Publications & References -

Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.
Carter TA, Wodicka LM, Shah NP, Velasco AM, Fabian MA, Treiber DK, Milanov ZV, Atteridge CE, Biggs WH 3rd, Edeen PT, Floyd M, Ford JM, Grotzfeld RM, Herrgard S, Insko DE, Mehta SA, Patel HK, Pao W, Sawyers CL, Varmus H, Zarrinkar PP, Lockhart DJ.. Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.. Proc Natl Acad Sci U S A. 2005 Aug 2;102(31):11011-6. Epub 2005 Jul 26.. PMID:16046538
A quantitative analysis of kinase inhibitor selectivity.
Karaman MW, Herrgard S, Treiber DK, Gallant P, Atteridge CE, Campbell BT, Chan KW, Ciceri P, Davis MI, Edeen PT, Faraoni R, Floyd M, Hunt JP, Lockhart DJ, Milanov ZV, Morrison MJ, Pallares G, Patel HK, Pritchard S, Wodicka LM, Zarrinkar PP.. A quantitative analysis of kinase inhibitor selectivity.. Nat Biotechnol. 2008 Jan;26(1):127-32.. PMID:18183025
High-throughput kinase profiling as a platform for drug discovery.
Goldstein DM, Gray NS, Zarrinkar PP.. High-throughput kinase profiling as a platform for drug discovery.. Nat Rev Drug Discov. 2008 May;7(5):391-7.. PMID:18404149
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Zarrinkar PP, Gunawardane RN, Cramer MD, Gardner MF, Brigham D, Belli B, Karaman MW, Pratz KW, Pallares G, Chao Q, Sprankle KG, Patel HK, Levis M, Armstrong RC, James J, Bhagwat SS.. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).. Blood. 2009 Oct 1;114(14):2984-92. Epub 2009 Aug 4.. PMID:19654408
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.
Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP, Treiber DK.. Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.. Chem Biol. 2010 Nov 24;17(11):1241-9.. PMID:21095574
An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction.
East SP, Bamford S, Dietz MG, Eickmeier C, Flegg A, Ferger B, Gemkow MJ, Heilker R, Hengerer B, Kotey A, Loke P, Schänzle G, Schubert HD, Scott J, Whittaker M, Williams M, Zawadzki P, Gerlach K.. An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction.. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4901-5. Epub 2010 Jun 25.. PMID:20638279
Structural determinants in the second intracellular loop of the human cannabinoid CB1 receptor mediate selective coupling to G(s) and G(i).
Chen XP, Yang W, Fan Y, Luo JS, Hong K, Wang Z, Yan JF, Chen X, Lu JX, Benovic JL, Zhou NM.. Structural determinants in the second intracellular loop of the human cannabinoid CB1 receptor mediate selective coupling to G(s) and G(i).. Br J Pharmacol. 2010 Dec;161(8):1817-34. doi: 10.1111/j.1476-5381.2010.01006.x.. PMID:20735408
Conserved water-mediated hydrogen bond network between TM-I, -II, -VI, and -VII in 7TM receptor activation.
Nygaard R, Valentin-Hansen L, Mokrosinski J, Frimurer TM, Schwartz TW.. Conserved water-mediated hydrogen bond network between TM-I, -II, -VI, and -VII in 7TM receptor activation.. J Biol Chem. 2010 Jun 18;285(25):19625-36. Epub 2010 Apr 15.. PMID:20395291
Falcarinol is a covalent cannabinoid CB1 receptor antagonist and induces pro-allergic effects in skin.
Leonti M, Casu L, Raduner S, Cottiglia F, Floris C, Altmann KH, Gertsch J.. Falcarinol is a covalent cannabinoid CB1 receptor antagonist and induces pro-allergic effects in skin.. Biochem Pharmacol. 2010 Jun 15;79(12):1815-26. Epub 2010 Mar 3.. PMID:20206138
Neuropeptide FF receptors have opposing modulatory effects on nociception.
Lameh J, Bertozzi F, Kelly N, Jacobi PM, Nguyen D, Bajpai A, Gaubert G, Olsson R, Gardell LR.. Neuropeptide FF receptors have opposing modulatory effects on nociception.. J Pharmacol Exp Ther. 2010 Jul;334(1):244-54. Epub 2010 Mar 30.. PMID:20354177
Preclinical characterization of BRL 44408: antidepressant- and analgesic-like activity through selective alpha2A-adrenoceptor antagonism.
Dwyer JM, Platt BJ, Rizzo SJ, Pulicicchio CM, Wantuch C, Zhang MY, Cummons T, Leventhal L, Bender CN, Zhang J, Kowal D, Lu S, Rajarao SJ, Smith DL, Shilling AD, Wang J, Butera J, Resnick L, Rosenzweig-Lipson S, Schechter LE, Beyer CE.. Preclinical characterization of BRL 44408: antidepressant- and analgesic-like activity through selective alpha2A-adrenoceptor antagonism.. Int J Neuropsychopharmacol. 2010 Oct;13(9):1193-205. Epub 2010 Jan 5.. PMID:20047711
Identification of potent 11mer glucagon-like peptide-1 receptor agonist peptides with novel C-terminal amino acids: Homohomophenylalanine analogs.
Haque TS, Lee VG, Riexinger D, Lei M, Malmstrom S, Xin L, Han S, Mapelli C, Cooper CB, Zhang G, Ewing WR, Krupinski J.. Identification of potent 11mer glucagon-like peptide-1 receptor agonist peptides with novel C-terminal amino acids: Homohomophenylalanine analogs.. Peptides. 2010 May;31(5):950-5. Epub 2010 Feb 4.. PMID:20138099
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.
