarkable enzymes with transformative potential for both biological research and clinical application. CRISPR-Cas nucleases likely evolved in their natural co...

journal_title：ACS chemical biology

authors： Tsai SQ

更新日期：2018-02-16 00:00:00

abstract：:Stapled peptides have great potential as modulators of protein-protein interactions (PPIs). However, there is a vast landscape of chemical features that can be varied for any given peptide, and identifying a set of features that maximizes cellular uptake and subsequent target engagement remains a key challenge. Herein...

journal_title：ACS chemical biology

authors： Wu Y,Kaur A,Fowler E,Wiedmann MM,Young R,Galloway WRJD,Olsen L,Sore HF,Chattopadhyay A,Kwan TT,Xu W,Walsh SJ,de Andrade P,Janecek M,Arumugam S,Itzhaki LS,Lau YH,Spring DR

更新日期：2019-03-15 00:00:00

abstract：:Toxic heavy metals have been considered to be harmful environmental contaminations. The molecular mechanisms of heavy-metals-induced cytotoxicity and carcinogenicity are still not well elucidated. Previous reports showed exposures to toxic heavy metals can cause a change of DNA cytosine methylation (5-methylcytosine, ...

journal_title：ACS chemical biology

authors： Xiong J,Liu X,Cheng QY,Xiao S,Xia LX,Yuan BF,Feng YQ

更新日期：2017-06-16 00:00:00

abstract：:C-methylation of aromatic small molecules by C-methyltransferases (C-MTs) is an important biological transformation that involves C-C bond formation using S-adenosyl-l-methionine (SAM) as the methyl donor. Here, two advances in the mechanistic understanding of C-methylation of the 8-position of coumarin substrates cat...

journal_title：ACS chemical biology

authors： Sadler JC,Chung CH,Mosley JE,Burley GA,Humphreys LD

更新日期：2017-02-17 00:00:00

abstract：:Desferrioxamine B (DFOB) was discovered in the late 1950s as a hydroxamic acid metabolite of the soil bacterium Streptomyces pilosus. The exquisite affinity of DFOB for Fe(III) identified its potential for removing excess iron from patients with transfusion-dependent hemoglobin disorders. Many studies have used semisy...

journal_title：ACS chemical biology

authors： Codd R,Richardson-Sanchez T,Telfer TJ,Gotsbacher MP

更新日期：2018-01-19 00:00:00

abstract：:Kinases constitute an important class of therapeutic targets being explored both by academia and the pharmaceutical industry. The major focus of this effort was directed toward the identification of ATP competitive inhibitors. Although it has long been recognized that the intracellular concentration of ATP is very dif...

journal_title：ACS chemical biology

authors： Thorarensen A,Banker ME,Fensome A,Telliez JB,Juba B,Vincent F,Czerwinski RM,Casimiro-Garcia A

更新日期：2014-07-18 00:00:00

abstract：:A Natural Compound Library containing myxobacterial secondary metabolites was screened in murine macrophages for novel activators of IL-1β maturation and secretion. The most potent of three hits in total was a so far undescribed metabolite, which was identified from the myxobacterium Hyalangium minutum strain Hym3. Wh...

journal_title：ACS chemical biology

authors： Surup F,Chauhan D,Niggemann J,Bartok E,Herrmann J,Keck M,Zander W,Stadler M,Hornung V,Müller R

更新日期：2018-10-19 00:00:00

abstract：:Dihydrofolate reductase (DHFR) is a potential drug target for Trypanosoma brucei, a human parasite, which is the causative agent for African sleeping sickness. No drug is available against this target, since none of the classical antifolates such as pyrimethamine (PYR), cycloguanil, or trimethoprim are effective as se...

journal_title：ACS chemical biology

authors： Vanichtanankul J,Taweechai S,Yuvaniyama J,Vilaivan T,Chitnumsub P,Kamchonwongpaisan S,Yuthavong Y

