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A sterol analog inhibits hedgehog pathway by blocking cholesterylation of smoothened Cell Chem. Bio. (IF 8.6) Pub Date : 2024-03-04 Yuan-Bin Liu, Li-Ming He, Ming Sun, Wen-Jun Luo, Zi-Cun Lin, Zhi-Ping Qiu, Yu-Liang Zhang, Ao Hu, Jie Luo, Wen-Wei Qiu, Bao-Liang Song
The hedgehog (Hh) signaling pathway has long been a hotspot for anti-cancer drug development due to its important role in cell proliferation and tumorigenesis. However, most clinically available Hh pathway inhibitors target the seven-transmembrane region (7TM) of smoothened (SMO), and the acquired drug resistance is an urgent problem in SMO inhibitory therapy. Here, we identify a sterol analog Q29
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Metabolic rewiring and communication in cancer immunity Cell Chem. Bio. (IF 8.6) Pub Date : 2024-02-29 Nicole M. Chapman, Hongbo Chi
The immune system shapes tumor development and progression. Although immunotherapy has transformed cancer treatment, its overall efficacy remains limited, underscoring the need to uncover mechanisms to improve therapeutic effects. Metabolism-associated processes, including intracellular metabolic reprogramming and intercellular metabolic crosstalk, are emerging as instructive signals for anti-tumor
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Allosteric inhibition of tRNA synthetase Gln4 by N-pyrimidinyl-β-thiophenylacrylamides exerts highly selective antifungal activity Cell Chem. Bio. (IF 8.6) Pub Date : 2024-02-22 Emily Puumala, David Sychantha, Elizabeth Lach, Shawn Reeves, Sunna Nabeela, Meea Fogal, AkshatKumar Nigam, Jarrod W. Johnson, Alán Aspuru-Guzik, Rebecca S. Shapiro, Priya Uppuluri, Subha Kalyaanamoorthy, Jakob Magolan, Luke Whitesell, Nicole Robbins, Gerard D. Wright, Leah E. Cowen
species are among the most prevalent causes of systemic fungal infections, which account for ∼1.5 million annual fatalities. Here, we build on a compound screen that identified the molecule N-pyrimidinyl-β-thiophenylacrylamide (NP-BTA), which strongly inhibits growth. NP-BTA was hypothesized to target glutaminyl-tRNA synthetase, Gln4. Here, we confirmed through amino-acylation assays NP-BTA is a potent
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CYP7B1-mediated 25-hydroxycholesterol degradation maintains quiescence-activation balance and improves therapeutic potential of mesenchymal stem cells Cell Chem. Bio. (IF 8.6) Pub Date : 2024-02-20 Zhaoqiang Zhang, Zepeng Su, Zhikun Li, Jinteng Li, Wenhui Yu, Guiwen Ye, Jiajie Lin, Yunshu Che, Peitao Xu, Yipeng Zeng, Yanfeng Wu, Huiyong Shen, Zhongyu Xie
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All the mutations that are fit to die Cell Chem. Bio. (IF 8.6) Pub Date : 2024-02-15 Emma Gebauer, Markus A. Seeliger
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Cellular reprogramming by protein degradation: The next frontier in cancer immunotherapy Cell Chem. Bio. (IF 8.6) Pub Date : 2024-02-15 Erik Ehinger, Anjana Rao
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Meet the authors: Cydney N. Johnson, Shyra Wilde, Elaine Tuomanen, and Jason W. Rosch Cell Chem. Bio. (IF 8.6) Pub Date : 2024-02-15 Cydney N. Johnson, Shyra Wilde, Elaine Tuomanen, Jason W. Rosch