Frost JM, Dart MJ, Tietje KR, Garrison TR, Grayson GK, Daza AV, El-Kouhen OF, Yao BB, Hsieh GC, Pai M, Zhu CZ, Chandran P, Meyer MD.. Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.. J Med Chem. 2010 Jan 14;53(1):295-315.. PMID:19921781
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists.
Cheung AW, Brinkman J, Firooznia F, Flohr A, Grimsby J, Gubler ML, Guertin K, Hamid R, Marcopulos N, Norcross RD, Qi L, Ramsey G, Tan J, Wen Y, Sarabu R.. 4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists.. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4140-6. Epub 2010 May 20.. PMID:20541935
AC-260584, an orally bioavailable M(1) muscarinic receptor allosteric agonist, improves cognitive performance in an animal model.
Bradley SR, Lameh J, Ohrmund L, Son T, Bajpai A, Nguyen D, Friberg M, Burstein ES, Spalding TA, Ott TR, Schiffer HH, Tabatabaei A, McFarland K, Davis RE, Bonhaus DW.. AC-260584, an orally bioavailable M(1) muscarinic receptor allosteric agonist, improves cognitive performance in an animal model.. Neuropharmacology. 2010 Feb;58(2):365-73. Epub 2009 Oct 14.. PMID:19835892
Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists.
Cole DC, Gross JL, Comery TA, Aschmies S, Hirst WD, Kelley C, Kim JI, Kubek K, Ning X, Platt BJ, Robichaud AJ, Solvibile WR, Stock JR, Tawa G, Williams MJ, Ellingboe JW.. Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists.. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1237-40. Epub 2009 Dec 4.. PMID:20042333
The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators.
Wang Y, Jiao X, Kayser F, Liu J, Wang Z, Wanska M, Greenberg J, Weiszmann J, Ge H, Tian H, Wong S, Schwandner R, Lee T, Li Y.. The first synthetic agonists of FFA2: Discovery and SAR of phenylacetamides as allosteric modulators.. Bioorg Med Chem Lett. 2010 Jan 15;20(2):493-8. Epub 2009 Nov 26.. PMID:20005104
Evaluation of nonradioactive cell-free cAMP assays for measuring in vitro phosphodiesterase activity.
Eapen MS, Sodhi R, Balakrishnan G, Dastidar S, Ray A, Vijayakrishnan L.. Evaluation of nonradioactive cell-free cAMP assays for measuring in vitro phosphodiesterase activity.. Pharmacology. 2010;85(5):280-5. Epub 2010 Apr 24.. PMID:20424496
Sulfonylureas uncouple glucose-dependence for GPR40-mediated enhancement of insulin secretion from INS-1E cells.
Yang M, Chisholm JW, Soelaiman S, Shryock JC.. Sulfonylureas uncouple glucose-dependence for GPR40-mediated enhancement of insulin secretion from INS-1E cells.. Mol Cell Endocrinol. 2010 Feb 5;315(1-2):308-13. Epub 2009 Oct 6.. PMID:19815053
Genetic interventions in mammalian cells; applications and uses in high-throughput screening and drug discovery.
Hampton SL, Kinnaird AI.. Genetic interventions in mammalian cells; applications and uses in high-throughput screening and drug discovery.. Cell Biol Toxicol. 2010 Feb;26(1):43-55. Epub 2009 Nov 11.. PMID:19904619

Displaying results 261-280 (of 400)

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Characterizing cannabinoid CB2 receptor ligands using DiscoverX PathHunter beta-arrestin assay.
McGuinness D, Malikzay A, Visconti R, Lin K, Bayne M, Monsma F, Lunn CA. Characterizing cannabinoid CB2 receptor ligands using DiscoveRx PathHunter beta-arrestin assay. J Biomol Screen. 2009 Jan;14(1):49-58. PMID:19171920
Pharmacological characterization of receptor redistribution and beta-arrestin recruitment assays for the cannabinoid receptor 1.
van der Lee MM, Blomenröhr M, van der Doelen AA, Wat JW, Smits N, Hanson BJ, van Koppen CJ, Zaman GJ. Pharmacological characterization of receptor redistribution and beta-arrestin recruitment assays for the cannabinoid receptor 1. J Biomol Screen 14(7):811-23. PMID:19520790
Using ligand-induced conformational change to screen for compounds targeting G-protein-coupled receptors.
O'Dowd BF, Alijaniaram M, Ji X, Nguyen T, Eglen RM, George SR.. Using ligand-induced conformational change to screen for compounds targeting G-protein-coupled receptors.. J Biomol Screen. 2007 Mar;12(2):175-85. Epub 2007 Feb 8.. PMID:17289935
GATA4 expression is primarily regulated via a miR-26b-dependent post-transcriptional mechanism during cardiac hypertrophy.
Han M, Yang Z, Sayed D, He M, Gao S, Lin L, Yoon S, Abdellatif M.. GATA4 expression is primarily regulated via a miR-26b-dependent post-transcriptional mechanism during cardiac hypertrophy.. Cardiovasc Res, Mar 2012; 93: 645 - 654.. PMID:22219180
Lipid G protein-coupled receptor ligand identification using beta-arrestin PathHunter assay.
Yin H, Chu A, Li W, Wang B, Shelton F, Otero F, Nguyen DG, Caldwell JS and Chen YA. Lipid G protein-coupled receptor ligand identification using beta-arrestin PathHunter assay. J Biol Chem 284(18):12328-38. PMID:19286662
A homogeneous enzyme fragment complementation-based beta-arrestin translocation assay for high-throughput screening of G-protein-coupled receptors.
