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A small-molecule inhibitor of the BRCA2-RAD51 interaction modulates RAD51 assembly and potentiates DNA damage-induced cell death

期刊: CELL CHEMICAL BIOLOGY, 2021; 28 (6)

BRCA2 controls RAD51 recombinase during homologous DNA recombination (HDR) through eight evolutionarily conserved BRC repeats, which individually enga......

Discovery of a sigma(1) receptor antagonist by combination of unbiased cell painting and thermal proteome profiling

期刊: CELL CHEMICAL BIOLOGY, 2021; 28 (6)

Phenotypic screening for bioactive small molecules is typically combined with affinity-based chemical proteomics to uncover the respective molecular t......

Phosphorylation-regulated HMGA1a-P53 interaction unveils the function of HMGA1a acidic tail phosphorylations via synthetic proteins

期刊: CELL CHEMICAL BIOLOGY, 2021; 28 (5)

As a typical member of intrinsically disordered proteins (IDPs), HMGA1a carries many post-translational modifications (PTMs). To study the undefined f......

Small-molecule probe reveals a kinase cascade that links stress signaling to TCF/LEF and Wnt responsiveness

期刊: CELL CHEMICAL BIOLOGY, 2021; 28 (5)

Wnt signaling plays a central role in tissue maintenance and cancer. Wnt activates downstream genes through beta-catenin, which interacts with TCF/LEF......

Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2

期刊: CELL CHEMICAL BIOLOGY, 2021; 28 (6)

The COVID-19 pandemic has been disastrous to society and effective drugs are urgently needed. The papain-like protease domain (PLpro) of SARS-CoV-2 (S......

A SUMO1-Derived Peptide Targeting SUMO-Interacting Motif Inhibits alpha-Synuclein Aggregation

期刊: CELL CHEMICAL BIOLOGY, 2021; 28 (2)

The accumulation of alpha-synuclein amyloid fibrils in the brain is linked to Parkinson's disease and other synucleinopathies. The intermediate specie......

Formation of an aminovinyl-cysteine residue in thioviridamides occurs through a path independent of known lanthionine synthetase activity

期刊: CELL CHEMICAL BIOLOGY, 2021; 28 (5)

2-Aminovinyl-cysteine (AviCys) is a thioether amino acid shared by a variety of ribosomally synthesized and posttranslationally modified peptides (RiP......

Quantitative chemoproteomics reveals O-GlcNAcylation of cystathionine gamma-lyase (CSE) represses trophoblast syncytialization

期刊: CELL CHEMICAL BIOLOGY, 2021; 28 (6)

Emerging evidence indicates the involvement of O-GlcNAc modification in placental development and pregnant health through mechanisms that are not well......

HER2-targeted antibody-drug conjugate induces host immunity against cancer stem cells

期刊: CELL CHEMICAL BIOLOGY, 2021; 28 (5)

We previously tested HER2-targeted antibody-drug conjugates (ADCs) in immunocompromised (SCID) mice, precluding evaluation of host immunity, impact on......

Hypomorph mutation-directed small-molecule protein-protein interaction inducers to restore mutant SMAD4-suppressed TGF-beta signaling

期刊: CELL CHEMICAL BIOLOGY, 2021; 28 (5)

Tumor suppressor genes represent a major class of oncogenic drivers. However, direct targeting of loss-offunction tumor suppressors remains challengin......

MGST1 is a redox-sensitive repressor of ferroptosis in pancreatic cancer cells

期刊: CELL CHEMICAL BIOLOGY, 2021; 28 (6)

Ferroptosis is a type of nonapoptotic cell death driven by lipid peroxidation. Here, we show a key role of MGST1 in inhibiting ferroptosis in cell cul......

Photoswitchable CAR-T Cell Function In Vitro and In Vivo via a Cleavable Mediator

期刊: CELL CHEMICAL BIOLOGY, 2021; 28 (1)

Chimeric antigen receptor (CAR)-T-based therapeutics are a breakthrough in cancer treatment; however, they are hampered by constitutive activation, wh......

Nuisance compounds in cellular assays

期刊: CELL CHEMICAL BIOLOGY, 2021; 28 (3)

Compounds that exhibit assay interference or undesirable mechanisms of bioactivity ("nuisance compounds'') are routinely encountered in cellular assay......

Autophagy-Dependent Ferroptosis: Machinery and Regulation

期刊: CELL CHEMICAL BIOLOGY, 2020; 27 (4)

Macroautophagy (hereafter referred to as autophagy) is an evolutionarily conserved cellular process capable of degr.:.:!ing various biological molecul......

Combined Omics Approach Identifies Gambogic Acid and Related Xanthones as Covalent Inhibitors of the Serine Palmitoyltransferase Complex

期刊: CELL CHEMICAL BIOLOGY, 2020; 27 (5)

In this study, we identify the natural product gambogic acid as well as structurally related synthetic xanthones as first-in-class covalent inhibitors......

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