S. Staben

发表

Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα).

C. Li, R. Rowntree, BinQing Wei, 2019, Bioorganic & medicinal chemistry letters.

Heterobifunctional molecules induce dephosphorylation of kinases - a proof of concept study.

Kui Lin, W. Fairbrother, Jie Lin, 2019, Journal of medicinal chemistry.

A Multifaceted Hit-Finding Approach Reveals Novel LC3 Family Ligands.

Melinda M. Mulvihill, D. Stoffler, M. Holliday, 2022, Biochemistry.

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.

Isoform Selective PI3K Inhibitors for Treating Cancer

S. Staben, 2017 .

Heterobifunctional Molecules Induce Dephosphorylation of Kinases - a Proof of Concept Study

Kui Lin, W. Fairbrother, Jie Lin, 2019 .

MCC950/CRID3 potently targets the NACHT domain of wild-type NLRP3 but not disease-associated mutants for inflammasome inhibition

J. Konvalinka, M. Lamkanfi, Victoria C. Pham, 2019, PLoS biology.

MCC950/CRID3 potently targets the NACHT domain of wild-type NLRP3 but not disease-associated mutants for inflammasome inhibition

J. Konvalinka, M. Lamkanfi, Victoria C. Pham, 2019, bioRxiv.

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.

Overcoming Preclinical Safety Obstacles to Discover (S)-N-((1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor.

Matthew S. Johnson, M. Ultsch, J. Veal, 2022, Journal of medicinal chemistry.

A General Strategy for the Construction of Functionalized Azaindolines via Domino Palladium-Catalyzed Heck Cyclization/Suzuki Coupling.

S. Staben, C. Stivala, Blake E. Daniels, 2017, Organic letters.

Gold(I)-catalyzed cyclizations of silyl enol ethers: application to the synthesis of (+)-lycopladine A.

F. Toste, S. Staben, B. Corkey, 2006, Angewandte Chemie.

Gold(I)-catalyzed stereoselective olefin cyclopropanation.

Magnus J. Johansson, F. Toste, David J Gorin, 2005, Journal of the American Chemical Society.

Gold(I)-catalyzed ring expansion of cyclopropanols and cyclobutanols.

F. Toste, S. Staben, Jordan P. Markham, 2005, Journal of the American Chemical Society.

Gold(I)-catalyzed 5-endo-dig carbocyclization of acetylenic dicarbonyl compounds.

F. Toste, S. Staben, J. Kennedy‐Smith, 2004, Angewandte Chemie.

Gold(I)-Catalyzed Conia-Ene Reaction of β-Ketoesters with Alkynes

F. Toste, S. Staben, J. Kennedy‐Smith, 2004 .

Design and Evaluation of Highly-Selective Human Immunoproteasome Inhibitors Reveals a Compensatory Process that Preserves Immune Cell Viability.

S. Steinbacher, M. Augustin, Celine Eidenschenk, 2019, Journal of medicinal chemistry.

Heteroarylation of azine N-oxides.

F. Gosselin, N. Blaquière, S. Staben, 2012, Organic letters.

Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K).

Adam R. Johnson, Jianwen A. Feng, Brandon J. Bravo, 2017, Journal of medicinal chemistry.

Enantioselective Synthesis of γ-Hydroxyenones by Chiral Base-Catalyzed Kornblum DeLaMare Rearrangement

F. Toste, S. Staben, Xin Linghu, 2006 .

Four-component synthesis of fully substituted 1,2,4-triazoles.

N. Blaquière, S. Staben, 2010, Angewandte Chemie.

Rapid synthesis of 1,3,5-substituted 1,2,4-triazoles from carboxylic acids, amidines, and hydrazines.

G. Castanedo, S. Trapp, N. Blaquière, 2011, The Journal of organic chemistry.

Au(I)-catalyzed ring expanding cycloisomerizations: total synthesis of ventricosene.

N. Shapiro, F. Toste, S. Staben, 2008, Organic 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.

Rapid Synthesis of 1,3,5‐Substituted 1,2,4‐Triazoles from Carboxylic Acids, Amidines, and Hydrazines.

G. Castanedo, S. Trapp, N. Blaquière, 2011 .

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.

