Publications & References -

Allosteric "beta-blocker" isolated from a DNA-encoded small molecule library.
Ahn S, Kahsai AW, Pani B, Wang QT, Zhao S, Wall AL, Strachan RT, Staus DP, Wingler LM, Sun LD, Sinnaeve J, Choi M, Cho T, Xu TT, Hansen GM, Burnett MB, Lamerdin JE, Bassoni DL, Gavino BJ, Husemoen G, Olsen EK, Franch T, Costanzi S, Chen X, Lefkowitz RJ. Allosteric "beta-blocker" isolated from a DNA-encoded small molecule library. Proc Natl Acad Sci U S A. 2017 Feb 14;114(7):1708-1713. PMID:28130548.
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
New Screening Strategy and Analysis for Identification of Allosteric Modulators for GLP-1 Receptor Using GLP-1(9-36)amide.
Nakane A, Gotoh Y, Ichihara J, Nagata H. New Screening Strategy and Analysis for Identification of Allosteric Modulators for GLP-1 Receptor Using GLP-1(9-36)amide. Anal Biochem. 2015 Sep 2. pii: S0003-2697(15)00412-1. PMID:26341912
Identification of resolvin D2 receptor mediating resolution of infections and organ protection.
Chiang N, Dalli J, Colas RA, Serhan CN. Identification of resolvin D2 receptor mediating resolution of infections and organ protection. J Exp Med. 2015 Jul 27;212(8):1203-17. PMID:26195725
Navigating CYP1A induction and arylhydrocarbon receptor agonism in drug discovery. A case history with S1P1 agonists.
Taylor SJ, Demont EH, Gray J, Deeks N, Patel A, Nguyen D, Taylor M, Hood S, Watson R, Bit RA, McClure F, Ashall H, Witherington J. Navigating CYP1A induction and arylhydrocarbon receptor agonism in drug discovery. A case history with S1P1 agonists. J Med Chem. 2015 Oct 1. PMID:26393276
Ligand-Based Discovery of a New Scaffold for Allosteric Modulation of the mu-Opioid Receptor.
Bisignano P, Burford NT, Shang Y, Marlow B, Livingston K, Fenton AM, Rockwell K, Budenholzer L, Traynor JR, Gerritz SW, Alt A, Filizola M. Ligand-Based Discovery of a New Scaffold for Allosteric Modulation of the mu-Opioid Receptor. J Chem Inf Model. 2015 Sep 28;55(9):1836-43. PMID:26347990
In vitro pharmacological characterization of vorapaxar, a novel platelet thrombin receptor antagonist.
Hawes BE, Zhai Y, Hesk D, Wirth M, Wei H, Chintala M, Seiffert D. In vitro pharmacological characterization of vorapaxar, a novel platelet thrombin receptor antagonist. Eur J Pharmacol. 2015 Sep 5;762:221-8. PMID:26022529
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
Re-Designing of Existing Pharmaceuticals for Environmental Biodegradability: A tiered approach with β-Blocker Propranolol as an example.
Rastogi T, Leder C, Kümmerer K. Re-Designing of Existing Pharmaceuticals for Environmental Biodegradability: A tiered approach with β-Blocker Propranolol as an example. Environ Sci Technol. 2015 Oct 6;49(19):11756-63. PMID:26291878
The novel, orally available and peripherally restricted selective cannabinoid CB2 -receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity.
Mukhopadhyay P, Baggelaar M, Erdelyi K, Cao Z, Cinar R, Fezza F, Ignatowska-Jankowska B, Wilkerson J, van Gils N, Hansen T, Ruben M, Soethoudt M, Heitman L, Kunos G, Maccarrone M, Lichtman A, Pacher P, van der Stelt M. The novel, orally available and peripherally restricted selective cannabinoid CB2 -receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity. Br J Pharmacol. 2015 Sep 23. PMID:26398481
In vitro pharmacological characterization of vorapaxar, a novel platelet thrombin receptor antagonist.
Hawes BE, Zhai Y, Hesk D, Wirth M, Wei H, Chintala M, Seiffert D. In vitro pharmacological characterization of vorapaxar, a novel platelet thrombin receptor antagonist. Eur J Pharmacol. 2015 Sep 5;762:221-8. PMID:26022529