更新日期：2011-09-16 00:00:00

abstract：:Drug resistance continues to be a growing global problem. The efficacy of small molecule inhibitors is threatened by pools of genetic diversity in all systems, including antibacterials, antifungals, cancer therapeutics, and antivirals. Resistant variants often include combinations of active site mutations and distal "...

journal_title：ACS chemical biology

authors： Henes M,Lockbaum GJ,Kosovrasti K,Leidner F,Nachum GS,Nalivaika EA,Lee SK,Spielvogel E,Zhou S,Swanstrom R,Bolon DNA,Kurt Yilmaz N,Schiffer CA

更新日期：2019-11-15 00:00:00

abstract：:To discover chemical probes to further under-stand the function of individual DNA polymerases, we established a generally applicable high-throughput screening. By applying this technique we discovered three novel inhibitor classes of human DNA polymerase λ (DNA Pol λ), a key enzyme to maintain the genetic integrity of...

journal_title：ACS chemical biology

authors： Strittmatter T,Bareth B,Immel TA,Huhn T,Mayer TU,Marx A

更新日期：2011-04-15 00:00:00

abstract：:N-Acetylneuraminic acid lyase (NAL) is a Class I aldolase that catalyzes the reversible condensation of pyruvate with N-acetyl-d-mannosamine (ManNAc) to yield the sialic acid N-acetylneuraminic acid (Neu5Ac). Aldolases are finding increasing use as biocatalysts for the stereospecific synthesis of complex molecules. In...

journal_title：ACS chemical biology

authors： Daniels AD,Campeotto I,van der Kamp MW,Bolt AH,Trinh CH,Phillips SE,Pearson AR,Nelson A,Mulholland AJ,Berry A

更新日期：2014-04-18 00:00:00

abstract：:WS9326A and annimycin are produced by Streptomyces asterosporus DSM 41452. WS9326A is a nonribosomal peptide synthetase-(NRPS-) derived depsipeptide containing a cinnamoyl moiety, while annimycin is a linear polyketide bearing a 2-amino-3-hydroxycyclopent-2-enone (C5N) group. Both gene clusters have been sequenced and...

journal_title：ACS chemical biology

authors： Zhu J,Zhang S,Zechel DL,Paululat T,Bechthold A

更新日期：2019-08-16 00:00:00

abstract：:Cell-permeable small molecules can be used to modulate protein function selectively, rapidly, reversibly, and conditionally with temporal and quantitative control in biological systems. The identification of these chemical probes can require the screening of large numbers of small molecules. With the advent of new tec...

journal_title：ACS chemical biology

authors： Nicholson RL,Welch M,Ladlow M,Spring DR

更新日期：2007-01-23 00:00:00

abstract：:Secreted tyrosinase from melanin-forming Streptomyces avermitilis MA4680 was involved in both ortho-hydroxylation and further oxidation of trans-resveratrol, leading to the formation of melanin. This finding was confirmed by constructing deletion mutants of melC(2) and melD(2) encoding extracellular and intracellular ...

journal_title：ACS chemical biology

authors： Lee N,Kim EJ,Kim BG

更新日期：2012-10-19 00:00:00

abstract：:Regorafenib (Stivarga) is an oral small molecule kinase inhibitor used to treat metastatic colorectal cancer, hepatocellular carcinomas, and gastrointestinal stromal tumors. Diarrhea is one of the most frequently observed adverse reactions associated with regorafenib. This toxicity may arise from the reactivation of t...

journal_title：ACS chemical biology

authors： Ervin SM,Hanley RP,Lim L,Walton WG,Pearce KH,Bhatt AP,James LI,Redinbo MR

更新日期：2019-12-20 00:00:00

abstract：:Fatty acylation or lipid modification of proteins controls their cellular activation and diverse roles in physiology. It mediates protein-protein and protein-membrane interactions and plays an important role in regulating cellular signaling pathways. Currently, there is need for visualizing lipid modifications of prot...

