36 results found
    1. Cancer Biology
    2. Cell Biology

    Inhibitor-induced HER2-HER3 heterodimerisation promotes proliferation through a novel dimer interface

    Jeroen Claus et al.
    The clinically approved HER2 inhibitor lapatinib causes HER2 and HER3 kinase domains to dimerise in a non-canonical, symmetric orientation, providing a platform for oligomerisation and predisposing to receptor-driven cell proliferation.
    1. Biochemistry and Chemical Biology

    Tyr1 phosphorylation promotes phosphorylation of Ser2 on the C-terminal domain of eukaryotic RNA polymerase II by P-TEFb

    Joshua E Mayfield et al.
    The phosphorylation of tyrosine in the heptad repeat of the C-terminal domain of the largest subunit of RNA polymerase II promotes Ser2 phosphorylation by P-TEFb for pausing release.
    1. Structural Biology and Molecular Biophysics

    Differential impact of BTK active site inhibitors on the conformational state of full-length BTK

    Raji E Joseph et al.
    The first-in-class kinase inhibitor, Ibrutinib, destabilizes its autoinhibited Bruton’s tyrosine kinase (BTK) target, and a remote resistance mutation causes global structural changes that activate BTK catalytic activity.
    1. Cell Biology
    2. Medicine

    Senotherapeutic drugs for human intervertebral disc degeneration and low back pain

    Hosni Cherif et al.
    Targeting senescent cells in human intervertebral discs, using senotherapeutics, provides a potential therapeutic strategy to prevent or reduce disc degeneration and pain.
    1. Cancer Biology
    2. Developmental Biology

    Targeting mutant RAS in patient-derived colorectal cancer organoids by combinatorial drug screening

    Carla S Verissimo et al.
    Libraries of patient-derived tumor organoids are a reliable and scalable model system that can help identify and optimize targeted therapies in a pre-clinical setting.
    1. Biochemistry and Chemical Biology
    2. Cancer Biology

    Identification of a novel toxicophore in anti-cancer chemotherapeutics that targets mitochondrial respiratory complex I

    Zoe A Stephenson et al.
    A novel toxicophore, a 1H-1,2,3-triazole, has been identified in a wide-number of therapeutically-relevant compounds, including two anti-cancer chemotherapeutics, which inhibits mitochondria function and is mechanistically linked to adverse cardiac-cell events.
    1. Cancer Biology

    MARCH5 mediates NOXA-dependent MCL1 degradation driven by kinase inhibitors and integrated stress response activation

    Seiji Arai et al.
    MARCH5 mediates a pathway driving MCL1 degradation in response to cellular stress, which sensitizes to BH3 mimetic drugs targeting BCLXL and provides a broadly effective therapeutic strategy for solid tumors.
    1. Biochemistry and Chemical Biology
    2. Cancer Biology

    Overcoming myelosuppression due to synthetic lethal toxicity for FLT3-targeted acute myeloid leukemia therapy

    Alexander A Warkentin et al.
    Anti-targets are proteins that cause problems when inhibited along with an intended target and our novel chemical strategy affords unprecedented selectivity in the context of FLT3 vs. KIT inhibition for treatment of a devastating blood cancer.
    1. Biochemistry and Chemical Biology

    Single-molecule functional anatomy of endogenous HER2-HER3 heterodimers

    Byoungsan Choi et al.
    Single-molecule immunoprecipitation method reveals that the high catalytic rate and multi-tasking capability make a concerted contribution to the strong signaling potency of the HER2-HER3 heterodimers.
    1. Cancer Biology

    Overcoming mutation-based resistance to antiandrogens with rational drug design

    Minna D Balbas et al.
    Mutagenesis studies identified an androgen receptor mutation that converts enzalutamide-a drug recently approved for the treatment of advanced prostate cancer-into an androgen receptor agonist, and modeling studies informed the design of novel drugs that are effective against the mutant receptor.

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