Errors in translation cause selective neurodegeneration.

abstract：:New methodologies for site-specifically radiolabeling proteins with (18)F are required to generate high quality radiotracers for preclinical and clinical applications with positron emission tomography. Herein, we report an approach by which we use lipoic acid ligase (LplA) to conjugate [(18)F]-fluorooctanoic acid to a...

journal_title：ACS chemical biology

authors： Drake CR,Sevillano N,Truillet C,Craik CS,VanBrocklin HF,Evans MJ

更新日期：2016-06-17 00:00:00

abstract：:Filamentous cyanobacteria belong to the most prolific producers of structurally unique and biologically active natural products, yet the majority of biosynthetic gene clusters predicted for these multicellular collectives are currently orphan. Here, we present a systems analysis of secondary metabolite gene expression...

journal_title：ACS chemical biology

authors： Dehm D,Krumbholz J,Baunach M,Wiebach V,Hinrichs K,Guljamow A,Tabuchi T,Jenke-Kodama H,Süssmuth RD,Dittmann E

更新日期：2019-06-21 00:00:00

abstract：:X-ray crystallographic analysis of a bovine antibody (BLV1H12) revealed a unique scaffold in its ultralong heavy chain complementarity determining region 3 (CDR3H) that folds into a solvent exposed, antiparallel β-stranded "stalk" fused with a disulfide cross-linked "knob" domain. This unusual variable region motif pr...

journal_title：ACS chemical biology

authors： Zhang Y,Wang D,Welzel G,Wang Y,Schultz PG,Wang F

更新日期：2013-10-18 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：:We have developed a chemically controlled very long-acting delivery system to support once-monthly administration of a peptidic GLP-1R agonist. Initially, the prototypical GLP-1R agonist exenatide was covalently attached to hydrogel microspheres by a self-cleaving β-eliminative linker; after subcutaneous injection in ...

journal_title：ACS chemical biology

authors： Schneider EL,Hearn BR,Pfaff SJ,Reid R,Parkes DG,Vrang N,Ashley GW,Santi DV

更新日期：2017-08-18 00:00:00

abstract：:RAGE (Receptor for Advanced Glycation End-Products) has emerged as a major receptor that mediates vascular inflammation. Signaling through RAGE by damage-associated molecular pattern molecules often leads to uncontrolled inflammation that exacerbates the impact of the underlying disease. Oligomerization of RAGE is bel...

journal_title：ACS chemical biology

authors： Xu D,Young JH,Krahn JM,Song D,Corbett KD,Chazin WJ,Pedersen LC,Esko JD

更新日期：2013-07-19 00:00:00

abstract：:Huntington's disease (HD) is a neurodegenerative disorder that is caused by abnormal expansion of CAG repeats in the HTT gene. The transcribed mutant RNA contains expanded CAG repeats that translate into a mutant huntingtin protein. This expanded CAG repeat also causes mis-splicing of pre-mRNA due to sequestration of ...

journal_title：ACS chemical biology

authors： Khan E,Tawani A,Mishra SK,Verma AK,Upadhyay A,Kumar M,Sandhir R,Mishra A,Kumar A

更新日期：2018-01-19 00:00:00

abstract：:RNAs are involved in interaction networks with other biomolecules and are crucial for proper cell function. Yet their biochemical analysis remains challenging. For Förster Resonance Energy Transfer (FRET), a common tool to study such interaction networks, two interacting molecules have to be fluorescently labeled. "Sp...

journal_title：ACS chemical biology

authors： Roszyk L,Kollenda S,Hennig S

更新日期：2017-12-15 00:00:00

abstract：:Small molecules are widely used in chemical biology without complete knowledge of their target profile, at risk of deriving conclusions that ignore potential confounding effects from unknown off-target interactions. The prediction and further experimental confirmation of novel affinities for PJ34 on Pim1 (IC(50) = 3.7...

journal_title：ACS chemical biology

authors： Antolín AA,Jalencas X,Yélamos J,Mestres J

更新日期：2012-12-21 00:00:00

abstract：:Functionally selective ligands stabilize conformations of G protein-coupled receptors (GPCRs) that induce a preference for signaling via a subset of the intracellular pathways activated by the endogenous agonists. The possibility to fine-tune the functional activity of a receptor provides opportunities to develop drug...

journal_title：ACS chemical biology

authors： Männel B,Jaiteh M,Zeifman A,Randakova A,Möller D,Hübner H,Gmeiner P,Carlsson J