journal_title：ACS chemical biology

authors： Hannoush RN,Arenas-Ramirez N

更新日期：2009-07-17 00:00:00

abstract：:Epitranscriptomic modifications play an important role in RNA function and can impact gene expression. Here, we apply a chemical proteomics approach to investigate readers of N1-methyladenosine (m1A), a poorly characterized modification on mammalian mRNA. We find that YTHDF proteins, known m6A readers, recognize m1A-m...

journal_title：ACS chemical biology

authors： Seo KW,Kleiner RE

更新日期：2020-01-17 00:00:00

abstract：:Polyhalogenated dibenzo-p-dioxins are arguably among the most toxic molecules known to man. In addition to anthropogenic sources, marine invertebrates also harbor polybrominated dibenzo-p-dioxins of as yet unknown biogenic origin. Here, we report that the bmp gene locus in marine bacteria, a recently characterized sou...

journal_title：ACS chemical biology

authors： Agarwal V,Moore BS

更新日期：2014-09-19 00:00:00

abstract：:Base deamination is a common type of DNA damage that occurs in all organisms. DNA repair mechanisms are critical to maintain genome integrity, in which the base excision repair pathway plays an essential role. In the BER pathway, the uracil DNA glycosylase superfamily is responsible for removing the deaminated bases f...

journal_title：ACS chemical biology

authors： Zhang Z,Shen J,Yang Y,Li J,Cao W,Xie W

更新日期：2016-06-17 00:00:00

abstract：:Dicamba monooxygenase (DMO) catalyzes the O-demethylation of dicamba (3,6-dichloro-2-methoxybenzoate) to produce 3,6-dichlorosalicylate and formaldehyde. Recent crystallographic studies suggest that DMO catalyzes the challenging oxidation of a saturated C-H bond within the methyl group of dicamba to form a hemiacetal ...

journal_title：ACS chemical biology

authors： Jiang W,Wilson MA,Weeks DP

更新日期：2013-08-16 00:00:00

abstract：:Botulinum neurotoxins (BoNTs) are the most potent toxins known to man and a significant threat as weapons of bioterrorism. BoNTs contain a metalloprotease domain that blocks neurotransmitter release in nerve terminals, resulting in a descending, flaccid paralysis with a 5-10% mortality rate. Existing treatment options...

journal_title：ACS chemical biology

authors： Garland M,Babin BM,Miyashita SI,Loscher S,Shen Y,Dong M,Bogyo M

更新日期：2019-01-18 00:00:00

abstract：:The anticancer molecule taxol (Paclitaxel) stands as one of the most medically and economically important natural products. However, despite decades of extensive study, its biosynthesis remains poorly understood. Unpredictable behavior of the first oxygenation enzyme, taxadiene-5α-hydroxylase, which produces a range o...

journal_title：ACS chemical biology

authors： Edgar S,Zhou K,Qiao K,King JR,Simpson JH,Stephanopoulos G

更新日期：2016-02-19 00:00:00

abstract：:Streptolysin S (SLS) is a post-translationally modified peptide cytolysin that is produced by the human pathogen Streptococcus pyogenes. SLS belongs to a large family of azole-containing natural products that are biosynthesized via an evolutionarily conserved pathway. SLS is an important virulence factor during S. pyo...

journal_title：ACS chemical biology

authors： Maxson T,Deane CD,Molloy EM,Cox CL,Markley AL,Lee SW,Mitchell DA

更新日期：2015-05-15 00:00:00

abstract：:The quest for ever more selective kinase inhibitors as potential future drugs has yielded a large repertoire of chemical probes that are selective for specific kinase conformations. These probes have been useful tools to obtain structural snapshots of kinase conformational plasticity. Similarly, kinetic and thermodyna...

journal_title：ACS chemical biology

authors： Tong M,Seeliger MA

更新日期：2015-01-16 00:00:00