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Showing 1–19 of 19 results
Advanced filters: Author: Michelle R. Arkin Clear advanced filters

  • Molecular glues have great potential for drug discovery if they can be systematically discovered. Konstantinidou, et al describe a scaffold-hopping approach using multicomponent reaction chemistry to design molecular glues that induce 14-3- 3σ/ERα formation in cells.

    • Markella Konstantinidou
    • Marios Zingiridis
    • Michelle R. Arkin
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-13

  • The authors used deep metric learning to characterize 650 neuroactive compounds by zebrafish behavioral profiles. After redesigning a large screen to overcome AI/ML shortcut learning, zebrafish behavioral similarity found compounds acting on the same human receptors as structurally dissimilar drugs.

    • Leo Gendelev
    • Jack Taylor
    • Michael J. Keiser
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-16

  • Braxton et al. report structures of human p97/VCP bound to the UBXD1 adaptor involved in autophagy. The structures reveal how UBXD1 utilizes multiple interaction domains to remodel and open the hexamer ring, revealing its role in p97 regulation.

    • Julian R. Braxton
    • Chad R. Altobelli
    • Daniel R. Southworth
    ResearchOpen Access
    Nature Structural & Molecular Biology
    Volume: 30, P: 2009-2019

  • Oxidative stress can promote neurodegeneration. Akassoglou and colleagues describe Tox-seq, a functional single-cell RNA sequencing method to identify oxidative stress transcriptional signatures in CNS-resident cells. Tox-seq identified coagulation and glutathione-redox pathway genes that are coupled to oxidative stress and that could be targeted by the glutathione-regulating small molecule acivicin.

    • Andrew S. Mendiola
    • Jae Kyu Ryu
    • Katerina Akassoglou
    Research
    Nature Immunology
    Volume: 21, P: 513-524

  • Fibrin deposition occurs after the blood–brain barrier is breached. Akassoglou and colleagues generate a therapeutic monoclonal antibody that targets a cryptic fibrin epitope to suppress activation of innate immune responses in the CNS and diminish neuroinflammation.

    • Jae Kyu Ryu
    • Victoria A. Rafalski
    • Katerina Akassoglou
    Research
    Nature Immunology
    Volume: 19, P: 1212-1223

  • The C termini sequences recognized by E3 ubiquitin ligase CHIP were identified via a peptide library screen. Caspase cleavage caused the exposure of aspartic acid at the C termini of Tau and caspase-6 that made them accessible to CHIP.

    • Matthew Ravalin
    • Panagiotis Theofilas
    • Jason E. Gestwicki
    Research
    Nature Chemical Biology
    Volume: 15, P: 786-794

  • Mechanisms that control gene expression variation in cells can affect factors such as population growth and adaptability. Here, the authors present a strategy that allows both the level and amount of variation in gene expression to be tuned in E. coli populations using the fimswitch.

    • Michelle Hung
    • Emily Chang
    • Han N. Lim
    Research
    Nature Communications
    Volume: 5, P: 1-11

  • Human, mouse and iPSC-derived microglia demonstrate that interaction between GRN and phagocytic receptors can rescue (MERTK) or worsen (AXL) FTD-disease features. CSF MERTK maybe a biomarker of symptomatic disease conversion in genetic FTD.

    • Claire Dudley Clelland
    • Li Fan
    • Li Gan
    ResearchOpen Access
    Communications Biology
    Volume: 8, P: 1-14

  • The development of selective ubiquitin-specific protease-7 (USP7) inhibitors GNE-6640 and GNE-6776, which induce tumour cell death and reveal differential kinetics of Lys-48 and Lys-63-linked ubiquitin chain depolymerization by USP7.

    • Lorna Kategaya
    • Paola Di Lello
    • Ingrid E. Wertz
    Research
    Nature
    Volume: 550, P: 534-538

  • Cataloging microbial genomes from Earth’s environments expands the known phylogenetic diversity of bacteria and archaea.

    • Stephen Nayfach
    • Simon Roux
    • Emiley A. Eloe-Fadrosh
    ResearchOpen Access
    Nature Biotechnology
    Volume: 39, P: 499-509

  • Steven Chen et al. develop an automated, time-lapsed, high-content screen to quantify the responses of Schistosoma mansoni larvae to chemical insult. They apply their method to evaluate 45 static and kinetic response endpoints for seven drugs and screen 1323 approved drugs. Their work identifies anti-schistosomal compounds and underscores the value of quantifying motion in phenotypic drug discovery.

    • Steven Chen
    • Brian M. Suzuki
    • Conor R. Caffrey
    ResearchOpen Access
    Communications Biology
    Volume: 3, P: 1-9

  • Entamoeba histolytica causes human amebiasis. Although antibiotic therapy for this infection exists, there are limited treatment options for this potentially fatal invasive disease. Anjan Debnath and colleagues now report their identification of auranofin, an approved treatment for rheumatoid arthritis, as a candidate new drug for combating E. histolytica infection.

    • Anjan Debnath
    • Derek Parsonage
    • Sharon L Reed
    Research
    Nature Medicine
    Volume: 18, P: 956-960

  • The reproducibility of biomedical research on novel drug targets has become suspect. Here, we highlight how drug discovery centres embedded in academic institutions, but with a translational imperative, can help address this reproducibility crisis.

    • Stephen V. Frye
    • Michelle R. Arkin
    • Barbara S. Slusher
    Comments & Opinion
    Nature Reviews Drug Discovery
    Volume: 14, P: 733-734

  • Individuals with exactly the same genetic make-up can differ from one another in their development and resulting phenotype when the genome contains a mutation — a phenomenon called 'partial penetrance'. Exploration of the genetic and stochastic factors controlling the proportion of abnormal 'twin' spores in mutant populations of the bacterium Bacillus subtilus now reveals how mutations affecting DNA replication and cell division may act in synergy to significantly increase the penetrance of twin sporulation.

    • Avigdor Eldar
    • Vasant K. Chary
    • Michael B. Elowitz
    Research
    Nature
    Volume: 460, P: 510-514