The orexin 1 receptor modulates kappa opioid receptor function via a JNK-dependent mechanism.
Robinson, JD., and McDonald, PH. The orexin 1 receptor modulates kappa opioid receptor function via a JNK-dependent mechanism. Cellular Signaling. 27(7):1449-56. PMID:25857454
Discovery, Synthesis and Molecular Pharmacology of Selective Positive Allosteric Modulators of the δ-Opioid Receptor.
Burford NT, Livingston K, Canals M, Ryan M, Budenholzer L, Han Y, Shang Y, Herbst JJ, O'Connell J, Banks M, Zhang L, Filizola M, Bassoni D, Wehrman TS, Christopoulos A, Traynor JR, Gerritz SW, Alt A. Discovery, Synthesis and Molecular Pharmacology of Selective Positive Allosteric Modulators of the δ-Opioid Receptor. J Med Chem. 58(10):4220-9. PMID:25901762
A novel insulinotropic mechanism of whole grain-derived γ-oryzanol via the suppression of local dopamine D2 receptor signaling in mouse islet.
Kozuka C, Sunagawa S, Ueda R, Higa M, Ohshiro Y, Tanaka H, Shimizu-Okabe C, Takayama C, Matsushita M, Tsutsui M, Ishiuchi S, Nakata M, Yada T, Miyazaki JI, Oyadomari S, Shimabukuro M, Masuzaki H. A novel insulinotropic mechanism of whole grain-derived γ-oryzanol via the suppression of local dopamine D2 receptor signaling in mouse islet. Br J Pharmacol. 2015 Jul 3. PMID:26140534
Identification of the first surrogate agonists for the G protein-coupled receptor GPR132.
Shehata MA, Christensen HB, Isberg V, Pedersen D, Bender A, Bräuner-Osborne H and Gloriam D. Identification of the first surrogate agonists for the G protein-coupled receptor GPR132. RSC Adv., 2015,5, 48551-48557.
Novel Human Cytomegalovirus Viral Chemokines, vCXCL-1s, Display Functional Selectivity for Neutrophil Signaling and Function.
Heo J, Dogra P, Masi TJ, Pitt EA, de Kruijf P, Smit MJ, Sparer TE. Novel Human Cytomegalovirus Viral Chemokines, vCXCL-1s, Display Functional Selectivity for Neutrophil Signaling and Function. J Immunol. 195(1):227-36. PMID:25987741
Boronic acid-containing CXCR1/2 antagonists: Optimization of metabolic stability, in vivo evaluation, and a proposed receptor binding model.
Maedaa DY, Pecka AM, Schulera AD, Quinnb MT, Kirpotinab LN, Wicombc WN, Autend RL, Gundlae R, Zebalaa JA. Boronic acid-containing CXCR1/2 antagonists: Optimization of metabolic stability, in vivo evaluation, and a proposed receptor binding model. Bioorg & Med Chem Let. 25(11):2280-4. PMID:25933594
CCR9-mediated signaling through β-catenin and identification of a novel CCR9 antagonist.
Lee S., Eileen L. Heinrich EL, Li L, Lu J, Choi AH, Levy RA, Wagner JE, Yip MLR, Vaidehi N, Kim J. CCR9-mediated signaling through β-catenin and identification of a novel CCR9 antagonist. Mol Oncol. 2015 May 12. PMID:26003048
4′-O-methylhonokiol increases levels of 2-arachidonoyl glycerol in mouse brain via selective inhibition of its COX-2-mediated oxygenation.
Chicca A, Gachet MS, Petrucci V, Schuehly W, Charles RP, Gertsch J. 4′-O-methylhonokiol increases levels of 2-arachidonoyl glycerol in mouse brain via selective inhibition of its COX-2-mediated oxygenation. J Neuroinflammation. 2015 May 13;12:89. PMID:25962384
Selectivity is species-dependent: Characterization of standard agonists and antagonists at human, rat, and mouse adenosine receptors.
Alnouri MW, Jepards S, Casari A, Schiedel AC, Hinz S, Müller CE. Selectivity is species-dependent: Characterization of standard agonists and antagonists at human, rat, and mouse adenosine receptors. Purinergic Signal. 2015 Sep;11(3):389-407. PMID:26126429