Zhao X, Jones A, Olson KR, Peng K, Wehrman T, Park A, Mallari R, Nebalasca D, Young SW and Xiao SH. A homogeneous enzyme fragment complementation-based beta-arrestin translocation assay for high-throughput screening of G-protein-coupled receptors. J Biomol Screen 13(8):737-47. PMID:18660457
C5a-stimulated recruitment of beta-arrestin2 to the nonsignaling 7-transmembrane decoy receptor C5L2.
Van Lith LH, Oosterom J, Van Elsas A, Zaman GJ. C5a-stimulated recruitment of beta-arrestin2 to the nonsignaling 7-transmembrane decoy receptor C5L2.. J Biomol Screen. 2009 Oct;14(9):1067-75. Epub 2009 Jul 29.. PMID:19641221

Displaying results 181-187 (of 187)

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A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)
Kaniskan HÜ1, Szewczyk MM, Yu Z, Eram MS, Yang X, Schmidt K, Luo X, Dai M, He F, Zang I, Lin Y,Kennedy S, Li F, Dobrovetsky E, Dong A, Smil D, Min SJ, Landon M, Lin-Jones J, Huang XP, Roth BL,Schapira M, Atadja P, Barsyte-Lovejoy D, Arrowsmith CH, Brown PJ, Zhao K, Jin J, Vedadi M. A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3). Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70. doi: 10.1002/anie.201412154. Epub 2015 Feb 27. PMID:25728001
Cell-based protein stabilization assays for the detection of interactions between small-molecule inhibitors and BRD4.
Schulze J, Moosmayer D, Weiske J, Fernández-Montalván A, Herbst C, Jung M, Haendler B, Bader B. Cell-based protein stabilization assays for the detection of interactions between small-molecule inhibitors and BRD4. J Biomol Screen. 2015 Feb;20(2):180-9. doi: 10.1177/1087057114552398. Epub 2014 Sep 29. PMID:25266565

A cellular target engagement assay for the characterization of SHP2 (PTPN11) phosphatase inhibitors
Celeste Romero , Lester J. Lambert , Douglas J. Sheffler , Laurent J.S. De Backer , Dhanya RaveendraPanickar , Maria Celeridad , Stefan Grotegut , Socorro Rodiles , John Holleran , Eduard Sergienko , Elena B. Pasquale3 , Nicholas D. P. Cosford , and Lutz Tautz. A cellular target engagement assay for the characterization of SHP2 (PTPN11) phosphatase inhibitors
Sorafenib activity and disposition in liver cancer does not depend on organic cation transporter 1 (OCT1).
Chen M, Neul C, Schaeffeler E, Frisch F, Winter S, Schwab M, Koepsell H, Hu S, Laufer S, Baker SD, Sparreboom A, Nies AT. Clin Pharmacol Ther. 2019 Jul 27
Activation of TrkB with TAM-163 results in opposite effects on body weight in rodents and non-human primates.
Perreault M, Feng G, Will S, Gareski T, Kubasiak D, Marquette K, Vugmeyster Y, Unger TJ, Jones J, Qadri A, Hahm S, Sun Y, Rohde CM, Zwijnenberg R, Paulsen J, Gimeno RE. Activation of TrkB with TAM-163 results in opposite effects on body weight in rodents and non-human primates. PLoS One. 2013 May 20;8(5):e62616. PMID:23700410
Development of Three Orthogonal Assays Suitable for the Identification and Qualification of PIKfyve Inhibitors.
Fogarty K, Kashem M, Bauer A, Bernardino A, Brennan D, Cook B, Farrow N, Molinaro T, Nelson R. Development of Three Orthogonal Assays Suitable for the Identification and Qualification of PIKfyve Inhibitors. Assay Drug Dev Technol. 2017 Jul;15(5):210-219. PMID:28723271
A High-Throughput Dose-Response Cellular Thermal Shift Assay for Rapid Screening of Drug Target Engagement in Living Cells, Exemplified Using SMYD3 and IDO1
McNulty DE, Bonnette WG, Qi H, Wang L, Ho TF, Waszkiewicz A, Kallal LA, Nagarajan RP, Stern M, Quinn AM, Creasy CL, Su DS, Graves AP, Annan RS, Sweitzer SM, Holbert MA. A High-Throughput Dose-Response Cellular Thermal Shift Assay for Rapid Screening of Drug Target Engagement in Living Cells, Exemplified Using SMYD1 and IDO1. SLAS Discov. 2017 Sep;1:2472555217732014. PMID:28957646
Structural characterization of nonactive site, TrkA-selective kinase inhibitors
Su HP1, Rickert K2, Burlein C3, Narayan K3, Bukhtiyarova M3, Hurzy DM4, Stump CA4, Zhang X4, Reid J4, Krasowska-Zoladek A5, Tummala S2, Shipman JM2, Kornienko M2, Lemaire PA3, Krosky D2, Heller A3, Achab A6, Chamberlin C6, Saradjian P6, Sauvagnat B6, Yang X6, Ziebell MR6, Nickbarg E6, Sanders JM4, Bilodeau MT4, Carroll SS3, Lumb KJ2, Soisson SM4, Henze DA5, Cooke AJ4. Structural characterization of nonactive site, TrkA-selective kinase inhibitors. Proc Natl Acad Sci U S A. 2017 Jan 17; 114 (3): E297-E306.
Multiplex quantitative assays indicate a need for reevaluating reported small-molecule TrkB agonists
Boltaev U1,2, Meyer Y1, Tolibzoda F1,2, Jacques T1, Gassaway M1,2, Xu Q3, Wagner F3, Zhang YL3, Palmer M3, Holson E3, Sames D4,2.. Multiplex quantitative assays indicate a need for reevaluating reported small-molecule TrkB agonists. Sci Signal. 2017 Aug 22; 10 (493).
Design, synthesis and SAR of substituted indoles as selective TrkA inhibitors.
