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BETting against wound healing Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-18 Irene Ylivinkka; Sara A. Wickström
A chemical screen identifies BET bromodomain inhibitors as inducers of an activated skin keratinocyte state that promotes the wound-healing capabilities of these cells. The study implicates epigenetic modifiers as potential targets for non-healing, chronic wounds.
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Desperately seeking sortase Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-18 James A. Van Deventer
Directed evolution on the yeast cell surface enables the discovery of sortase variants with altered specificity capable of modifying Aβ peptides under physiologically relevant conditions.
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Structural basis for non-radical catalysis by TsrM, a radical SAM methylase Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-18 Hayley L. Knox; Percival Yang-Ting Chen; Anthony J. Blaszczyk; Arnab Mukherjee; Tyler L. Grove; Erica L. Schwalm; Bo Wang; Catherine L. Drennan; Squire J. Booker
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Structure of Erm-modified 70S ribosome reveals the mechanism of macrolide resistance Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-18 Maxim S. Svetlov; Egor A. Syroegin; Elena V. Aleksandrova; Gemma C. Atkinson; Steven T. Gregory; Alexander S. Mankin; Yury S. Polikanov
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Characterizing the portability of phage-encoded homologous recombination proteins Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-18 Gabriel T. Filsinger; Timothy M. Wannier; Felix B. Pedersen; Isaac D. Lutz; Julie Zhang; Devon A. Stork; Anik Debnath; Kevin Gozzi; Helene Kuchwara; Verena Volf; Stan Wang; Xavier Rios; Christopher J. Gregg; Marc J. Lajoie; Seth L. Shipman; John Aach; Michael T. Laub; George M. Church
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BET bromodomain inhibitors regulate keratinocyte plasticity Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-18 Gabi Schutzius; Christian Kolter; Sebastian Bergling; Federico Tortelli; Florian Fuchs; Steffen Renner; Vito Guagnano; Simona Cotesta; Heinrich Rueeger; Michael Faller; Laure Bouchez; Adrian Salathe; Florian Nigsch; Shola M. Richards; Malvina Louis; Viktoria Gruber; Alexandra Aebi; Jonathan Turner; Frederic Grandjean; Jun Li; Chris Dimitri; Jason R. Thomas; Markus Schirle; Jutta Blank; Peter Drueckes;
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Publisher Correction: Rational discovery of molecular glue degraders via scalable chemical profiling Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-15 Cristina Mayor-Ruiz; Sophie Bauer; Matthias Brand; Zuzanna Kozicka; Marton Siklos; Hana Imrichova; Ines H. Kaltheuner; Elisa Hahn; Kristina Seiler; Anna Koren; Georg Petzold; Michaela Fellner; Christoph Bock; André C. Müller; Johannes Zuber; Matthias Geyer; Nicolas H. Thomä; Stefan Kubicek; Georg E. Winter
An amendment to this paper has been published and can be accessed via a link at the top of the paper.
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A cytochrome c is the natural electron acceptor for nicotine oxidoreductase Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-11 Mark Dulchavsky; Christopher T. Clark; James C. A. Bardwell; Frederick Stull
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Hierarchical chemical determination of amyloid polymorphs in neurodegenerative disease Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-11 Dan Li; Cong Liu
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Laboratory evolution of a sortase enzyme that modifies amyloid-β protein Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-11 Christopher J. Podracky; Chihui An; Alexandra DeSousa; Brent M. Dorr; Dominic M. Walsh; David R. Liu
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Robust direct digital-to-biological data storage in living cells Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-11 Sung Sun Yim; Ross M. McBee; Alan M. Song; Yiming Huang; Ravi U. Sheth; Harris H. Wang
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Harnessing nanotechnology to expand the toolbox of chemical biology Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-07 Ryan M. Williams; Shi Chen; Rachel E. Langenbacher; Thomas V. Galassi; Jackson D. Harvey; Prakrit V. Jena; Januka Budhathoki-Uprety; Minkui Luo; Daniel A. Heller
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Conformational rearrangement during activation of a metabotropic glutamate receptor Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-04 Brandon Wey-Hung Liauw; Hamid Samareh Afsari; Reza Vafabakhsh
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Molecular basis for ubiquitin ligase CRL2 FEM1C -mediated recognition of C-degron Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-04 Xiaojie Yan; Xiaolu Wang; Yao Li; Mengqi Zhou; Yanjun Li; Lili Song; Wenyi Mi; Jinrong Min; Cheng Dong
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Bottom-up de novo design of functional proteins with complex structural features Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-04 Che Yang; Fabian Sesterhenn; Jaume Bonet; Eva A. van Aalen; Leo Scheller; Luciano A. Abriata; Johannes T. Cramer; Xiaolin Wen; Stéphane Rosset; Sandrine Georgeon; Theodore Jardetzky; Thomas Krey; Martin Fussenegger; Maarten Merkx; Bruno E. Correia
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Molecular basis for arginine C-terminal degron recognition by Cul2 FEM1 E3 ligase Nat. Chem. Biol. (IF 12.587) Pub Date : 2021-01-04 Xinyan Chen; Shanhui Liao; Yaara Makaros; Qiong Guo; Zhongliang Zhu; Rina Krizelman; Karin Dahan; Xiaoming Tu; Xuebiao Yao; Itay Koren; Chao Xu
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Living materials fabricated via gradient mineralization of light-inducible biofilms Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-12-21 Yanyi Wang; Bolin An; Bin Xue; Jiahua Pu; Xiuli Zhang; Yuanyuan Huang; Yi Yu; Yi Cao; Chao Zhong
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Author Correction: Ion channels as lipid sensors: from structures to mechanisms Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-12-17 Mackenzie J. Thompson; John E. Baenziger
A Correction to this paper has been published: https://doi.org/10.1038/s41589-020-00722-1.
