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James Inglese

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Derek S Welsbie; Tian Xue; Zhiyong Yang; King-Wai Yau; Xinrong Zhou; Douglas Auld; CYNTHIA BERLINICKE; Richard Blouin; Sanford L Boye; Li-hui Cao; Chung-ha O Davis; Aaron DiAntonio; Raymond A Enke; Jie Fu; John Fuller; Yan Ge; Lucie Germain; Laszlo Hackler; Bing Han; Justin Hanes; William W Hauswirth; Syu-ichi Hirai; James Inglese; Nicholas Marsh-Armstrong; Scott E Martin; Shannath L Merbs; Katherine L Mitchell; Judy V Nguyen; Robert W Nickells; Harry A Quigley; Caroline Simard-Bisson; Donald J Zack
Functional genomic screening identifies dual leucine zipper kinase as a key mediator of retinal ganglion cell death.
Patricia Dranchak; David H Drewry; Rajarshi Guha; Ryan MacArthur; William J Zuercher; Douglas S Auld; James Inglese
Profile of the GSK published protein kinase inhibitor set across ATP-dependent and-independent luciferases: implications for reporter-gene assays.
Ken C-C Cheng; James Inglese
A coincidence reporter-gene system for high-throughput screening.

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2013: Derek S Welsbie; Tian Xue; Zhiyong Yang; King-Wai Yau; Xinrong Zhou; Douglas Auld; CYNTHIA BERLINICKE; Richard Blouin; Sanford L Boye; Li-hui Cao; Chung-ha O Davis; Aaron DiAntonio; Raymond A Enke; Jie Fu; John Fuller; Yan Ge; Lucie Germain; Laszlo Hackler; Bing Han; Justin Hanes; William W Hauswirth; Syu-ichi Hirai; James Inglese; Nicholas Marsh-Armstrong; Scott E Martin; Shannath L Merbs; Katherine L Mitchell; Judy V Nguyen; Robert W Nickells; Harry A Quigley; Caroline Simard-Bisson; Donald J Zack
Functional genomic screening identifies dual leucine zipper kinase as a key mediator of retinal ganglion cell death.
Proceedings of the National Academy of Sciences of the United States of America 2013;110(10):4045-50.
2013: Patricia Dranchak; David H Drewry; Rajarshi Guha; Ryan MacArthur; William J Zuercher; Douglas S Auld; James Inglese
Profile of the GSK published protein kinase inhibitor set across ATP-dependent and-independent luciferases: implications for reporter-gene assays.
PloS one 2013;8(3):e57888.
2012: Ken C-C Cheng; James Inglese
A coincidence reporter-gene system for high-throughput screening.
Nature methods 2012;9(10):937.
2012: Dimitrios Anastasiou; John M Asara; Douglas S Auld; Christopher P Austin; Matthew B Boxer; Kyle R Brimacombe; Lewis C Cantley; Heather R Christofk; Kevin D Courtney; Lenny Dang; Shawn M Davidson; Svetoslav Dimov; Brian P Fiske; Marian H Harris; Bum Soo Hong; James Inglese; William J Israelsen; Abhishek Jha; Jian-Kang Jiang; Shengfang Jin; Zachary R Johnson; Tahsin M Khan; Charles Kung; Kaiko Kunii; William Leister; Sophia Y Lunt; Scott Malstrom; Katherine R Mattaini; Christian M Metallo; Hee-Won Park; Francesco G Salituro; Min Shen; Amanda P Skoumbourdis; Noel Southall; Gregory Stephanopoulos; Wolfram Tempel; Craig J Thomas; Henrike Veith; Martin J Walsh; Hua Yang; Katharine E Yen; Yimin Yu; Matthew G Vander Heiden
Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.
Nature chemical biology 2012;8(10):839-47.
2012: Natasha Thorne; Douglas S Auld; Wendy A Lea; Scott Lovell; Min Shen; Anton Simeonov; James Inglese
Firefly luciferase in chemical biology: a compendium of inhibitors, mechanistic evaluation of chemotypes, and suggested use as a reporter.
Chemistry & biology 2012;19(8):1060-72.
2012: Sung-Wook Jang; Camila Lopez-Anido; Ryan MacArthur; John Svaren; James Inglese
Identification of drug modulators targeting gene-dosage disease CMT1A.
ACS chemical biology 2012;7(7):1205-13.
2011: Patricia G Cruz; James Inglese; Scott Lovell; Ryan MacArthur; Pamela J Schultz; Min Shen; Douglas S Auld; Kevin P Battaile; Giselle Tamayo; David H Sherman
Titration-based screening for evaluation of natural product extracts: identification of an aspulvinone family of luciferase inhibitors.
Chemistry & biology 2011;18(11):1442-52.
2011: Junjun Chen; Thomas S Dexheimer; James Inglese; Ajit Jadhav; Qin Liang; David J Maloney; Anton Simeonov; Mark A Villamil; Yongxing Ai; Zhihao Zhuang
Selective and cell-active inhibitors of the USP1/ UAF1 deubiquitinase complex reverse cisplatin resistance in non-small cell lung cancer cells.
Chemistry & biology 2011;18(11):1390-400.
2011: James Inglese; Samuel A Hasson
Biology-driven library design for probe discovery.
Chemistry & biology 2011;18(10):1204-5.
2011: Wenwei Huang; James Inglese; Srilatha Sakamuru; Matias S Attene-Ramos; Christopher P Austin; Erika E Englund; Ruili Huang; Menghang Xia
Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitors.
Bioorganic & medicinal chemistry letters 2011;21(18):5239-43.
2011: Jing Yuan; Thomas E Wellems; Christopher P Austin; Ken Chih-Chien Cheng; Fidock David; Rajarshi Guha; Ruili Huang; James Inglese; Ronald L Johnson; Anna Liu; Sittiporn Pattaradilokrat; Xin-zhuan Su
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
Science (New York, N.Y.) 2011;333(6043):724-9.