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When CDK4/6i meets GPX4i: Stop dividing to die iron hard Cell Chem. Bio. (IF 8.6) Pub Date : 2024-02-15 Deguang Liang, Xuejun Jiang
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Identification of differential biological activity and synergy between the PARP inhibitor rucaparib and its major metabolite Cell Chem. Bio. (IF 8.6) Pub Date : 2024-02-08 Huabin Hu, Carme Serra, Wenjie Zhang, Aurora Scrivo, Irene Fernández-Carasa, Antonella Consiglio, Alvaro Aytes, Miguel Angel Pujana, Amadeu Llebaria, Albert A. Antolin
The (poly)pharmacology of drug metabolites is seldom comprehensively characterized in drug discovery. However, some drug metabolites can reach high plasma concentrations and display activity. Here, we use computational and experimental methods to comprehensively characterize the kinase polypharmacology of M324, the major metabolite of the PARP1 inhibitor rucaparib. We demonstrate that M324 displays
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The cyclimids: Degron-inspired cereblon binders for targeted protein degradation Cell Chem. Bio. (IF 8.6) Pub Date : 2024-02-05 Saki Ichikawa, N. Connor Payne, Wenqing Xu, Chia-Fu Chang, Nandini Vallavoju, Spencer Frome, Hope A. Flaxman, Ralph Mazitschek, Christina M. Woo
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Anti-tumor immunotherapy using engineered bacterial outer membrane vesicles fused to lysosome-targeting chimeras mediated by transferrin receptor Cell Chem. Bio. (IF 8.6) Pub Date : 2024-02-02 Ling-Yan Su, Yang Tian, Qiang Zheng, Yu Cao, Mengyu Yao, Shuangping Wang, Wen Xu, Chuyu Xi, Andrea Clocchiatti, Guangjun Nie, Hejiang Zhou
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Identification and characterization of a potent and selective HUNK inhibitor for treatment of HER2+ breast cancer Cell Chem. Bio. (IF 8.6) Pub Date : 2024-02-01 Tinslee Dilday, Melissa Abt, Nicole Ramos-Solís, Neetu Dayal, Elizabeth Larocque, Adrian L. Oblak, Herman O. Sintim, Elizabeth S. Yeh
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Beyond antibiotic resistance: The whiB7 transcription factor coordinates an adaptive response to alanine starvation in mycobacteria Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-23 Nicholas C. Poulton, Michael A. DeJesus, Vanisha Munsamy-Govender, Mariko Kanai, Cameron G. Roberts, Zachary A. Azadian, Barbara Bosch, Karl Matthew Lin, Shuqi Li, Jeremy M. Rock
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PARP trapping is governed by the PARP inhibitor dissociation rate constant Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-22 Angelica A. Gopal, Bianca Fernandez, Justin Delano, Ralph Weissleder, J. Matthew Dubach
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30th anniversary celebrations: Inspiring innovation in biology and medicine Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-18 T, h, e, , C, e, l, l, , C, h, e, m, i, c, a, l, , B, i, o, l, o, g, y, , e, d, i, t, o, r, i, a, l, , t, e, a, m
Abstract not available
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Cultivating creativity and belonging in science Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-18 M, e, g, a, n, , K, e, n
In this Stories piece, Megan Ken, a Fellow at The Scripps Research Institute, discusses the importance of inclusion, mentoring, and creativity to discovery and growth in science.
