Cell Chemical Biology

Article	Citations
Targeted protein degradation: A promise for undruggable proteins	137
Targeted degradation of transcription factors by TRAFTACs: TRAnscription Factor TArgeting Chimeras	112
MGST1 is a redox-sensitive repressor of ferroptosis in pancreatic cancer cells	111
Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product function	107
Targeted degradation of the enhancer lysine acetyltransferases CBP and p300	105
Recent advances in identifying protein targets in drug discovery	89
Haven't got a glue: Protein surface variation for the design of molecular glue degraders	88
Discovery of a Functional Covalent Ligand Targeting an Intrinsically Disordered Cysteine within MYC	80
Expanding the arsenal of E3 ubiquitin ligases for proximity-induced protein degradation	75
Development of a potent and selective chemical probe for the pleiotropic kinase CK2	75
Structure-Aided Development of Small-Molecule Inhibitors of ENPP1, the Extracellular Phosphodiesterase of the Immunotransmitter cGAMP	71
Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2	69
FADS2-dependent fatty acid desaturation dictates cellular sensitivity to ferroptosis and permissiveness for hepatitis C virus replication	67
The role of reversible and irreversible covalent chemistry in targeted protein degradation	66
An E3 ligase guide to the galaxy of small-molecule-induced protein degradation	66
Eradicating Bacterial Persisters with Combinations of Strongly and Weakly Metabolism-Dependent Antibiotics	65
Using the Oxytosis/Ferroptosis Pathway to Understand and Treat Age-Associated Neurodegenerative Diseases	65
How to untie G-quadruplex knots and why?	56
An automatic pipeline for the design of irreversible derivatives identifies a potent SARS-CoV-2 Mpro inhibitor	54
Chemogenomics identifies acetyl-coenzyme A synthetase as a target for malaria treatment and prevention	53
Context-dependent regulation of ferroptosis sensitivity	52
Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors	51
Chemo-proteomics exploration of HDAC degradability by small molecule degraders	50
A potent and selective PARP14 inhibitor decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants	48
Chemoproteomics-enabled discovery of a covalent molecular glue degrader targeting NF-κB	48

Morphological profiling of small molecules	48
A Robust, GFP-Orthogonal Photoswitchable Inhibitor Scaffold Extends Optical Control over the Microtubule Cytoskeleton	48
HSP90 Inhibition Enhances Cancer Immunotherapy by Modulating the Surface Expression of Multiple Immune Checkpoint Proteins	48
Discovery and characterization of a selective IKZF2 glue degrader for cancer immunotherapy	47
A biaryl-linked tripeptide from Planomonospora reveals a widespread class of minimal RiPP gene clusters	47
The proteasome and its role in the nervous system	45
Dual targeting of DDX3 and eIF4A by the translation inhibitor rocaglamide A	45
Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2	44
A fine-tuned azobenzene for enhanced photopharmacology in vivo	43
Degradation from the outside in: Targeting extracellular and membrane proteins for degradation through the endolysosomal pathway	42
Nuisance compounds in cellular assays	41
Gene editing and synthetically accessible inhibitors reveal role for TPC2 in HCC cell proliferation and tumor growth	41
DogCatcher allows loop-friendly protein-protein ligation	40
Acriflavine, a clinically approved drug, inhibits SARS-CoV-2 and other betacoronaviruses	39
Assessing IRAK4 Functions in ABC DLBCL by IRAK4 Kinase Inhibition and Protein Degradation	39
Rapamycin targets STAT3 and impacts c-Myc to suppress tumor growth	38
Optical control of targeted protein degradation	37
Small-molecule allosteric inhibitors of GPX4	37
Exploring the target scope of KEAP1 E3 ligase-based PROTACs	37
Identification of structurally diverse FSP1 inhibitors that sensitize cancer cells to ferroptosis	37
CysDB: a human cysteine database based on experimental quantitative chemoproteomics	37
