C. Lesburg

发表

Crystal structure of pentalenene synthase: mechanistic insights on terpenoid cyclization reactions in biology.

D. Cane, D. Christianson, C. Lesburg, 1997, Science.

Evaluation of in vitro PXR-based assays and in silico modeling approaches for understanding the binding of a structurally diverse set of drugs to PXR.

Li Xiao, Michael R. Ziebell, Charles A. Lesburg, 2011, Biochemical pharmacology.

Construction and characterization of a fully active PXR/SRC-1 tethered protein with increased stability.

V. Madison, K. Cheng, C. Lesburg, 2008, Protein engineering, design & selection : PEDS.

I. Novel HCV NS5B polymerase inhibitors: discovery of indole 2-carboxylic acids with C3-heterocycles.

B. Feld, R. Palermo, J. Duca, 2011, Bioorganic & medicinal chemistry letters.

Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants.

B. Hawes, Zhuyan Guo, W. Geissler, 2020, Bioorganic & medicinal chemistry letters.

Structure-activity relationship (SAR) development and discovery of potent indole-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase.

B. Feld, J. Duca, F. G. Njoroge, 2012, Journal of medicinal chemistry.

A novel class of highly potent irreversible hepatitis C virus NS5B polymerase inhibitors.

B. Feld, J. Duca, F. G. Njoroge, 2012, Journal of medicinal chemistry.

Histidine --> carboxamide ligand substitutions in the zinc binding site of carbonic anhydrase II alter metal coordination geometry but retain catalytic activity.

C. Fierke, D. Christianson, C. Lesburg, 1997, Biochemistry.

X-Ray Crystallographic Studies of Engineered Hydrogen Bond Networks in a Protein-Zinc Binding Site

D. Christianson, C. Lesburg, 1995 .

Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds.

X. Fradera, Haiyan Xu, M. Bittinger, 2021, ACS medicinal chemistry letters.

Projected Dose Optimization of Amino- and Hydroxypyrrolidine Purine PI3Kδ Immunomodulators.

M. Altman, X. Fradera, Hongshi Yu, 2021, Journal of medicinal chemistry.

Optimization of Versatile Oxindoles as Selective PI3Kδ Inhibitors.

M. Augustin, X. Fradera, Karin M. Otte, 2020, ACS medicinal chemistry letters.

Structure Overhaul Affords a Potent Purine PI3Kδ Inhibitor with Improved Tolerability.

T. Fischmann, M. Altman, X. Fradera, 2019, Journal of medicinal chemistry.

Oxetane Promise Delivered: Discovery of Long-Acting IDO1 Inhibitors Suitable for Q3W Oral or Parenteral Dosing.

Theodore A. Martinot, Yongxin Han, N. Solban, 2022, Journal of medicinal chemistry.

Development of a New Structural Class of Broadly Acting HCV Non‐Nucleoside Inhibitors Leading to the Discovery of MK‐8876

A. Palani, M. Holloway, N. Liverton, 2017, ChemMedChem.

Discovery of SCH 900188: A Potent Hepatitis C Virus NS5B Polymerase Inhibitor Prodrug As a Development Candidate.

F. G. Njoroge, K. Cheng, S. Agrawal, 2014, ACS medicinal chemistry letters.

Discovery and Optimization of Rationally Designed Bicyclic Inhibitors of Human Arginase to Enhance Cancer Immunotherapy.

Theodore A. Martinot, J. O'neil, J. Cumming, 2020, ACS medicinal chemistry letters.

Optimization of potency and pharmacokinetics of tricyclic indole derived inhibitors of HCV NS5B polymerase. Identification of ester prodrugs with improved oral pharmacokinetics.

J. Duca, F. G. Njoroge, S. Agrawal, 2014, Bioorganic & medicinal chemistry.

Synthesis of new 4,5-dihydrofuranoindoles and their evaluation as HCV NS5B polymerase inhibitors.

José Duca, J. Duca, F. G. Njoroge, 2012, Organic letters.

Strategic Incorporation of Polarity in Heme-Displacing Inhibitors of Indoleamine-2,3-dioxygenase-1 (IDO1).

Patrick J. Curran, Mee Ra Heo, M. Augustin, 2020, ACS medicinal chemistry letters.

Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.

Theodore A. Martinot, Michael J. Ardolino, Xiao Wang, 2019, ACS medicinal chemistry letters.

Discovery of an irreversible HCV NS5B polymerase inhibitor.

J. Gesell, J. Duca, F. G. Njoroge, 2013, Bioorganic & medicinal chemistry letters.

Discovery of 5-Amino-N-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Inhibitors of IRAK4.

T. Fischmann, M. Altman, Ruojing Yang, 2015, ACS medicinal chemistry letters.

Crystallization of an apo form of human arginase: using all the tools in the toolbox simultaneously.

J. Newman, T. Peat, C. Strickland, 2011, Acta crystallographica. Section F, Structural biology and crystallization communications.

Effects of genotypic variations on hepatitis C virus nonstructural protein 5B structure and activity

Z. Hong, W. Zhong, C. Lesburg, 2003 .

Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.

Andrew M Haidle, Matthew L. Maddess, J. Cumming, 2022, Journal of medicinal chemistry.

A kinase-cGAS cascade to synthesize a therapeutic STING activator

Steven P. Miller, Paul N. Devine, Matthew L. Maddess, 2022, Nature.