Displaying results 81-100 (of 418)

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Antagonists for the orphan G-protein-coupled receptor GPR55 based on a coumarin scaffold.
Rempel V, Volz N, Gläser F, Nieger M, Bräse S and Müller CE. Antagonists for the orphan G-protein-coupled receptor GPR55 based on a coumarin scaffold. J Med Chem56(11):4798-810. PMID:23679955
8-benzamidochromen-4-one-2-carboxylic acids - potent and selective agonists for the orphan G protein-coupled receptor GPR35.
Funke M, Thimm D, Schiedel AC and Müller CE. 8-benzamidochromen-4-one-2-carboxylic acids - potent and selective agonists for the orphan G protein-coupled receptor GPR35. J Med Chem 56(12):5182-97. PMID:23713606
Bicyclic imidazole-4-one derivatives: a new class of antagonists for the orphan G protein-coupled receptors GPR18 and GPR55.
Rempel V, Atzler K, Behrenswerth A, Karcz T, Schoeder C, Hinz S, Kaleta M, Thimm D, Kiec-Kononowiczb K, Müller CE. Bicyclic imidazole-4-one derivatives: a new class of antagonists for the orphan G protein-coupled receptors GPR18 and GPR55. MedChemComm 5, 632-49.
The natural product magnolol as a lead structure for the development of potent cannabinoid receptor agonists.
Fuchs A, Rempel V and Muller CE. The natural product magnolol as a lead structure for the development of potent cannabinoid receptor agonists. PLoS One. 2013 Oct 30;8(10):e77739. PMID:24204944
Identification of a novel small-molecule agonist for human G protein-coupled receptor 3.
Ye C, Zhang Z, Wang Z, Hua Q, Zhang R, Xie X. Identification of a novel small-molecule agonist for human G protein-coupled receptor 3. J Pharmacol Exp Ther. 349(3):437-43. PMID:24633425
Blockade of SDF-1 after irradiation inhibits tumor recurrences of autochthonous brain tumors in rats.
Liu S, Alomran R, Chernikova SB, Lartey F, Stafford J, Jang T, Merchant M, Zboralski D, Zollner S, Kruschinski A, Klussmann S, Recht L, and Brown MJ. Blockade of SDF-1 after irradiation inhibits tumor recurrences of autochthonous brain tumors in rats. Neuro-Oncol 16(1): 21–8. PMID:24335554
Identification and characterization of small molecule modulators of the Epstein-Barr virus-induced gene 2 (EBI2) receptor.
Gessier F, Preuss I, Yin H, Rosenkilde MM, Laurent S, Endres R, Chen YA, Marsilje TH, Seuwen K, Nguyen DG, Sailer AW. Identification and characterization of small molecule modulators of the Epstein-Barr virus-induced gene 2 (EBI2) receptor. J Med Chem. 57(8):3358-68. PMID:24678947
Molecular characterization of oxysterol binding to the Epstein-Barr virus-induced gene 2 (GPR183).
Benned-Jensen T, Norn C, Laurent S, Madsen CM, Larsen HM, Arfelt KN, Wolf RM, Frimurer T, Sailer AW, Rosenkilde MM. Molecular characterization of oxysterol binding to the Epstein-Barr virus-induced gene 2 (GPR183). J Biol Chem 287(42):35470-83. PMID:22875855
Small molecule antagonism of oxysterol-induced Epstein-Barr virus induced gene 2 (EBI2) activation.
Benned-Jensen T, Madsen CM, Arfelt KN, Smethurts C, Blanchard A, Jepras R, Rosenkilde MM. Small molecule antagonism of oxysterol-induced Epstein-Barr virus induced gene 2 (EBI2) activation. FEBS Open Bio. 19;3:156-60. PMID:23772388
GnRH-(1-5) Transactivates EGFR in Ishikawa Human Endometrial Cells via an Orphan G Protein-Coupled Receptor.
Cho-Clark M, Larco DO, Semsarzadeh NN, Vasta F, Mani SK, Wu TJ. GnRH-(1-5) Transactivates EGFR in Ishikawa Human Endometrial Cells via an Orphan G Protein-Coupled Receptor. Mol Endocrinol 28(1):80-98. PMID:24264576
