Characterization of an Antibacterial Agent Targeting Ferrous Iron Transport Protein FeoB against Staphylococcus aureus and Gram-Positive Bacteria.

abstract：:Apicomplexan parasites, including Plasmodium falciparum and Toxoplasma gondii, the causative agents of severe malaria and toxoplasmosis, respectively, undergo several critical developmental transitions during their lifecycle. Most important for human pathogenesis is the asexual cycle, in which parasites undergo rounds...

journal_title：ACS chemical biology

authors： Howard BL,Harvey KL,Stewart RJ,Azevedo MF,Crabb BS,Jennings IG,Sanders PR,Manallack DT,Thompson PE,Tonkin CJ,Gilson PR

更新日期：2015-04-17 00:00:00

abstract：:N-methyl-d-aspartate receptors (NMDARs) mediate glutamatergic signaling that is critical to cognitive processes in the central nervous system, and NMDAR hypofunction is thought to contribute to cognitive impairment observed in both schizophrenia and Alzheimer's disease. One approach to enhance the function of NMDAR is...

journal_title：ACS chemical biology

authors： Kutchukian PS,Warren L,Magliaro BC,Amoss A,Cassaday JA,O'Donnell G,Squadroni B,Zuck P,Pascarella D,Culberson JC,Cooke AJ,Hurzy D,Schlegel KS,Thomson F,Johnson EN,Uebele VN,Hermes JD,Parmentier-Batteur S,Finley M

更新日期：2017-02-17 00:00:00

abstract：:ABCG2 is a membrane-localized, human transporter protein that has been demonstrated to reduce the intracellular accumulation of substrates through ATP-dependent efflux. Highly expressed in placental syncytiotrophoblasts, brain microvasculature, and the gastrointestinal tract, ABCG2 has been shown to mediate normal tis...

journal_title：ACS chemical biology

authors： Henrich CJ,Robey RW,Takada K,Bokesch HR,Bates SE,Shukla S,Ambudkar SV,McMahon JB,Gustafson KR

更新日期：2009-08-21 00:00:00

abstract：:Chemical cross-linking is well-established for investigating protein-protein interactions. Traditionally, photo cross-linking is used but is associated with problems of selectivity and UV toxicity in a biological context. We here describe, with live cells and under normal growth conditions, selective cross-linking of ...

journal_title：ACS chemical biology

authors： Vannecke W,Ampe C,Van Troys M,Beltramo M,Madder A

更新日期：2017-08-18 00:00:00

abstract：:Changes in glycosylation are correlated to disease and associated with differentiation processes. Experimental tools are needed to investigate the physiological implications of these changes either by labeling of the modified glycans or by blocking their biosynthesis. N-Acetylgalactosamine (GalNAc) is a monosaccharide...

journal_title：ACS chemical biology

authors： Pouilly S,Bourgeaux V,Piller F,Piller V

更新日期：2012-04-20 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：:Proteotoxicity has long been considered a key factor in mitochondrial dysfunction and human disease. The origin of the endogenous offending toxic substrates and the regulatory pathways to deal with these insults, however, have remained unclear. Mitochondria maintain a compartmentalized gene expression system that in a...

journal_title：ACS chemical biology

authors： Battersby BJ,Richter U,Safronov O

更新日期：2019-11-15 00:00:00

abstract：:Lipids are emerging as key regulators of fundamental cellular processes including cell survival, division, and death. Apoptosis, a form of programmed cell death, is accompanied by numerous membrane-related phenotypic changes. However, we have an incomplete understanding of the involvement of specific lipid structures ...

journal_title：ACS chemical biology

authors： Li N,Lizardo DY,Atilla-Gokcumen GE

更新日期：2016-09-16 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：:Sublancin 168 is a member of a small group of glycosylated antimicrobial peptides known as glycocins. The solution structure of sublancin 168, a 37-amino-acid peptide produced by Bacillus subtilis 168, has been solved by nuclear magnetic resonance (NMR) spectroscopy. Sublancin comprises two α-helices and a well-define...

journal_title：ACS chemical biology

authors： Garcia De Gonzalo CV,Zhu L,Oman TJ,van der Donk WA

更新日期：2014-03-21 00:00:00

abstract：:Cutaneous leishmaniasis remains ignored in therapeutic drug discovery programs worldwide. This is mainly because cutaneous leishmaniasis is frequently a disease of impoverished populations in countries where funds are limited for research and patient care. However, the health burden of individuals in endemic areas man...