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Voices of chemical biology Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-12-16
We asked a collection of chemical biologists, “What is the most exciting frontier area in chemical biology and what key technology is needed to advance knowledge and applications in this area?” and reveal some of the perspectives we received.
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Controlling and enhancing CRISPR systems Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-12-16 Haridha Shivram; Brady F. Cress; Gavin J. Knott; Jennifer A. Doudna
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Linkage-specific ubiquitin chain formation depends on a lysine hydrocarbon ruler Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-12-07 Joanna Liwocha; David T. Krist; Gerbrand J. van der Heden van Noort; Fynn M. Hansen; Vinh H. Truong; Ozge Karayel; Nicholas Purser; Daniel Houston; Nicole Burton; Mark J. Bostock; Michael Sattler; Matthias Mann; Joseph S. Harrison; Gary Kleiger; Huib Ovaa; Brenda A. Schulman
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Cryptic phosphorylation in nucleoside natural product biosynthesis Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-30 Matthew M. Draelos; Anyarat Thanapipatsiri; Hilda Sucipto; Kenichi Yokoyama
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Making use of surplus sugar Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-16 Niels Agerbirk
Insects have many ways of disabling plant chemical defenses during feeding. Plant phloem feeders use surplus ingested sugar to block the activation of glucosinolate toxins, providing a target for precise resistance breeding.
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Delimiting lipids Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-16
This themed issue features a collection of articles that explore long-standing questions in the study of lipids and membranes.
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The conformational cycle of a prototypical voltage-gated sodium channel Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-16 William A. Catterall; Goragot Wisedchaisri; Ning Zheng
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Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-16 James Schiemer; Reto Horst; Yilin Meng; Justin I. Montgomery; Yingrong Xu; Xidong Feng; Kris Borzilleri; Daniel P. Uccello; Carolyn Leverett; Stephen Brown; Ye Che; Matthew F. Brown; Matthew M. Hayward; Adam M. Gilbert; Mark C. Noe; Matthew F. Calabrese
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Defining new chemical space for drug penetration into Gram-negative bacteria Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-16 Shibin Zhao; Justyna W. Adamiak; Vincent Bonifay; Jitender Mehla; Helen I. Zgurskaya; Derek S. Tan
We live in the era of antibiotic resistance, and this problem will progressively worsen if no new solutions emerge. In particular, Gram-negative pathogens present both biological and chemical challenges that hinder the discovery of new antibacterial drugs. First, these bacteria are protected from a variety of structurally diverse drugs by a low-permeability barrier composed of two membranes with distinct
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Ion channels as lipid sensors: from structures to mechanisms Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-16 Mackenzie J. Thompson; John E. Baenziger
Ion channels play critical roles in cellular function by facilitating the flow of ions across the membrane in response to chemical or mechanical stimuli. Ion channels operate in a lipid bilayer, which can modulate or define their function. Recent technical advancements have led to the solution of numerous ion channel structures solubilized in detergent and/or reconstituted into lipid bilayers, thus
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Cell type-selective secretome profiling in vivo Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-16 Wei Wei; Nicholas M. Riley; Andrew C. Yang; Joon T. Kim; Stephanie M. Terrell; Veronica L. Li; Marta Garcia-Contreras; Carolyn R. Bertozzi; Jonathan Z. Long