Synthesis of aromatic bisabolene natural products via palladium-catalyzed cross-couplings of organozinc reagents.

James R. Vyvyan, R. Looper, S. Staben, 2004, The Journal of organic 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.

Cancer II

N. Gray, N. Stiefl, M. Waring, 2018 .

Selective activation of PFKL suppresses the phagocytic oxidative burst

M. Bogyo, V. Dixit, J. Kollman, 2021, Cell.

Identifying transcriptional programs underlying cancer drug response with TraCe-seq

Z. Modrušan, Matthew T. Chang, S. Malek, 2021, Nature Biotechnology.

The crystal structure of the catalytic domain of the NF-κB inducing kinase reveals a narrow but flexible active site.

Adam R. Johnson, Jianwen A. Feng, Lawren C. Wu, 2012, Structure.

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.

Siew K. Yeap, M. Ultsch, C. Eigenbrot, 2022, Journal of medicinal chemistry.

RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy

W. Forrest, Kyung Song, L. Friedman, 2021, bioRxiv.

NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus

Adam R. Johnson, Z. Modrušan, J. DeVoss, 2018, Nature Communications.

NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus

Adam R. Johnson, Z. Modrušan, J. DeVoss, 2018, Nature Communications.

Ternary complex dissociation kinetics contribute to mutant-selective EGFR degradation.

Ivana Yen, S. Malek, F. Shanahan, 2023, Cell chemical biology.

Monomeric targeted protein degraders.

Jun Liang, R. Blake, N. Blaquière, 2020, Journal of medicinal chemistry.

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.

Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.

Jianwen A. Feng, M. Belvin, K. Hoeflich, 2014, Journal of medicinal chemistry.

Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase.

Jianwen A. Feng, P. McEwan, Lawren C. Wu, 2018, Journal of medicinal chemistry.

Enantioselective Synthesis of γ‐Hydroxyenones by Chiral Base‐Catalyzed Kornblum DeLaMare Rearrangement.

F. Toste, S. Staben, Xin Linghu, 2007 .

Filling a nick in NIK: extending the half-life of a NIK inhibitor through structure-based drug design.

Matthew L Landry, P. McEwan, Adam Johnson, 2023, Bioorganic & medicinal chemistry letters.

Identifying transcriptional programs underlying cancer drug response with TraCe-seq

Z. Modrušan, Matthew T. Chang, S. Malek, 2021, Nature Biotechnology.

Medicinal chemistry of inhibiting RING-type E3 ubiquitin ligases.

Elisia Villemure, N. Blaquière, S. Staben, 2020, Journal of medicinal chemistry.

Abstract 156: Preclinical characterization of GDC-0077, a specific PI3K alpha inhibitor in early clinical development

M. Belvin, Kyung Song, L. Friedman, 2017 .

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties.

Melinda M. Mulvihill, Karen E Gascoigne, R. Rowntree, 2021, Journal of medicinal chemistry.

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

A. K. Forrest, BinQing Wei, M. Ultsch, 2017, ACS 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.

Structure-Based Design of Potent, Selective, and Orally Bioavailable VPS34 Kinase Inhibitors.

John G. Moffat, L. Salphati, Huifen Chen, 2021, Journal of medicinal chemistry.

Structure Based Design of Potent Selective Inhibitors of Protein Kinase D1 (PKD1).

Jianwen A. Feng, P. McEwan, R. Godemann, 2019, ACS medicinal chemistry letters.

Primary Amine Tethered Small Molecules Promote the Degradation of X-Linked Inhibitor of Apoptosis Protein.

Melinda M. Mulvihill, I. Wertz, W. Fairbrother, 2021, Journal of the American Chemical Society.

Targeted degradation via direct 26S proteasome recruitment

C. Ciferri, N. Popovych, I. Wertz, 2022, Nature Chemical Biology.

From Discovery to Market Readiness: The Research and Development of the β-Sparing Phosphatidylinositol 3-Kinase Inhibitor Taselisib

A. Schuster, S. Staben, R. Angelaud, 2019, ACS Symposium Series.

Abstract DDT02-01: Discovery of GDC-0077, a highly isoform selective inhibitor of PI3Kα that promotes selective loss of mutant-p110α

S. Staben, 2017 .