Sequence-specific polypeptoids: A diverse family of heteropolymers with stable secondary structure

Kent Kirshenbaum, Annelise E. Barron, Richard Goldsmith, +6

Proceedings of the National Academy of Sciences

GDC-0449—A potent inhibitor of the hedgehog pathway

Kirk Robarge, Shirley A. Brunton, Georgette M. Castanedo, +28

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologySignaling PathwayMolecular PathwayMedicinePharmacology +4

Small Molecule Inhibition of GDC-0449 Refractory Smoothened Mutants and Downstream Mechanisms of Drug Resistance

Gerrit J.P. Dijkgraaf, Bruno Alicke, Lasse Weinmann, +11

Cancer Research

Molecular BiologyGliomaSmall Molecule InhibitionTumor BiologyDrug Resistance +16

NMR determination of the major solution conformation of a peptoid pentamer with chiral side chains

Philippe Armand, Kent Kirshenbaum, Richard Goldsmith, +8

Proceedings of the National Academy of Sciences

Discovery of a Potent, Selective, and Orally Available Class I Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor (GDC-0980) for the Treatment of Cancer

Daniel P. Sutherlin, Linda Bao, Megan Berry, +28

Journal of Medicinal Chemistry

Translational PharmacologyPre-clinical PharmacologyMolecular PharmacologyMedicinal ChemistryReceptor Tyrosine Kinase +18

[25] Synthesis of N-substituted glycine peptoid libraries

Gianine Figliozzi, Richard Goldsmith, Simon C. Ng, +2

Methods in enzymology on CD-ROM/Methods in enzymology

PeptoidPeptide SynthesisBiochemistryGlycosylation

Discovery of 2-{3-[2-(1-Isopropyl-3-methyl-1<i>H</i>-1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-<i>d</i>][1,4]oxazepin-9-yl]-1<i>H</i>-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β-Sparing Phosphoinositide 3-Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity

Chudi Ndubaku, Timothy P. Heffron, Steven T. Staben, +26

Journal of Medicinal Chemistry

Drug TargetUnbound Drug ExposurePharmacotherapyIntrinsic ClearanceTumor Biology +19

Discovery of (Thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer

Daniel P. Sutherlin, Deepak Sampath, Megan Berry, +25

Journal of Medicinal Chemistry

Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform

Timothy P. Heffron, BinQing Wei, Alan G. Olivero, +18

Journal of Medicinal Chemistry

Peptide ScienceChemical BiologyExhibit SelectivityMolecular PharmacologyMedicinal Chemistry +17

The Design and Identification of Brain Penetrant Inhibitors of Phosphoinositide 3-Kinase α

Timothy P. Heffron, Laurent Salphati, Bruno Alicke, +18

Journal of Medicinal Chemistry

Pi3k InhibitorsPharmacotherapyHigh-grade GliomasCancer BiologyGlioma +22