Hurzy DM1, Henze DA2, Cabalu TD3, Narayan K4, Heller A5, Cooke AJ6. Design, synthesis and SAR of substituted indoles as selective TrkA inhibitors. Bioorg Med Chem Lett. 2017 Jun 15; 27 (12): 2695-2701.
Small-Molecule Target Engagement in Cells.
Schürmann M, Janning P, Ziegler S, Waldmann H. Small-Molecule Target Engagement in Cells. Cell Chem Biol. 2016 Apr 21;23(4):435-41. doi:10.1016/j.chembiol.2016.03.008. Epub 2016 Mar 31. PMID:27049669
Examining Ligand-Based Stabilization of Proteins in Cells with MEK1 Kinase Inhibitors.
Auld DS, Davis CA, Jimenez M, Knight S, Orme JP. Examining Ligand-Based Stabilization of Proteins in Cells with MEK1 Kinase Inhibitors. Assay Drug Dev Technol. 2015 Jun;13(5):266-76. PMID:26107610
Discovery of MINC1, a GTPase-Activating Protein Small Molecule Inhibitor, Targeting MgcRacGAP
van Adrichem AJ, Fagerholm A, Turunen L, Lehto A, Saarela J, Koskinen A, Repasky GA, Wennerberg K. Discovery of MINC1, a GTPase-Activating Protein Small Molecule Inhibitor, Targeting MgcRacGAP. Comb Chem High Throughput Screen. 2015;18(1):3-17. PMID:25479424
The Use of TrkA-PathHunter Assay in High-Throughput Screening to identify Compounds That Affect Nerve Growth Factor Signaling.
Forsell P, Almqvist H, Hillertz P, Akerud T, Otrocka M, Eisele L, Sun K, Andersson H, Trivedi S, Wollberg AR, Dekker N, Rottici D, Sandberg K. The Use of TrkA-PathHunter Assay in High-Throughput Screening to Identify Compounds That Affect Nerve Growth Factor Signaling. J Biomol Screen. 2013 Mar 4. PMID:19940259
Development of a Highly Selective c-Src Kinase Inhibitor
Kristoffer R. Brandvold, Michael E. Steffey, Christel C. Fox, and Matthew B. Soellner. Development of a Highly Selective c-Src Kinase Inhibitor. ACS Chem Biol. 2012 Aug 17;7(8):1393-8. Epub 2012 Jun 4. PMID:22594480
Comprehensive analysis of kinase inhibitor selectivity
Mindy I Davis, Jeremy P Hunt, Sanna Herrgard, Pietro Ciceri, Lisa M Wodicka, Gabriel Pallares, Michael Hocker, Daniel K Treiber & Patrick P Zarrinkar. Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol. 2011 Oct 30;29(11):1046-51. doi: 10.1038/nbt.1990.. PMID:22037378
Trends in kinase selectivity: insights for target class-focused library screening.
Posy SL, Hermsmeier MA, Vaccaro W, Ott KH, Todderud G, Lippy JS, Trainor GL, Loughney DA, Johnson SR.. Trends in kinase selectivity: insights for target class-focused library screening.. J Med Chem. 2011 Jan 13;54(1):54-66. Epub 2010 Dec 3.. PMID:21128601
Why do kinase inhibitors cause cardiotoxicity and what can be done about it?
Cheng H, Force T.. Why do kinase inhibitors cause cardiotoxicity and what can be done about it?. Prog Cardiovasc Dis. 2010 Sep-Oct;53(2):114-20.. PMID:20728698
Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.
Kwiatkowski N, Jelluma N, Filippakopoulos P, Soundararajan M, Manak MS, Kwon M, Choi HG, Sim T, Deveraux QL, Rottmann S, Pellman D, Shah JV, Kops GJ, Knapp S, Gray NS.. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.. Nat Chem Biol. 2010 May;6(5):359-68. Epub 2010 Apr 11.. PMID:20383151
Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.
Milkiewicz KL, Weinberg LR, Albom MS, Angeles TS, Cheng M, Ghose AK, Roemmele RC, Theroff JP, Underiner TL, Zificsak CA, Dorsey BD.. Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.. Bioorg Med Chem. 2010 Jun 15;18(12):4351-62. Epub 2010 Apr 29.. PMID:20483621
Pathway to the clinic: inhibition of P38 MAP kinase. A review of ten chemotypes selected for development.
Goldstein DM, Gabriel T.. Pathway to the clinic: inhibition of P38 MAP kinase. A review of ten chemotypes selected for development.. Curr Top Med Chem. 2005;5(10):1017-29.. PMID:16178744

Discovery of Benzimidazole Oxazolidinediones as Novel and Selective Nonsteroidal Mineralocorticoid Receptor Antagonists
Christine Yang, Jaume Balsells, Hong D. Chu, Jason M. Cox, Alejandro Crespo, Xiuying Ma, Lisa Contino, Patricia Brown, Sheng Gao, Beata Zamlynny, Judyann Wiltsie, Joseph Clemas, JeanMarie Lisnock, Jack Gibson, Gaochao Zhou, Margarita Garcia-Calvo, Thomas J. Bateman, Vincent Tong, Ling Xu, Martin Crook, Peter Sinclair, Hong C. Shen. Discovery of Benzimidazole Oxazolidinediones as Novel and Selective Nonsteroidal Mineralocorticoid Receptor Antagonists. ACS Med. Chem. Lett., 2015, 6 (4), pp 461–465. 10.1021/acsmedchemlett.5b00010
Discovery of a novel isoxazoline derivative of prednisolone endowed with a robust anti-inflammatory profile and suitable for topical pulmonary administration.