更新日期：2017-10-20 00:00:00

abstract：:The anxiolytic, anticonvulsant, muscle-relaxant, and sedative-hypnotic effects of benzodiazepine site ligands are mainly elicited by allosteric modulation of GABAA receptors via their extracellular αx+/γ2- ( x = 1, 2, 3, 5) interfaces. In addition, a low affinity binding site at the homologous α+/β- interfaces was rep...

journal_title：ACS chemical biology

authors： Siebert DCB,Bampali K,Puthenkalam R,Varagic Z,Sarto-Jackson I,Scholze P,Sieghart W,Mihovilovic MD,Schnürch M,Ernst M

更新日期：2018-08-17 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：:A DNA-encoded macrocyclic peptide library was designed and synthesized with 2.4 × 1012 members composed of 4-20 natural and non-natural amino acids. Affinity-based selection was performed against two therapeutic targets, VHL and RSV N protein. On the basis of selection data, some peptides were selected for resynthesis...

journal_title：ACS chemical biology

authors： Zhu Z,Shaginian A,Grady LC,O'Keeffe T,Shi XE,Davie CP,Simpson GL,Messer JA,Evindar G,Bream RN,Thansandote PP,Prentice NR,Mason AM,Pal S

更新日期：2018-01-19 00:00:00

abstract：:A new chemical method for the traceless labeling of glycoproteins with synthetic boronic acid (BA)-tosyl probes was successfully developed. The BA moiety acts as an affinity head to direct the formation of a cyclic boronate diester with the diol groups of glycans. Following this step, the electrophilic tosyl group is ...

journal_title：ACS chemical biology

authors： Yang YL,Lee YP,Yang YL,Lin PC

更新日期：2014-02-21 00:00:00

abstract：:The mitochondrial ADP/ATP carrier (AAC) is a prominent actor in the energetic regulation of the cell, importing ADP into the mitochondria and exporting ATP toward the cytoplasm. Severe genetic diseases have been ascribed to specific mutations in this membrane protein. How minute, well-localized modifications of the tr...

journal_title：ACS chemical biology

authors： Ravaud S,Bidon-Chanal A,Blesneac I,Machillot P,Juillan-Binard C,Dehez F,Chipot C,Pebay-Peyroula E

更新日期：2012-07-20 00:00:00

abstract：:Albicidin is a potent antibiotic and phytotoxin produced by Xanthomonas albilineans which targets the plant and bacterial DNA gyrase. We now report on a new albicidin derivative which is carbamoylated at the N-terminal coumaric acid by the action of the ATP-dependent O-carbamoyltransferase Alb15, present in the albici...

journal_title：ACS chemical biology

authors： Petras D,Kerwat D,Pesic A,Hempel BF,von Eckardstein L,Semsary S,Arasté J,Marguerettaz M,Royer M,Cociancich S,Süssmuth RD

更新日期：2016-05-20 00:00:00

abstract：:The steady increase in the prevalence of multidrug-resistant Staphylococcus aureus has made the search for novel antibiotics to combat this clinically important pathogen an urgent matter. In an effort to discover antibacterials with new chemical structures and mechanisms, we performed a growth inhibition screen of a s...

journal_title：ACS chemical biology

authors： Wang J,Ye X,Yang X,Cai Y,Wang S,Tang J,Sachdeva M,Qian Y,Hu W,Leeds JA,Yuan Y

更新日期：2020-07-17 00:00:00

abstract：:The heat shock response is an evolutionarily conserved, stress-responsive signaling pathway that adapts cellular proteostasis in response to pathologic insult. In metazoans, the heat shock response primarily functions through the posttranslational activation of heat shock factor 1 (HSF1), a stress-responsive transcrip...

journal_title：ACS chemical biology

authors： Ryno LM,Genereux JC,Naito T,Morimoto RI,Powers ET,Shoulders MD,Wiseman RL

更新日期：2014-06-20 00:00:00

abstract：:The clinical application of siRNA is limited largely by the lack of efficient, cell-specific delivery systems. Antibodies are attractive delivery vehicles for targeted therapy due to their high specificity. In this study we describe the use of a humanized monoclonal antibody (mAb), hu3S193, against Lewis-Y (Le(y)), as...

journal_title：ACS chemical biology

authors： Ma Y,Kowolik CM,Swiderski PM,Kortylewski M,Yu H,Horne DA,Jove R,Caballero OL,Simpson AJ,Lee FT,Pillay V,Scott AM

