PDZ-Reactive Peptide Activates Ephrin-B Reverse Signaling and Inhibits Neuronal Chemotaxis.


: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, which subsequently inhibited SDF-1 induced neuronal chemotaxis of human neuroblastoma cells and mouse cerebellar granule neurons. Our work provides direct evidence that PDZ-RGS3 bridges ephrin-B reverse signaling and SDF-1 induced G protein signaling for the first time.


ACS Chem Biol


ACS chemical biology


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




Has Abstract


2016-01-15 00:00:00












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    abstract::Regulators of G protein signaling (RGS) proteins are key players in regulating signaling via G protein-coupled receptors. RGS proteins directly bind to the Gα-subunits of activated heterotrimeric G-proteins, and accelerate the rate of GTP hydrolysis, thereby rapidly deactivating G-proteins. Using atomistic simulations...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Vashisth H,Storaska AJ,Neubig RR,Brooks CL 3rd

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  • Structural and Functional Evidence Indicates Selective Oxygen Signaling in Caldanaerobacter subterraneus H-NOX.

    abstract::Acute and specific sensing of diatomic gas molecules is an essential facet of biological signaling. Heme nitric oxide/oxygen binding (H-NOX) proteins are a family of gas sensors found in diverse classes of bacteria and eukaryotes. The most commonly characterized bacterial H-NOX domains are from facultative anaerobes a...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Hespen CW,Bruegger JJ,Phillips-Piro CM,Marletta MA

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  • In vitro and in vivo characterization of a tunable dual-reactivity probe of the Nrf2-ARE pathway.

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


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

    更新日期:2013-08-16 00:00:00

  • CRISPRi and CRISPRa Screens in Mammalian Cells for Precision Biology and Medicine.

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    journal_title:ACS chemical biology

    pub_type: 杂志文章,评审


    authors: Kampmann M

    更新日期:2018-02-16 00:00:00

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    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

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Poh WH,Barraud N,Guglielmo S,Lazzarato L,Rolando B,Fruttero R,Rice SA

    更新日期:2017-08-18 00:00:00

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Parrish AR,She X,Xiang Z,Coin I,Shen Z,Briggs SP,Dillin A,Wang L

    更新日期:2012-07-20 00:00:00

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Kim WH,Jung DW,Kim J,Im SH,Hwang SY,Williams DR

    更新日期:2012-04-20 00:00:00

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Klim JR,Fowler AJ,Courtney AH,Wrighton PJ,Sheridan RT,Wong ML,Kiessling LL

    更新日期:2012-03-16 00:00:00

  • Molecular tweezers inhibit islet amyloid polypeptide assembly and toxicity by a new mechanism.

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Lopes DH,Attar A,Nair G,Hayden EY,Du Z,McDaniel K,Dutt S,Bravo-Rodriguez K,Mittal S,Klärner FG,Wang C,Sanchez-Garcia E,Schrader T,Bitan G

    更新日期:2015-06-19 00:00:00

  • Topology specific stabilization of promoter over telomeric G-quadruplex DNAs by bisbenzimidazole carboxamide derivatives.

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Dhamodharan V,Harikrishna S,Bhasikuttan AC,Pradeepkumar PI

    更新日期:2015-03-20 00:00:00

  • Chemical Proteomics and Structural Biology Define EPHA2 Inhibition by Clinical Kinase Drugs.

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    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

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Rinaldi S,Assimon VA,Young ZT,Morra G,Shao H,Taylor IR,Gestwicki JE,Colombo G

    更新日期:2018-11-16 00:00:00

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Henares BM,Higgins KE,Boon EM

    更新日期:2012-08-17 00:00:00

  • Structural Insights into the CotB2-Catalyzed Cyclization of Geranylgeranyl Diphosphate to the Diterpene Cyclooctat-9-en-7-ol.

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Tomita T,Kim SY,Teramoto K,Meguro A,Ozaki T,Yoshida A,Motoyoshi Y,Mori N,Ishigami K,Watanabe H,Nishiyama M,Kuzuyama T

    更新日期:2017-06-16 00:00:00

  • Enzymatic synthesis of polybrominated dioxins from the marine environment.