Ubiquitin ligases in cancer: Functions and clinical potentials	37
Capsaicin ameliorates inflammation in a TRPV1-independent mechanism by inhibiting PKM2-LDHA-mediated Warburg effect in sepsis	36
Identification and selectivity profiling of small-molecule degraders via multi-omics approaches	35
Target protein localization and its impact on PROTAC-mediated degradation	35
Quantitative Imaging of Labile Zn2+ in the Golgi Apparatus Using a Localizable Small-Molecule Fluorescent Probe	34
Decoding the messaging of the ubiquitin system using chemical and protein probes	34
A NSD3-targeted PROTAC suppresses NSD3 and cMyc oncogenic nodes in cancer cells	34
An antibody-based proximity labeling map reveals mechanisms of SARS-CoV-2 inhibition of antiviral immunity	33
Ferroptosis inhibition by lysosome-dependent catabolism of extracellular protein	33
Directed evolution of potent neutralizing nanobodies against SARS-CoV-2 using CDR-swapping mutagenesis	33
Hit Triage and Validation in Phenotypic Screening: Considerations and Strategies	33
The chemical tools for imaging dopamine release	31
A Small Molecule that Binds an RNA Repeat Expansion Stimulates Its Decay via the Exosome Complex	31
ND3 Cys39 in complex I is exposed during mitochondrial respiration	31
A small-molecule inhibitor of the BRCA2-RAD51 interaction modulates RAD51 assembly and potentiates DNA damage-induced cell death	31
Piperlongumine conjugates induce targeted protein degradation	30
Functional mimicry revealed by the crystal structure of an eIF4A:RNA complex bound to the interfacial inhibitor, desmethyl pateamine A	30
Morphological profiling by means of the Cell Painting assay enables identification of tubulin-targeting compounds	30
High-content phenotypic and pathway profiling to advance drug discovery in diseases of unmet need	30
Cell-free production of personalized therapeutic phages targeting multidrug-resistant bacteria	30
Endogenous vitamin E metabolites mediate allosteric PPARγ activation with unprecedented co-regulatory interactions	29
Small molecule targeting of biologically relevant RNA tertiary and quaternary structures	29
3D two-photon brain imaging reveals dihydroartemisinin exerts antiepileptic effects by modulating iron homeostasis	29
An IMiD-inducible degron provides reversible regulation for chimeric antigen receptor expression and activity	29
Human iPSC modeling of heart disease for drug development	28
Proteomics-Based Identification of DUB Substrates Using Selective Inhibitors	28
The future of phenotypic drug discovery	28
Increased energy demand from anabolic-catabolic processes drives β-lactam antibiotic lethality	28
Identification of a PCSK9-LDLR disruptor peptide with in vivo function	27

Bifunctional modalities for repurposing protein function	27
Exploiting ubiquitin ligase cereblon as a target for small-molecule compounds in medicine and chemical biology	27
Making the cut with protease engineering	26
Engineering DNA-Templated Nonribosomal Peptide Synthesis	26
Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization	25
Thermal proteome profiling identifies the membrane-bound purinergic receptor P2X4 as a target of the autophagy inhibitor indophagolin	25
The non-canonical target PARP16 contributes to polypharmacology of the PARP inhibitor talazoparib and its synergy with WEE1 inhibitors	25
Chemically modified guide RNAs enhance CRISPR-Cas13 knockdown in human cells	25
Y box binding protein 1 inhibition as a targeted therapy for ovarian cancer	25
Inhibition of glucose transport synergizes with chemical or genetic disruption of mitochondrial metabolism and suppresses TCA cycle-deficient tumors	25
TK216 targets microtubules in Ewing sarcoma cells	25
Chemoproteomic-enabled phenotypic screening	25
A synthetic small molecule stalls pre-mRNA splicing by promoting an early-stage U2AF2-RNA complex	24
Inhibition of Nonfunctional Ras	24
Aberrant human ClpP activation disturbs mitochondrial proteome homeostasis to suppress pancreatic ductal adenocarcinoma	24
