1,186 results found
    1. Biochemistry and Chemical Biology
    2. Neuroscience

    Cell type-specific pharmacology of NMDA receptors using masked MK801

    Yunlei Yang et al.
    The small molecule NMDA-receptor antagonist MK801 has been genetically targeted to specific cell types in brain tissue to examine the role of NMDA receptors in cocaine-induced synaptic plasticity.
    1. Cancer Biology

    Convergent organization of aberrant MYB complex controls oncogenic gene expression in acute myeloid leukemia

    Sumiko Takao et al.
    Definition of leukemia gene expression mechanisms reveals general principles of cancer gene control and offers a pharmacologic strategy for its therapeutic reprogramming.
    1. Computational and Systems Biology

    Systematic integration of biomedical knowledge prioritizes drugs for repurposing

    Daniel Scott Himmelstein et al.
    Project Rephetio combines data integration and systematic analysis to enable drug repurposing predictions on an unprecedented scale.
    1. Cancer Biology

    The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer

    James D Joseph et al.
    GDC-0810 is a novel, orally bioavailable SERD that exhibits robust pre-clinical activity in models of ER+ breast cancer, including models of tamoxifen resistance, and those that express the ERα mutations, ER.Y537S and ER.D538G.
    1. Structural Biology and Molecular Biophysics

    Domain–domain interactions determine the gating, permeation, pharmacology, and subunit modulation of the IKs ion channel

    Mark A Zaydman et al.
    Contrary to a generally accepted principle, the pore properties of KCNQ1 channels depend on the states of voltage-sensing domains activation; KCNE1 alters the voltage-sensing domains-pore coupling to modulate KCNQ1 channel properties.
    1. Cell Biology
    2. Neuroscience

    The orphan receptor GPR88 blunts the signaling of opioid receptors and multiple striatal GPCRs

    Thibaut Laboute et al.
    GPR88 inhibits G-protein signaling of nearby GPCRs, and dampens b-arrestin recruitment by all GPCRs tested, likely by sequestration in intracellular compartments.
    1. Biochemistry and Chemical Biology

    Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site

    Rajendra Uprety et al.
    The structure-based design established a new approach to control pathway-selective activation of opioid receptors, resulting in new dual MOR/KOR G-protein biased agonist analgesics with attenuated liabilities.
    1. Neuroscience

    Optical electrophysiology for probing function and pharmacology of voltage-gated ion channels

    Hongkang Zhang et al.
    Optogenetic tools enable sophisticated measurements of a voltage-gated sodium channel implicated in pain, as well as high-throughput screening of candidate channel blockers.
    1. Biochemistry and Chemical Biology

    Pharmacologic ATF6 activating compounds are metabolically activated to selectively modify endoplasmic reticulum proteins

    Ryan Paxman et al.
    The small molecule, 147, is a pro-drug that preferentially activates ATF6 signaling through a mechanism involving localized metabolic activation and selective covalent modification of ER resident proteins involved in regulating ATF6 activity.
    1. Cancer Biology
    2. Cell Biology

    MELK is not necessary for the proliferation of basal-like breast cancer cells

    Hai-Tsang Huang et al.
    The inhibitory or deletion effect of MELK does not impair the proliferation of basal-like breast cancer cell lines.

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