2011: Ronald L Johnson; Jennifer Wichterman; Jong Yeon Hwang; James Inglese; Leggy Arnold; Indre Augustinaite; Christopher P Austin; R Kiplin Guy; Ruili Huang; Wenwei Huang
A quantitative high-throughput screen identifies novel inhibitors of the interaction of thyroid receptor beta with a peptide of steroid receptor coactivator 2.
Journal of biomolecular screening 2011;16(6):618-27.
2011: Lauren E Brown; Ken Chih-Chien Cheng; Wan-Guo Wei; Pingwei Yuan; Peng Dai; Richard Trilles; Feng Ni; Jing Yuan; Ryan MacArthur; Rajarshi Guha; Ronald L Johnson; Xin-zhuan Su; Melissa M Dominguez; John K Snyder; Aaron B Beeler; Scott E Schaus; James Inglese; John A Porco
Discovery of new antimalarial chemotypes through chemical methodology and library development.
Proceedings of the National Academy of Sciences of the United States of America 2011;108(17):6775-80.
2011: Jong Yeon Hwang; Wenwei Huang; Leggy Arnold; Ruili Huang; Ramy R Attia; Michele Connelly; Jennifer Wichterman; Fangyi Zhu; Indre Augustinaite; Christopher P Austin; James Inglese; Ronald L Johnson; R Kiplin Guy
Methylsulfonylnitrobenzoates, a new class of irreversible inhibitors of the interaction of the thyroid hormone receptor and its obligate coactivators that functionally antagonizes thyroid hormone.
The Journal of biological chemistry 2011;286(14):11895-908.
2010: James Inglese; Andrew Napper; Douglas Auld
Improving success by balanced critical evaluations of assay methods.
Assay and drug development technologies 2010;8(4):1.
2010: Natasha Thorne; James Inglese; Douglas S Auld
Illuminating insights into firefly luciferase and other bioluminescent reporters used in chemical biology.
Chemistry & biology 2010;17(6):646-57.
2010: Jian-kang Jiang; Matthew B Boxer; Matthew G Vander Heiden; Min Shen; Amanda P Skoumbourdis; Noel Southall; Henrike Veith; William Leister; Christopher P Austin; Hee Won Park; James Inglese; Lewis C Cantley; Douglas S Auld; Craig J Thomas
Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Bioorganic & medicinal chemistry letters 2010;20(11):3387-93.
2010: Natasha Thorne; Douglas S Auld; James Inglese
Apparent activity in high-throughput screening: origins of compound-dependent assay interference.
Current opinion in chemical biology 2010;14(3):315-24.
2010: Ke Liu; Noel Southall; Steve A Titus; James Inglese; Robert L Eskay; Paul Shinn; Christopher P Austin; Markus A Heilig; Wei Zheng
A multiplex calcium assay for identification of GPCR agonists and antagonists.
Assay and drug development technologies 2010;8(3):367-79.
2010: Sharon Terry; Christopher Austin; James Inglese; David Meeker; Patrick Terry
Assay, preclinical, and clinical brick walls and opportunities for system change through GRANDRx.
Assay and drug development technologies 2010;8(2):128-34.
2010: Adam Yasgar; John Shultz; Wenhui Zhou; Hui Wang; Fen Huang; Nancy Murphy; Erika L Abel; John DiGiovanni; James Inglese; Anton Simeonov
A high-throughput 1,536-well luminescence assay for glutathione S-transferase activity.
Assay and drug development technologies 2010;8(2):200-11.
2010: Douglas S Auld; Scott Lovell; Natasha Thorne; Wendy A Lea; David J Maloney; Min Shen; Ganesha Rai; Kevin P Battaile; Craig J Thomas; Anton Simeonov; Robert P Hanzlik; James Inglese
Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124.
Proceedings of the National Academy of Sciences of the United States of America 2010;107(11):4878-83.
2010: Matthew B Boxer; Jian-kang Jiang; Matthew G Vander Heiden; Min Shen; Amanda P Skoumbourdis; Noel Southall; Henrike Veith; William Leister; Christopher P Austin; Hee Won Park; James Inglese; Lewis C Cantley; Douglas S Auld; Craig J Thomas
Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Journal of medicinal chemistry 2010;53(3):1048-55.
2010: Adam Yasgar; Timothy L Foley; Ajit Jadhav; James Inglese; Michael D Burkart; Anton Simeonov
A strategy to discover inhibitors of Bacillus subtilis surfactin-type phosphopantetheinyl transferase.
Molecular bioSystems 2010;6(2):365-75.
2010: Bryan T Mott; Rafaela S Ferreira; Anton Simeonov; Ajit Jadhav; Kenny Kean-Hooi Ang; William Leister; Min Shen; Julia T Silveira; Patricia S Doyle; Michelle R Arkin; James H McKerrow; James Inglese; Christopher P Austin; Craig J Thomas; Brian Shoichet; David J Maloney
Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB.
Journal of medicinal chemistry 2010;53(1):52-60.
2010: Ajit Jadhav; Rafaela S Ferreira; Carleen Klumpp; Bryan T Mott; Christopher P Austin; James Inglese; Craig J Thomas; David J Maloney; Brian Shoichet; Anton Simeonov
Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease.
Journal of medicinal chemistry 2010;53(1):37-51.
2009: Cordelle Tanega; Min Shen; Bryan T Mott; Craig J Thomas; Ryan MacArthur; James Inglese; Douglas S Auld
Comparison of bioluminescent kinase assays using substrate depletion and product formation.
Assay and drug development technologies 2009;7(6):606-14.
2009: Bryan T Mott; Cordelle Tanega; Min Shen; David J Maloney; Paul Shinn; William Leister; Juan J Marugan; James Inglese; Christopher P Austin; Tom Misteli; Douglas S Auld; Craig J Thomas
Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk).
