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Blocking smoothened cholesterylation: A strategy for overcoming drug resistance in cancer Cell Chem. Bio. (IF 6.6) Pub Date : 2024-07-18
In this issue of Cell Chemical Biology, Liu et al.1 report the identification of Q29, a synthetic diterpenoid that blocks covalent cholesterol modification of smoothened (SMO) and inhibits hedgehog signaling. Q29 is capable of suppressing tumor cell growth, both in vitro and in vivo, and overcoming resistance to SMO inhibitors.
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STX-bpc: “Brightening” the path to neuronal inhibition Cell Chem. Bio. (IF 6.6) Pub Date : 2024-07-18
In this issue of Cell Chemical Biology, Elleman et al.1 introduce a transformative chemical approach to control neuronal activity with high spatial and temporal resolution. The authors present STX-bpc, a potent neurotoxin that naturally inhibits voltage-gated sodium channels (NaVs), complementing available optogenetic methods for manipulating neuronal activity, cellular communication, and behavior
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A new light on PLCβ! Cell Chem. Bio. (IF 6.6) Pub Date : 2024-07-18
In this issue of Cell Chemical Biology, Kim et al.1 present a novel optogenetic tool, opto-PLCβ, to control PLCβ signaling optically. In addition to eliciting PIP2 hydrolysis and downstream signaling in cells, opto-PLCβ also enabled probing the impact of PLCβ signaling on amygdala synaptic plasticity and fear learning in mice.
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CBLs downregulation foretells T cell ubiquitination leading to autoimmunity Cell Chem. Bio. (IF 6.6) Pub Date : 2024-07-18
In a study published in the July issue of Immunity, Li et al.1 demonstrate that expression of the E3 ubiquitin ligases CBL and CBL-B is downregulated in Tfh cells in SLE with Tfh cell expansion and autoimmunity. This leads to reduced ubiquitination of the T cell costimulator ICOS which regulates proteostasis of the Tfh cell transcription factor BCL6 via chaperone-mediated autophagy.
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Rescuing T cells from stiff tumors Cell Chem. Bio. (IF 6.6) Pub Date : 2024-07-18
In a recent issue of Cell, Zhang et al.1 demonstrate that mechanical features of a solid tumor can drive T cells into dysfunctionality and identify pathways that revert this “exhausted” state.
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Therapeutic potential of inhibiting the PI3Kγ complex for leukemia Cell Chem. Bio. (IF 6.6) Pub Date : 2024-07-18
In their recent paper published in Nature, Luo et al.1 investigate the cancer-cell-intrinsic roles of the PI3Kγ complex in leukemia. Their findings pinpoint PI3Kγ inhibition as a possible novel treatment avenue for a subset of acute leukemias.
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Development of covalent chemogenetic K2P channel activators Cell Chem. Bio. (IF 6.6) Pub Date : 2024-07-18
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Discovery of a mu-opioid receptor modulator that in combination with morphinan antagonists induces analgesia Cell Chem. Bio. (IF 6.6) Pub Date : 2024-07-17
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The hydrophobicity of the CARD8 N-terminus tunes inflammasome activation Cell Chem. Bio. (IF 6.6) Pub Date : 2024-07-10
Mounting evidence indicates that proteotoxic stress is a primary activator of the CARD8 inflammasome, but the complete array of signals that control t…
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The physiological and pathological roles of RNA modifications in T cells Cell Chem. Bio. (IF 6.6) Pub Date : 2024-07-09 Yu Deng, Jing Zhou, Hua-Bing Li
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The anti-tubercular callyaerins target the Mycobacterium tuberculosis-specific non-essential membrane protein Rv2113 Cell Chem. Bio. (IF 6.6) Pub Date : 2024-07-08 David Podlesainski, Emmanuel T. Adeniyi, Yvonne Gröner, Florian Schulz, Violetta Krisilia, Nidja Rehberg, Tim Richter, Daria Sehr, Huzhuyue Xie, Viktor E. Simons, Anna-Lene Kiffe-Delf, Farnusch Kaschani, Thomas R. Ioerger, Markus Kaiser, Rainer Kalscheuer
