Evolving sensitivity.

abstract：:Siderophores are iron-chelating molecules produced by microorganisms and plants to acquire exogenous iron. Siderophore biosynthetic enzymology often produces elaborate and unique molecules through unusual reactions to enable specific recognition by the producing organisms. Herein, we report the structure of two sidero...

journal_title：ACS chemical biology

authors： Vinnik V,Zhang F,Park H,Cook TB,Throckmorton K,Pfleger BF,Bugni TS,Thomas MG

更新日期：2021-01-15 00:00:00

abstract：:Epigenetic regulation of gene expression is essential in many biological processes, and its deregulation contributes to pathology including tumor formation. We used an image-based cell assay that measures the induction of a silenced GFP-estrogen receptor reporter to identify novel classes of small molecules involved i...

journal_title：ACS chemical biology

authors： Tran TA,Wichterman-Kouznetsova J,Varghese D,Huang R,Huang W,Becker M,Austin CP,Inglese J,Johnson RL,Martinez ED

更新日期：2014-11-21 00:00:00

abstract：:The ever-growing drug resistance problem worldwide highlights the urgency to discover and develop new drugs. Microbial natural products are a prolific source of drugs. Genome sequencing has revealed a tremendous amount of uncharacterized natural product biosynthetic gene clusters (BGCs) encoded within microbial genome...

journal_title：ACS chemical biology

authors： Zhang Q,Ren JW,Wang W,Zhai J,Yang J,Liu N,Huang Y,Chen Y,Pan G,Fan K

更新日期：2020-09-18 00:00:00

abstract：:Seasonal and pandemic influenza viruses continue to be a leading global health concern. Emerging resistance to the current drugs and the variable efficacy of vaccines underscore the need for developing new flu drugs that will be broadly effective against wild-type and drug-resistant influenza strains. Here, we report ...

journal_title：ACS chemical biology

authors： Bauman JD,Patel D,Baker SF,Vijayan RS,Xiang A,Parhi AK,Martínez-Sobrido L,LaVoie EJ,Das K,Arnold E

更新日期：2013-11-15 00:00:00

abstract：:Miniproteins have a size between that of larger biologics and small molecules and presumably possess the advantages of both; they represent an expanding class of promising scaffolds for the design of affinity reagents, enzymes, and therapeutics. Conventional strategies to promote cellular uptake of miniproteins rely o...

journal_title：ACS chemical biology

authors： Meng X,Li T,Zhao Y,Wu C

更新日期：2018-11-16 00:00:00

abstract：:Transpeptidases, members of the penicillin-binding protein (PBP) families, catalyze cross-linking of the bacterial cell wall. This transformation is critical for the survival of bacteria, and it is the target of inhibition by β-lactam antibiotics. We report herein our structural insights into catalysis by the essentia...

journal_title：ACS chemical biology

authors： Bernardo-García N,Mahasenan KV,Batuecas MT,Lee M,Hesek D,Petráčková D,Doubravová L,Branny P,Mobashery S,Hermoso JA

更新日期：2018-03-16 00:00:00

abstract：:RNA methyltransferases (RNMTs) play important roles in RNA stability, splicing, and epigenetic mechanisms. They constitute a promising target class that is underexplored by the medicinal chemistry community. Information of relevance to drug design can be extracted from the rich structural coverage of human RNMTs. In t...

journal_title：ACS chemical biology

authors： Schapira M

更新日期：2016-03-18 00:00:00

abstract：:The indole side chain of tryptophan has latent nucleophilic reactivity at both N1 and all six (nonbridgehead) carbons, which is not generally manifested in post-translational reactions of proteins. On the other hand, all seven positions can be prenylated by the primary metabolite Δ(2)-isopentenyl diphosphate by dimeth...