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Chemically informed analyses of metabolomics mass spectrometry data with Qemistree Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-16 Anupriya Tripathi; Yoshiki Vázquez-Baeza; Julia M. Gauglitz; Mingxun Wang; Kai Dührkop; Mélissa Nothias-Esposito; Deepa D. Acharya; Madeleine Ernst; Justin J. J. van der Hooft; Qiyun Zhu; Daniel McDonald; Asker D. Brejnrod; Antonio Gonzalez; Jo Handelsman; Markus Fleischauer; Marcus Ludwig; Sebastian Böcker; Louis-Félix Nothias; Rob Knight; Pieter C. Dorrestein
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Dynamics of an LPS translocon induced by substrate and an antimicrobial peptide Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-16 Francesco Fiorentino; Joshua B. Sauer; Xingyu Qiu; Robin A. Corey; C. Keith Cassidy; Benjamin Mynors-Wallis; Shahid Mehmood; Jani R. Bolla; Phillip J. Stansfeld; Carol V. Robinson
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Cholesterol access in cellular membranes controls Hedgehog signaling Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-16 Arun Radhakrishnan; Rajat Rohatgi; Christian Siebold
The Hedgehog (Hh) signaling pathway coordinates cell–cell communication in development and regeneration. Defects in this pathway underlie diseases ranging from birth defects to cancer. Hh signals are transmitted across the plasma membrane by two proteins, Patched 1 (PTCH1) and Smoothened (SMO). PTCH1, a transporter-like tumor-suppressor protein, binds to Hh ligands, but SMO, a G-protein-coupled-receptor
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Structural and functional consequences of reversible lipid asymmetry in living membranes Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-16 Milka Doktorova; Jessica L. Symons; Ilya Levental
Maintenance of lipid asymmetry across the two leaflets of the plasma membrane (PM) bilayer is a ubiquitous feature of eukaryotic cells. Loss of this asymmetry has been widely associated with cell death. However, increasing evidence points to the physiological importance of non-apoptotic, transient changes in PM asymmetry. Such transient scrambling events are associated with a range of biological functions
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The importance of the membrane for biophysical measurements Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-16 Dror S. Chorev; Carol V. Robinson
Within cell membranes numerous protein assemblies reside. Among their many functions, these assemblies regulate the movement of molecules between membranes, facilitate signaling into and out of cells, allow movement of cells by cell-matrix attachment, and regulate the electric potential of the membrane. With such critical roles, membrane protein complexes are of considerable interest for human health
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YY1 interacts with guanine quadruplexes to regulate DNA looping and gene expression Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-16 Lin Li; Preston Williams; Wendan Ren; Michelle Y. Wang; Zi Gao; Weili Miao; Ming Huang; Jikui Song; Yinsheng Wang
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Chemical reversal of abnormalities in cells carrying mitochondrial DNA mutations Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-09 Hiroki Kobayashi; Hideyuki Hatakeyama; Haruna Nishimura; Mutsumi Yokota; Sadafumi Suzuki; Yuri Tomabechi; Mikako Shirouzu; Hiroyuki Osada; Masakazu Mimaki; Yu-ichi Goto; Minoru Yoshida
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Production of Tyrian purple indigoid dye from tryptophan in Escherichia coli Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-11-02 Jeongchan Lee; Joonwon Kim; Ji Eun Song; Won-Suk Song; Eun-Jung Kim; Yun-Gon Kim; Hee-Jin Jeong; Hye Rim Kim; Kwon-Young Choi; Byung-Gee Kim
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Synthetic yeast brews neuroactive compounds Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-28 Yang Gu; Peng Xu
Metabolic engineering offers the flexibility to meet market demand for bioactive natural products but can be hampered when a necessary protein or intermediate is toxic. In yeast, modifying the subcellular localization of biosynthetic enzymes can alleviate toxicity and increase production titer.
