听力与言语-语言病理学

行为科学

医学伦理学

你正在浏览ACS Chemical Biology期刊下所有文献
  • Engineered EGF-A Peptides with Improved Affinity for Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9).

    abstract::The epidermal growth-factor-like domain A (EGF-A) of the low-density lipoprotein (LDL) receptor is a promising lead for therapeutic inhibition of proprotein convertase subtilisin/kexin type 9 (PCSK9). However, the clinical potential of EGF-A is limited by its suboptimal affinity for PCSK9. Here, we use phage display t...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00991

    authors: Tombling BJ,Lammi C,Lawrence N,Li J,Arnoldi A,Craik DJ,Wang CK

    更新日期:2021-01-29 00:00:00

  • High Throughput Screen Identifies Small Molecule Effectors That Modulate Thin Filament Activation in Cardiac Muscle.

    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

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00908

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

    更新日期:2021-01-15 00:00:00

  • Structural and Biosynthetic Analysis of the Fabrubactins, Unusual Siderophores from Agrobacterium fabrum Strain C58.

    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

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00809

    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

  • HIV-1 Env-Dependent Cell Killing by Bifunctional Small-Molecule/Peptide Conjugates.

    abstract::A strategy has been established for the synthesis of a family of bifunctional HIV-1 inhibitor covalent conjugates with the potential to bind simultaneously to both the gp120 and gp41 subunits of the HIV-1 envelope glycoprotein trimeric complex (Env). One component of the conjugates is derived from BNM-III-170, a small...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00888

    authors: Gaffney A,Nangarlia A,Ang CG,Gossert S,Rashad Ahmed AA,Hossain MA,Abrams CF,Smith AB 3rd,Chaiken I

    更新日期:2021-01-15 00:00:00

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

    abstract::The emergence of multidrug-resistant Staphylococcus aureus strains has become a serious clinical problem. Iron is absolutely required for the bacterial growth, virulence associated with colonization, and survival from the host immune system. The FeoB protein is a major iron permease in bacterial ferrous iron transport...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00842

    authors: Shin M,Jin Y,Park J,Mun D,Kim SR,Payne SM,Kim KH,Kim Y

    更新日期:2021-01-15 00:00:00

  • Structural Insights into the Interaction of Clinically Relevant Phosphorothioate mRNA Cap Analogs with Translation Initiation Factor 4E Reveal Stabilization via Electrostatic Thio-Effect.

    abstract::mRNA-based therapies and vaccines constitute a disruptive technology with the potential to revolutionize modern medicine. Chemically modified 5' cap structures have provided access to mRNAs with superior translational properties that could benefit the currently flourishing mRNA field. Prime examples of compounds that ...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00864

    authors: Warminski M,Kowalska J,Nowak E,Kubacka D,Tibble R,Kasprzyk R,Sikorski PJ,Gross JD,Nowotny M,Jemielity J

    更新日期:2021-01-13 00:00:00

  • Small Molecule Phenotypic Screen Identifies Novel Regulators of LDLR Expression.

    abstract::Alzheimer's Disease (AD) is a progressive neurodegenerative disease and the most common cause of dementia. The current treatment options for AD are limited to ameliorating cognitive decline temporarily and not reversing or preventing the progression of dementia. Hence, more effective therapeutic strategies are needed ...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00851

    authors: Krishnan N,Chen X,Donnelly-Roberts D,Mohler EG,Holtzman DM,Gopalakrishnan SM

    更新日期:2020-12-18 00:00:00

  • Biochemical and Structural Investigation of GnnA in the Lipopolysaccharide Biosynthesis Pathway of Acidithiobacillus ferrooxidans.

    abstract::Lipopolysaccharide (LPS) is a crucial component in the outer membrane of Gram-negative bacteria that contributes to both pathogenicity as well as immunity against pathogenic bacteria. Typical LPS contains GlcN disaccharide as the core of lipid A. However, some bacteria such as Acidithiobacillus ferrooxidans and Leptos...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00791

    authors: Manissorn J,Sitthiyotha T,Montalban JRE,Chunsrivirot S,Thongnuek P,Wangkanont K

    更新日期:2020-12-18 00:00:00

  • The Importance of Charge in Perturbing the Aromatic Glue Stabilizing the Protein-Protein Interface of Homodimeric tRNA-Guanine Transglycosylase.