Ghidini E, Capelli AM, Carnini C, Cenacchi V, Marchini G, Virdis A, Italia A, Facchinetti F. Discovery of a novel isoxazoline derivative of prednisolone endowed with a robust anti-inflammatory profile and suitable for topical pulmonary administration. Steroids. 2015 Mar;95:88-95. doi: 10.1016/j.steroids.2014.12.016. Epub 2014 Dec 31. PMID:25556984
The translational efficacy of a nonsteroidal progesterone receptor antagonist, 4-[3-cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy,-2,6-dimethylbenzonitrile (PF-02413873), on endometrial growth in macaque and human.
Howe DC, Mount NM, Bess K, Brown A, Bungay P, Gibson KR, Hawcock T, Richard J, Jones G, Walley R, McLeod A, Apfeldorfer C, Ramsey S, Tweedy S, Pullen N.. The translational efficacy of a nonsteroidal progesterone receptor antagonist, 4-[3-cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy,-2,6-dimethylbenzonitrile (PF-02413873), on endometrial growth in macaque and human.. J Pharmacol Exp Ther. 2011 Nov;339(2):642-53. Epub 2011 Aug 17.. PMID:21849626
Acute inhibition of 11beta-hydroxysteroid dehydrogenase type-1 improves memory in rodent models of cognition.
Mohler EG, Browman KE, Roderwald VA, Cronin EA, Markosyan S, Scott Bitner R, Strakhova MI, Drescher KU, Hornberger W, Rohde JJ, Brune ME, Jacobson PB, Rueter LE.. Acute inhibition of 11beta-hydroxysteroid dehydrogenase type-1 improves memory in rodent models of cognition.. J Neurosci. 2011 Apr 6;31(14):5406-13.. PMID:21471376
Resveratrol modulates the expression of PTGS2 and cellular proliferation in the normal rat endometrium in an AKT-dependent manner.
Singh M, Parent S, Leblanc V, Asselin E.. Resveratrol modulates the expression of PTGS2 and cellular proliferation in the normal rat endometrium in an AKT-dependent manner.. Biol Reprod. 2011 May;84(5):1045-52. Epub 2011 Jan 19.. PMID:21248286
Cleavage of zearalenone by Trichosporon mycotoxinivorans to a novel nonestrogenic metabolite.
Vekiru E, Hametner C, Mitterbauer R, Rechthaler J, Adam G, Schatzmayr G, Krska R, Schuhmacher R.. Cleavage of zearalenone by Trichosporon mycotoxinivorans to a novel nonestrogenic metabolite.. Appl Environ Microbiol. 2010 Apr;76(7):2353-9. Epub 2010 Jan 29.. PMID:20118365
Expression of Human Nuclear Receptors in Plants for the Discovery of Plant-Derived Ligands.
Doukhanina EV, Apuya NR, Yoo HD, Wu CY, Davidow P, Krueger S, Flavell RB, Hamilton R, Bobzin SC.. Expression of Human Nuclear Receptors in Plants for the Discovery of Plant-Derived Ligands.. J Biomol Screen. 2007 Apr;12(3):385-95.. PMID:17438068

Active participation of cellular chaperone Hsp90 in regulating the function of rotavirus nonstructural protein 3 (NSP3).
Dutta D, Chattopadhyay S, Bagchi P, Halder UC, Nandi S, Mukherjee A, Kobayashi N, Taniguchi K, Chawla-Sarkar M.. Active participation of cellular chaperone Hsp90 in regulating the function of rotavirus nonstructural protein 3 (NSP3).. J Biol Chem. 2011 Jun 3;286(22):20065-77. Epub 2011 Apr 13.. PMID:21489987
Beta-Galactosidase enzyme fragment complementation for the measurement of Wnt/beta-catenin signaling
Verkaar F, van der Stelt M, Blankesteijn WM, van der Doelen AA, Zaman GJ. Beta-Galactosidase enzyme fragment complementation for the measurement of Wnt/beta-catenin signaling. FASEB J. 2010 Apr;24(4):1205-17. PMID:19940259

A Next-Generation Risk Assessment Case Study for Coumarin in Cosmetic Products
Baltazar MT, Cable S, Carmichael PL, Cubberley R, Cull T, Delagrange M, Dent MP, Hatherell S, Houghton J, Kukic P, Li H, Lee M-Y, Malcomber S, Middleton AM, Moxon TE, Nathanail AV, Nicol B, Pendlington R, Reynolds G, Reynolds J, White A, Westmoreland C. A Next-Generation Risk Assessment Case Study for Coumarin in Cosmetic Products. Toxicol Sci. 2020;176(1):236-252.
Btk inhibition treats TLR7/IFN driven murine lupus
Bender AT, Pereira A, Fu K, Samy E, Wu Y, Liu-Bujalski L, Caldwell R, Chen Y-Y, Tian H, Morandi F, Head J, Koehler U, Genest M, Okitsu SL, Xu D, Grenningloh R. Btk inhibition treats TLR7/IFN driven murine lupus. Clinical Immunology. 2016;164:65-77.
Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin.
Smith SH, Peredo CE, Takeda Y, Bui T, Neil J, Rickard D, Millerman E, Therrien J-P, Nicodeme E, Brusq J-M, Birault V, Viviani F, Hofland H, Jetten AM, Cote-Sierra J. Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin. PLOS ONE. 2016;11(2):e0147979.
Targeting JAK2 reduces GVHD and xenograft rejection through regulation of T cell differentiation.
Betts BC, Bastian D, Iamsawat S, Nguyen H, Heinrichs JL, Wu Y, Daenthanasanmak A, Veerapathran A, O’Mahony A, Walton K, Reff J, Horna P, Sagatys EM, Lee MC, Singer J, Chang Y-J, Liu C, Pidala J, Anasetti C, Yu X-Z. Targeting JAK2 reduces GVHD and xenograft rejection through regulation of T cell differentiation. PNAS. 2018;115(7):1582-1587.
