A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models

Elayne Chan-Penebre, Kristy G. Kuplast, Christina R. Majer, +27

Nature Chemical Biology

Vitro PotencySignal TransductionMedicineMcl ModelsSelective Inhibitor +8

A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC

Helai P. Mohammad, Kimberly N. Smitheman, Chandrashekhar D. Kamat, +30

Cancer Cell

Oncogenic AgentMedicineEpigenetic ChangePharmacologyLsd1 Inhibitors +7

Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia

Melissa B. Pappalardi, Kathryn Keenan, Mark Cockerill, +59

Nature Cancer

Hematological MalignancyMedicineAcute Myeloid LeukemiaMixed-phenotype Acute LeukemiaPharmacology +7

4-Aryl-1,2,3-triazole:  A Novel Template for a Reversible Methionine Aminopeptidase 2 Inhibitor, Optimized To Inhibit Angiogenesis in Vivo

Lara S. Kallander, Qing Lü, Wenfang Chen, +21

Journal of Medicinal Chemistry

Mouse Matrigel ModelEndothelial Cell GrowthPharmacotherapyChemical BiologyPharmaceutical Chemistry +15

Structure of human neutrophil collagenase reveals large S1′ specificity pocket

Travis Stams, John Spurlino, Douglas L. Smith, +5

Nature Structural & Molecular Biology

Protein FunctionGranulocyteMedicineNatural SciencesMolecular Biology +8

Discovery and Characterization of a Cell-Permeable, Small-Molecule c-Abl Kinase Activator that Binds to the Myristoyl Binding Site

Jingsong Yang, Nino Campobasso, Mangatt P. Biju, +27

Chemistry & Biology

Signal TransductionCell SignalingMyristoyl Binding SiteNatural SciencesMacromolecular Machine +9

Steady-State Kinetic Characterization of Substrates and Metal-Ion Specificities of the Full-Length and N-Terminally Truncated Recombinant Human Methionine Aminopeptidases (Type 2)

Guang Yang, Robert B. Kirkpatrick, Thau Ho, +10

Biochemistry

Molecular BiologyChemical BiologyProtein FoldingBioanalysisStructure-function Enzyme Kinetics +15

C-terminal region of USP7/HAUSP is critical for deubiquitination activity and contains a second mdm2/p53 binding site

Jianhong Ma, John D. Martin, Yu Xue, +8

Archives of Biochemistry and Biophysics

Second Mdm2/p53C-terminal RegionDeubiquitination ActivityNatural SciencesSignal Recognition +4

A Second p53 Binding Site in the Central Domain of Mdm2 Is Essential for p53 Ubiquitination

Jianhong Ma, John D. Martin, Hong Zhang, +8

Biochemistry

Crystal structure of the kinase domain of serum and glucocorticoid‐regulated kinase 1 in complex with AMP–PNP

Baoguang Zhao, Ruth Lehr, Angela Smallwood, +6

Protein Science

Crystal StructureMolecular RegulationAtp Binding SiteMolecular BiologySgk1 Crystal Structure +17