journal_title：ACS chemical biology

authors： Walsh CT

更新日期：2014-12-19 00:00:00

abstract：:One-third of all human cancers harbor somatic RAS mutations. This leads to aberrant activation of downstream signaling pathways involving the RAF kinases. Current ATP-competitive RAF inhibitors are active in cancers with somatic RAF mutations, such as BRAF(V600) mutant melanomas. However, they paradoxically promote th...

journal_title：ACS chemical biology

authors： Molzan M,Kasper S,Röglin L,Skwarczynska M,Sassa T,Inoue T,Breitenbuecher F,Ohkanda J,Kato N,Schuler M,Ottmann C

更新日期：2013-09-20 00:00:00

abstract：:HIV infection is pandemic in humans and is responsible for millions of deaths every year. The discovery of new cellular targets that can be used to prevent the infection process represents a new opportunity for developing more effective antiviral drugs. In this context, dendritic cell-specific ICAM-3 grabbing non-inte...

journal_title：ACS chemical biology

authors： Sattin S,Daghetti A,Thépaut M,Berzi A,Sánchez-Navarro M,Tabarani G,Rojo J,Fieschi F,Clerici M,Bernardi A

更新日期：2010-03-19 00:00:00

abstract：:FAT10 is a ubiquitin-like protein suggested to target proteins for proteasomal degradation. It is highly upregulated upon pro-inflammatory cytokines, namely, TNFα, IFNγ, and IL6, and was found to be highly expressed in various epithelial cancers. Evidence suggests that FAT10 is involved in cancer development and may h...

journal_title：ACS chemical biology

authors： Reznik N,Kozer N,Eisenberg-Lerner A,Barr H,Merbl Y,London N

更新日期：2019-12-20 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

abstract：:Access to well-defined ubiquitin conjugates has been key to elucidating the biochemical functions of proteins in the ubiquitin signaling network. Yet, we have a poor understanding of how deubiquitinases and ubiquitin-binding proteins respond to ubiquitin modifications when anchored to a protein other than ubiquitin or...

journal_title：ACS chemical biology

authors： Chang LH,Strieter ER

更新日期：2018-09-21 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：:Methods for the rapid identification of defined cell growth conditions are lacking. This deficiency is a major barrier to the investigation and application of human embryonic stem (ES) cells. To address this problem, we developed a method for generating arrays of self-assembled monolayers (SAMs) in which each element ...

journal_title：ACS chemical biology

authors： Derda R,Li L,Orner BP,Lewis RL,Thomson JA,Kiessling LL

更新日期：2007-05-22 00:00:00

abstract：:Many cellular processes are regulated by posttranslational modifications that are recognized by specific domains in protein binding partners. These interactions are often weak, thus allowing a highly dynamic and combinatorial regulatory network of protein-protein interactions. We report an efficient strategy that over...

journal_title：ACS chemical biology

authors： Tripsianes K,Chu NK,Friberg A,Sattler M,Becker CF

更新日期：2014-02-21 00:00:00

abstract：:We evaluated the abilities of an antisense oligonucleotide (ASO), a small interfering RNA (siRNA), and a single-stranded siRNA (ss-siRNA) to inhibit expression from the PTEN gene in mice when formulated identically with lipid nanoparticles (LNPs). Significantly greater reductions in levels of PTEN mRNA were observed f...

journal_title：ACS chemical biology

authors： Prakash TP,Lima WF,Murray HM,Elbashir S,Cantley W,Foster D,Jayaraman M,Chappell AE,Manoharan M,Swayze EE,Crooke ST

更新日期：2013-07-19 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：:Protein arginine N-methyltransferase 3 (PRMT3) belongs to the family of type I PRMTs and harbors the activity to use S-adenosyl-l-methionine (SAM) as a methyl-donor cofactor for protein arginine labeling. However, PRMT3's functions remain elusive with the lacked knowledge of its target scope in cellular settings. Insp...