Bioorganic & medicinal chemistry letters 2009;19(23):6700-5.
2009: Ruili Huang; Noel Southall; Menghang Xia; Ming-Hsuang Cho; Ajit Jadhav; Dac-Trung Nguyen; James Inglese; Raymond R Tice; Christopher P Austin
Weighted feature significance: a simple, interpretable model of compound toxicity based on the statistical enrichment of structural features.
Toxicological sciences : an official journal of the Society of Toxicology 2009;112(2):385-93.
2009: Henrike Veith; Noel Southall; Ruili Huang; Tim James; Darren Fayne; Natalia Artemenko; Min Shen; James Inglese; Christopher P Austin; David Lloyd; Douglas S Auld
Comprehensive characterization of cytochrome P450 isozyme selectivity across chemical libraries.
Nature biotechnology 2009;27(11):1050-5.
2009: Menghang Xia; Ruili Huang; Yi Sun; Gregg L Semenza; Shelley Force Aldred; Kristine L Witt; James Inglese; Raymond R Tice; Christopher P Austin
Identification of chemical compounds that induce HIF-1alpha activity.
Toxicological sciences : an official journal of the Society of Toxicology 2009;112(1):153-63.
2009: Ganesha Rai; Ahmed A Sayed; Wendy A Lea; Hans F Luecke; Harinath Chakrapani; Stefanie Prast-Nielsen; Ajit Jadhav; William Leister; Min Shen; James Inglese; Christopher P Austin; Larry Keefer; Elias Arnér; Anton Simeonov; David J Maloney; David L Williams; Craig J Thomas
Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis.
Journal of medicinal chemistry 2009;52(20):6474-83.
2009: Jing Yuan; Ronald L Johnson; Ruili Huang; Jennifer Wichterman; Hongying Jiang; Karen Hayton; Fidock David; Thomas E Wellems; James Inglese; Christopher P Austin; Xin-zhuan Su
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
Nature chemical biology 2009;5(10):765-71.
2009: Ronald L Johnson; Ruili Huang; Ajit Jadhav; Noel Southall; Jennifer Wichterman; Ryan MacArthur; Menghang Xia; Kun Bi; John Printen; Christopher P Austin; James Inglese
A quantitative high-throughput screen for modulators of IL-6 signaling: a model for interrogating biological networks using chemical libraries.
Molecular bioSystems 2009;5(9):1039-50.
2009: Alex Crowe; Wenwei Huang; Carlo Ballatore; Ronald L Johnson; Anne-Marie L Hogan; Ruili Huang; Jennifer Wichterman; Joshua McCoy; Donna Huryn; Douglas S Auld; Amos B Smith; James Inglese; John Q Trojanowski; Christopher P Austin; Kurt R Brunden; Virginia M-Y Lee
Identification of aminothienopyridazine inhibitors of tau assembly by quantitative high-throughput screening.
Biochemistry 2009;48(32):7732-45.
2009: Susanne Neumann; Wenwei Huang; Steve Titus; Gerd Krause; Gunnar Kleinau; Anna Teresa Alberobello; Wei Zheng; Noel Southall; James Inglese; Christopher P Austin; Francesco S Celi; Oksana Gavrilova; Craig J Thomas; Bruce M Raaka; Marvin C Gershengorn
Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice.
Proceedings of the National Academy of Sciences of the United States of America 2009;106(30):12471-6.
2009: Ping Jun Zhu; John P Hobson; Noel Southall; Cunping Qiu; Craig J Thomas; Jiamo Lu; James Inglese; Wei Zheng; Stephen H Leppla; Thomas H Bugge; Christopher P Austin; Shihui Liu
Quantitative high-throughput screening identifies inhibitors of anthrax-induced cell death.
Bioorganic & medicinal chemistry 2009;17(14):5139-45.
2009: Amanda P Skoumbourdis; Christopher A Leclair; Eduard Stefan; Adrian G Turjanski; William Maguire; Steven A Titus; Ruili Huang; Douglas S Auld; James Inglese; Christopher P Austin; Stephen W Michnick; Menghang Xia; Craig J Thomas
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
Bioorganic & medicinal chemistry letters 2009;19(13):3686-92.
2009: Kyle R Brimacombe; Matthew D Hall; Douglas S Auld; James Inglese; Christopher P Austin; Michael M Gottesman; King-Leung Fung
A dual-fluorescence high-throughput cell line system for probing multidrug resistance.
Assay and drug development technologies 2009;7(3):233-49.
2009: Ryan MacArthur; William Leister; Henrike Veith; Paul Shinn; Noel Southall; Christopher P Austin; James Inglese; Douglas S Auld
Monitoring compound integrity with cytochrome P450 assays and qHTS.
Journal of biomolecular screening 2009;14(5):538-46.
2009: Sunita J Shukla; Dac-Trung Nguyen; Ryan Macarthur; Anton Simeonov; William J Frazee; Tina M Hallis; Bryan D Marks; Upinder Singh; Hildegard C Eliason; John Printen; Christopher P Austin; James Inglese; Douglas S Auld
Identification of pregnane X receptor ligands using time-resolved fluorescence resonance energy transfer and quantitative high-throughput screening.
Assay and drug development technologies 2009;7(2):143-69.
2009: Douglas S Auld; Ya-Qin Zhang; Noel Southall; Ganesha Rai; Marc Landsman; Jennifer MacLure; Daniel Langevin; Craig J Thomas; Christopher P Austin; James Inglese
A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution.
Journal of medicinal chemistry 2009;52(5):1450-8.
2009: Douglas S Auld; Natasha Thorne; William F Maguire; James Inglese
Mechanism of PTC124 activity in cell-based luciferase assays of nonsense codon suppression.