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    journal_title:ACS chemical biology

    pub_type: 信件


    authors: Agarwal V,Moore BS

    更新日期:2014-09-19 00:00:00

  • Two-Way Gold Nanoparticle Label-Free Sensing of Specific Sequence and Small Molecule Targets Using Switchable Concatemers.

    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

    pub_type: 杂志文章


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

    更新日期:2017-05-19 00:00:00

  • Catalytic mechanisms and biocatalytic applications of aspartate and methylaspartate ammonia lyases.

    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

    pub_type: 杂志文章


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

    更新日期:2012-10-19 00:00:00

  • Generation of Optogenetically Modified Adenovirus Vector for Spatiotemporally Controllable Gene Therapy.

    abstract::Gene therapy is expected to be utilized for the treatment of various diseases. However, the spatiotemporal resolution of current gene therapy technology is not high enough. In this study, we generated a new technology for spatiotemporally controllable gene therapy. We introduced optogenetic and CRISPR/Cas9 techniques ...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Takayama K,Mizuguchi H

    更新日期:2018-02-16 00:00:00

  • Inhibition of DC-SIGN-mediated HIV infection by a linear trimannoside mimic in a tetravalent presentation.

    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

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    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

  • 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


    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

  • Peptides derived from the transmembrane domain of Bcl-2 proteins as potential mitochondrial priming tools.

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Andreu-Fernández V,Genoves A,Lee TH,Stellato M,Lucantoni F,Orzáez M,Mingarro I,Aguilar MI,Pérez-Payá E

    更新日期:2014-08-15 00:00:00

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    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


    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

  • Chemoproteomics-Enabled Covalent Ligand Screening Reveals ALDH3A1 as a Lung Cancer Therapy Target.

    abstract::Chemical genetics is a powerful approach for identifying therapeutically active small molecules, but identifying the mechanisms of action underlying hit compounds remains challenging. Chemoproteomic platforms have arisen to tackle this challenge and enable rapid mechanistic deconvolution of small-molecule screening hi...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Counihan JL,Wiggenhorn AL,Anderson KE,Nomura DK

    更新日期:2018-08-17 00:00:00

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    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

  • A comparative study of bioorthogonal reactions with azides.

    abstract::Detection of metabolites and post-translational modifications can be achieved using the azide as a bioorthogonal chemical reporter. Once introduced into target biomolecules, either metabolically or through chemical modification, the azide can be tagged with probes using one of three highly selective reactions: the Sta...

    journal_title:ACS chemical biology

    pub_type: 信件


    authors: Agard NJ,Baskin JM,Prescher JA,Lo A,Bertozzi CR

    更新日期:2006-11-21 00:00:00

  • Mad2 Inhibitor-1 (M2I-1): A Small Molecule Protein-Protein Interaction Inhibitor Targeting the Mitotic Spindle Assembly Checkpoint.

    abstract::The genetic integrity of each organism depends on the faithful segregation of its genome during mitosis. To meet this challenge, a cellular surveillance mechanism, termed the spindle assembly checkpoint (SAC), evolved that monitors the correct attachment of chromosomes and blocks progression through mitosis if correct...

    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Kastl J,Braun J,Prestel A,Möller HM,Huhn T,Mayer TU

    更新日期:2015-07-17 00:00:00

  • Targeting native adult heart progenitors with cardiogenic small molecules.

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: Russell JL,Goetsch SC,Aguilar HR,Frantz DE,Schneider JW

    更新日期:2012-06-15 00:00:00

  • Lipid nanoparticles improve activity of single-stranded siRNA and gapmer antisense oligonucleotides in animals.

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    journal_title:ACS chemical biology

    pub_type: 信件


    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

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    journal_title:ACS chemical biology

    pub_type: 杂志文章


    authors: NaveenKumar SK,SharathBabu BN,Hemshekhar M,Kemparaju K,Girish KS,Mugesh G

    更新日期:2018-08-17 00:00:00