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30th anniversary of Cell Chemical Biology: A conversation with founding editors K.C. Nicolaou and Gregory Verdine Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-18 K.C. Nicolaou, Gregory L. Verdine
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Voices: Challenges and opportunities in RNA biology Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-18 Ling-Ling Chen, Nicholas T. Ingolia, Megan L. Insco, Jin Billy Li, Shalini Oberdoerffer, Kevin M. Weeks
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Mo’ m1A, mo’ problems Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-18 Linamarie Miller, James Shorter
CAG-repeat expansions underlie fatal neurodegenerative disorders. In a lodestar study published in a recent issue of Nature, Sun et al.1 identify a writer and eraser of N1-methyladenosine (m1A) modifications of CAG-repeat RNA. They establish that m1A modifications in CAG-repeat expanded RNA promote neurodegeneration and aberrant phase transitions of TDP-43. These findings suggest therapeutic strategies
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Bioorthogonal click labeling of an amber-free HIV-1 provirus for in-virus single molecule imaging Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-16 Yuanyun Ao, Jonathan R. Grover, Levi Gifford, Yang Han, Guohua Zhong, Revansiddha Katte, Wenwei Li, Rajanya Bhattacharjee, Baoshan Zhang, Stephanie Sauve, Wenyi Qin, Dibya Ghimire, Md Anzarul Haque, James Arthos, Mahmoud Moradi, Walther Mothes, Edward A. Lemke, Peter D. Kwong, Gregory B. Melikyan, Maolin Lu
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The interaction between NLRP1 and oxidized TRX1 involves a transient disulfide bond Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-11 Michael B. Geeson, Jeffrey C. Hsiao, Lydia P. Tsamouri, Daniel P. Ball, Daniel A. Bachovchin
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Regulation of bacterial gene expression by non-coding RNA: It is all about time! Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-10 Adrien Chauvier, Nils G. Walter
Commensal and pathogenic bacteria continuously evolve to survive in diverse ecological niches by efficiently coordinating gene expression levels in their ever-changing environments. Regulation through the RNA transcript itself offers a faster and more cost-effective way to adapt than protein-based mechanisms and can be leveraged for diagnostic or antimicrobial purposes. However, RNA can fold into numerous
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Causes, functions, and therapeutic possibilities of RNA secondary structure ensembles and alternative states Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-09 Ritwika Bose, Irfana Saleem, Anthony M. Mustoe
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Discovery of a PROTAC degrader for METTL3-METTL14 complex Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-08 Wenhao Du, Yuting Huang, Xiaoai Chen, Yue Deng, Yaoliang Sun, Hong Yang, Qiongyu Shi, Feifei Wu, Guobin Liu, He Huang, Jian Ding, Xun Huang, Shilin Xu
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An acyl-CoA thioesterase is essential for the biosynthesis of a key dauer pheromone in C. elegans Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-05 Subhradeep Bhar, Chi-Su Yoon, Kevin Mai, Jungsoo Han, Dilip V. Prajapati, Yuting Wang, Candy L. Steffen, Laura S. Bailey, Kari B. Basso, Rebecca A. Butcher
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Discovery of dual-active ethionamide boosters inhibiting the Mycobacterium tuberculosis ESX-1 secretion system Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-04 Raphael Gries, Jason Chhen, Edeltraud van Gumpel, Sebastian J. Theobald, Lindsay Sonnenkalb, Christian Utpatel, Fabian Metzen, Manuel Koch, Tobias Dallenga, Kamel Djaout, Alain Baulard, Michael Dal Molin, Jan Rybniker
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Modifying the antiviral innate immune response by selective writing, erasing, and reading of m6A on viral and cellular RNA Cell Chem. Bio. (IF 8.6) Pub Date : 2024-01-03 Caroline J. Aufgebauer, Katherine M. Bland, Stacy M. Horner
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Recognition of the tRNA structure: Everything everywhere but not all at once Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-29 J, i, n, w, e, i, , Z, h, a, n, g
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Bivalent inhibitors of the BTB E3 ligase KEAP1 enable instant NRF2 activation to suppress acute inflammatory response Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-28 Mengchen Lu, Jianai Ji, Yifei Lv, Jing Zhao, Yuting Liu, Qiong Jiao, Tian Liu, Yi Mou, Qidong You, Zhengyu Jiang