    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

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00700

    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

  • Parietal Structures of Escherichia coli Can Impact the D-Cateslytin Antibacterial Activity.

    abstract::Bacterial resistance to conventional antibiotics is of major concern. Antimicrobial peptides (AMPs) are considered excellent alternatives. Among them, D-cateslytin (D-Ctl, derivative of a host defense peptide) has shown high efficiency against a broad spectrum of bacteria. The first target of AMPs is the outer membran...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00622

    authors: Quilès F,Barth D,Peric O,Fantner GE,Francius G

    更新日期:2020-10-16 00:00:00

  • Unraveling the Mechanism of a LOV Domain Optogenetic Sensor: A Glutamine Lever Induces Unfolding of the Jα Helix.

    abstract::Light-activated protein domains provide a convenient, modular, and genetically encodable sensor for optogenetics and optobiology. Although these domains have now been deployed in numerous systems, the precise mechanism of photoactivation and the accompanying structural dynamics that modulate output domain activity rem...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00543

    authors: Iuliano JN,Collado JT,Gil AA,Ravindran PT,Lukacs A,Shin S,Woroniecka HA,Adamczyk K,Aramini JM,Edupuganti UR,Hall CR,Greetham GM,Sazanovich IV,Clark IP,Daryaee T,Toettcher JE,French JB,Gardner KH,Simmerling CL,Meech

    更新日期:2020-10-16 00:00:00

  • Enzymatic Plasticity Inspired by the Diterpene Cyclase CotB2.

    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

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00645

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

    更新日期:2020-10-16 00:00:00

  • Cell-Penetrating Peptides Escape the Endosome by Inducing Vesicle Budding and Collapse.

    abstract::Cell-penetrating peptides (CPPs) are capable of delivering membrane-impermeable cargoes (including small molecules, peptides, proteins, nucleic acids, and nanoparticles) into the cytosol of mammalian cells and have the potential to revolutionize biomedical research and drug discovery. However, the mechanism of action ...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00478

    authors: Sahni A,Qian Z,Pei D

    更新日期:2020-09-18 00:00:00

  • A Versatile Transcription-Translation in One Approach for Activation of Cryptic Biosynthetic Gene Clusters.

    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

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00581

    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

  • Functional and Structural Insights into a Novel Promiscuous Ketoreductase of the Lugdunomycin Biosynthetic Pathway.

    abstract::Angucyclines are a structurally diverse class of actinobacterial natural products defined by their varied polycyclic ring systems, which display a wide range of biological activities. We recently discovered lugdunomycin (1), a highly rearranged polyketide antibiotic derived from the angucycline backbone that is synthe...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00564

    authors: Xiao X,Elsayed SS,Wu C,van der Heul HU,Metsä-Ketelä M,Du C,Prota AE,Chen CC,Liu W,Guo RT,Abrahams JP,van Wezel GP

    更新日期:2020-09-18 00:00:00

  • Cyanobacterial Dihydroxyacid Dehydratases Are a Promising Growth Inhibition Target.

    abstract::Microbes are essential to the global ecosystem, but undesirable microbial growth causes issues ranging from food spoilage and infectious diseases to harmful cyanobacterial blooms. The use of chemicals to control microbial growth has achieved significant success, while specific roles for a majority of essential genes i...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00507

    authors: Zhang P,MacTavish BS,Yang G,Chen M,Roh J,Newsome KR,Bruner SD,Ding Y

    更新日期:2020-08-21 00:00:00

  • Precursor-Guided Mining of Marine Sponge Metabolomes Lends Insight into Biosynthesis of Pyrrole-Imidazole Alkaloids.