The activities of drug inactive ingredients on biological targets.
Pottel J, Armstrong D, Zou L, Fekete A, Huang X-P, Torosyan H, Bednarczyk D, Whitebread S, Bhhatarai B, Liang G, Jin H, Ghaemi SN, Slocum S, Lukacs KV, Irwin JJ, Berg EL, Giacomini KM, Roth BL, Shoichet BK, Urban L. The activities of drug inactive ingredients on biological targets. Science. 2020;369(6502):403-413.
Application of a phenotypic drug discovery strategy to identify biological and chemical starting points for inhibition of TSLP production in lung epithelial cells.
Orellana A, García-González V, López R, Pascual-Guiral S, Lozoya E, Díaz J, Casals D, Barrena A, Paris S, Andrés M, Segarra V, Vilella D, Malhotra R, Eastwood P, Planagumà A, Miralpeix M, Nueda A. Application of a phenotypic drug discovery strategy to identify biological and chemical starting points for inhibition of TSLP production in lung epithelial cells. PLOS ONE. 2018;13(1):e0189247.
Pharmacological Profile of the Novel Antiepileptic Drug Candidate Padsevonil: Interactions with Synaptic Vesicle 2 Proteins and the GABAA Receptor.
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Human Cell-Based in vitro Phenotypic Profiling for Drug Safety-Related Attrition.
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Comparative phenotypic profiling of the JAK2 inhibitors ruxolitinib, fedratinib, momelotinib, and pacritinib reveals distinct mechanistic signatures.
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Efficacy and Pharmacodynamic Modeling of the BTK Inhibitor Evobrutinib in Autoimmune Disease Models.
Haselmayer P, Camps M, Liu-Bujalski L, Nguyen N, Morandi F, Head J, O’Mahony A, Zimmerli SC, Bruns L, Bender AT, Schroeder P, Grenningloh R. Efficacy and Pharmacodynamic Modeling of the BTK Inhibitor Evobrutinib in Autoimmune Disease Models. The Journal of Immunology. 2019 Apr 15; ji1800583.
Advancing nonclinical innovation and safety in pharmaceutical testing.
Baker EJ, Beck NA, Berg EL, Clayton-Jeter HD, Chandrasekera PC, Curley JL, Donzanti BA, Ewart LC, Gunther JM, Kenna JG, LeCluyse EL, Liebman MN, Pugh CL, Watkins PB, Sullivan KM. Advancing nonclinical innovation and safety in pharmaceutical testing. Drug Discovery Today. 2019;24(2):624–628.
Rational discovery of dual-action multi-target kinase inhibitor for precision anti-cancer therapy using structural systems pharmacology.
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Predictive gene signatures determine tumor sensitivity to MDM2 inhibition.
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Small-molecule activators of protein phosphatase 2A for the treatment of castration-resistant prostate cancer.
McClinch K, Avelar RA, Callejas D, Izadmehr S, Wiredja D, Perl A, Sangodkar J, Kastrinsky DB, Schlatzer D, Cooper M, Kiselar J, Stachnik A, Yao S, Hoon D, McQuaid D, Zaware N, Gong Y, Brautigan DL, Plymate SR, Sprenger CCT, Oh WK, Levine AC, Kirschenbaum A, Sfakianos JP, Sears R, DiFeo A, Ioannou Y, Ohlmeyer M, Narla G, Galsky MD. Small-molecule activators of protein phosphatase 2A for the treatment of castration-resistant prostate cancer. Cancer Research. 2018;78(8):2065–2080.
Assessing bioactivity-exposure profiles of fruit and vegetable extracts in the BioMAP profiling system.
Wetmore BA, Clewell RA, Cholewa B, Parks B, Pendse SN, Black MB, Mansouri K, Haider S, Berg EL, Judson RS, Houck KA, Martin M, Clewell HJ 3rd, Andersen ME, Thomas RS, McMullen PD. Assessing bioactivity-exposure profiles of fruit and vegetable extracts in the BioMAP profiling system. Toxicology in Vitro. 2019;54:41–57.
Mechanism of action of the third generation benzopyrans and evaluation of their broad anti-cancer activity in vitro and in vivo.
Stevenson AJ, Ager EI, Proctor MA, Škalamera D, Heaton A, Brown D, Gabrielli BG. Mechanism of action of the third generation benzopyrans and evaluation of their broad anti-cancer activity in vitro and in vivo. Scientific Reports. 2018;8(1).
Efficacy of the highly selective focal adhesion kinase inhibitor BI 853520 in adenocarcinoma xenograft models is linked to a mesenchymal tumor phenotype.
Hirt UA, Waizenegger IC, Schweifer N, Haslinger C, Gerlach D, Braunger J, Weyer-Czernilofsky U, Stadtmüller H, Sapountzis I, Bader G, Zoephel A, Bister B, Baum A, Quant J, Kraut N, Garin-Chesa P, Adolf GR. Efficacy of the highly selective focal adhesion kinase inhibitor BI 853520 in adenocarcinoma xenograft models is linked to a mesenchymal tumor phenotype. Oncogenesis. 2018;7(2):21.
Mebendazole stimulates CD14+ myeloid cells to enhance T-cell activation and tumour cell killing.
Rubin J, Mansoori S, Blom K, Berglund M, Lenhammar L, Andersson C, Loskog A, Fryknäs M, Nygren P, Larsson R. Mebendazole stimulates CD14+ myeloid cells to enhance T-cell activation and tumour cell killing. Oncotarget. 2018;9(56):30805-30813.