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One-pot trimodal mapping of unmethylated, hydroxymethylated, and open chromatin sites unveils distinctive 5hmC roles at dynamic chromatin loci Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-27 Kotryna Skardžiūtė, Kotryna Kvederavičiūtė, Inga Pečiulienė, Milda Narmontė, Povilas Gibas, Janina Ličytė, Saulius Klimašauskas, Edita Kriukienė
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A dual-targeting succinate dehydrogenase and F1Fo-ATP synthase inhibitor rapidly sterilizes replicating and non-replicating Mycobacterium tuberculosis Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-26 Cara Adolph, Chen-Yi Cheung, Matthew B. McNeil, William J. Jowsey, Zoe C. Williams, Kiel Hards, Liam K. Harold, Ashraf Aboelela, Richard S. Bujaroski, Benjamin J. Buckley, Joel D.A. Tyndall, Zhengqiu Li, Julian D. Langer, Laura Preiss, Thomas Meier, Adrie J.C. Steyn, Kyu Y. Rhee, Michael Berney, Michael J. Kelso, Gregory M. Cook
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Tag, you’re it: G-ICAT identifies p120-cysteine glutathionylation triggering E-cadherin destabilization Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-21 Kevin T. Fridianto, Yimon Aye
Current methods have limited ability in directly quantifying the extent of glutathionylation on specific protein-cysteines. In this issue of Cell Chemical Biology, Ahn et al.1 report G-ICAT (glutathione-based isotope-coded affinity tag), aimed at addressing this limitation. G-ICAT identifies Cysteine-692 within p120-catenin—a member of cadherin complex essential for cell–cell-contact maintenance—where
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Knocking off cancer’s HAT: CSS1477 disrupts oncogenic programs Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-21 Luyao Kevin Xu, Panagiotis Ntziachristos
EP300/CBP are histone acetyltransferases recruited onto chromatin by oncogenic transcription factors and control the transcriptional program via their activity in enhancer areas. In the December issue of Cancer Cell, Nicosia et al.1 offer new promise in targeting EP300/CBP using the small-molecule inhibitor CSS1477 in patients with blood tumors and no other therapeutic options.
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A game of networks: Do different lipids interact to orchestrate inflammatory homeostasis? Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-21 Alessandro Leuti, Marina Fava, Mauro Maccarrone
Resolution of inflammation is the physiological process whereby endogenous pro-resolving lipids constrain inflammatory stimuli that would otherwise cause chronic inflammation. In this issue of Cell Chemical Biology, Peltner et al.1 report that the cannabis component cannabidiol induces production of pro-resolving lipids directly activating 15-lipoxygenase and inhibiting 5-lipoxygenase in human macrophages
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A histone deacetylase network regulates epigenetic reprogramming and viral silencing in HIV-infected cells Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-21 Jackson J. Peterson, Catherine A. Lewis, Samuel D. Burgos, Ashokkumar Manickam, Yinyan Xu, Allison A. Rowley, Genevieve Clutton, Brian Richardson, Fei Zou, Jeremy M. Simon, David M. Margolis, Nilu Goonetilleke, Edward P. Browne
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Development of an intracellular quantitative assay to measure compound binding kinetics Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-21 Charles S. Lay, Daniel A. Thomas, John P. Evans, Matthew Campbell, Kristopher McCombe, Alexander N. Phillipou, Laurie J. Gordon, Emma J. Jones, Kristin Riching, Mahnoor Mahmood, Cassie Messenger, Charlotte E. Carver, Kelly M. Gatfield, Peter D. Craggs
Abstract not available
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Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-19 Ka Yang, Rebecca L. Whitehouse, Shane L. Dawson, Lu Zhang, Jeffrey G. Martin, Douglas S. Johnson, Joao A. Paulo, Steven P. Gygi, Qing Yu
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Protein semisynthesis underscores the role of a conserved lysine in activation and desensitization of acid-sensing ion channels Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-18 Debayan Sarkar, Iacopo Galleano, Stephanie Andrea Heusser, Sofie Yuewei Ou, Gül Refika Uzun, Keith K. Khoo, Gerbrand Jan van der Heden van Noort, Joseph Scott Harrison, Stephan Alexander Pless