Inhibitors of the ATPase p97/VCP: From basic research to clinical applications	24
A photo-cross-linking GlcNAc analog enables covalent capture of N-linked glycoprotein-binding partners on the cell surface	24
A Pseudomonas aeruginosa PQS quorum-sensing system inhibitor with anti-staphylococcal activity sensitizes polymicrobial biofilms to tobramycin	24
Formation of an aminovinyl-cysteine residue in thioviridamides occurs through a path independent of known lanthionine synthetase activity	23
Ligand-induced interactions between butyrophilin 2A1 and 3A1 internal domains in the HMBPP receptor complex	23
CETSA interaction proteomics define specific RNA-modification pathways as key components of fluorouracil-based cancer drug cytotoxicity	23
Combined morphological and proteome profiling reveals target-independent impairment of cholesterol homeostasis	22
Ainsliadimer A induces ROS-mediated apoptosis in colorectal cancer cells via directly targeting peroxiredoxin 1 and 2	22
Identification of cell wall synthesis inhibitors active against Mycobacterium tuberculosis by competitive activity-based protein profiling	22
Metabolic targeting of cancer by a ubiquinone uncompetitive inhibitor of mitochondrial complex I	22
Selective autophagy as the basis of autophagy-based degraders	22
Protein acylation by saturated very long chain fatty acids and endocytosis are involved in necroptosis	22
A direct high-throughput protein quantification strategy facilitates discovery and characterization of a celastrol-derived BRD4 degrader	22
Quantitative chemoproteomics reveals O-GlcNAcylation of cystathionine γ-lyase (CSE) represses trophoblast syncytialization	22
Development and pre-clinical testing of a novel hypoxia-activated KDAC inhibitor	22
The rise of degrader drugs	21
Re-wiring the regulation of the formicamycin biosynthetic gene cluster to enable the development of promising antibacterial compounds	21
A synthetic diterpene analogue inhibits mycobacterial persistence and biofilm formation by targeting (p)ppGpp synthetases	21
Modulation of lanosterol synthase drives 24,25-epoxysterol synthesis and oligodendrocyte formation	21
Ligand-directed bias of G protein signaling at the dopamine D2 receptor	21
Light-controllable RNA-protein devices for translational regulation of synthetic mRNAs in mammalian cells	21
Identification and validation of selective deubiquitinase inhibitors	20
Identification of covalent inhibitors that disrupt M. tuberculosis growth by targeting multiple serine hydrolases involved in lipid metabolism	20
Dipyridamole Inhibits Lipogenic Gene Expression by Retaining SCAP-SREBP in the Endoplasmic Reticulum	20
PALP: A rapid imaging technique for stratifying ferroptosis sensitivity in normal and tumor tissues in situ	20
Photoswitchable CAR-T Cell Function In Vitro and In Vivo via a Cleavable Mediator	20
Fatty acid chain length drives lysophosphatidylserine-dependent immunological outputs	20
Mechanism-Based Personalized Medicine for Cystic Fibrosis by Suppressing Pseudo Exon Inclusion	19
Periplasmic expression of SpyTagged antibody fragments enables rapid modular antibody assembly	19
Systemic delivery of a targeted synthetic immunostimulant transforms the immune landscape for effective tumor regression	19
Temporal resolution of gene derepression and proteome changes upon PROTAC-mediated degradation of BCL11A protein in erythroid cells	19
Proteostasis Regulators Restore Function of Epilepsy-Associated GABAA Receptors	19
Re-defining synthetic lethality by phenotypic profiling for precision oncology	19
Hypomorph mutation-directed small-molecule protein-protein interaction inducers to restore mutant SMAD4-suppressed TGF-β signaling	19
The impact of iron and heme availability on the healthy human gut microbiome in vivo and in vitro	19
Glycopeptidolipid glycosylation controls surface properties and pathogenicity in Mycobacterium abscessus	18
Potent macrocycle inhibitors of the human SAGA deubiquitinating module	18
A PROTAC targets splicing factor 3B1	18