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Visualizing a protonated RNA state that modulates microRNA-21 maturation Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-26 Jared T. Baisden; Joshua A. Boyer; Bo Zhao; Scott M. Hammond; Qi Zhang
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Interhelical interactions within the STIM1 CC1 domain modulate CRAC channel activation Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-26 Petr Rathner; Marc Fahrner; Linda Cerofolini; Herwig Grabmayr; Ferdinand Horvath; Heinrich Krobath; Agrim Gupta; Enrico Ravera; Marco Fragai; Matthias Bechmann; Thomas Renger; Claudio Luchinat; Christoph Romanin; Norbert Müller
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Rerouting plant terpene biosynthesis enables momilactone pathway elucidation Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-26 Ricardo De La Peña; Elizabeth S. Sattely
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Structural basis for persulfide-sensing specificity in a transcriptional regulator Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-26 Daiana A. Capdevila; Brenna J. C. Walsh; Yifan Zhang; Christopher Dietrich; Giovanni Gonzalez-Gutierrez; David P. Giedroc
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SARS-CoV-2 M pro inhibitors and activity-based probes for patient-sample imaging Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-22 Wioletta Rut; Katarzyna Groborz; Linlin Zhang; Xinyuanyuan Sun; Mikolaj Zmudzinski; Bartlomiej Pawlik; Xinyu Wang; Dirk Jochmans; Johan Neyts; Wojciech Młynarski; Rolf Hilgenfeld; Marcin Drag
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Bi-paratopic and multivalent VH domains block ACE2 binding and neutralize SARS-CoV-2 Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-20 Colton J. Bracken; Shion A. Lim; Paige Solomon; Nicholas J. Rettko; Duy P. Nguyen; Beth Shoshana Zha; Kaitlin Schaefer; James R. Byrnes; Jie Zhou; Irene Lui; Jia Liu; Katarina Pance; Xin X. Zhou; Kevin K. Leung; James A. Wells
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Cuticle thickness affects dynamics of volatile emission from petunia flowers Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-19 Pan Liao; Shaunak Ray; Benoît Boachon; Joseph H. Lynch; Arnav Deshpande; Scott McAdam; John A. Morgan; Natalia Dudareva
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Hijacking protein degradation Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-16
Targeted protein degradation provides a powerful complement to small-molecule inhibition in modulating protein activity and allows access to otherwise intractable drug targets.
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Advanced rules of relays Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-16 Sonja Lorenz; Katrin Rittinger
Transfer of ubiquitin onto target proteins requires controlled interplay between E2 conjugating enzymes and E3 ligases. The structure of a trapped E2~Ub/RCR E3 transfer intermediate provides novel insight into the diversity of mechanisms used to fine tune this relay.
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A two-pronged attack Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-16 Joshua J. Feng; Chao Zhang
Targeted small-molecule inhibition of BRAFV600E faces seemingly insurmountable obstacles in the clinic, such as rapid emergence of drug resistance. A recent study illustrates the potential of an alternative therapeutic strategy via PROTAC-mediated degradation of the oncogenic BRAF.
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Reversal of nucleobase methylation by dioxygenases Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-16 Guo-Liang Xu; Matthias Bochtler
The repertoire of nucleobase methylation in DNA and RNA, introduced by chemical agents or enzymes, is large. Most methylation can be reversed either directly by restoration of the original nucleobase or indirectly by replacement of the methylated nucleobase with an unmodified nucleobase. In many direct and indirect demethylation reactions, ALKBH (AlkB homolog) and TET (ten eleven translocation) hydroxylases
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Peroxisome compartmentalization of a toxic enzyme improves alkaloid production Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-12 Parbir S. Grewal; Jennifer A. Samson; Jordan J. Baker; Brian Choi; John E. Dueber
Eukaryotic cells compartmentalize metabolic pathways in organelles to achieve optimal reaction conditions and avoid crosstalk with cytosolic factors. We found that cytosolic expression of norcoclaurine synthase (NCS), the enzyme that catalyzes the first committed reaction in benzylisoquinoline alkaloid biosynthesis, is toxic in Saccharomyces cerevisiae and, consequently, restricts (S)-reticuline production
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Discovery of iron-sensing bacterial riboswitches Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-05 Siladitya Bandyopadhyay; Susmitnarayan Chaudhury; Dolly Mehta; Arati Ramesh
Despite the central role of iron in biology, our understanding of how cells sense iron is limited to protein-dependent mechanisms. Here, we report the discovery of iron-sensing riboswitches (named Sensei). Present across bacterial phyla, these RNAs reside in the 5′ untranslated regions or within coding regions of messenger RNAs (mRNAs) encoding iron-related proteins. These riboswitches bind the reduced
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Sulfated glycans engage the Ang–Tie pathway to regulate vascular development Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-10-05 Matthew E. Griffin; Alexander W. Sorum; Gregory M. Miller; William A. Goddard; Linda C. Hsieh-Wilson
The angiopoietin (Ang)–Tie pathway is essential for the proper maturation and remodeling of the vasculature. Despite its importance in disease, the mechanisms that control signal transduction through this pathway are poorly understood. Here, we demonstrate that heparan sulfate glycosaminoglycans (HS GAGs) regulate Ang–Tie signaling through direct interactions with both Ang ligands and Tie1 receptors
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Designer adhesion GPCR tells its signaling story Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-09-28 Eugenia V. Gurevich; Vsevolod V. Gurevich
The ADGRL3 receptor, a member of the adhesion G-protein-coupled receptor family, is implicated in many neurological diseases. Using a novel technique involving controlled proteolysis of the receptor’s extracellular domain, this study demonstrated that ADGRL3 signals via G12/13 G proteins.
