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"Minimalist" cyclopropene-containing photo-cross-linkers suitable for live-cell imaging and affinity-based protein labeling.
TLDR
Novel minimalist linkers containing both an alkyl diazirine and a cyclopropene are developed, which could be used for simultaneous in situ imaging and covalent labeling of endogenous BRD-4 (an important epigenetic protein) via a rapid, copper-free, tetrazine-cyclopropene ligation reaction. Expand
Oxygenated phosphatidylethanolamine navigates phagocytosis of ferroptotic cells by interacting with TLR2
TLDR
This work demonstrates that SAPE-OOH on ferroptotic cell surface acts as an eat-me signal and navigates phagocytosis by targeting TLR2 on macrophages. Expand
Tetrazole Photoclick Chemistry: Reinvestigating Its Suitability as a Bioorthogonal Reaction and Potential Applications.
TLDR
Tetrazoles were incorporated into Bodipy and Acedan dyes, providing novel photo-crosslinkers with one- and two-photon fluorescence Turn-ON properties that may be developed into protein-detecting biosensors that are capable of photoinduced, no-wash imaging of endogenous kinase activities in live mammalian cells. Expand
Assembly of indole-2-carboxylic acid esters through a ligand-free copper-catalysed cascade process.
A straightforward synthesis of indole-2-carboxylic esters was developed through a ligand-free copper-catalysed condensation/coupling/deformylation cascade process from 2-halo aryl aldehydes orExpand
Synthesis of aza-fused polycyclic quinolines through copper-catalyzed cascade reactions.
A new and efficient method for the synthesis of aza-fused polycyclic quinolines (e.g., benzimidazo[1,2-a]quinolines) is described. This protocol includes an intermolecular condensation followed by aExpand
Pericyte-targeting prodrug overcomes tumor resistance to vascular disrupting agents.
TLDR
Evidence is provided to support a hypothesis that shifting the target of VDAs from tumor vessel endothelial cells to pericytes disrupts tumor peripheral vessels and the viable rim, circumventing VDA treatment resistance. Expand
AMPK mediates a pro‐survival autophagy downstream of PARP‐1 activation in response to DNA alkylating agents
TLDR
Data from this study reveal a novel mechanism in controlling MNNG‐mediated autophagy via AMPK activation downstream of PARP‐1 activation and ATP depletion. Expand
Multiplex Imaging and Cellular Target Identification of Kinase Inhibitors via an Affinity-Based Proteome Profiling Approach
TLDR
This work reports the first photoaffinity-based, small molecule AKA probe capable of both live-cell imaging of AKA activities and in situ proteome profiling of potential off-targets of MLN8237 (including AKA-associating proteins). Expand
Tetrazole-Based Probes for Integrated Phenotypic Screening, Affinity-Based Proteome Profiling, and Sensitive Detection of a Cancer Biomarker.
TLDR
This work combined phenotypic screening of a fully functionalized small-molecule library with competitive affinity-based proteome profiling to map and functionally characterize the targets of screening hits to identify ANXA2, PDIA3/4, FLAD1, and NOS2 as primary cellular targets of two bioactive molecules that inhibit cancer cell proliferation. Expand
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