Discriminating phenotypic signatures identified for tocilizumab, adalimumab, and tofacitinib monotherapy and their combinations with methotrexate.
O’Mahony A, John MR, Cho H, Hashizume M, Choy EH. Discriminating phenotypic signatures identified for tocilizumab, adalimumab, and tofacitinib monotherapy and their combinations with methotrexate. Journal of Translational Medicine. 2018;16(156).
Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation.
Thomenius MJ, Totman J, Harvey D, Mitchell LH, Riera TV, Cosmopoulos K, Grassian AR, Klaus C, Foley M, Admirand EA, Jahic H, Majer C, Wigle T, Jacques SL, Gureasko J, Brach D, Lingaraj T, West K, Smith S, Rioux N, Waters NJ, Tang C, Raimondi A, Munchhof M, Mills JE, Ribich S, Porter Scott M, Kuntz KW, Janzen WP, Moyer M, Smith JJ, Chesworth R, Copeland RA, Boriack-Sjodin PA. Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation. PLOS ONE. 2018;13(6):e0197372.
Anti-tumor efficacy of a novel CLK inhibitor via targeting RNA splicing and MYC-dependent vulnerability.
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Mechanisms of skin toxicity associated with metabotropic glutamate receptor 5 negative allosteric modulators.
Shah F, Stepan AF, O’Mahony A, Velichko S, Folias AE, Houle C, Shaffer CL, Marcek J, Whritenour J, Stanton R, Berg EL. Mechanisms of skin toxicity associated with metabotropic glutamate receptor 5 negative allosteric modulators. Cell Chemical Biology. 2017;24(7):858–869.e5.
Phenotypic chemical biology for predicting safety and efficacy.
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Empirical drug discovery: a view from the proteome.
Lee JA, Carragher NO, Berg EL. Empirical drug discovery: a view from the proteome. Drug Discovery Today: Technologies. 2017;23:1–5.
Identification of a chemical probe for family VIII bromodomains through optimization of a fragment hit.
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CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses.
Hammitzsch A, Tallant C, Fedorov O, O’Mahony A, Brennan PE, Hay DA, Martinez FO, Al-Mossawi MH, de Wit J, Vecellio M, Wells C, Wordsworth P, Müller S, Knapp S, Bowness P. CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. PNAS. 2015;112(34):10768–10773.
DMF, but not other fumarates, inhibits NF-κB activity in vitro in an Nrf2-independent manner.
Gillard GO, Collette B, Anderson J, Chao J, Scannevin RH, Huss DJ, Fontenot JD. DMF, but not other fumarates, inhibits NF-κB activity in vitro in an Nrf2-independent manner. Journal of Neuroimmunology. 2015;283:74–85.
Elucidating mechanisms of toxicity using phenotypic data from primary human cell systems—a chemical biology approach for thrombosis-related side effects.
Berg EL, Polokoff MA, O’Mahony A, Nguyen D, Li X. Elucidating mechanisms of toxicity using phenotypic data from primary human cell systems—a chemical biology approach for thrombosis-related side effects. International Journal of Molecular Sciences. 2015;16(1):1008–1029.
Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694.
Zhong Y, Dong S, Strattan E, Ren L, Butchar JP, Thornton K, Mishra A, Porcu P, Bradshaw JM, Bisconte A, Owens TD, Verner E, Brameld KA, Funk JO, Hill RJ, Johnson AJ, Dubovsky JA. Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694. Journal of Biological Chemistry. 2015;290(10):5960–5978.
Complex Primary Human Cell Systems for Drug Discovery. In: Human-based Systems for Translational Research.
Berg EL, O’Mahony A. Complex Primary Human Cell Systems for Drug Discovery. In: Human-based Systems for Translational Research. The Royal Society of Chemistry; 2014; p.88–109. Chapter 5; Edited by Robert Coleman.
Phenotypic screening of the ToxCast chemical library to classify toxic and therapeutic mechanisms.
Kleinstreuer NC, Yang J, Berg EL, Knudsen TB, Richard AM, Martin MT, Reif DM, Judson RS, Polokoff M, Dix DJ, Kavlock RJ, Houck KA. Phenotypic screening of the ToxCast chemical library to classify toxic and therapeutic mechanisms. Nature Biotechnology. 2014;32(6):583–591.
Characterization of novel PI3Kδ inhibitors as potential therapeutics for SLE and lupus nephritis in pre-clinical studies.
Haselmayer P, Camps M, Muzerelle M, El Bawab S, Waltzinger C, Bruns L, Abla N, Polokoff MA, Jond-Necand C, Gaudet M, Benoit A, Bertschy Meier D, Martin C, Gretener D, Lombardi MS, Grenningloh R, Ladel C, Petersen JS, Gaillard P, Ji H. Characterization of novel PI3Kδ inhibitors as potential therapeutics for SLE and lupus nephritis in pre-clinical studies. Frontiers in Immunology. 2014;5:233.
Consideration of the cellular microenvironment: physiologically relevant co-culture systems in drug discovery.
Berg EL, Hsu Y-C, Lee JA. Consideration of the cellular microenvironment: physiologically relevant co-culture systems in drug discovery. Advanced Drug Delivery Reviews. 2014;69–70:190–204.
Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
Ciceri P, Müller S, O’Mahony A, Fedorov O, Filippakopoulos P, Hunt JP, Lasater EA, Pallares G, Picaud S, Wells C, Martin S, Wodicka LM, Shah NP, Treiber DK, Knapp S. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nature Chemical Biology. 2014;10(4):305–312.
Building predictive models for mechanism-of-action classification from phenotypic assay data sets.
