MARCKS-ED peptide as a curvature and lipid sensor.

abstract：:3-Oxo-β-sultams are four-membered ring ambident electrophiles that can react with nucleophiles either at the carbonyl carbon or at the sulfonyl sulfur atoms, and that have been reported to inhibit serine hydrolases via acylation of the active-site serine residue. We have developed a panel of 3-oxo-β-sultam inhibitors ...

journal_title：ACS chemical biology

authors： Carvalho LAR,Almeida VT,Brito JA,Lum KM,Oliveira TF,Guedes RC,Gonçalves LM,Lucas SD,Cravatt BF,Archer M,Moreira R

更新日期：2020-04-17 00:00:00

abstract：:Ammonia lyases catalyze the formation of α,β-unsaturated bonds by the elimination of ammonia from their substrates. This conceptually straightforward reaction has been the emphasis of many studies, with the main focus on the catalytic mechanism of these enzymes and/or the use of these enzymes as catalysts for the synt...

journal_title：ACS chemical biology

authors： de Villiers M,Puthan Veetil V,Raj H,de Villiers J,Poelarends GJ

更新日期：2012-10-19 00:00:00

abstract：:Lanthipeptides are ribosomally synthesized and post-translationally modified peptides bearing the characteristic amino acids lanthionine and/or labionin. Here, we report on the discovery and characterization of the stackepeptins, produced by the Actinomycete Stackebrandtia nassauensis DSM-44728(T). The stackepeptins a...

journal_title：ACS chemical biology

authors： Jungmann NA,van Herwerden EF,Hügelland M,Süssmuth RD

更新日期：2016-01-15 00:00:00

abstract：:Leishmaniases affect the poorest people on earth and have no effective drug therapy. Here, we present the crystal structure of the mitochondrial isoform of class I fumarate hydratase (FH) from Leishmania major and compare it to the previously determined cytosolic Leishmania major isoform. We further describe the mecha...

journal_title：ACS chemical biology

authors： Feliciano PR,Drennan CL,Nonato MC

更新日期：2019-02-15 00:00:00

abstract：:There is a pressing need for new molecular tools to target protein surfaces with high affinity and specificity. Here, we describe cyclic messenger RNA display with a trillion-member covalent peptide macrocycle library. Using this library, we have designed a number of high-affinity, redox-insensitive, cyclic peptides t...

journal_title：ACS chemical biology

authors： Millward SW,Fiacco S,Austin RJ,Roberts RW

更新日期：2007-09-21 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：:Current therapeutic interventions for both heart disease and heart failure are largely insufficient and associated with undesired side effects. Biomedical research has emphasized the role of sarcomeric protein function for the normal performance and energy efficiency of the heart, suggesting that directly targeting th...

journal_title：ACS chemical biology

authors： Parijat P,Kondacs L,Alexandrovich A,Gautel M,Cobb AJA,Kampourakis T

更新日期：2021-01-15 00:00:00

abstract：:Calicheamicin γ1I (1) is an enediyne antitumor compound produced by Micromonospora echinospora spp. calichensis, and its biosynthetic gene cluster has been previously reported. Despite extensive analysis and biochemical study, several genes in the biosynthetic gene cluster of 1 remain functionally unassigned. Using a ...

journal_title：ACS chemical biology

authors： Elshahawi SI,Ramelot TA,Seetharaman J,Chen J,Singh S,Yang Y,Pederson K,Kharel MK,Xiao R,Lew S,Yennamalli RM,Miller MD,Wang F,Tong L,Montelione GT,Kennedy MA,Bingman CA,Zhu H,Phillips GN Jr,Thorson JS

更新日期：2014-10-17 00:00:00

abstract：:Glycosaminoglycans (GAGs), such as heparin or heparan sulfate, are required for the in vivo function of chemokines. Chemokines play a crucial role in the recruitment of leukocyte subsets to sites of inflammation and lymphocytes trafficking. GAG-chemokine interactions mediate cell migration and determine which leukocyt...

journal_title：ACS chemical biology

authors： de Paz JL,Moseman EA,Noti C,Polito L,von Andrian UH,Seeberger PH

更新日期：2007-11-20 00:00:00

abstract：:To combat the increasing spread of antimicrobial resistance and the shortage of novel anti-infectives, one strategy for the development of new antibiotics is to optimize known chemical scaffolds. Here, we focus on the biosynthetic engineering of Amycolatopsis sulphurea for derivatization of the atypical tetracycline c...

journal_title：ACS chemical biology

authors： Lukežič T,Fayad AA,Bader C,Harmrolfs K,Bartuli J,Groß S,Lešnik U,Hennessen F,Herrmann J,Pikl Š,Petković H,Müller R

更新日期：2019-03-15 00:00:00

abstract：:Fe(III) delivery from blood plasma to cells via the transferrin (Tf) cycle was studied intensively due to its crucial role in Fe homeostasis. Tf-cycle disruptions are linked to anemia, infections, immunodeficiency, and neurodegeneration. Biolayer interferometry (BLI) enabled direct kinetic and thermodynamic measuremen...