    abstract::Pyrrole-imidazole alkaloids are natural products isolated from marine sponges, holobiont metazoans that are associated with symbiotic microbiomes. Pyrrole-imidazole alkaloids have attracted attention due to their chemical complexity and their favorable pharmacological properties. However, insights into how these molec...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00375

    authors: Mohanty I,Moore SG,Yi D,Biggs JS,Gaul DA,Garg N,Agarwal V

    更新日期:2020-08-21 00:00:00

  • Validating Signal Transducer and Activator of Transcription (STAT) Protein-Inhibitor Interactions Using Biochemical and Cellular Thermal Shift Assays.

    abstract::Signal transducer and activator of transcription (STAT) proteins have important biological functions; however, deregulation of STAT signaling is a driving force behind the onset and progression of inflammatory diseases and cancer. While their biological roles suggest that STAT proteins would be valuable targets for de...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00046

    authors: Attarha S,Reithmeier A,Busker S,Desroses M,Page BDG

    更新日期:2020-07-17 00:00:00

  • How ATP-Competitive Inhibitors Allosterically Modulate Tyrosine Kinases That Contain a Src-like Regulatory Architecture.

    abstract::Small molecule kinase inhibitors that stabilize distinct ATP binding site conformations can differentially modulate the global conformation of Src-family kinases (SFKs). However, it is unclear which specific ATP binding site contacts are responsible for modulating the global conformation of SFKs and whether these inhi...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00429

    authors: Fang L,Vilas-Boas J,Chakraborty S,Potter ZE,Register AC,Seeliger MA,Maly DJ

    更新日期:2020-07-17 00:00:00

  • Discovery of Novel Antibiotics as Covalent Inhibitors of Fatty Acid Synthesis.

    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

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b00982

    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

  • RNA Phosphorothioate Modification in Prokaryotes and Eukaryotes.

    abstract::RNA modifications play important roles in RNA structures and regulation of gene expression and translation. We report the first RNA modification on the phosphate, the RNA phosphorothioate (PS) modification, discovered in both prokaryotes and eukaryotes. The PS modification is also first reported on nucleic acids of eu...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00163

    authors: Wu Y,Tang Y,Dong X,Zheng YY,Haruehanroengra P,Mao S,Lin Q,Sheng J

    更新日期:2020-06-19 00:00:00

  • Characterization of Class IB Terpene Synthase: The First Crystal Structure Bound with a Substrate Surrogate.

    abstract::Terpene synthases (TS) are classified into two broad types, Class I and II, based on the chemical strategy for initial carbocation formation and motif sequences of the catalytic site. We have recently identified a new class of enzymes, Class IB, showing the acceptability of long (C20-C35) prenyl-diphosphates as substr...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00145

    authors: Stepanova R,Inagi H,Sugawara K,Asada K,Nishi T,Ueda D,Yasuno Y,Shinada T,Miki K,Fujihashi M,Sato T

    更新日期:2020-06-19 00:00:00

  • Cyanopyrrolidine Inhibitors of Ubiquitin Specific Protease 7 Mediate Desulfhydration of the Active-Site Cysteine.

    abstract::Ubiquitin specific protease 7 (USP7) regulates the protein stability of key cellular regulators in pathways ranging from apoptosis to neuronal development, making it a promising therapeutic target. Here we used an engineered, activated variant of the USP7 catalytic domain to perform structure-activity studies of elect...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00031

    authors: Bashore C,Jaishankar P,Skelton NJ,Fuhrmann J,Hearn BR,Liu PS,Renslo AR,Dueber EC

    更新日期:2020-06-19 00:00:00

  • Biosynthetic Incorporation of Site-Specific Isotopes in β-Lactam Antibiotics Enables Biophysical Studies.