journal_title：ACS chemical biology

authors： Sharlow ER,Leimgruber S,Murray S,Lira A,Sciotti RJ,Hickman M,Hudson T,Leed S,Caridha D,Barrios AM,Close D,Grögl M,Lazo JS

更新日期：2014-03-21 00:00:00

abstract：:Invertebrate animal models (mainly the nematode Caenorhabditis elegans and the fruit fly Drosophila melanogaster) are gaining momentum as screening tools in drug discovery. These organisms combine genetic amenability, low cost, and culture conditions compatible with large-scale screens. Their main advantage is to allo...

journal_title：ACS chemical biology

authors： Ségalat L

更新日期：2007-04-24 00:00:00

abstract：:The rational design of environmentally sensitive dyes with superior properties is critical for elucidating the fundamental biological processes and understanding the biophysical behavior of cell membranes. In this study, a novel group of fluorene-based push-pull probes was developed for imaging membrane lipids. The de...

journal_title：ACS chemical biology

authors： Shaya J,Collot M,Bénailly F,Mahmoud N,Mély Y,Michel BY,Klymchenko AS,Burger A

更新日期：2017-12-15 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：:This Letter reports a family of novel antimicrobial compounds obtained by combining peptide library screening with structure-based design. Library screening led to the identification of a human LL-37 peptide resistant to chymotrypsin. This d-amino-acid-containing peptide template was active against Escherichia coli bu...

journal_title：ACS chemical biology

authors： Wang G,Hanke ML,Mishra B,Lushnikova T,Heim CE,Chittezham Thomas V,Bayles KW,Kielian T

更新日期：2014-09-19 00:00:00

abstract：:Bacterial tRNA-guanine transglycosylase (Tgt) is involved in the biosynthesis of the modified tRNA nucleoside queuosine present in the anticodon wobble position of tRNAs specific for aspartate, asparagine, histidine, and tyrosine. Inactivation of the tgt gene leads to decreased pathogenicity of Shigella bacteria. Ther...

journal_title：ACS chemical biology

authors： Nguyen A,Nguyen D,Phong Nguyen TX,Sebastiani M,Dörr S,Hernandez-Alba O,Debaene F,Cianférani S,Heine A,Klebe G,Reuter K

更新日期：2020-11-20 00:00:00

abstract：:A complication of diabetes is the inability of wounds to heal in diabetic patients. Diabetic wounds are refractory to healing due to the involvement of activated matrix metalloproteinases (MMPs), which remodel the tissue resulting in apoptosis. There are no readily available methods that identify active unregulated MM...

journal_title：ACS chemical biology

authors： Gooyit M,Peng Z,Wolter WR,Pi H,Ding D,Hesek D,Lee M,Boggess B,Champion MM,Suckow MA,Mobashery S,Chang M

更新日期：2014-01-17 00:00:00

abstract：:Replacing the two Mn(2+) ions normally present in human Arginase I with Co(2+) resulted in a significantly lowered K(M) value without a concomitant reduction in k(cat). In addition, the pH dependence of the reaction was shifted from a pK(a) of 8.5 to a pK(a) of 7.5. The combination of these effects led to a 10-fold in...

journal_title：ACS chemical biology

authors： Stone EM,Glazer ES,Chantranupong L,Cherukuri P,Breece RM,Tierney DL,Curley SA,Iverson BL,Georgiou G

更新日期：2010-03-19 00:00:00

abstract：:Zinc plays both physiological and pathological roles in biology, making it of increasing interest. To date, intracellular free zinc has been measured in cell types supplemented with or enriched in zinc, such as hippocampal neurons. Here we quantitatively image intracellular exchangeable zinc in an ordinary resting cel...

journal_title：ACS chemical biology

authors： Bozym RA,Thompson RB,Stoddard AK,Fierke CA

更新日期：2006-03-17 00:00:00

abstract：:BRD4, a member of the bromodomain and extraterminal domain (BET) family, has emerged as a promising epigenetic target in cancer and inflammatory disorders. All reported BET family ligands bind within the bromodomain acetyl-lysine binding sites and competitively inhibit BET protein interaction with acetylated chromatin...

journal_title：ACS chemical biology

authors： Olp MD,Sprague DJ,Goetz CJ,Kathman SG,Wynia-Smith SL,Shishodia S,Summers SB,Xu Z,Statsyuk AV,Smith BC