A structure-specific small molecule inhibits a miRNA-200 family member precursor and reverses a type 2 diabetes phenotype	18
Inhibition of Staphylococcus aureus biofilm-forming functional amyloid by molecular tweezers	18
Avoid the trap: Targeting PARP1 beyond human malignancy	18
Artemisinin inhibits NRas palmitoylation by targeting the protein acyltransferase ZDHHC6	18
Cytidine acetylation yields a hypoinflammatory synthetic messenger RNA	18
Photocontrol of Endogenous Glycine Receptors In Vivo	18
A highly selective, cell-permeable furin inhibitor BOS-318 rescues key features of cystic fibrosis airway disease	18
Metabolic and chemical architecture of the mammalian circadian clock	18
Sensitization of cancer cells to ferroptosis coincident with cell cycle arrest	18
Discovery of compounds that reactivate p53 mutants in vitro and in vivo	17
Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190	17
On-tissue spatially resolved glycoproteomics guided by N-glycan imaging reveal global dysregulation of canine glioma glycoproteomic landscape	17
Phenotypic screening with target identification and validation in the discovery and development of E3 ligase modulators	17
A high-performance genetically encoded fluorescent biosensor for imaging physiological peroxynitrite	17
Development of red genetically encoded biosensor for visualization of intracellular glucose dynamics	17
Evolution of kinase polypharmacology across HSP90 drug discovery	17
Sulfotyrosine-Mediated Recognition of Human Thrombin by a Tsetse Fly Anticoagulant Mimics Physiological Substrates	17
In vivo bioluminescence imaging of granzyme B activity in tumor response to cancer immunotherapy	17
A synthetic RNA-based biosensor for fructose-1,6-bisphosphate that reports glycolytic flux	17
Redox proteomics combined with proximity labeling enables monitoring of localized cysteine oxidation in cells	16
Temporal proteomics reveal specific cell cycle oncoprotein downregulation by p97/VCP inhibition	16
Proximity-labeling chemoproteomics defines the subcellular cysteinome and inflammation-responsive mitochondrial redoxome	16
Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE	16
Multiple PDE3A modulators act as molecular glues promoting PDE3A-SLFN12 interaction and induce SLFN12 dephosphorylation and cell death	16
Systematic Activity Maturation of a Single-Domain Antibody with Non-canonical Amino Acids through Chemical Mutagenesis	16
Addressing the Enzyme-independent tumor-promoting function of NAMPT via PROTAC-mediated degradation	16
Autotaxin facilitates selective LPA receptor signaling	16

Site-specific dual encoding and labeling of proteins via genetic code expansion	16
Targeting SUMOylation dependency in human cancer stem cells through a unique SAE2 motif revealed by chemical genomics	16
Discovery of an Inhibitor for Bacterial 3-Mercaptopyruvate Sulfurtransferase that Synergistically Controls Bacterial Survival	16
Pharmacological Targeting of Vacuolar H+-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer	16
Chemical insights into flexizyme-mediated tRNA acylation	15
Multiple unbiased approaches identify oxidosqualene cyclase as the molecular target of a promising anti-leishmanial	15
Discovery of a σ1 receptor antagonist by combination of unbiased cell painting and thermal proteome profiling	15
A SUMO1-Derived Peptide Targeting SUMO-Interacting Motif Inhibits α-Synuclein Aggregation	15
Controlled Inhibition of Apoptosis by Photoactivatable Caspase Inhibitors	15
Discovery of cellular substrates of human RNA-decapping enzyme DCP2 using a stapled bicyclic peptide inhibitor	15
Discovery of Protein-Protein Interaction Inhibitors by Integrating Protein Engineering and Chemical Screening Platforms	15
Chemoproteomics profiling of surfactin-producing nonribosomal peptide synthetases in living bacterial cells	15
Naturally occurring three-way junctions can be repurposed as genetically encoded RNA-based sensors	15
Small molecule targeting of transcription-replication conflict for selective chemotherapy	14