Proceedings of the National Academy of Sciences of the United States of America 2009;106(9):3585-90.
2009: Fang Yi; Pingjun Zhu; Noel Southall; James Inglese; Christopher P Austin; Wei Zheng; Lynne Regan
An AlphaScreen-based high-throughput screen to identify inhibitors of Hsp90-cochaperone interaction.
Journal of biomolecular screening 2009;14(3):273-81.
2009: Menghang Xia; Ruili Huang; Vicky Guo; Noel Southall; Ming-Hsuang Cho; James Inglese; Christopher P Austin; Marshall Nirenberg
Identification of compounds that potentiate CREB signaling as possible enhancers of long-term memory.
Proceedings of the National Academy of Sciences of the United States of America 2009;106(7):2412-7.
2009: Menghang Xia; Kun Bi; Ruili Huang; Ming-Hsuang Cho; Srilatha Sakamuru; Susanne C Miller; Hua Li; Yi Sun; John Printen; Christopher P Austin; James Inglese
Identification of small molecule compounds that inhibit the HIF-1 signaling pathway.
Molecular cancer 2009;8():117.
2009: Craig J Thomas; Douglas S Auld; Ruili Huang; Wenwei Huang; Ajit Jadhav; Ronald L Johnson; William Leister; David J Maloney; Juan J Marugan; Sam Michael; Anton Simeonov; Noel Southall; Menghang Xia; Wei Zheng; James Inglese; Christopher P Austin
The pilot phase of the NIH Chemical Genomics Center.
Current topics in medicinal chemistry 2009;9(13):1181-93.
2009: Christophe Marchand; Wendy A Lea; Ajit Jadhav; Thomas S Dexheimer; Christopher P Austin; James Inglese; Yves Pommier; Anton Simeonov
Identification of phosphotyrosine mimetic inhibitors of human tyrosyl-DNA phosphodiesterase I by a novel AlphaScreen high-throughput assay.
Molecular cancer therapeutics 2009;8(1):240-8.
2008: Daniel J Urban; Wei Zheng; Ozlem Goker-Alpan; Ajit Jadhav; Mary E Lamarca; James Inglese; Ellen Sidransky; Christopher P Austin
Optimization and validation of two miniaturized glucocerebrosidase enzyme assays for high throughput screening.
Combinatorial chemistry & high throughput screening 2008;11(10):817-24.
2008: Sam Michael; Douglas S Auld; Carleen Klumpp; Ajit Jadhav; Wei Zheng; Natasha Thorne; Christopher P Austin; James Inglese; Anton Simeonov
A robotic platform for quantitative high-throughput screening.
Assay and drug development technologies 2008;6(5):637-57.
2008: Douglas S Auld; Natasha Thorne; Dac-Trung Nguyen; James Inglese
A specific mechanism for nonspecific activation in reporter-gene assays.
ACS chemical biology 2008;3(8):463-70.
2008: Ping Jun Zhu; Wei Zheng; Douglas S Auld; Ajit Jadhav; Ryan Macarthur; Keith R Olson; Kun Peng; Hyna Dotimas; Christopher P Austin; James Inglese
A miniaturized glucocorticoid receptor translocation assay using enzymatic fragment complementation evaluated with qHTS.
Combinatorial chemistry & high throughput screening 2008;11(7):545-59.
2008: Wendy A Lea; Ajit Jadhav; Ganesha Rai; Ahmed A Sayed; Cynthia L Cass; James Inglese; David L Williams; Christopher P Austin; Anton Simeonov
A 1,536-well-based kinetic HTS assay for inhibitors of Schistosoma mansoni thioredoxin glutathione reductase.
Assay and drug development technologies 2008;6(4):551-5.
2008: Steven A Titus; Xiao Li; Noel Southall; Jianming Lu; James Inglese; Michael Brasch; Christopher P Austin; Wei Zheng
A cell-based PDE4 assay in 1536-well plate format for high-throughput screening.
Journal of biomolecular screening 2008;13(7):609-18.
2008: Adam Jordan Kimple; Adam Yasgar; Mark Hughes; Ajit Jadhav; Francis S Willard; Robin E Muller; Christopher P Austin; James Inglese; Gordon C Ibeanu; David Siderovski; Anton Simeonov
A high throughput fluorescence polarization assay for inhibitors of the GoLoco motif/G-alpha interaction.
Combinatorial chemistry & high throughput screening 2008;11(5):396-409.
2008: Christine C Chung; Kenji Ohwaki; Jonathan E Schneeweis; Erica Stec; Jeffrey P Varnerin; Paul N Goudreau; Amy Chang; Jason Cassaday; Lihu Yang; Takeru Yamakawa; Oleg Kornienko; Peter Hodder; James Inglese; Marc Ferrer; Berta Strulovici; Jun Kusunoki; Michael R Tota; Toshimitsu Takagi
A fluorescence-based thiol quantification assay for ultra-high-throughput screening for inhibitors of coenzyme A production.
Assay and drug development technologies 2008;6(3):361-74.
2008: Ming-Hsuang Cho; Andrew Niles; Ruili Huang; James Inglese; Christopher P Austin; Terry Riss; Menghang Xia
A bioluminescent cytotoxicity assay for assessment of membrane integrity using a proteolytic biomarker.
Toxicology in vitro : an international journal published in association with BIBRA 2008;22(4):1099-106.
2008: Douglas S Auld; Noel Southall; Ajit Jadhav; Ronald L Johnson; David J Diller; Anton Simeonov; Christopher P Austin; James Inglese
Characterization of chemical libraries for luciferase inhibitory activity.
Journal of medicinal chemistry 2008;51(8):2372-86.
2008: Anton Simeonov; Ajit Jadhav; Craig J Thomas; Yuhong Wang; Ruili Huang; Noel Southall; Paul Shinn; Jeremy Smith; Christopher P Austin; Douglas S Auld; James Inglese
Fluorescence spectroscopic profiling of compound libraries.
