Antitumor Activity and Pharmacology of a Selective Focal Adhesion Kinase Inhibitor, PF-562,271

W. Gregory Roberts, Ethan Ung, Pamela Whalen, +21

Cancer Research

Antitumor ActivityCell AdhesionFocal Adhesion PlaquesPharmacotherapyCancer Biology +16

Spontaneous α-N-6-Phosphogluconoylation of a “His Tag” inEscherichia coli:The Cause of Extra Mass of 258 or 178 Da in Fusion Proteins

Kieran F. Geoghegan, H. B. F. Dixon, Philip J. Rosner, +10

Analytical Biochemistry

Protein ExpressionBiochemistryNatural SciencesMedicineProtein Biosynthesis +8

Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1 <i>H</i> -pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the Treatment of Schizophrenia†Coordinates of the PDE10A crystal structures have been deposited in the Protein Data Bank for compound 1 (3HQW), 2 (3HQY), 3 (3HQW) and 9 (3HR1).

Patrick R. Verhoest, Douglas S. Chapin, Michael L. Corman, +13

Journal of Medicinal Chemistry

Structural basis for effectiveness of siderophore-conjugated monocarbams against clinically relevant strains of<i>Pseudomonas aeruginosa</i>

Seungil Han, Richard P. Zaniewski, Eric S. Marr, +5

Proceedings of the National Academy of Sciences

Hydration Site EnergiesBiomolecular Structure PredictionMolecular BiologyAntimicrobial ChemotherapyBacterial Pathogens +24

Crystal structures of interleukin 17A and its complex with IL-17 receptor A

Shenping Liu, Xi Song, Boris A. Chrunyk, +4

Nature Communications

InflammationCytokineMolecular ImmunologyImmune RegulationImmunology +9

Discovery of a Series of 6,7-Dimethoxy-4-pyrrolidylquinazoline PDE10A Inhibitors

Thomas A. Chappie, John M. Humphrey, Martin P. Allen, +11

Journal of Medicinal Chemistry

Combinatorial Chemistry6,7-Dimethoxy-4-pyrrolidylquinazoline Pde10a InhibitorsPharmacotherapyAryl EtherHeterocycle Chemistry +14

Theoretical and Experimental Design of Atypical Kinase Inhibitors:  Application to p38 MAP Kinase

Kim F. McClure, Yuriy A. Abramov, Ellen R. Laird, +21

Journal of Medicinal Chemistry

Atypical Kinase InhibitorsDrug TargetP38 KinaseP38 InhibitorsPharmacotherapy +20

Synthesis and structure based optimization of novel Akt inhibitors

Blaise Lippa, Gonghua Pan, Matthew S. Corbett, +17

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicineRational Drug DesignNovel Akt InhibitorsDrug Development +3

Identification of a Brain Penetrant PDE9A Inhibitor Utilizing Prospective Design and Chemical Enablement as a Rapid Lead Optimization Strategy

Patrick R. Verhoest, Caroline Proulx-LaFrance, Michael L. Corman, +14

Journal of Medicinal Chemistry

Pyridone-Conjugated Monobactam Antibiotics with Gram-Negative Activity

Matthew F. Brown, Mark J. Mitton‐Fry, Joel T. Arcari, +28

Journal of Medicinal Chemistry

AntibioticsCompound 17MedicineEscherichia ColiAntibacterial Agent +9