Morphological subprofile analysis for bioactivity annotation of small molecules	14
CYP27A1-dependent anti-melanoma activity of limonoid natural products targets mitochondrial metabolism	14
CRAGE-CRISPR facilitates rapid activation of secondary metabolite biosynthetic gene clusters in bacteria	14
ROTACs leverage signaling-incompetent R-spondin for targeted protein degradation	14
Screening in serum-derived medium reveals differential response to compounds targeting metabolism	14
Characterization of Small-Molecule-Induced Changes in Parkinson's-Related Trafficking via the Nedd4 Ubiquitin Signaling Cascade	14
Investigating the NRAS 5′ UTR as a target for small molecules	14
Light-inducible deformation of mitochondria in live cells	14
Regulation of Calcium Oscillations in β-Cells by Co-activated Cannabinoid Receptors	14
Allosteric HSP70 inhibitors perturb mitochondrial proteostasis and overcome proteasome inhibitor resistance in multiple myeloma	14
Targeted kinase degradation via the KLHDC2 ubiquitin E3 ligase	14
Structural and mechanistic investigations of protein S-glycosyltransferases	14
Structurally distinct PARP7 inhibitors provide new insights into the function of PARP7 in regulating nucleic acid-sensing and IFN-β signaling	13
Phenotypic screen identifies calcineurin-sparing FK506 analogs as BMP potentiators for treatment of acute kidney injury	13
Shipworm symbiosis ecology-guided discovery of an antibiotic that kills colistin-resistant Acinetobacter	13
Phosphorylation barcodes direct biased chemokine signaling at CXCR3	13
Ferroptosis inhibition by oleic acid mitigates iron-overload-induced injury	13
The Plasmodium falciparum ABC transporter ABCI3 confers parasite strain-dependent pleiotropic antimalarial drug resistance	13
SIM imaging resolves endocytosis of SARS-CoV-2 spike RBD in living cells	13
A photocaged orexin-B for spatiotemporally precise control of orexin signaling	13
NUDT15-mediated hydrolysis limits the efficacy of anti-HCMV drug ganciclovir	13
Discovery of a covalent inhibitor of heat shock protein 90 with antitumor activity that blocks the co-chaperone binding via C-terminal modification	13
Identification of Small-Molecule Activators of the Ubiquitin Ligase E6AP/UBE3A and Angelman Syndrome-Derived E6AP/UBE3A Variants	13
The role of SERPIN citrullination in thrombosis	13
A Method for Conditional Regulation of Protein Stability in Native or Near-Native Form	13
An allosteric inhibitor of bacterial Hsp70 chaperone potentiates antibiotics and mitigates resistance	13
Exploiting polypharmacology to dissect host kinases and kinase inhibitors that modulate endothelial barrier integrity	13
Rapid in vitro prototyping of O-methyltransferases for pathway applications in Escherichia coli	13
Combined Omics Approaches Reveal the Roles of Non-canonical WNT7B Signaling and YY1 in the Proliferation of Human Pancreatic Progenitor Cells	13
Proteomics of broad deubiquitylase inhibition unmasks redundant enzyme function to reveal substrates and assess enzyme specificity	13
Designed Parasite-Selective Rhomboid Inhibitors Block Invasion and Clear Blood-Stage Malaria	13
Phosphorylation-regulated HMGA1a-P53 interaction unveils the function of HMGA1a acidic tail phosphorylations via synthetic proteins	12
Taming transcription factors with TRAFTACs	12
Synergistic PIM kinase and proteasome inhibition as a therapeutic strategy for MYC-overexpressing triple-negative breast cancer	12
K27-Linked Diubiquitin Inhibits UCHL3 via an Unusual Kinetic Trap	12
Targeted degradation of PCNA outperforms stoichiometric inhibition to result in programed cell death	12
Targeting ribosomal G-quadruplexes with naphthalene-diimides as RNA polymerase I inhibitors for colorectal cancer treatment	12
Bioreporters for direct mode of action-informed screening of antibiotic producer strains	12
Targeted epigenetic induction of mitochondrial biogenesis enhances antitumor immunity in mouse model	12