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The art of designed coiled-coils for the regulation of mammalian cells Cell Chem. Bio. (IF 6.6) Pub Date : 2024-07-05 Tjaša Plaper, Erik Rihtar, Taja Železnik Ramuta, Vida Forstnerič, Vid Jazbec, Filip Ivanovski, Mojca Benčina, Roman Jerala
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Synthetic gene circuit evolution: Insights and opportunities at the mid-scale Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-25 Christopher Helenek, Rafał Krzysztoń, Julia Petreczky, Yiming Wan, Mariana Cabral, Damiano Coraci, Gábor Balázsi
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C646 degrades Exportin-1 to modulate p300 chromatin occupancy and function Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-24 Yi Fan Chen, Atikur Rahman, Joel L. Sax, Matthew J. Atala Pleshinger, Ryan M. Friedrich, Drew J. Adams
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Induced proximity in biology and therapeutics Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-20 The Cell Chemical Biology editorial team
No Abstract
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Meet the authors: Markella Konstantinidou and Michelle R. Arkin Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-20 Markella Konstantinidou, Michelle R. Arkin
In an interview with Dr. Ying Li, a scientific editor of Cell Chemical Biology, the authors of the Review titled “Molecular glues for protein-protein interactions: Progressing toward a new dream” share their perspectives on their field and life as scientists.
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Meet the authors: Lauren Kageler, Jonathan Perr, and Ryan A. Flynn Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-20 Lauren Kageler, Jonathan Perr, Ryan A. Flynn
In an interview with Dr. Mishtu Dey, editor-in-chief of Cell Chemical Biology, the authors of the review titled “Tools to investigate the cell surface: Proximity as a central concept in glycoRNA biology”—Lauren Kageler, Jonathan Perr, and Dr. Ryan A. Flynn—tell us more about their career paths and what excites them about science.
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The culinary chemist: Out of the lab and into the tent Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-20 Joshua P. Smalley
In this Stories piece, Josh Smalley, a postdoctoral research associate at the University of Leicester and finalist of The Great British Bake Off, discusses the parallels between chemistry and baking, revealing how he successfully combines the two.
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Application of induced proximity for therapeutic discovery Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-20 Angela Cacace, Danette Daniels, Fleur M. Ferguson, Cristina Mayor-Ruiz, Christina Woo
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Velcrin compounds activate the SLFN12 tRNase to induce tomoptosis Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-20 Heidi Greulich
Velcrins are molecular glues that induce complex formation between PDE3A and SLFN12. The PDE3A-SLFN12 complex activates the SLFN12 RNase, resulting in cleavage of the specific substrate, tRNA-Leu-TAA, global inhibition of translation, and death of cells expressing sufficient levels of both proteins. Here, unanswered questions about the mechanism of action and therapeutic promise of velcrin compounds
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Get your receptors in a knot with new Wnt signaling agonists Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-20 Lucie Wolf, Stephane Angers
Pharmacological modulation of the Wnt/β-catenin signaling pathway holds promises for both basic research and therapeutic applications. In this issue of Cell Chemical Biology, Kschonsak et al.1 engineered knotted peptides that promote Wnt signaling by targeting ZNRF3 and serve as pharmacological tools for studying Wnt biology and supporting organoid growth.
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A double whammy for KEAP1 Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-20 Jan Gerhartz, Radosław P. Nowak
In this issue of Cell Chemical Biology, Lu et al.1 report the discovery of a bivalent KEAP1 inhibitor (biKEAP1), which more rapidly activates NRF2 compared to previously reported monovalent KEAP1 inhibitors. biKEAP1suppresses acute inflammation in animal models.
