Structural Basis for AMPK Activation: Natural and Synthetic Ligands Regulate Kinase Activity from Opposite Poles by Different Molecular Mechanisms

Matthew F. Calabrese, Francis Rajamohan, Melissa S. Harris, +24

Structure

Opposite PolesMolecular PhysiologySignal TransductionBiochemistrySignaling Pathway +7

Pyrrolopyridine Inhibitors of Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MK-2)

David R. Anderson, Marvin J. Meyers, William F. Vernier, +7

Journal of Medicinal Chemistry

Identification of <i>N</i>-{<i>cis</i>-3-[Methyl(7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases

Michael L. Vazquez, Neelu Kaila, Joseph W. Strohbach, +32

Journal of Medicinal Chemistry

ImmunodeficienciesJanus KinasesImmunologyPharmacotherapyImmunotherapy +20

Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1<i>H</i>-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy

Kimberly O. Cameron, Daniel W. Kung, Amit S. Kalgutkar, +30

Journal of Medicinal Chemistry

Renal InflammationPharmacotherapyInsulin SignalingMolecular PharmacologyMedicinal Chemistry +17

A Thermodynamic Ligand Binding Study of the Third PDZ Domain (PDZ3) from the Mammalian Neuronal Protein PSD-95

Dorina Saro, Tao Li, Chamila N. Rupasinghe, +3

Biochemistry

Covalent Inhibitors of Interleukin-2 Inducible T Cell Kinase (Itk) with Nanomolar Potency in a Whole-Blood Assay

Christoph W. Zapf, Brian S. Gerstenberger, Xing Li, +12

Journal of Medicinal Chemistry

Distinctive Attributes of β-Lactam Target Proteins in <i>Acinetobacter baumannii</i> Relevant to Development of New Antibiotics

Seungil Han, Nicole Caspers, Richard P. Zaniewski, +5

Journal of the American Chemical Society

BacteriologyMolecular BiologyNew AntibioticsPenicillin-binding ProteinsAnalytical Ultracentrifugation +22

Thermodynamic and Structure Guided Design of Statin Based Inhibitors of 3-Hydroxy-3-Methylglutaryl Coenzyme A Reductase

Ronald W. Sarver, Elizabeth Bills, Gary L. Bolton, +10

Journal of Medicinal Chemistry

Medicinal ChemistryBiochemistryCardiovascular DiseaseStructure Guided DesignStatin Inhibitors +13

Probing the enzyme kinetics, allosteric modulation and activation of α1- and α2-subunit-containing AMP-activated protein kinase (AMPK) heterotrimeric complexes by pharmacological and physiological activators

Francis Rajamohan, Allan R. Reyes, Richard K. Frisbie, +9

Biochemical Journal

Molecular BiologyPeptide ScienceAllosteric ModulationEnzyme KineticsMolecular Pharmacology +18

Structural and Inhibition Analysis Reveals the Mechanism of Selectivity of a Series of Aggrecanase Inhibitors

Micky D. Tortorella, Alfredo G. Tomasselli, Karl J. Mathis, +8

Journal of Biological Chemistry

Aggrecanase InhibitorsBioorganic ChemistryGlycobiologyMolecular BiologyPolysaccharide +17