Scribble sub-cellular localization modulates recruitment of YES1 to regulate YAP1 phosphorylation	12
Ferroptosis execution: Is it all about ACSL4?	12
Development of potent dimeric inhibitors of GAS41 YEATS domain	12
Spike-protein proteolytic antibodies in COVID-19 convalescent plasma contribute to SARS-CoV-2 neutralization	12
Targeting METTL3 reprograms the tumor microenvironment to improve cancer immunotherapy	12
Acylation probing of “generic” RNA libraries reveals critical influence of loop constraints on reactivity	12
Splicing modulators elicit global translational repression by condensate-prone proteins translated from introns	12
Dioctatin Activates ClpP to Degrade Mitochondrial Components and Inhibits Aflatoxin Production	12
Intracellular H2S production is an autophagy-dependent adaptive response to DNA damage	12
Resolving the deceptive isoform and complex selectivity of HDAC1/2 inhibitors	12
Context-dependent regulation of ferroptosis sensitivity	12
Repurposing of glycine transport inhibitors for the treatment of erythropoietic protoporphyria	12
Native mass spectrometry and gas-phase fragmentation provide rapid and in-depth topological characterization of a PROTAC ternary complex	12
A selective PPM1A inhibitor activates autophagy to restrict the survival of Mycobacterium tuberculosis	11
Reprogramming CBX8-PRC1 function with a positive allosteric modulator	11
Clionamines stimulate autophagy, inhibit Mycobacterium tuberculosis survival in macrophages, and target Pik1	11
Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input	11
N6-methyladenosine modification in 18S rRNA promotes tumorigenesis and chemoresistance via HSF4b/HSP90B1/mutant p53 axis	11
Mechanistic Studies of the Multiple Myeloma and Melanoma Cell-Selective Toxicity of the Rpn13-Binding Peptoid KDT-11	11
A genome-wide CRISPR-Cas9 screen identifies CENPJ as a host regulator of altered microtubule organization during Plasmodium liver infection	11
Molecular basis of C-S bond cleavage in the glycyl radical enzyme isethionate sulfite-lyase	11
Proteome-wide structural analysis identifies warhead- and coverage-specific biases in cysteine-focused chemoproteomics	11
Efficient inhibition of O-glycan biosynthesis using the hexosamine analog Ac5GalNTGc	11
Discovery of Covalent MKK4/7 Dual Inhibitor	11
Identification of proteomic landscape of drug-binding proteins in live cells by proximity-dependent target ID	11
Neuropeptidomic Analysis of a Genetically Defined Cell Type in Mouse Brain and Pituitary	11
SARS-COV-2 spike binding to ACE2 in living cells monitored by TR-FRET	11
Mitigating the risk of antimalarial resistance via covalent dual-subunit inhibition of the Plasmodium proteasome	11
Resident and elicited murine macrophages differ in expression of their glycomes and glycan-binding proteins	11
Targeting non-canonical pathways as a strategy to modulate the sodium iodide symporter	11
Motif-dependent immune co-receptor interactome profiling by photoaffinity chemical proteomics	11
Generation of glycan-specific nanobodies	11
Genome- and metabolome-guided discovery of marine BamA inhibitors revealed a dedicated darobactin halogenase	10
TRIM21 is a druggable target for the treatment of metastatic colorectal cancer through ubiquitination and activation of MST2	10
Small molecules as tools for functional assessment of deubiquitinating enzyme function	10
Peptidoglycan NlpC/P60 peptidases in bacterial physiology and host interactions	10
HDAC3 and HDAC8 PROTAC dual degrader reveals roles of histone acetylation in gene regulation	10
Temsavir blocks the immunomodulatory activities of HIV-1 soluble gp120	10
A phospholipid mimetic targeting LRH-1 ameliorates colitis	10
IFNα primes cancer cells for Fusicoccin-induced cell death via 14-3-3 PPI stabilization	10
Identification of a highly efficient dual type I/II FMS-like tyrosine kinase inhibitor that disrupts the growth of leukemic cells	10
Identifying enhancers of innate immune signaling as broad-spectrum antivirals active against emerging viruses	10