Journal of medicinal chemistry 2008;51(8):2363-71.
2008: Kerim Babaoglu; Anton Simeonov; John J Irwin; Michael E Nelson; Brian Feng; Craig J Thomas; Laura Cancian; M Paola Costi; David A Maltby; Ajit Jadhav; James Inglese; Christopher P Austin; Brian Shoichet
Comprehensive mechanistic analysis of hits from high-throughput and docking screens against beta-lactamase.
Journal of medicinal chemistry 2008;51(8):2502-11.
2008: Ronald L Johnson; Wenwei Huang; Ajit Jadhav; Christopher P Austin; James Inglese; Elisabeth D Martinez
A quantitative high-throughput screen identifies potential epigenetic modulators of gene expression.
Analytical biochemistry 2008;375(2):237-48.
2008: Ahmed A Sayed; Anton Simeonov; Craig J Thomas; James Inglese; Christopher P Austin; David L Williams
Identification of oxadiazoles as new drug leads for the control of schistosomiasis.
Nature medicine 2008;14(4):407-12.
2008: Anton Simeonov; Adam Yasgar; Ajit Jadhav; G L Lokesh; Carleen Klumpp; Sam Michael; Christopher P Austin; Amarnath Natarajan; James Inglese
Dual-fluorophore quantitative high-throughput screen for inhibitors of BRCT-phosphoprotein interaction.
Analytical biochemistry 2008;375(1):60-70.
2008: Menghang Xia; Ruili Huang; Kristine L Witt; Noel Southall; Jennifer Fostel; Ming-Hsuang Cho; Ajit Jadhav; Cynthia S Smith; James Inglese; Christopher Portier; Raymond R Tice; Christopher P Austin
Compound cytotoxicity profiling using quantitative high-throughput screening.
Environmental health perspectives 2008;116(3):284-91.
2008: Ruili Huang; Noel Southall; Ming-Hsuang Cho; Menghang Xia; James Inglese; Christopher P Austin
Characterization of diversity in toxicity mechanism using in vitro cytotoxicity assays in quantitative high throughput screening.
Chemical research in toxicology 2008;21(3):659-67.
2008: Amanda P Skoumbourdis; Ruili Huang; Noel Southall; William Leister; Vicky Guo; Ming-Hsuang Cho; James Inglese; Marshall Nirenberg; Christopher P Austin; Menghang Xia; Craig J Thomas
Identification of a potent new chemotype for the selective inhibition of PDE4.
Bioorganic & medicinal chemistry letters 2008;18(4):1297-303.
2008: Steve Titus; Susanne Neumann; Wei Zheng; Noel Southall; Sam Michael; Carleen Klumpp; Adam Yasgar; Paul Shinn; Craig J Thomas; James Inglese; Marvin C Gershengorn; Christopher P Austin
Quantitative high-throughput screening using a live-cell cAMP assay identifies small-molecule agonists of the TSH receptor.
Journal of biomolecular screening 2008;13(2):120-7.
2008: Ke Liu; Steve Titus; Noel Southall; Pingjun Zhu; James Inglese; Christopher P Austin; Wei Zheng
Comparison on functional assays for Gq-coupled GPCRs by measuring inositol monophospate-1 and intracellular calcium in 1536-well plate format.
Current chemical genomics 2008;1():70-8.
2008: Anton Simeonov; Ajit Jadhav; Ahmed A Sayed; Yuhong Wang; Michael E Nelson; Craig J Thomas; James Inglese; David L Williams; Christopher P Austin
Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade.
PLoS neglected tropical diseases 2008;2(1):e127.
2008: Yuli Xie; ShiXian Deng; Craig J Thomas; Yidong Liu; Ya-Qin Zhang; Alison Rinderspacher; Wenwei Huang; Gangli Gong; Michael Wyler; Efithia Cayanis; Nathalie Aulner; Udo Többen; Caty Chung; Sergey Pampou; Noel Southall; Dusica Vidović; Stephen Schuerer; Lars Branden; R Eric Davis; Louis M Staudt; James Inglese; Christopher P Austin; Donald W Landry; Deborah H. Smith; Douglas S Auld
Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation.
Bioorganic & medicinal chemistry letters 2008;18(1):329-35.
2007: Anton Simeonov; Adam Yasgar; Carleen Klumpp; Wei Zheng; Naeem Shafqat; Udo Oppermann; Christopher P Austin; James Inglese
Evaluation of micro-parallel liquid chromatography as a method for HTS-coupled actives verification.
Assay and drug development technologies 2007;5(6):815-24.
2007: Nicolette S Honson; Ronald L Johnson; Wenwei Huang; James Inglese; Christopher P Austin; Jeffrey Kuret
Differentiating Alzheimer disease-associated aggregates with small molecules.
Neurobiology of disease 2007;28(3):251-60.
2007: Wenwei Huang; Wei Zheng; Daniel J Urban; James Inglese; Ellen Sidransky; Christopher P Austin; Craig J Thomas
N4-phenyl modifications of N2-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease.
Bioorganic & medicinal chemistry letters 2007;17(21):5783-9.
2007: Wei Zheng; Janak Padia; Daniel J Urban; Ajit Jadhav; Ozlem Goker-Alpan; Anton Simeonov; Ehud Goldin; Douglas S Auld; Mary E LaMarca; James Inglese; Christopher P Austin; Ellen Sidransky
Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease.
Proceedings of the National Academy of Sciences of the United States of America 2007;104(32):13192-7.
2007: James Inglese; Ronald L Johnson; Anton Simeonov; Menghang Xia; Wei Zheng; Christopher P Austin; Douglas S Auld
High-throughput screening assays for the identification of chemical probes.
Nature chemical biology 2007;3(8):466-79.