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NAMPT-targeting PROTAC and nicotinic acid co-administration elicit safe and robust anti-tumor efficacy in NAPRT-deficient pan-cancers Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-20 Xiaotong Zhu, Ye Li, Haixia Liu, Yuetong Wang, Renhong Sun, Zhenzhou Jiang, Chun Hou, Xianyu Hou, Suming Huang, Huijuan Zhang, Haopeng Wang, Biao Jiang, Xiaobao Yang, Bin Xu, Gaofeng Fan
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Chemoproteomic profiling of substrate specificity in gut microbiota-associated bile salt hydrolases Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-17 Lin Han, Augustus Pendleton, Adarsh Singh, Raymond Xu, Samantha A. Scott, Jaymee A. Palma, Peter Diebold, Kien P. Malarney, Ilana L. Brito, Pamela V. Chang
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RNATACs: Multispecific small molecules targeting RNA by induced proximity Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-13 Yan Song, Jia Cui, Jiaqiang Zhu, Boseon Kim, Mei-Ling Kuo, Patrick Ryan Potts
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Induced proximity labeling and editing for epigenetic research Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-11 Chenwei Zhou, Sarah Wagner, Fu-Sen Liang
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Molecular glues and bifunctional compounds: Therapeutic modalities based on induced proximity Cell Chem. Bio. (IF 6.6) Pub Date : 2024-06-10 Stuart L. Schreiber
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Mitochondrial RelA empowers mtDNA G-quadruplex formation for hypoxia adaptation in cancer cells Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-30 Gui-Xue Tang, Mao-Lin Li, Cui Zhou, Zhi-Shu Huang, Shuo-Bin Chen, Xiu-Cai Chen, Jia-Heng Tan
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Specificity profiling of deubiquitylases against endogenously generated ubiquitin-protein conjugates Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-28 Valentina Rossio, Joao A. Paulo, Xinyue Liu, Steven P. Gygi, Randall W. King
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AspSnFR: A genetically encoded biosensor for real-time monitoring of aspartate in live cells Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-27 Lars Hellweg, Martin Pfeifer, Miroslaw Tarnawski, Shao Thing-Teoh, Lena Chang, Andrea Bergner, Jana Kress, Julien Hiblot, Tabea Wiedmer, Giulio Superti-Furga, Jürgen Reinhardt, Kai Johnsson, Philipp Leippe
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Chemical interplay between gut microbiota and epigenetics: Implications in circadian biology Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-21 Samskrathi Aravinda Sharma, Sarah Olanrewaju Oladejo, Zheng Kuang
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Tools to investigate the cell surface: Proximity as a central concept in glycoRNA biology Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-20 Lauren Kageler, Jonathan Perr, Ryan A. Flynn
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Meet the authors: Jordan B. Jastrab and Jonathan C. Kagan Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-16
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Meet the Authors: Harkamal S. Jhajj and Peter M. Tessier Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-16 Harkamal S. Jhajj, Peter M. Tessier
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Finding my leadership style Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-16 Helen Walden
In this Stories piece, Dr. Helen Walden—Professor and Head of the School of Molecular Biosciences at the University of Glasgow—shares how her past experiences and academic journey have shaped her leadership style.
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Voices: Challenges and opportunities in regulating the immune system Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-16 Yuezhou Chen, Fiachra Humphries, Ming O. Li, Thirumala-Devi Kanneganti, Dan Ye
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Sharks give a handle to potent anti-tumor multiparatopic antibodies inducing membrane depletion of PD-L1 Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-16 Gordana Wozniak-Knopp, Veronica Natale
Despite the immense clinical success of the antibody therapeutics that neutralize programmed death receptor ligand 1 (PD-L1) and thus resurrect T cell antitumor activity, the patient response rates remain low. In this issue of Cell Chemical Biology, Ludwig et al.1 reveal novel topologies of multiparatopic antibodies that mediate potent PD-L1 downregulation.