更新日期：2020-04-17 00:00:00

abstract：:The innate immune system provides the first line of defense against pathogens through the recognition of nonspecific patterns in RNA to protect the cell in a generalized way. The human RNA-activated protein kinase, PKR, is a dsRNA binding protein and an essential sensor in the innate immune response, which recognizes ...

journal_title：ACS chemical biology

authors： Hull CM,Anmangandla A,Bevilacqua PC

更新日期：2016-04-15 00:00:00

abstract：:The Pygo-BCL9 complex is a chromatin reader, facilitating β-catenin-mediated oncogenesis, and is thus emerging as a potential therapeutic target for cancer. Its function relies on two ligand-binding surfaces of Pygo's PHD finger that anchor the histone H3 tail methylated at lysine 4 (H3K4me) with assistance from the B...

journal_title：ACS chemical biology

authors： Miller TC,Rutherford TJ,Birchall K,Chugh J,Fiedler M,Bienz M

更新日期：2014-12-19 00:00:00

abstract：:Nature uses four methods of carbon chain elongation for the production of 2-ketoacids, fatty acids, polyketides, and isoprenoids. Using a combination of quantum mechanical (QM) modeling, protein-substrate modeling, and protein and metabolic engineering, we have engineered the enzymes involved in leucine biosynthesis f...

journal_title：ACS chemical biology

authors： Marcheschi RJ,Li H,Zhang K,Noey EL,Kim S,Chaubey A,Houk KN,Liao JC

更新日期：2012-04-20 00:00:00

abstract：:Endocytosis is a key process in cellular delivery of macromolecules by molecular transporters, although the mechanism of internalization remains unclear. Here, we probe the cellular uptake of streptavidin using biotinylated guanidinoneomycin (biotinGNeo), a low molecular weight guanidinium-rich molecular transporter. ...

journal_title：ACS chemical biology

authors： Inoue M,Tong W,Esko JD,Tor Y

更新日期：2013-07-19 00:00:00

abstract：:Intracellular reactions on nonenzymatic proteins that activate cellular signals are rarely found. We report one example here that a designed peptide derivative undergoes a nucleophilic reaction specifically with a cytosolic PDZ protein inside cells. This reaction led to the activation of ephrin-B reverse signaling, wh...

journal_title：ACS chemical biology

authors： Yu Y,Liu M,Ng TT,Huang F,Nie Y,Wang R,Yao ZP,Li Z,Xia J

更新日期：2016-01-15 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：:Widespread use and misuse of antibiotics has allowed for the selection of resistant bacteria capable of avoiding the effects of antibiotics. The primary mechanism for resistance to aminoglycosides, a broad-spectrum class of antibiotics, is through covalent enzymatic modification of the drug, waning their bactericidal ...

journal_title：ACS chemical biology

authors： Bassenden AV,Rodionov D,Shi K,Berghuis AM

更新日期：2016-05-20 00:00:00

abstract：:Phenotypic screening of compound libraries is a significant trend in drug discovery, yet success can be hindered by difficulties in identifying the underlying cellular targets. Current approaches rely on tethering bioactive compounds to a capture tag or surface to allow selective enrichment of interacting proteins for...

journal_title：ACS chemical biology

authors： Ohana RF,Kirkland TA,Woodroofe CC,Levin S,Uyeda HT,Otto P,Hurst R,Robers MB,Zimmerman K,Encell LP,Wood KV

更新日期：2015-10-16 00:00:00

abstract：:A two-way colorimetric biosensor based on unmodified gold nanoparticles (GNPs) and a switchable double-stranded DNA (dsDNA) concatemer have been demonstrated. Two hairpin probes (H1 and H2) were first designed that provided the fuels to assemble the dsDNA concatemers via hybridization chain reaction (HCR). A functiona...

journal_title：ACS chemical biology

authors： Zhu L,Shao X,Luo Y,Huang K,Xu W

更新日期：2017-05-19 00:00:00

abstract：:RUVBL1 and RUVBL2 are ATPases associated with diverse cellular activities (AAAs) that form a complex involved in a variety of cellular processes, including chromatin remodeling and regulation of gene expression. RUVBLs have a strong link to oncogenesis, where overexpression is correlated with tumor growth and poor pro...

journal_title：ACS chemical biology

authors： Assimon VA,Tang Y,Vargas JD,Lee GJ,Wu ZY,Lou K,Yao B,Menon MK,Pios A,Perez KC,Madriaga A,Buchowiecki PK,Rolfe M,Shawver L,Jiao X,Le Moigne R,Zhou HJ,Anderson DJ

更新日期：2019-02-15 00:00:00