Crystal structure of the RNA-dependent RNA polymerase from hepatitis C virus reveals a fully encircled active site

Charles A. Lesburg, P. Weber, Z. Hong, 1999, Nature Structural Biology.

Template/Primer Requirements and Single Nucleotide Incorporation by Hepatitis C Virus Nonstructural Protein 5B Polymerase

C. Cameron, Z. Hong, W. Zhong, 2000, Journal of Virology.

Comprehensive Strategies to Bicyclic Prolines: Applications in the Synthesis of Potent Arginase Inhibitors.

Theodore A. Martinot, J. Cumming, A. Palani, 2021, ACS medicinal chemistry letters.

Inhibitors of hepatitis C virus polymerase: synthesis and characterization of novel 2-oxy-6-fluoro-N-((S)-1-hydroxy-3-phenylpropan-2-yl)-benzamides.

Sony Agrawal, Charles A. Lesburg, Gerald W. Shipps, 2010, Bioorganic & medicinal chemistry letters.

Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.

M. Augustin, X. Fradera, A. Bass, 2019, Bioorganic & medicinal chemistry letters.

An orally available non-nucleotide STING agonist with antitumor activity

Andrew M Haidle, J. Cumming, I. Kariv, 2020, Science.

Carbamate and N-Pyrimidine Mitigate Amide Hydrolysis: Structure-Based Drug Design of Tetrahydroquinoline IDO1 Inhibitors.

Patrick J. Curran, Theodore A. Martinot, Yongxin Han, 2021, ACS medicinal chemistry letters.

Augmenting Hit Identification by Virtual Screening Techniques in Small Molecule Drug Discovery

Xin Cindy Yan, John Sanders, Ying Duo Gao, 2020, J. Chem. Inf. Model..

Crystallization and preliminary X‐ray diffraction analysis of recombinant pentalenene synthase

M. D. Lloyd, D. Cane, D. Christianson, 1995, Protein science : a publication of the Protein Society.

Design of selective PI3Kδ inhibitors using an iterative scaffold-hopping workflow.

M. Augustin, M. Altman, X. Fradera, 2019, Bioorganic & medicinal chemistry letters.

Structure Overhaul Affords a Potent Purine PI3K delta Inhibitor with Improved Tolerability.

T. Fischmann, X. Fradera, T. Guzi, 2019 .

Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors.

Yongxin Han, N. Solban, X. Fradera, 2020, ACS medicinal chemistry letters.

Discovery of novel tricyclic indole derived inhibitors of HCV NS5B RNA dependent RNA polymerase.

J. Duca, F. G. Njoroge, S. Agrawal, 2013, Bioorganic & medicinal chemistry.

Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors.

Michael J. Ardolino, Karin M. Otte, M. Kennedy, 2021, Journal of medicinal chemistry.

Managing and manipulating carbocations in biology: terpenoid cyclase structure and mechanism.

D. Christianson, J. Caruthers, C. Lesburg, 1998, Current opinion in structural biology.

The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.

Duan Liu, J. Klappenbach, X. Fradera, 2017, Journal of medicinal chemistry.

Discovery of a new series of PI3K-δ inhibitors from Virtual Screening.

M. Augustin, M. Altman, X. Fradera, 2021, Bioorganic & medicinal chemistry letters.

Discovery of a Novel cGAMP Competitive Ligand of the Inactive Form of STING.

M. Altman, H. Hatch, B. Pan, 2018, ACS medicinal chemistry letters.

Discovery and Optimization of Potent, Selective, and Brain-Penetrant 1-Heteroaryl-1H-Indazole LRRK2 Kinase Inhibitors for the Treatment of Parkinson's Disease.

Theodore A. Martinot, Michael J. Ardolino, Matthew L. Maddess, 2022, Journal of medicinal chemistry.

Reversal of the hydrogen bond to zinc ligand histidine-119 dramatically diminishes catalysis and enhances metal equilibration kinetics in carbonic anhydrase II.

C. Fierke, D. Christianson, C. Lesburg, 1996, Biochemistry.

Identification of Potent Reverse Indazole Inhibitors for HPK1.

X. Fradera, Haiyan Xu, M. Bittinger, 2021, ACS medicinal chemistry letters.

Active-site engineering of carbonic anhydrase and its application to biosensors.

C. Fierke, D. Christianson, R. Thompson, 2000, EXS.

Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation.

Duan Liu, T. Fischmann, M. Altman, 2017, Bioorganic & medicinal chemistry letters.

XGen: Real-Space Fitting of Complex Ligand Conformational Ensembles to X-Ray Electron Density Maps.

Ajay N. Jain, A. Cleves, M. Reibarkh, 2020, Journal of medicinal chemistry.

Thermodynamics of nucleotide and inhibitor binding to wild-type and ispinesib-resistant forms of human kinesin spindle protein.

A. Basso, J. Duca, P. Sheth, 2009, Biochemistry.

Conformational Strain of Macrocyclic Peptides in Ligand-Receptor Complexes Based on Advanced Refinement of Bound-State Conformers.

Ajay N. Jain, J. Alvarez, A. Cleves, 2021, Journal of Medicinal Chemistry.

Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation.

Duan Liu, T. Fischmann, M. Altman, 2017, Bioorganic & medicinal chemistry letters.