journal_title：ACS chemical biology

authors： Levina A,Lay PA

更新日期：2019-05-17 00:00:00

abstract：:Post-translational modifications of histones alter chromatin structure and play key roles in gene expression and specification of cell states. Small molecules that target chromatin-modifying enzymes selectively are useful as probes and have promise as therapeutics, although very few are currently available. G9a (also ...

journal_title：ACS chemical biology

authors： Yuan Y,Wang Q,Paulk J,Kubicek S,Kemp MM,Adams DJ,Shamji AF,Wagner BK,Schreiber SL

更新日期：2012-07-20 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：: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：:Photoinduced cross-linking (PIC) has become a powerful tool in chemical biology for the identification and mapping of stable or transient interactions between biomacromolecules and their (unknown) ligands. However, the value of PIC for in vitro and in vivo structural proteomics can be realized only if cross-linking re...

journal_title：ACS chemical biology

authors： Preston GW,Radford SE,Ashcroft AE,Wilson AJ

更新日期：2014-03-21 00:00:00

abstract：:The development of HIV-1 protease inhibitors has been the historic paradigm of rational structure-based drug design, where structural and thermodynamic analyses have assisted in the discovery of novel inhibitors. While the total enthalpy and entropy change upon binding determine the affinity, often the thermodynamics ...

journal_title：ACS chemical biology

authors： King NM,Prabu-Jeyabalan M,Bandaranayake RM,Nalam MN,Nalivaika EA,Özen A,Haliloğlu T,Yilmaz NK,Schiffer CA

更新日期：2012-09-21 00:00:00

abstract：:The cell utilizes the Keap1/Nrf2-ARE signaling pathway to detoxify harmful chemicals in order to protect itself from oxidative stress and to maintain its reducing environment. When exposed to oxidative stress and xenobiotic inducers, the redox sensitive Keap1 is covalently modified at specific cysteine residues. Conse...

journal_title：ACS chemical biology

authors： Wang R,Mason DE,Choe KP,Lewin AS,Peters EC,Luesch H

更新日期：2013-08-16 00:00:00

abstract：:Numerous cytochrome P450 (CYP) 2B6 substrates including drugs and environmental chemicals are halogenated. To assess the role of halogen-π bonds in substrate selectivity and orientation in the active site, structures of four CYP2B6 monoterpenoid complexes were solved by X-ray crystallography. Bornyl bromide exhibited ...

journal_title：ACS chemical biology

authors： Shah MB,Liu J,Zhang Q,Stout CD,Halpert JR

更新日期：2017-05-19 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：: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：:Phosphoinositides are critical cell-signal mediators present on the plasma membrane. The dynamic change of phosphoinositide concentrations on the membrane including clustering and declustering mediates signal transduction. The importance of phosphoinositides is scored by the fact that they participate in almost all ce...

journal_title：ACS chemical biology

authors： Mondal S,Rakshit A,Pal S,Datta A

更新日期：2016-07-15 00:00:00

abstract：:Protein dimerization provides a mechanism for the modulation of cellular signaling events. In α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA) receptors, the rapidly desensitizing, activated state has been correlated with a weakly dimeric, glutamate-binding domain conformation. Allosteric modulators can fo...

journal_title：ACS chemical biology

authors： Ptak CP,Hsieh CL,Weiland GA,Oswald RE

更新日期：2014-01-17 00:00:00

abstract：:Reactive oxygen species (ROS) play an important role in the onset of Parkinson's disease (PD), and deciphering protective mechanisms is a major goal for therapeutic development. Here, DJ-1 (PARK7) gained major attention when a conserved cysteine residue with a putative role in oxidative stress sensing/protection was l...

journal_title：ACS chemical biology

authors： Drechsel J,Mandl FA,Sieber SA

更新日期：2018-08-17 00:00:00

abstract：:Bacteria harbor an immense reservoir of potentially new and therapeutic small molecules in the form of "silent" biosynthetic gene clusters (BGCs). These BGCs can be identified bioinformatically but are sparingly expressed under normal laboratory growth conditions, or not at all, and therefore do not produce significan...

journal_title：ACS chemical biology

authors： Moon K,Xu F,Zhang C,Seyedsayamdost MR

更新日期：2019-04-19 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：: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：:The Morita-Baylis-Hillman reaction forms a carbon-carbon bond between the α-carbon of a conjugated carbonyl compound and a carbon electrophile. The reaction mechanism involves Michael addition of a nucleophile catalyst at the carbonyl β-carbon, followed by bond formation with the electrophile and catalyst disassociati...

journal_title：ACS chemical biology

authors： Bjelic S,Nivón LG,Çelebi-Ölçüm N,Kiss G,Rosewall CF,Lovick HM,Ingalls EL,Gallaher JL,Seetharaman J,Lew S,Montelione GT,Hunt JF,Michael FE,Houk KN,Baker D

更新日期：2013-04-19 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：: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：: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