2007: James Inglese; Caroline E Shamu; R Kiplin Guy
Reporting data from high-throughput screening of small-molecule libraries.
Nature chemical biology 2007;3(8):438-41.
2007: Brian Y Feng; Anton Simeonov; Ajit Jadhav; Kerim Babaoglu; James Inglese; Brian Shoichet; Christopher P Austin
A high-throughput screen for aggregation-based inhibition in a large compound library.
Journal of medicinal chemistry 2007;50(10):2385-90.
2007: R Eric Davis; Ya-Qin Zhang; Noel Southall; Louis M Staudt; Christopher P Austin; James Inglese; Douglas S Auld
A cell-based assay for IkappaBalpha stabilization using a two-color dual luciferase-based sensor.
Assay and drug development technologies 2007;5(1):85-103.
2006: James Inglese; Douglas S Auld; Ajit Jadhav; Ronald L Johnson; Anton Simeonov; Adam Yasgar; Wei Zheng; Christopher P Austin
Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries.
Proceedings of the National Academy of Sciences of the United States of America 2006;103(31):11473-8.
2006: Koc-Kan Ho; Douglas S Auld; Adolph C Bohnstedt; Paolo Conti; Wim Dokter; Shawn Erickson; Daming Feng; James Inglese; Celia Kingsbury; Steven G Kultgen; Rong-Qiang Liu; Christopher M Masterson; Michael Ohlmeyer; Yajing Rong; Martijn Rooseboom; Andrew Roughton; Philippe Samama; Martin-Jan Smit; Ellen Son; Jaap van der Louw; Gerard Vogel; Maria Webb; Jac Wijkmans; Ming You
Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists.
Bioorganic & medicinal chemistry letters 2006;16(10):2724-8.
2006: Douglas S Auld; Ronald L Johnson; Ya-qin Zhang; Henrike Veith; Ajit Jadhav; Adam Yasgar; Anton Simeonov; Wei Zheng; Elisabeth D Martinez; John K Westwick; Christopher P Austin; James Inglese
Fluorescent protein-based cellular assays analyzed by laser-scanning microplate cytometry in 1536-well plate format.
Methods in enzymology 2006;414():566-89.
2005: Marc Ferrer; Jim Maiolo; Patricia Kratz; Jessica L Jackowski; Dennis J Murphy; Simon Delagrave; James Inglese
Directed evolution of PDZ variants to generate high-affinity detection reagents.
Protein engineering, design & selection : PEDS 2005;18(4):165-73.
2004: Paul Zuck; Edward M Murray; Erica Stec; Jay A Grobler; Adam J Simon; Berta Strulovici; James Inglese; Osvaldo A Flores; Marc Ferrer
A cell-based beta-lactamase reporter gene assay for the identification of inhibitors of hepatitis C virus replication.
Analytical biochemistry 2004;334(2):344-55.
2004: Oleg Kornienko; Raul Lacson; Priya Kunapuli; Jonathan Schneeweis; Ira Hoffman; Todd Smith; Melissa Alberts; James Inglese; Berta Strulovici
Miniaturization of whole live cell-based GPCR assays using microdispensing and detection systems.
Journal of biomolecular screening 2004;9(3):186-95.
2004: Michael Weber; Marc Ferrer; Wei Zheng; James Inglese; Berta Strulovici; Priya Kunapuli
A 1536-well cAMP assay for Gs- and Gi-coupled receptors using enzyme fragmentation complementation.
Assay and drug development technologies 2004;2(1):39-49.
2003: Norbert T Peekhaus; Marc Ferrer; Tina Chang; Oleg Kornienko; Jonathan E Schneeweis; Todd S Smith; Ira Hoffman; Lyndon J Mitnaul; Jayne Chin; Paul A Fischer; Timothy A Blizzard; Elizabeth T Birzin; Wanda Chan; James Inglese; Berta Strulovici; Susan P Rohrer; James M Schaeffer
A beta-lactamase-dependent Gal4-estrogen receptor beta transactivation assay for the ultra-high throughput screening of estrogen receptor beta agonists in a 3456-well format.
Assay and drug development technologies 2003;1(6):789-800.
2003: Marc Ferrer; Paul Zuck; Garrett Kolodin; Shi-Shan Mao; Richard Peltier; Carolyn Bailey; Stephen J Gardell; Berta Strulovici; James Inglese
Miniaturizable homogenous time-resolved fluorescence assay for carboxypeptidase B activity.
Analytical biochemistry 2003;317(1):94-8.
2003: Marc Ferrer; Garrett D Kolodin; Paul Zuck; Richard Peltier; Kurtis Berry; Suzanne Mandala; Hugh Rosen; Hisashi Ota; Satoshi Ozaki; James Inglese; Berta Strulovici
A fully automated [35S]GTPgammaS scintillation proximity assay for the high-throughput screening of Gi-linked G protein-coupled receptors.
Assay and drug development technologies 2003;1(2):261-73.
2003: James Inglese; John R Raymond
Professor Robert J. Lefkowitz, M.D., scientist and mentor extraordinaire.
Assay and drug development technologies 2003;1(2):227-31.
2003: Priya Kunapuli; Richard W Ransom; Kathy L Murphy; Douglas J Pettibone; Julie Kerby; Sarah Grimwood; Paul Zuck; Peter Hodder; Raul Lacson; Ira Hoffman; James Inglese; Berta Strulovici
Development of an intact cell reporter gene beta-lactamase assay for G protein-coupled receptors for high-throughput screening.
Analytical biochemistry 2003;314(1):16-29.
2003: Aaron C Hamilton; James Inglese; Marc Ferrer
A PDZ domain-based assay for measuring HIV protease activity: assay design considerations.
Protein science : a publication of the Protein Society 2003;12(3):458-67.