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Metabolism-inflammasome crosstalk shapes innate and adaptive immunity Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-16 Jun Wu, Xuan Sun, Peng Jiang
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Transient hydroxycholesterol treatment restrains TCR signaling to promote long-term immunity Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-16 Zhengxu Ren, Kun Wang, Yong Zhang, Hui Chen, Yiming Zhu, Hua Li, Jizhong Lou, Haopeng Wang, Chenqi Xu
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One-carbon unit supplementation fuels purine synthesis in tumor-infiltrating T cells and augments checkpoint blockade Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-16 Xincheng Xu, Zihong Chen, Caroline R. Bartman, Xi Xing, Kellen Olszewski, Joshua D. Rabinowitz
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Behavioral control through the direct, focal silencing of neuronal activity Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-09 Anna V. Elleman, Nikola Milicic, Damian J. Williams, Jane Simko, Christine J. Liu, Allison L. Haynes, David E. Ehrlich, Christopher D. Makinson, J. Du Bois
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Stimulating STING for cancer therapy: Taking the extracellular route Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-08 Lingyin Li
Ten years ago, the second messenger cGAMP was discovered as the activator of the anti-cancer STING pathway. The characterization of cGAMP’s paracrine action and dominant extracellular hydrolase ENPP1 cemented cGAMP as an intercellular immunotransmitter that coordinates the innate and adaptive immune systems to fight cancer. In this Perspective, I look back at a decade of discovery of extracellular
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Molecular glues for protein-protein interactions: Progressing toward a new dream Cell Chem. Bio. (IF 6.6) Pub Date : 2024-05-02 Markella Konstantinidou, Michelle R. Arkin
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Molecular glues and induced proximity: An evolution of tools and discovery Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-29 Stephanie Anne Robinson, Jennifer Anne Co, Steven Mark Banik
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Multiparatopic antibodies induce targeted downregulation of programmed death-ligand 1 Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-27 Seth D. Ludwig, Bunyarit Meksiriporn, Jiacheng Tan, Rakeeb Kureshi, Akhilesh Mishra, Kyle J. Kaeo, Angela Zhu, Georgia Stavrakis, Stephen J. Lee, David J. Schodt, Michael J. Wester, Dhiraj Kumar, Keith A. Lidke, Andrea L. Cox, Helen M. Dooley, Sridhar Nimmagadda, Jamie B. Spangler
No Abstract
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Current advances in photocatalytic proximity labeling Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-24 Steve D. Knutson, Benito F. Buksh, Sean W. Huth, Danielle C. Morgan, David W.C. MacMillan
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Repurposing AS1411 for constructing ANM-PROTACs Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-23 Xuekun Fu, Jin Li, Xinxin Chen, Hongzhen Chen, Zhuqian Wang, Fang Qiu, Duoli Xie, Jie Huang, Siran Yue, Chunhao Cao, Yiying Liang, Aiping Lu, Chao Liang
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Facile generation of biepitopic antibodies with intrinsic agonism for activating tumor necrosis factor receptors Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-22 Harkamal S. Jhajj, John S. Schardt, Namir Khalasawi, Emily L. Yao, Timon S. Lwo, Na-Young Kwon, Ryen L. O’Meara, Alec A. Desai, Peter M. Tessier
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Meet the authors: Lori Emert-Sedlak and Tom Smithgall Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-18 Lori Emert-Sedlak, Tom Smithgall
In an interview with Samantha Nelson, a scientific editor of Cell Chemical Biology, the first and corresponding authors of the research article entitled “PROTAC-mediated degradation of HIV-1 Nef efficiently restores cell-surface CD4 and MHC-I expression and blocks HIV-1 replication” share insights on their paper and life as scientists.
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Meet the Authors: Christopher R. Mansfield and Emily R. Derbyshire Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-18 Christopher R. Mansfield, Emily R. Derbyshire
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Dual-action compounds unleash a one-two punch against tuberculosis Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-18 Wendy Le Mouëllic, Yannick Poquet, Olivier Neyrolles
In this issue of Cell Chemical Biology, Gries et al.1 employ an innovative screening approach to identify anti-tuberculosis compounds with dual modes of action: anti-virulence against the type VII secretion system ESX-1 and enhanced ethionamide efficacy. These compounds hold promise for developing multi-target tuberculosis drugs with potential clinical applications.