    abstract::A biophysical understanding of the mechanistic, chemical, and physical origins underlying antibiotic action and resistance is vital to the discovery of novel therapeutics and the development of strategies to combat the growing emergence of antibiotic resistance. The site-specific introduction of stable-isotope labels ...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b01054

    authors: Kozuch J,Schneider SH,Boxer SG

    更新日期:2020-05-15 00:00:00

  • Heterologous Biosynthesis of Type II Polyketide Products Using E. coli.

    abstract::The heterologous biosynthesis of complex natural products has enabled access to polyketide, nonribosomal peptide, isoprenoid, and other compounds with wide-spanning societal value. Though several surrogate host systems exist, Escherichia coli is often a preferred choice due to its rapid growth kinetics and extensive m...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b00827

    authors: Liu X,Hua K,Liu D,Wu ZL,Wang Y,Zhang H,Deng Z,Pfeifer BA,Jiang M

    更新日期:2020-05-15 00:00:00

  • 3-Oxo-β-sultam as a Sulfonylating Chemotype for Inhibition of Serine Hydrolases and Activity-Based Protein Profiling.

    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

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00090

    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

  • Covalent-Fragment Screening of BRD4 Identifies a Ligandable Site Orthogonal to the Acetyl-Lysine Binding Sites.

    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

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00058

    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

  • Conformational Changes in Alkyl Chains Determine the Thermodynamic and Kinetic Binding Profiles of Carbonic Anhydrase Inhibitors.

    abstract::Thermodynamics and kinetics of protein-ligand binding are both important aspects for the design of novel drug molecules. Presently, thermodynamic data are collected with isothermal titration calorimetry, while kinetic data are mostly derived from surface plasmon resonance. The new method of kinITC provides both thermo...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b00895

    authors: Glöckner S,Ngo K,Sager CP,Hüfner-Wulsdorf T,Heine A,Klebe G

    更新日期:2020-03-20 00:00:00

  • Molecular Networking and Whole-Genome Analysis Aid Discovery of an Angucycline That Inactivates mTORC1/C2 and Induces Programmed Cell Death.

    abstract::Rediscovery of known compounds and time consumed in identification, especially high molecular weight compounds with complex structure, have let down interest in drug discovery. In this study, whole-genome analysis of microbe and Global Natural Products Social (GNPS) molecular networking helped in initial understanding...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.0c00026

    authors: Dan VM,J S V,C J S,Sanawar R,Lekshmi A,Kumar RA,Santhosh Kumar TR,Marelli UK,Dastager SG,Pillai MR

    更新日期:2020-03-20 00:00:00

  • Profiling Cysteine Reactivity and Oxidation in the Endoplasmic Reticulum.

    abstract::The endoplasmic reticulum (ER) is the initial site of biogenesis of secretory pathway proteins, including proteins localized to the ER, Golgi, lysosomes, intracellular vesicles, plasma membrane, and extracellular compartments. Proteins within the secretory pathway contain a high abundance of disulfide bonds to protect...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b01014

    authors: Bechtel TJ,Li C,Kisty EA,Maurais AJ,Weerapana E

    更新日期:2020-02-21 00:00:00

  • A Multimodal Ca(II) Responsive Near IR-MR Contrast Agent Exhibiting High Cellular Uptake.

    abstract::Ca(II) ions are critical for the proper function of neurons by contributing to synaptic signaling and regulating neuronal plasticity. Dysregulation of Ca(II) is associated with a number of pathologies that cause neurodegeneration; therefore the ability to monitor Ca(II) intracellularly is an important target for molec...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b00638

    authors: Adams CJ,Krueger R,Meade TJ

    更新日期:2020-02-21 00:00:00

  • Engineered Reader Proteins for Enhanced Detection of Methylated Lysine on Histones.

    abstract::Histone post-translational modifications (PTMs) are crucial for many cellular processes including mitosis, transcription, and DNA repair. The cellular readout of histone PTMs is dependent on both the chemical modification and histone site, and the array of histone PTMs on chromatin is dynamic throughout the eukaryotic...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b00651

    authors: Albanese KI,Krone MW,Petell CJ,Parker MM,Strahl BD,Brustad EM,Waters ML

    更新日期:2020-01-17 00:00:00

  • YTHDF2 Recognition of N1-Methyladenosine (m1A)-Modified RNA Is Associated with Transcript Destabilization.