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CueR activates transcription through a DNA distortion mechanism Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-09-28 Chengli Fang; Steven J. Philips; Xiaoxian Wu; Kui Chen; Jing Shi; Liqiang Shen; Juncao Xu; Yu Feng; Thomas V. O’Halloran; Yu Zhang
The MerR-family transcription factors (TFs) are a large group of bacterial proteins responding to cellular metal ions and multiple antibiotics by binding within central RNA polymerase-binding regions of a promoter. While most TFs alter transcription through protein–protein interactions, MerR TFs are capable of reshaping promoter DNA. To address the question of which mechanism prevails, we determined
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Glucosylation prevents plant defense activation in phloem-feeding insects Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-09-28 Osnat Malka; Michael L. A. E. Easson; Christian Paetz; Monika Götz; Michael Reichelt; Beate Stein; Katrin Luck; Aleksa Stanišić; Ksenia Juravel; Diego Santos-Garcia; Lilach L. Mondaca; Simon Springate; John Colvin; Stephan Winter; Jonathan Gershenzon; Shai Morin; Daniel G. Vassão
The metabolic adaptations by which phloem-feeding insects counteract plant defense compounds are poorly known. Two-component plant defenses, such as glucosinolates, consist of a glucosylated protoxin that is activated by a glycoside hydrolase upon plant damage. Phloem-feeding herbivores are not generally believed to be negatively impacted by two-component defenses due to their slender piercing-sucking
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An ultrasensitive biosensor for high-resolution kinase activity imaging in awake mice Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-09-28 Jin-Fan Zhang; Bian Liu; Ingie Hong; Albert Mo; Richard H. Roth; Brian Tenner; Wei Lin; Jason Z. Zhang; Rosana S. Molina; Mikhail Drobizhev; Thomas E. Hughes; Lin Tian; Richard L. Huganir; Sohum Mehta; Jin Zhang
Protein kinases control nearly every facet of cellular function. These key signaling nodes integrate diverse pathway inputs to regulate complex physiological processes, and aberrant kinase signaling is linked to numerous pathologies. While fluorescent protein-based biosensors have revolutionized the study of kinase signaling by allowing direct, spatiotemporally precise kinase activity measurements
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Selective regulation of human TRAAK channels by biologically active phospholipids Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-09-28 Samantha Schrecke; Yun Zhu; Jacob W. McCabe; Mariah Bartz; Charles Packianathan; Minglei Zhao; Ming Zhou; David Russell; Arthur Laganowsky
TRAAK is an ion channel from the two-pore domain potassium (K2P) channel family with roles in maintaining the resting membrane potential and fast action potential conduction. Regulated by a wide range of physical and chemical stimuli, the affinity and selectivity of K2P4.1 toward lipids remains poorly understood. Here we show the two isoforms of K2P4.1 have distinct binding preferences for lipids dependent
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PROTAC-mediated degradation reveals a non-catalytic function of AURORA-A kinase Nat. Chem. Biol. (IF 12.587) Pub Date : 2020-09-28 Bikash Adhikari; Jelena Bozilovic; Mathias Diebold; Jessica Denise Schwarz; Julia Hofstetter; Martin Schröder; Marek Wanior; Ashwin Narain; Markus Vogt; Nevenka Dudvarski Stankovic; Apoorva Baluapuri; Lars Schönemann; Lorenz Eing; Pranjali Bhandare; Bernhard Kuster; Andreas Schlosser; Stephanie Heinzlmeir; Christoph Sotriffer; Stefan Knapp; Elmar Wolf
The mitotic kinase AURORA-A is essential for cell cycle progression and is considered a priority cancer target. Although the catalytic activity of AURORA-A is essential for its mitotic function, recent reports indicate an additional non-catalytic function, which is difficult to target by conventional small molecules. We therefore developed a series of chemical degraders (PROTACs) by connecting a clinical
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