2003: Peter Hodder; Jason Cassaday; Richard Peltier; Kurtis Berry; James Inglese; Bradley P Feuston; Chris Culberson; Leo Bleicher; Nicholas Cosford; Chris Bayly; Carla M Suto; Mark A Varney; Berta Strulovici
Identification of metabotropic glutamate receptor antagonists using an automated high-throughput screening system.
Analytical biochemistry 2003;313(2):246-54.
2002: James Inglese
Engaging science and technology for drug development.
Assay and drug development technologies 2002;1(1 Pt 1):1.
2002: James Inglese
Expanding the HTS paradigm.
Drug discovery today 2002;7(18 Suppl):S105-6.
2002: Mike Whitney; Jeffrey H Stack; Paul L Darke; Wei Zheng; Joe Terzo; James Inglese; Berta Strulovici; Lawrence C Kuo; Brian A Pollock
A collaborative screening program for the discovery of inhibitors of HCV NS2/3 cis-cleaving protease activity.
Journal of biomolecular screening 2002;7(2):149-54.
2002: Marc Ferrer; Aaron C Hamilton; James Inglese
A PDZ domain-based detection system for enzymatic assays.
Analytical biochemistry 2002;301(2):207-16.
2001: Wei Zheng; S S Carroll; James Inglese; R Graves; L Howells; Berta Strulovici
Miniaturization of a hepatitis C virus RNA polymerase assay using a -102 degrees C cooled CCD camera-based imaging system.
Analytical biochemistry 2001;290(2):214-20.
1999: James Inglese; J F Glickman
Radiolabeling of receptor ligands by chemical incorporation of phosphorylation sites.
Analytical biochemistry 1999;274(1):104-9.
1999: Paul Zuck; Z Lao; S Skwish; J F Glickman; K Yang; J Burbaum; James Inglese
Ligand-receptor binding measured by laser-scanning imaging.
Proceedings of the National Academy of Sciences of the United States of America 1999;96(20):11122-7.
1998: RH Stoffel; James Inglese; Alexander D Macrae; Robert J Lefkowitz; Richard T Premont
Palmitoylation increases the kinase activity of the G protein-coupled receptor kinase, GRK6.
Biochemistry 1998;37(46):16053-9.
1998: James Inglese; P Samama; S Patel; J Burbaum; Ilana L Stroke; Kenneth C Appell
Chemokine receptor-ligand interactions measured using time-resolved fluorescence.
Biochemistry 1998;37(8):2372-7.
1997: K Cha; C Bruel; James Inglese; H Gobind Khorana
Rhodopsin kinase: expression in baculovirus-infected insect cells, and characterization of post-translational modifications.
Proceedings of the National Academy of Sciences of the United States of America 1997;94(20):10577-82.
1997: Ingrid Boekhoff; K Touhara; S Danner; James Inglese; M J Lohse; Heinz Breer; Robert J Lefkowitz
Phosducin, potential role in modulation of olfactory signaling.
The Journal of biological chemistry 1997;272(7):4606-12.
1996: James Inglese; Richard T Premont
Lipid modifications of G-protein-coupled receptor kinases.
Biochemical Society transactions 1996;24(3):714-7.
1996: Richard T Premont; Alexander D Macrae; RH Stoffel; N Chung; Julie A Pitcher; C Ambrose; James Inglese; M E MacDonald; R J Lefkowitz
Characterization of the G protein-coupled receptor kinase GRK4. Identification of four splice variants.
The Journal of biological chemistry 1996;271(11):6403-10.
1996: M Diverse-Pierluissi; James Inglese; RH Stoffel; R J Lefkowitz; Kathleen Dunlap
G protein-coupled receptor kinase mediates desensitization of norepinephrine-induced Ca2+ channel inhibition.
Neuron 1996;16(3):579-85.
1995: María I Colombo; James Inglese; Crislyn D'Souza-Schorey; W Beron; Philip D Stahl
Heterotrimeric G proteins interact with the small GTPase ARF. Possibilities for the regulation of vesicular traffic.
The Journal of biological chemistry 1995;270(41):24564-71.
1995: C K Chen; James Inglese; R J Lefkowitz; James B Hurley
Ca(2+)-dependent interaction of recoverin with rhodopsin kinase.
The Journal of biological chemistry 1995;270(30):18060-6.
1995: Krzysztof Palczewski; H Ohguro; Richard T Premont; James Inglese
Rhodopsin kinase autophosphorylation. Characterization of site-specific mutations.
The Journal of biological chemistry 1995;270(25):15294-8.
1995: L A Nair; James Inglese; RH Stoffel; Walter J Koch; R J Lefkowitz; Madan M Kwatra; Augustus O Grant
Cardiac muscarinic potassium channel activity is attenuated by inhibitors of G beta gamma.
Circulation research 1995;76(5):832-8.
1995: James Inglese; Walter J Koch; K Touhara; R J Lefkowitz
G beta gamma interactions with PH domains and Ras-MAPK signaling pathways.
Trends in biochemical sciences 1995;20(4):151-6.
1995: Richard T Premont; James Inglese; R J Lefkowitz
Protein kinases that phosphorylate activated G protein-coupled receptors.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology 1995;9(2):175-82.
1995: James Inglese
Prenylation-dependent targeting of G-protein-coupled receptor kinases.
Methods in enzymology 1995;250():149-58.
1994: B E Hawes; K Touhara; H Kurose; R J Lefkowitz; James Inglese
Determination of the G beta gamma-binding domain of phosducin. A regulatable modulator of G beta gamma signaling.
The Journal of biological chemistry 1994;269(47):29825-30.
1994: RH Stoffel; Richard R Randall; Richard T Premont; R J Lefkowitz; James Inglese
Palmitoylation of G protein-coupled receptor kinase, GRK6. Lipid modification diversity in the GRK family.
The Journal of biological chemistry 1994;269(45):27791-4.