    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

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b00655

    authors: Seo KW,Kleiner RE

    更新日期:2020-01-17 00:00:00

  • Cytosolic Delivery of Macromolecules in Live Human Cells Using the Combined Endosomal Escape Activities of a Small Molecule and Cell Penetrating Peptides.

    abstract::Ineffective cellular delivery is a common problem in numerous biological applications. Developing delivery reagents that work robustly in a variety of experimental settings remains a challenge. Herein, we report how peptides derived from the prototypical cell penetrating peptide TAT can be used in combination with a s...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b00585

    authors: Allen J,Najjar K,Erazo-Oliveras A,Kondow-McConaghy HM,Brock DJ,Graham K,Hager EC,Marschall ALJ,Dübel S,Juliano RL,Pellois JP

    更新日期:2019-12-20 00:00:00

  • Phenotypic Screen Identifies JAK2 as a Major Regulator of FAT10 Expression.

    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

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b00667

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

    更新日期:2019-12-20 00:00:00

  • Targeting Regorafenib-Induced Toxicity through Inhibition of Gut Microbial β-Glucuronidases.

    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

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b00663

    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

  • Mutations of Triad Determinants Changes the Substrate Alignment at the Catalytic Center of Human ALOX5.

    abstract::For the specificity of ALOX15 orthologs of different mammals, the geometry of the amino acids Phe353, Ile418, Met419, and Ile593 ("triad determinants") is important, and mutagenesis of these residues altered the reaction specificity of these enzymes. Here we expressed wild-type human ALOX5 and its F359W/A424I/N425M/A6...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b00674

    authors: Ivanov I,Golovanov AB,Ferretti C,Canyelles-Niño M,Heydeck D,Stehling S,Lluch JM,González-Lafont À,Kühn H

    更新日期:2019-12-20 00:00:00

  • Surprising Non-Additivity of Methyl Groups in Drug-Kinase Interaction.

    abstract::Drug optimization is guided by biophysical methods with increasing popularity. In the context of lead structure modifications, the introduction of methyl groups is a simple but potentially powerful approach. Hence, it is crucial to systematically investigate the influence of ligand methylation on biophysical character...

    journal_title:ACS chemical biology

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b00476

    authors: Wienen-Schmidt B,Schmidt D,Gerber HD,Heine A,Gohlke H,Klebe G

    更新日期:2019-12-20 00:00:00

  • Chemical Modulation of Human Mitochondrial ClpP: Potential Application in Cancer Therapeutics.

    abstract::The human ClpP proteolytic complex (HsClpP) is a serine protease located in the mitochondrial matrix and participates in the maintenance of the mitochondrial proteome among other cellular functions. HsClpP typically forms a multimeric complex with the AAA+ protein unfoldase HsClpX. Notably, compared to that of normal,...

    journal_title:ACS chemical biology

    pub_type: 杂志文章,评审

    doi:10.1021/acschembio.9b00347

    authors: Wong KS,Houry WA

    更新日期:2019-11-15 00:00:00

  • Mitochondrial Nascent Chain Quality Control Determines Organelle Form and Function.

    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

    pub_type: 杂志文章

    doi:10.1021/acschembio.9b00518

    authors: Battersby BJ,Richter U,Safronov O

    更新日期:2019-11-15 00:00:00

341 条记录 1/9 页 « 123456789 »