Publications by authors named "Anupong Tangpeerachaikul"
Article Synopsis
- Three generations of tyrosine kinase inhibitors (TKIs) exist for ALK fusion-positive non-small cell lung cancer, but they fail to effectively address resistance, brain activity, and TRK inhibition issues.* -
- NVL-655, a new TKI, shows superior selectivity and potency against ALK mutations, significantly outperforming current approved ALK TKIs in preclinical studies.* -
- Preliminary results from a phase I/II trial indicate NVL-655's promise for treating heavily pretreated patients, including those with brain metastases and resistance mutations, potentially making it a fourth-generation advancement for ALK-driven cancers.*
Article Synopsis
- NVL-520 shows strong effectiveness in targeting ROS1 and can handle various ROS1 resistance mutations.
- It selectively targets the ROS1 G2032R mutation better than TRK, making it a promising option.
- The drug also penetrates the brain, offering potential benefits for ROS1 fusion-positive patients compared to older TKIs.
Cortistatin A (CA) is a highly selective inhibitor of the Mediator kinases CDK8 and CDK19. Using CA, we now report a large-scale identification of Mediator kinase substrates in human cells (HCT116). We identified over 16,000 quantified phosphosites including 78 high-confidence Mediator kinase targets within 64 proteins, including DNA-binding transcription factors and proteins associated with chromatin, DNA repair, and RNA polymerase II.
View Article and Find Full Text PDFSuper-enhancers (SEs), which are composed of large clusters of enhancers densely loaded with the Mediator complex, transcription factors and chromatin regulators, drive high expression of genes implicated in cell identity and disease, such as lineage-controlling transcription factors and oncogenes. BRD4 and CDK7 are positive regulators of SE-mediated transcription. By contrast, negative regulators of SE-associated genes have not been well described.
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- Azides that can chelate copper facilitate faster "Click chemistry" reactions (CuAAC) compared to non-chelating azides under biocompatible conditions.
- This enhanced reaction speed enables effective site-specific protein labeling on live cell surfaces using low copper concentrations (10–40 µM), achieving better signal detection than previous methods.
- The approach also improves the detection sensitivity for alkyne-modified proteins and RNA, which can be labeled through metabolic feeding.
The inverse-electron-demand Diels-Alder cycloaddition between trans-cyclooctenes and tetrazines is biocompatible and exceptionally fast. We utilized this chemistry for site-specific fluorescence labeling of proteins on the cell surface and inside living mammalian cells by a two-step protocol. Escherichia coli lipoic acid ligase site-specifically ligates a trans-cyclooctene derivative onto a protein of interest in the first step, followed by chemoselective derivatization with a tetrazine-fluorophore conjugate in the second step.
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