更新日期：2011-09-16 00:00:00

abstract：:Clostridium difficile, a leading cause of hospital-acquired infection, possesses a dense surface layer (S-layer) that mediates host-pathogen interactions. The key structural components of the S-layer result from proteolytic cleavage of a precursor protein, SlpA, into high- and low-molecular-weight components. Here we ...

journal_title：ACS chemical biology

authors： Dang TH,de la Riva L,Fagan RP,Storck EM,Heal WP,Janoir C,Fairweather NF,Tate EW

更新日期：2010-03-19 00:00:00

abstract：:The receptor tyrosine kinase EPHA2 (Ephrin type-A receptor 2) plays important roles in oncogenesis, metastasis, and treatment resistance, yet therapeutic targeting, drug discovery, or investigation of EPHA2 biology is hampered by the lack of appropriate inhibitors and structural information. Here, we used chemical pro...

journal_title：ACS chemical biology

authors： Heinzlmeir S,Kudlinzki D,Sreeramulu S,Klaeger S,Gande SL,Linhard V,Wilhelm M,Qiao H,Helm D,Ruprecht B,Saxena K,Médard G,Schwalbe H,Kuster B

更新日期：2016-12-16 00:00:00

abstract：:Labeling of virus opens new pathways for the understanding of viruses themselves and facilitates the utilization of viruses in modern biology, medicine, and materials. Based on the characteristic that viruses hijack their host cellular machineries to survive and reproduce themselves, a host-cell-assisted strategy is p...

journal_title：ACS chemical biology

authors： Huang BH,Lin Y,Zhang ZL,Zhuan F,Liu AA,Xie M,Tian ZQ,Zhang Z,Wang H,Pang DW

更新日期：2012-04-20 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：: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：:Ebselen modulates target proteins through redox reactions with selenocysteine/cysteine residues, or through binding to the zinc finger domains. However, a recent contradiction in ebselen inhibition of kidney type glutaminase (KGA) stimulated our interest in investigating its inhibition mechanism with glutamate dehydro...

journal_title：ACS chemical biology

authors： Yu Y,Jin Y,Zhou J,Ruan H,Zhao H,Lu S,Zhang Y,Li D,Ji X,Ruan BH

更新日期：2017-12-15 00:00:00

abstract：:A major goal of personalized medicine in oncology is the identification of drugs with predictable efficacy based on a specific trait of the cancer cell, as has been demonstrated with gleevec (presence of Bcr-Abl protein), herceptin (Her2 overexpression), and iressa (presence of a specific EGFR mutation). This is a cha...

journal_title：ACS chemical biology

authors： Parkinson EI,Bair JS,Cismesia M,Hergenrother PJ

更新日期：2013-10-18 00:00:00

abstract：:Deubiquitinating enzymes play an important role in a plethora of therapeutically relevant processes and are emerging as pioneering drug targets. Herein, we present a novel probe, Ubiquitin Specific Protease (USP) inhibitor, alongside an alkyne-tagged activity-based probe analogue. Activity-based proteome profiling ide...

journal_title：ACS chemical biology

authors： Ward JA,McLellan L,Stockley M,Gibson KR,Whitlock GA,Knights C,Harrigan JA,Jacq X,Tate EW

更新日期：2016-12-16 00:00:00

abstract：:Transcriptional activity is exquisitely sensitive to changes in promoter DNA topology. Transcription factors may therefore control gene activity by modulating the relative positioning of -10 and -35 promoter elements. The plant pathogen Pectobacterium atrosepticum, which causes soft rot in potatoes, must alter gene ex...

journal_title：ACS chemical biology

authors： Deochand DK,Meariman JK,Grove A

更新日期：2016-07-15 00:00:00

abstract：:Methicillin resistance in Staphylococcus aureus depends on the production of mecA, which encodes penicillin-binding protein 2A (PBP2A), an acquired peptidoglycan transpeptidase (TP) with reduced susceptibility to β-lactam antibiotics. PBP2A cross-links nascent peptidoglycan when the native TPs are inhibited by β-lacta...

journal_title：ACS chemical biology

authors： Campbell J,Singh AK,Santa Maria JP Jr,Kim Y,Brown S,Swoboda JG,Mylonakis E,Wilkinson BJ,Walker S

更新日期：2011-01-21 00:00:00

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