J. Nonomiya

发表

Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.

P. Savy, E. Bradley, M. Ultsch, 2012, Journal of medicinal chemistry.

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

C. Ly, S. Sideris, S. Malek, 2011, Journal of medicinal chemistry.

Native Mass Spectrometry for the Study of PROTAC GNE‐987‐Containing Ternary Complexes

Melinda M. Mulvihill, R. Quinn, Miaomiao Liu, 2021, ChemMedChem.

Pharmacologic properties of AG-012986, a pan-cyclin-dependent kinase inhibitor with antitumor efficacy

P. O'Connor, S. Bender, B. Jessen, 2008, Molecular Cancer Therapeutics.

Preclinical Characterization of PF-00868554, a Potent Nonnucleoside Inhibitor of the Hepatitis C Virus RNA-Dependent RNA Polymerase

C. Lewis, S. Shi, S. Binford, 2009, Antimicrobial Agents and Chemotherapy.

Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis.

Kevin Chen, Ping Wu, Stephen Schmidt, 2015, ACS medicinal chemistry letters.

Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.

Adam R. Johnson, N. C. Ray, Rohan V Mendonca, 2019, Bioorganic & medicinal chemistry letters.

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.

Steve Price, E. Bradley, BinQing Wei, 2013, Journal of medicinal chemistry.

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

C. Ly, S. Sideris, S. Malek, 2012, Journal of medicinal chemistry.

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.

BinQing Wei, D. Sutherlin, L. Friedman, 2011, Journal of medicinal chemistry.

High-Throughput Kinetic Characterization of Irreversible Covalent Inhibitors of KRASG12C by Intact Protein MS and Targeted MRM.

Melinda M. Mulvihill, W. Phung, Amy Gustafson, 2022, Analytical chemistry.

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.

D. Sutherlin, S. Sideris, L. Friedman, 2010, Journal of medicinal chemistry.

Characterization of Antineovascularization Activity and Ocular Pharmacokinetics of Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GNE-947

J. Lubach, Xingrong Liu, C. Hop, 2020, Drug Metabolism and Disposition.

Characterization of Antineovascularization Activity and Ocular Pharmacokinetics of Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GNE-947

J. Lubach, Xingrong Liu, C. Hop, 2020, Drug Metabolism and Disposition.

Abstract DDT02-01: Discovery of GDC-0032: A beta-sparing PI3K inhibitor active against PIK3CA mutant tumors.

M. Belvin, E. Bradley, M. Ultsch, 2013 .

Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.

Steve Price, A. Nadin, BinQing Wei, 2013, Bioorganic & medicinal chemistry letters.

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.

S. Sideris, S. Malek, J. Lyssikatos, 2013, Bioorganic & medicinal chemistry letters.

Cis-amide isosteric replacement in thienobenzoxepin inhibitors of PI3-kinase.

E. Bradley, BinQing Wei, J. Lesnick, 2013, Bioorganic & medicinal chemistry letters.

Structure-based design of thienobenzoxepin inhibitors of PI3-kinase.

D. Sutherlin, S. Sideris, Leslie B. Lee, 2011, Bioorganic & medicinal chemistry letters.

Rational design of phosphoinositide 3-kinase α inhibitors that exhibit selectivity over the phosphoinositide 3-kinase β isoform.

BinQing Wei, D. Sutherlin, J. Lesnick, 2011, Journal of medicinal chemistry.

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.

D. Sutherlin, L. Friedman, Leslie B. Lee, 2010, Bioorganic & medicinal chemistry letters.

Discovery of (R)-6-cyclopentyl-6-(2-(2,6-diethylpyridin-4-yl)ethyl)-3-((5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methyl)-4-hydroxy-5,6-dihydropyran-2-one (PF-00868554) as a potent and orally available hepatitis C virus polymerase inhibitor.

Hui Li, Xiu Yu, M. Hickey, 2009, Journal of medicinal chemistry.

GDC-0980 Is a Novel Class I PI3K/mTOR Kinase Inhibitor with Robust Activity in Cancer Models Driven by the PI3K Pathway

M. Belvin, J. Spoerke, D. Sutherlin, 2011, Molecular Cancer Therapeutics.

GDC-0980IsaNovelClassIPI3K/mTORKinaseInhibitorwith RobustActivityinCancerModelsDrivenbythePI3KPathway

M. Belvin, J. Spoerke, D. Sutherlin, 2011 .

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR

S. Sideris, Leslie B. Lee, K. Edgar, 2016, ACS medicinal chemistry letters.

Loss of the intracellular enzyme QPCTL limits chemokine function and reshapes myeloid infiltration to augment tumor immunity

S. Rutz, Z. Modrušan, James Ziai, 2022, Nature Immunology.

Peripheral white blood cell toxicity induced by broad spectrum cyclin‐dependent kinase inhibitors

B. Jessen, C. Lewis, S. Price, 2007, Journal of applied toxicology : JAT.

The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).

S. Steinbacher, Steve Price, E. Gancia, 2016, Journal of medicinal chemistry.

Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.

P. Savy, Steve Price, A. Nadin, 2012, Journal of medicinal chemistry.

The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer

K. Walter, Andiliy G. Lai, J. Giltnane, 2016, eLife.

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor.

D. Sutherlin, S. Sideris, Irina S. Chuckowree, 2010, Bioorganic & medicinal chemistry letters.

Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity.

S. Steinbacher, BinQing Wei, C. Eigenbrot, 2017, Journal of medicinal chemistry.

Structure of the catalytic domain of human polo-like kinase 1.

A. Cheng, T. Wynn, C. Lewis, 2007, Biochemistry.

Structure of the catalytic domain of human protein kinase C beta II complexed with a bisindolylmaleimide inhibitor.

Djamal Bouzida, D. Bouzida, N. Grodsky, 2006, Biochemistry.

Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).

S. Sideris, L. Friedman, S. Malek, 2013, Journal of medicinal chemistry.

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

M. Belvin, C. Ly, S. Sideris, 2013, ACS medicinal chemistry letters.

Fragment-based identification and optimization of a class of potent pyrrolo[2,1-f][1,2,4]triazine MAP4K4 inhibitors.

Anthony M Giannetti, Ping Wu, Brandon J. Bravo, 2014, Bioorganic & medicinal chemistry letters.

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.

S. Sideris, Leslie B. Lee, K. Edgar, 2012, Journal of medicinal chemistry.

AG-024322 is a multi-targeted CDK inhibitor with potent antitumor activity in vivo

Gennady M Verkhivker, D. Knighton, C. Lewis, 2005 .

AG-024322 is a potent and selective multi-targeted CDK inhibitor with broad spectrum anti-proliferative activity

Gennady M Verkhivker, D. Knighton, C. Lewis, 2005 .

Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles.

A. K. Forrest, BinQing Wei, M. Ultsch, 2017, ACS medicinal chemistry letters.

Identification of GNE-293, a potent and selective PI3Kδ inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.

Steve Price, BinQing Wei, D. Sutherlin, 2013, Bioorganic & medicinal chemistry letters.

Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.

Steve Price, M. Belvin, BinQing Wei, 2013, Bioorganic & medicinal chemistry letters.

Discovery of selective 4-Amino-pyridopyrimidine inhibitors of MAP4K4 using fragment-based lead identification and optimization.

Anthony M Giannetti, Ping Wu, Brandon J. Bravo, 2014, Journal of medicinal chemistry.

Characterization of Anti-Neovascularization Activity and Ocular Pharmacokinetics of PI3K/mTOR Inhibitor GNE-947

C. Hop, S. Shahidi-Latham, J. Nonomiya, 2020 .