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1,279 results
  • A Novel Flow Cytometric Assay to Identify Inhibitors of RBPJ-DNA Interactions. [Journal Article]
    SLAS Discov. 2020 Jun 22 [Online ahead of print]Lake RJ, Haynes MK, … Fan HY
  • Notch signaling is often involved in cancer cell initiation and proliferation. Aberrant Notch activation underlies more than 50% of T-cell acute lymphoblastic leukemia (T-ALL); accordingly, chemicals disrupting Notch signaling are of potential to treat Notch-dependent cancer. Here, we developed a flow cytometry-based high-throughput assay to identify compounds that disrupt the interactions of DNA…
  • Paracrine regulation and improvement of β-cell function by thioredoxin. [Journal Article]
    Redox Biol. 2020 May 16; 34:101570.Hanschmann EM, Petry SF, … Linn T
  • The failure of insulin-producing β-cells is the underlying cause of hyperglycemia in diabetes mellitus. β-cell decay has been linked to hypoxia, chronic inflammation, and oxidative stress. Thioredoxin (Trx) proteins are major actors in redox signaling and essential for signal transduction and the cellular stress response. We have analyzed the cytosolic, mitochondrial, and extracellular Trx system…
  • Redox Modulation and Induction of Ferroptosis as a New Therapeutic Strategy in Hepatocellular Carcinoma. [Journal Article]
    Transl Oncol. 2020 Aug; 13(8):100785.Lippmann J, Petri K, … Liese J
  • Ferroptosis, a newly discovered form of cell death mediated by reactive oxygen species (ROS) and lipid peroxidation, has recently been shown to have an impact on various cancer types; however, so far there are only few studies about its role in hepatocellular carcinoma (HCC). The delicate equilibrium of ROS in cancer cells has found to be crucial for cell survival, thus increased levels may trigg…
  • "Direct to Drug" screening as a precision medicine tool in multiple myeloma. [Journal Article]
    Blood Cancer J. 2020 May 11; 10(5):54.Bonolo de Campos C, Meurice N, … Stewart AK
  • Seventy-six FDA-approved oncology drugs and emerging therapeutics were evaluated in 25 multiple myeloma (MM) and 15 non-Hodgkin's lymphoma cell lines and in 113 primary MM samples. Ex vivo drug sensitivities were mined for associations with clinical phenotype, cytogenetic, genetic mutation, and transcriptional profiles. In primary MM samples, proteasome inhibitors, dinaciclib, selinexor, venetocl…
  • ESI MS studies highlight the selective interaction of Auranofin with protein free thiols. [Journal Article]
    Dalton Trans. 2020 May 14; 49(18):5906-5913.Zoppi C, Messori L, Pratesi A
  • The clinically established gold drug Auranofin was reacted individually with a group of representative proteins, namely ubiquitin, ribonuclease A, carbonic anhydrase, haemoglobin and superoxide dismutase, and adduct formation was monitored in the various cases by ESI-MS analysis. We found that the reaction is highly selective for solvent exposed free cysteines that are modified through coordinati…
  • Comprehensive chemical proteomics for target deconvolution of the redox active drug auranofin. [Journal Article]
    Redox Biol. 2020 May; 32:101491.Saei AA, Gullberg H, … Zubarev RA
  • Chemical proteomics encompasses novel drug target deconvolution methods in which compound modification is not required. Herein we use Thermal Proteome Profiling, Functional Identification of Target by Expression Proteomics and multiplexed redox proteomics for deconvolution of auranofin targets to aid elucidation of its mechanisms of action. Auranofin (Ridaura®) was approved for treatment of rheum…
  • Rhenium-Based Complexes and in Vivo Testing: A Brief History. [Journal Article]
    Chembiochem. 2020 Mar 20 [Online ahead of print]Capper MS, Packman H, Rehkämper M
  • The success of metal-based anticancer therapeutics in the treatment of cancer is best exemplified by cisplatin. Currently used in 32/78 cancer regimens, metal-based drugs have a clear role in cancer therapy. Despite this, metal-based anticancer therapeutics are not without drawbacks, with issues such as toxic side effects and the development of resistance mechanisms. This has led to investigation…
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