Activation of GPR18 by cannabinoid compounds: a tale of biased agonism.
Console-Bram L, Brailoiu E, Brailoiu GC, Sharir H, Abood ME. Activation of GPR18 by cannabinoid compounds: a tale of biased agonism. Br J Pharmacol. 171(16):3908-17. PMID:24762058
Boronic Acids as Probes for Investigation of Allosteric Modulation of the Chemokine Receptor CXCR3.
Bernat V, Admas TH, Brox R, Heinemann FW, Tschammer N. Boronic Acids as Probes for Investigation of Allosteric Modulation of the Chemokine Receptor CXCR3. ACS Chem Biol. 9(11):2664-77. PMID:25233453
Chemokine receptor antagonist development.
Garin A, Johnson Z, Hermant A, Beltran F, Ratinaud Y, Michel A, Krohn S, Gaudet M, Carboni S, Ji H, Missotten M, Leger O, Power C and Proudfoot A. Chemokine receptor antagonist development. Methods Mol Biol 1013:67-92. PMID:23625494
A novel CMKLR1 small molecule antagonist suppresses CNS autoimmune inflammatory disease.
Graham KL, Zhang JV, Lewén S, Burke TM, Dang T, Zoudilova M, Sobel RA, Butcher EC, Zabel BA. A novel CMKLR1 small molecule antagonist suppresses CNS autoimmune inflammatory disease. PLoS One. 9(12):e112925. PMID:25437209
Inhibition of metastasis of rhabdomyosarcoma by a novel neutralizing antibody to CXC chemokine receptor-4.
Kashima K, Watanabe M, Sato Y, Hata J, Ishii N, Aoki Y. Inhibition of metastasis of rhabdomyosarcoma by a novel neutralizing antibody to CXC chemokine receptor-4. Cancer Sci 105(10):1343-50. PMID:25154453
Ligand-Biased and Probe-Dependent Modulation of Chemokine Receptor CXCR3 Signaling by Negative Allosteric Modulators.
Bernat V, Brox R, Heinrich MR, Auberson YP, Tschammer N. Ligand-Biased and Probe-Dependent Modulation of Chemokine Receptor CXCR3 Signaling by Negative Allosteric Modulators. ChemMedChem. 10(3):566-74. PMID:25655398
Chemokine cooperativity is caused by competitive glycosaminoglycan binding.
Verkaar F, van Offenbeek J, van der Lee MM, van Lith LH, Watts AO, Rops AL, Aguilar DC, Ziarek JJ, van der Vlag J, Handel TM, Volkman BF, Proudfoot AE, Vischer HF, Zaman GJ, Smit MJ. Chemokine cooperativity is caused by competitive glycosaminoglycan binding. J Immunol 192(8):3908-14. PMID:24639348
Extracellular disulfide bridges serve different purposes in two homologous chemokine receptors, CCR1 and CCR5.
Rummel PC, Thiele S, Hansen LS, Petersen TP, Sparre-Ulrich AH, Ulven T and Rosenkilde MM. Extracellular disulfide bridges serve different purposes in two homologous chemokine receptors, CCR1 and CCR5. Mol Pharm 84(3):335-45. PMID:23765404
Identifying bias in CCR1 antagonists using radiolabelled binding, receptor internalization, β-arrestin translocation andchemotaxis assays.
Gilchrist A, Gauntner TD, Fazzini A, Alley KM, Pyen DS, Ahn J, Ha SJ, Willett A, Sansom SE, Yarfi JL, Bachovchin KA, Mazzoni MR, Merritt JR. Identifying bias in CCR1 antagonists using radiolabelled binding, receptor internalization, β-arrestin translocation andchemotaxis assays. Br J Pharmacol. 171(22):5127-38. PMID:24990525
Surrogate antibodies that specifically bind and neutralize CCL17 but not CCL22.
Santulli-Marotto S, Fisher J, Petley T, Boakye K, Panavas T, Luongo J, Kavalkovich K, Rycyzyn M, Wu B, Gutshall L, Coelho A, Hogaboam CM and Ryan, M. Surrogate antibodies that specifically bind and neutralize CCL17 but not CCL22. Monoclon Antib Immunodiagn Immunother 32(3):162-71. PMID:23750473