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Targeting cap1 RNA methyltransferases as an antiviral strategy Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-12 Yuta Tsukamoto, Manabu Igarashi, Hiroki Kato
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Profiling nuclear cysteine ligandability and effects on nuclear localization using proximity labeling-coupled chemoproteomics Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-11 Qianni Peng, Eranthie Weerapana
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Irreversible inhibition of TRF2TRFH recruiting functions by a covalent cyclic peptide induces telomeric replication stress in cancer cells Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-07 Alexander P. Sobinoff, Salvatore Di Maro, Ronnie R.J. Low, Rosaria Benedetti, Stefano Tomassi, Antonia D'Aniello, Rosita Russo, Ilaria Baglivo, Ugo Chianese, Paolo V. Pedone, Angela Chambery, Anthony J. Cesare, Lucia Altucci, Hilda A. Pickett, Sandro Cosconati
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Subtype-selective prenylated isoflavonoids disrupt regulatory drivers of MYCN-amplified cancers Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-06 Michael E. Stokes, Alessandro Vasciaveo, Jonnell Candice Small, Arie Zask, Eduard Reznik, Nailah Smith, Qian Wang, Jacob Daniels, Farhad Forouhar, Presha Rajbhandari, Andrea Califano, Brent R. Stockwell
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Potent and selective binders of the E3 ubiquitin ligase ZNRF3 stimulate Wnt signaling and intestinal organoid growth Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-05 Yvonne T. Kschonsak, Xinxin Gao, Stephen E. Miller, Sunhee Hwang, Hadir Marei, Ping Wu, Yanjie Li, Karen Ruiz, Kristel Dorighi, Loryn Holokai, Pirunthan Perampalam, Wen-Ting K. Tsai, Yee-Seir Kee, Nicholas J. Agard, Seth F. Harris, Rami N. Hannoush, Felipe de Sousa e Melo
Selective and precise activation of signaling transduction cascades is key for cellular reprogramming and tissue regeneration. However, the development of small- or large-molecule agonists for many signaling pathways has remained elusive and is rate limiting to realize the full clinical potential of regenerative medicine. Focusing on the Wnt pathway, here we describe a series of disulfide-constrained
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Convergent impact of vaccination and antibiotic pressures on pneumococcal populations Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-04 Cydney N. Johnson, Shyra Wilde, Elaine Tuomanen, Jason W. Rosch
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Selective and brain-penetrant HCN1 inhibitors reveal links between synaptic integration, cortical function, and working memory Cell Chem. Bio. (IF 8.6) Pub Date : 2023-12-01 Eva Harde, Markus Hierl, Michael Weber, David Waiz, Roger Wyler, Jean-Yves Wach, Rachel Haab, Anja Gundlfinger, Weiping He, Patrick Schnider, Manuel Paina, Jean-Francois Rolland, Andrea Greiter-Wilke, Rodolfo Gasser, Michael Reutlinger, Amanda Dupont, Sonia Roberts, Eoin C. O'Connor, Björn Bartels, Benjamin J. Hall
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HER-096 is a CDNF-derived brain-penetrating peptidomimetic that protects dopaminergic neurons in a mouse synucleinopathy model of Parkinson’s disease Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-30 Natalia Kulesskaya, Arnab Bhattacharjee, Kira M. Holmström, Päivi Vuorio, Alexandre Henriques, Noëlle Callizot, Henri J. Huttunen
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Multiplex miRNA reporting platform for real-time profiling of living cells Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-29 Yaxin Hu, Cheuk Yin Li, Qiuyu Lu, Yi Kuang
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Discovery of antibiotics that selectively kill metabolically dormant bacteria Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-28 Erica J. Zheng, Jacqueline A. Valeri, Ian W. Andrews, Aarti Krishnan, Parijat Bandyopadhyay, Melis N. Anahtar, Alice Herneisen, Fabian Schulte, Brooke Linnehan, Felix Wong, Jonathan M. Stokes, Lars D. Renner, Sebastian Lourido, James J. Collins
There is a need to discover and develop non-toxic antibiotics that are effective against metabolically dormant bacteria, which underlie chronic infections and promote antibiotic resistance. Traditional antibiotic discovery has historically favored compounds effective against actively metabolizing cells, a property that is not predictive of efficacy in metabolically inactive contexts. Here, we combine
