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Showing 1–10 of 10 results
Advanced filters: Author: Darcie Miller Clear advanced filters

  • To maintain the efficacy of drugs metabolized by CYP3A4, pan-CYP3A inhibitor is often co-administered, but the high homology between CYP3A4 and CYP3A5 has hampered the development of selective CYP3A4 inhibitors. Here, the authors report a series of selective CYP3A4 inhibitors and show that differential C-terminal loop conformations and two distinct ligand binding surfaces disfavour the binding of selective CYP3A4 inhibitors to CYP3A5.

    • Jingheng Wang
    • Stanley Nithianantham
    • Taosheng Chen
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-19

  • PXR is a receptor activated by diverse compounds that triggers detoxification pathways in the cell, and blocking this receptor may increase the effectiveness of certain drugs. Here, the authors present the structural basis of PXR inhibition.

    • Efren Garcia-Maldonado
    • Andrew D. Huber
    • Taosheng Chen
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-14

  • Kelch-domain KLHDCX E3 ligases bind substrate C-terminal glycines. This study reveals substrate selectivity by E3s with similar structures; C-degrons are perceived by a “C-terminus anchor motif”, whose display on different Kelch propeller blades along with distal interactions establish specificity.

    • Daniel C. Scott
    • Sagar Chittori
    • Brenda A. Schulman
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-17

  • KLHDC2 is a promising E3 ligase for targeted protein degradation (TPD). In this study, the authors demonstrate that heterobifunctional degraders induce cooperative ternary complexes with KLHDC2 and BRD3. They highlight exit vector, neo-substrate, E3 ligase selectivity, and prodrug choice can effectively leverage C-degron E3s for TPD.

    • Daniel C. Scott
    • Suresh Dharuman
    • Brenda A. Schulman
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-19

  • CX-5461 recently progressed through phase I clinical trial as a first-inhuman inhibitor of RNA-POL I. Here, the authors demonstrate that CX-5461 synergizes with topoisomerase I inhibitors to inhibit neuroblastoma cells and that its primary target in this disease is topoisomerase II beta and not RNA-POL I.

    • Min Pan
    • William C. Wright
    • Paul Geeleher
    ResearchOpen Access
    Nature Communications
    Volume: 12, P: 1-20

  • Cryo-electron microscopy, nuclear magnetic resonance and X-ray crystallography are used to provide structural and mechanistic details of the activation of anaplastic lymphoma kinase by the ligands ALKAL1 and ALKAL2.

    • Andrey V. Reshetnyak
    • Paolo Rossi
    • Charalampos G. Kalodimos
    Research
    Nature
    Volume: 600, P: 153-157

  • Testis-restricted melanoma antigen (MAGE) proteins function as substrate adapters for E3 ubiquitin ligases. Biochemical and structural analyses of MAGE-A11 provide insight into the substrate binding mode of MAGE proteins and enable discovery of potent, cytotoxic inhibitors of MAGE-A11:substrate interaction.

    • Seung Wook Yang
    • Xin Huang
    • Patrick Ryan Potts
    ResearchOpen Access
    Nature Communications
    Volume: 11, P: 1-14

  • DesT is a bacterial transcription factor that regulates targets which are in turn involved in controlling the unsaturated:saturated fatty acid ratio available for membrane lipid biosynthesis. The structures of DesT bound to various fatty acids now indicates the conformational changes involved in altering DNA binding site affinity, providing a structural basis for responding to changes in the ratio of unsaturated:saturated fatty acids.

    • Darcie J Miller
    • Yong-Mei Zhang
    • Stephen W White
    Research
    Nature Structural & Molecular Biology
    Volume: 17, P: 971-975