journal_title：ACS chemical biology

authors： Guo H,Wang R,Zheng W,Chen Y,Blum G,Deng H,Luo M

更新日期：2014-02-21 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：:Chromophore-assisted light inactivation (CALI) is a potentially powerful tool for the acute disruption of a target protein inside living cells with high spatiotemporal resolution. This technology, however, has not been widely utilized, mainly because of the lack of an efficient chromophore as the photosensitizing agen...

journal_title：ACS chemical biology

authors： Takemoto K,Matsuda T,McDougall M,Klaubert DH,Hasegawa A,Los GV,Wood KV,Miyawaki A,Nagai T

更新日期：2011-05-20 00:00:00

abstract：:Endothelial progenitor cells (EPCs) and endothelial cells (ECs) play a vital role in endothelialization and vascularization for tissue regeneration. Various EPC/EC targeting biomolecules have been investigated to improve tissue regeneration with limited success often due to their limited functional specificity and str...

journal_title：ACS chemical biology

authors： Hao D,Xiao W,Liu R,Kumar P,Li Y,Zhou P,Guo F,Farmer DL,Lam KS,Wang F,Wang A

更新日期：2017-04-21 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：:Though phenotypic and target-based high-throughput screening approaches have been employed to discover new antibiotics, the identification of promising therapeutic candidates remains challenging. Each approach provides different information, and understanding their results can provide hypotheses for a mechanism of act...

journal_title：ACS chemical biology

authors： Santa Maria JP Jr,Park Y,Yang L,Murgolo N,Altman MD,Zuck P,Adam G,Chamberlin C,Saradjian P,Dandliker P,Boshoff HIM,Barry CE 3rd,Garlisi C,Olsen DB,Young K,Glick M,Nickbarg E,Kutchukian PS

更新日期：2017-09-15 00:00:00

abstract：:Lasso peptides are bacterial ribosomally synthesized and post-translationally modified peptides. They have sparked increasing interest in peptide-based drug development because of their compact, interlocked structure, which offers superior stability and protein-binding capacity. Disulfide bond-containing lasso peptide...

journal_title：ACS chemical biology

authors： Li Y,Ducasse R,Zirah S,Blond A,Goulard C,Lescop E,Giraud C,Hartke A,Guittet E,Pernodet JL,Rebuffat S

更新日期：2015-11-20 00:00:00

abstract：:Unrelated ligands, often found in drug discovery campaigns, can bind to the same receptor, even with the same protein residues. To investigate how this might occur, and whether it might be typically possible to find unrelated ligands for the same drug target, we sought examples of topologically unrelated ligands that ...

journal_title：ACS chemical biology

authors： Pottel J,Levit A,Korczynska M,Fischer M,Shoichet BK

更新日期：2018-09-21 00:00:00

abstract：:The goal of incorporating renewable carbon into the fuel and chemical enterprise will most likely be successful when combined systems of biocatalysts and chemical catalysts are exploited. Significant efforts in the biocatalytic release of sugars from biomass are being pursued for subsequent use in fermentation. Two re...

journal_title：ACS chemical biology

authors： Shanks BH

更新日期：2007-08-17 00:00:00

abstract：:Dopamine, a biogenic amine with important biological functions, is produced from l-DOPA by DOPA decarboxylase (DDC). DDC is a potential target to modulate the production of dopamine in several pathological states. Known inhibitors of DDC have been used for treatment of Parkinson's disease but suffered low specificity ...

journal_title：ACS chemical biology

authors： Ren J,Zhang Y,Jin H,Yu J,Zhou Y,Wu F,Zhang W

更新日期：2014-04-18 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：:Nonribosomal peptides are important natural products biosynthesized by nonribosomal peptide synthetases (NRPSs). Adenylation (A) domains of NRPSs are highly specific for the substrate they recognize. This recognition is determined by 10 residues in the substrate-binding pocket, termed the specificity code. This findin...

journal_title：ACS chemical biology

authors： Throckmorton K,Vinnik V,Chowdhury R,Cook T,Chevrette MG,Maranas C,Pfleger B,Thomas MG

更新日期：2019-09-20 00:00:00