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PIM1 targeted degradation prevents the emergence of chemoresistance in prostate cancer Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-27 Pedro Torres-Ayuso, Meghri Katerji, Dawid Mehlich, Sophia A. Lookingbill, Venkata R. Sabbasani, Hope Liou, Andrea L. Casillas, Shailender S. Chauhan, Remigiusz Serwa, Maxine R. Rubin, Anna A. Marusiak, Rolf E. Swenson, Noel A. Warfel, John Brognard
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Antiplasmodial peptaibols act through membrane directed mechanisms Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-22 Jennifer E. Collins, Jin Woo Lee, Frances Rocamora, Gagandeep S. Saggu, Karen L. Wendt, Charisse Flerida A. Pasaje, Sebastian Smick, Natalia Mojica Santos, Raphaella Paes, Tiantian Jiang, Nimisha Mittal, Madeline R. Luth, Taylor Chin, Howard Chang, James L. McLellan, Beatriz Morales-Hernandez, Kirsten K. Hanson, Jacquin C. Niles, Sanjay A. Desai, Elizabeth A. Winzeler, Robert H. Cichewicz, Debopam
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Serotonin is a common thread linking different classes of antidepressants Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-21 Colby E. Witt, Sergio Mena, Jordan Holmes, Melinda Hersey, Anna Marie Buchanan, Brenna Parke, Rachel Saylor, Lauren E. Honan, Shane N. Berger, Sara Lumbreras, Frederik H. Nijhout, Michael C. Reed, Janet Best, James Fadel, Patrick Schloss, Thorsten Lau, Parastoo Hashemi
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2′-OH as a universal handle for studying intracellular RNAs Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-21 Lu Xiao, Linglan Fang, Eric T. Kool
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Genetic retargeting of E3 ligases to enhance CAR T cell therapy Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-20 Isabel C. Lane, Gabriele Kembuan, Jeannie Carreiro, Michael C. Kann, William Lin, Amanda A. Bouffard, Johannes Kreuzer, Robert Morris, Emily M. Schneider, Joanna Y. Kim, Charles Zou, Diego Salas-Benito, Jessica A. Gasser, Mark B. Leick, Mikołaj Słabicki, Wilhelm Haas, Marcela V. Maus, Max Jan
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Enabling inclusion and looking ahead Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-16 Mishtu Dey
Abstract not available
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New advisory board members speak on challenges and opportunities in chemical biology Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-16 Xiang David Li, Chengqi Yi, Hang Hubert Yin, Hong Zhang
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CryoEM structures of adhesion in GPCR CD97: Filling in some of the gaps Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-16 Brian E. Krumm, Bryan L. Roth
CD97 (ADGRE5) is an adhesion GPCR (aGPCR) that plays crucial roles in the immune system and cancer. In this issue of Cell Chemical Biology, Wang et al.1 present the cryoEM structures of CD97 in complex with G13, Gq, and Gs G protein subtypes, revealing in-depth insight into aGPCR activation and G protein selectivity.
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Raf protomers: Drug binding preferences in living cells Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-16 Kevin N. Dalby
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Fine-tuning chemical genetics to identify physiologic drug targets Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-16 Lauren E. Vostal, Tarun M. Kapoor
Genetics-based approaches can enable drug target identification in human cells. In this issue of Cell Chemical Biology, Nguyen et al.1 use inducible degradation of a mismatch repair protein to tune the mutation rate in HCT116 cells, thereby increasing sensitivity and selectivity in identifying resistance-conferring mutations for several cytotoxic small molecules.
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Addicted to proteostasis: How KRAS-driven cancers acquire resistance to clinical KRAS inhibitors Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-16 Austin T. Klein, Marc L. Mendillo
The development of KRAS inhibitors was a remarkable feat, yet their efficacy is limited by inevitable resistance. In the September issue of Science, Lv et al.1 demonstrate how KRAS-driven cancers rewire signaling to restore protein homeostasis and acquire resistance to KRAS inhibitors with implications for novel combination therapeutic strategies.
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Come for the atmosphere, stay for the interactions: Deciphering small molecule partitioning into biomolecular condensates Cell Chem. Bio. (IF 8.6) Pub Date : 2023-11-16 Bakhtyar Sepehri, Kevin Drew, José A. Villegas