1994: E Reuveny; P A Slesinger; James Inglese; J M Morales; Jorge A Iniguez-Lluhi; R J Lefkowitz; Henry R Bourne; Yuh Nung Jan; Lily Yeh Jan
Activation of the cloned muscarinic potassium channel by G protein beta gamma subunits.
Nature 1994;370(6485):143-6.
1994: James Inglese; Louis M Luttrell; Jorge A Iniguez-Lluhi; K Touhara; Walter J Koch; R J Lefkowitz
Functionally active targeting domain of the beta-adrenergic receptor kinase: an inhibitor of G beta gamma-mediated stimulation of type II adenylyl cyclase.
Proceedings of the National Academy of Sciences of the United States of America 1994;91(9):3637-41.
1994: K Touhara; James Inglese; Julie A Pitcher; G Shaw; R J Lefkowitz
Binding of G protein beta gamma-subunits to pleckstrin homology domains.
The Journal of biological chemistry 1994;269(14):10217-20.
1994: Richard T Premont; Walter J Koch; James Inglese; R J Lefkowitz
Identification, purification, and characterization of GRK5, a member of the family of G protein-coupled receptor kinases.
The Journal of biological chemistry 1994;269(9):6832-41.
1994: Walter J Koch; B E Hawes; James Inglese; Louis M Luttrell; R J Lefkowitz
Cellular expression of the carboxyl terminus of a G protein-coupled receptor kinase attenuates G beta gamma-mediated signaling.
The Journal of biological chemistry 1994;269(8):6193-7.
1994: Ingrid Boekhoff; James Inglese; S Schleicher; Walter J Koch; R J Lefkowitz; Heinz Breer
Olfactory desensitization requires membrane targeting of receptor kinase mediated by beta gamma-subunits of heterotrimeric G proteins.
The Journal of biological chemistry 1994;269(1):37-40.
1993: James Inglese; N J Freedman; Walter J Koch; R J Lefkowitz
Structure and mechanism of the G protein-coupled receptor kinases.
The Journal of biological chemistry 1993;268(32):23735-8.
1993: Walter J Koch; James Inglese; W C Stone; R J Lefkowitz
The binding site for the beta gamma subunits of heterotrimeric G proteins on the beta-adrenergic receptor kinase.
The Journal of biological chemistry 1993;268(11):8256-60.
1993: R J Lefkowitz; S Cotecchia; M A Kjelsberg; Julie A Pitcher; Walter J Koch; James Inglese; Marc G Caron
Adrenergic receptors: recent insights into their mechanism of activation and desensitization.
Advances in second messenger and phosphoprotein research 1993;28():1-9.
1992: James Inglese; Walter J Koch; Marc G Caron; R J Lefkowitz
Isoprenylation in regulation of signal transduction by G-protein-coupled receptor kinases.
Nature 1992;359(6391):147-50.
1992: P Chen; U Schulze-Gahmen; Enrico STURA; James Inglese; D L Johnson; A Marolewski; Stephen J Benkovic; Ian A Wilson
Crystal structure of glycinamide ribonucleotide transformylase from Escherichia coli at 3.0 A resolution. A target enzyme for chemotherapy.
Journal of molecular biology 1992;227(1):283-92.
1992: Julie A Pitcher; James Inglese; J B Higgins; J L Arriza; Patrick J Casey; C Kim; J L Benovic; Madan M Kwatra; Marc G Caron; R J Lefkowitz
Role of beta gamma subunits of G proteins in targeting the beta-adrenergic receptor kinase to membrane-bound receptors.
Science (New York, N.Y.) 1992;257(5074):1264-7.
1992: James Inglese; J F Glickman; W Lorenz; Marc G Caron; R J Lefkowitz
Isoprenylation of a protein kinase. Requirement of farnesylation/alpha-carboxyl methylation for full enzymatic activity of rhodopsin kinase.
The Journal of biological chemistry 1992;267(3):1422-5.
1992: R J Lefkowitz; James Inglese; Walter J Koch; Julie A Pitcher; H Attramadal; Marc G Caron
G-protein-coupled receptors: regulatory role of receptor kinases and arrestin proteins.
Cold Spring Harbor symposia on quantitative biology 1992;57():127-33.
1991: W Lorenz; James Inglese; K Palczewski; J J Onorato; Marc G Caron; R J Lefkowitz
The receptor kinase family: primary structure of rhodopsin kinase reveals similarities to the beta-adrenergic receptor kinase.
Proceedings of the National Academy of Sciences of the United States of America 1991;88(19):8715-9.
1990: James Inglese; J M Smith; Stephen J Benkovic
Active-site mapping and site-specific mutagenesis of glycinamide ribonucleotide transformylase from Escherichia coli.
Biochemistry 1990;29(28):6678-87.
1990: James Inglese; D L Johnson; A Shiau; J M Smith; Stephen J Benkovic
Subcloning, characterization, and affinity labeling of Escherichia coli glycinamide ribonucleotide transformylase.
Biochemistry 1990;29(6):1436-43.
1989: Enrico STURA; D L Johnson; James Inglese; J M Smith; Stephen J Benkovic; Ian A Wilson
Preliminary crystallographic investigations of glycinamide ribonucleotide transformylase.
The Journal of biological chemistry 1989;264(16):9703-6.
1989: James Inglese; R A Blatchly; Stephen J Benkovic
A multisubstrate adduct inhibitor of a purine biosynthetic enzyme with a picomolar dissociation constant.
Journal of medicinal chemistry 1989;32(5):937-40.
1985: John Galivan; James Inglese; John J McGuire; Z Nimec; James K Coward
gamma-Fluoromethotrexate: synthesis and biological activity of a potent inhibitor of dihydrofolate reductase with greatly diminished ability to form poly-gamma-glutamates.
Proceedings of the National Academy of Sciences of the United States of America 1985;82(9):2598-602.