Berg EL, Yang J, Polokoff MA. Building predictive models for mechanism-of-action classification from phenotypic assay data sets. Journal of Biomolecular Screening. 2013;18(10):1260–1269.
Regulation of IL-17A production is distinct from IL-17F in a primary human cell co-culture model of T cell-mediated B cell activation.
Melton AC, Melrose J, Alajoki L, Privat S, Cho H, Brown N, Plavec AM, Nguyen D, Johnston ED, Yang J, Polokoff MA, Plavec I, Berg EL, O’Mahony A. Regulation of IL-17A production is distinct from IL-17F in a primary human cell co-culture model of T cell-mediated B cell activation. PLOS ONE. 2013;8(3):e58966.
A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation.
Bergamini G, Bell K, Shimamura S, Werner T, Cansfield A, Müller K, Perrin J, Rau C, Ellard K, Hopf C, Doce C, Leggate D, Mangano R, Mathieson T, O'Mahony A, Plavec I, Rharbaoui F, Reinhard F, Savitski MM, Ramsden N, Hirsch E, Drewes G, Rausch O, Bantscheff M, Neubauer G. A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation. Nature Chemical Biology. 2012;8(6):576–582.
A novel framework for predicting in vivo toxicities from in vitro data using optimal methods for dense and sparse matrix reordering and logistic regression.
DiMaggio PA, Subramani A, Judson RS, Floudas CA. A novel framework for predicting in vivo toxicities from in vitro data using optimal methods for dense and sparse matrix reordering and logistic regression. Toxicological Sciences. 2010;118(1):251–265.
Discovery of dual inhibitors of the immune cell PI3Ks p110δ and p110γ: a prototype for new anti-inflammatory drugs.
Williams O, Houseman BT, Kunkel EJ, Aizenstein B, Hoffman R, Knight ZA, Shokat KM. Discovery of dual inhibitors of the immune cell PI3Ks p110δ and p110γ: a prototype for new anti-inflammatory drugs. Chemistry & Biology. 2010;17(2):123–134.
Chemical target and pathway toxicity mechanisms defined in primary human cell systems.
Berg EL, Yang J, Melrose J, Nguyen D, Privat S, Rosler E, Kunkel EJ, Ekins S. Chemical target and pathway toxicity mechanisms defined in primary human cell systems. Journal of Pharmacological and Toxicological Methods. 2010;61(1):3–15.
Profiling bioactivity of the ToxCast chemical library using BioMAP primary human cell systems.
Houck KA, Dix DJ, Judson RS, Kavlock RJ, Yang J, Berg EL. Profiling bioactivity of the ToxCast chemical library using BioMAP primary human cell systems. Journal of Biomolecular Screening. 2009;14(9):1054–1066.
Characterization of compound mechanisms and secondary activities by BioMAP analysis.
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Biological complexity and drug discovery: a practical systems biology approach.
Berg EL, Kunkel EJ, Hytopoulos E. Biological complexity and drug discovery: a practical systems biology approach. Systems Biology. 2005;152(4):201–206.
Can cell systems biology rescue drug discovery?
Butcher EC. Can cell systems biology rescue drug discovery? Nature Reviews Drug Discovery. 2005; 4(6):461–467.
Rapid structure-activity and selectivity analysis of kinase inhibitors by BioMAP analysis in complex human primary cell-based models.
Kunkel EJ, Plavec I, Nguyen D, Melrose J, Rosler ES, Kao LT, Wang Y, Hytopoulos E, Bishop AC, Bateman R, Shokat KM, Butcher EC, Berg EL. Rapid structure-activity and selectivity analysis of kinase inhibitors by BioMAP analysis in complex human primary cell-based models. Assay and Drug Development Technologies. 2004;2(4):431–441.
An integrative biology approach for analysis of drug action in models of human vascular inflammation.
Kunkel EJ, Dea M, Ebens A, Hytopoulos E, Melrose J, Nguyen D, Ota KS, Plavec I, Wang Y, Watson SR, Butcher EC, Berg EL. An integrative biology approach for analysis of drug action in models of human vascular inflammation. FASEB Journal. 2004;18(11):1279–1281.

Cross-site and cross-platform variability of automated patch clamp assessments of drug effects on human cardiac currents in recombinant cells.
Kramer J, Himmel HM, Lindqvist A, Stoelzle-Feix S, Chaudhary KW, Li D, Bohme GA, Bridgland-Taylor M, Hebeisen S, Fan J, Renganathan M, Imredy J, Humphries E, Brinkwirth N, Strassmaier T, Ohtsuki A, Danker T, Vanoye C, Polonchuk L, Fermini B, Beck Pierson J, Gintant G. Cross-site and cross-platform variability of automated patch clamp assessments of drug effects on human cardiac currents in recombinant cells. Scientific Reports. 2020 Mar 27;10(1):5627
A systematic strategy for estimating hERG block potency and its implications in a new cardiac safety paradigm.
Ridder BJ, Leishman DJ, Bridgland-Taylor M, Samieegohar M, Han X, Wu WW, Randolph A, Tran P, Sheng J, Danker T, Lindqvist A, Konrad D, Hebeisen S, Polonchuk L, Gissinger E, Renganathan M, Koci B, Wei H, Fan J, Levesque P, Kwagh J, Imredy J, Zhai J, Rogers M, Humphries E, Kirby R, Stoelzle-Feix S, Brinkwirth N, Rotordam MG, Becker N, Friis S, Rapedius M, Goetze TA, Strassmaier T, Okeyo G, Kramer J, Kuryshev Y, Wu C, Himmel H, Mirams GR, Strauss DG, Bardenet R, Li Z. A systematic strategy for estimating hERG block potency and its implications in a new cardiac safety paradigm. Toxicol Appl Pharmacol. May 1;394. 2020

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