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METTL3: Melting the tumor microenvironment for improved immunotherapy Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-18 Longfei Gao, Lei Ding
The tumor microenvironment (TME) dictates the outcome of cancer immunotherapy. In this issue of Cell Chemical Biology, Yu et al.1 report that targeting Mettl3 leads to a more inflamed, “hot” TME and effective anti-PD-1 therapy. This study points to a new target in remodeling the TME for improved immunotherapy.
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SARS-CoV-2 resistance to monoclonal antibodies and small-molecule drugs Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-18 Sho Iketani, David D. Ho
Over four years have passed since the beginning of the COVID-19 pandemic. The scientific response has been rapid and effective, with many therapeutic monoclonal antibodies and small molecules developed for clinical use. However, given the ability for viruses to become resistant to antivirals, it is perhaps no surprise that the field has identified resistance to nearly all of these compounds. Here,
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Strategies of bacterial detection by inflammasomes Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-17 Jordan B. Jastrab, Jonathan C. Kagan
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Heterogeneity of tethered agonist signaling in adhesion G protein-coupled receptors Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-11 Andrew N. Dates, Daniel T.D. Jones, Jeffrey S. Smith, Meredith A. Skiba, Maria F. Rich, Maggie M. Burruss, Andrew C. Kruse, Stephen C. Blacklow
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Identification of an inhibitory pocket in falcilysin provides a new avenue for malaria drug development Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-08 Grennady Wirjanata, Jianqing Lin, Jerzy Michal Dziekan, Abbas El Sahili, Zara Chung, Seth Tjia, Nur Elyza Binte Zulkifli, Josephine Boentoro, Roy Tham, Lai Si Jia, Ka Diam Go, Han Yu, Anthony Partridge, David Olsen, Nayana Prabhu, Radoslaw M. Sobota, Pär Nordlund, Julien Lescar, Zbynek Bozdech
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A light-controlled phospholipase C for imaging of lipid dynamics and controlling neural plasticity Cell Chem. Bio. (IF 6.6) Pub Date : 2024-04-05 Yeon-Jeong Kim, Suguru Tohyama, Takashi Nagashima, Masashi Nagase, Yamato Hida, Shun Hamada, Ayako M. Watabe, Toshihisa Ohtsuka
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Multiparatopic antibodies induce targeted downregulation of programmed death-ligand 1 Cell Chem. Bio. (IF 6.6) Pub Date : 2024-03-27 Seth D. Ludwig, Bunyarit Meksiriporn, Jiacheng Tan, Rakeeb Kureshi, Akhilesh Mishra, Kyle J. Kaeo, Angela Zhu, Georgia Stavrakis, Stephen J. Lee, David. J. Schodt, Michael J. Wester, Dhiraj Kumar, Keith A. Lidke, Andrea L. Cox, Helen M. Dooley, Sridhar Nimmagadda, Jamie B. Spangler
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Discovery of YAP1/TAZ pathway inhibitors through phenotypic screening with potent anti-tumor activity via blockade of Rho-GTPase signaling Cell Chem. Bio. (IF 6.6) Pub Date : 2024-03-26 Keith Graham, Philip Lienau, Benjamin Bader, Stefan Prechtl, Jan Naujoks, Ralf Lesche, Joerg Weiske, Julia Kuehnlenz, Krzysztof Brzezinka, Lisette Potze, Francesca Zanconato, Barbara Nicke, Anna Montebaur, Wilhelm Bone, Sven Golfier, Stefan Kaulfuss, Charlotte Kopitz, Sabine Pilari, Holger Steuber, Sikander Hayat, Atanas Kamburov, Andreas Steffen, Andreas Schlicker, Philipp Buchgraber, Nico Braeuer
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Chemical proteomics to study metabolism, a reductionist approach applied at the systems level Cell Chem. Bio. (IF 6.6) Pub Date : 2024-03-21 Md Yousuf Ali, Liron Bar-Peled
Cellular metabolism encompasses a complex array of interconnected biochemical pathways that are required for cellular homeostasis. When dysregulated, metabolism underlies multiple human pathologies. At the heart of metabolic networks are enzymes that have been historically studied through a reductionist lens, and more recently, using high throughput approaches including genomics and proteomics. Merging