Displaying results 81-100 (of 187)

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Discovering cell-active BCL6 inhibitors: effectively combining biochemical HTS with multiple biophysical techniques, X-ray crystallography and cell-based assays
Olivier A. Pierrat, Manjuan Liu, Gavin W. Collie, Kartika Shetty, Matthew J. Rodrigues, Yann-Vaï Le Bihan, Emma A. Gunnell, P. Craig McAndrew, Mark Stubbs, Martin G. Rowlands, Norhakim Yahya, Erald Shehu, Rachel Talbot, Lisa Pickard, Benjamin R. Bellenie, Kwai-Ming J. Cheung, Ludovic Drouin, Paolo Innocenti, Hannah Woodward, Owen A. Davis, Matthew G. Lloyd, Ana Varela, Rosemary Huckvale, Fabio Broccatelli, …Rob L. M. van Montfort
C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays
Yann-Vaï Le Bihana, Rachel M.Lanigana, et al. Eur J of Med. Chem. 2019 Sept 1 (177): 316-337. doi.org/10.1016/j.ejmech.2019.05.041
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

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

Displaying results 21-21 (of 21)

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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

Inhibition of Bitter Taste from Oral Tenofovir Alafenamide.
Schwiebert E, Wang Y, Xi R, Choma K, Streiff J, Flammer LJ, Rivers N, Ozdener MH, Margolskee RF, Christensen CM, Rawson NE, Jiang P, Breslin PAS. Inhibition of Bitter Taste from Oral Tenofovir Alafenamide. Mol Pharmacol. 2021 May;99(5):319-327.
Small-molecule allosteric activators of PDE4 long form cyclic AMP phosphodiesterases.
Omar F, Findlay JE, Carfray G, Allcock RW, Jiang Z, Moore C, Muir AL, Lannoy M, Fertig BA, Mai D, Day JP, Bolger G, Baillie GS, Schwiebert E, Klussmann E, Pyne NJ, Ong ACM, Bowers K, Adam JM, Adams DR, Houslay MD, Henderson DJP. Small-molecule allosteric activators of PDE4 long form cyclic AMP phosphodiesterases. Proc Natl Acad Sci U S A. 2019 Jul 2;116(27):13320-13329.
Use of a rapid human primary cell-based disease screening model to compare next generation products to combustible cigarettes.
Simms L, Mason E, Berg EL, Yu F, Rudd K, Czekala L, Trelles Sticken E, Brinster O, Wieczorek R, Stevenson M, Walele T.
Use of a rapid human primary cell-based disease screening model to compare next generation products to combustible cigarettes.
Current Research in Toxicology. 2021;2:309-321.
Expanding the drug discovery space with predicted metabolite–target interactions.
Nuzzo A, Saha S, Berg E, Jayawickreme C, Tocker J, Brown JR. Expanding the drug discovery space with predicted metabolite–target interactions. Commun Biol. 2021;4:288.
Investigating Molecular Mechanisms of Immunotoxicity and the Utility of ToxCast for Immunotoxicity Screening of Chemicals Added to Food.
Naidenko OV, Andrews DQ, Temkin AM, Stoiber T, Uche UI, Evans S, Perrone-Gray S. Investigating Molecular Mechanisms of Immunotoxicity and the Utility of ToxCast for Immunotoxicity Screening of Chemicals Added to Food. Int J Environ Res Public Health. 2021;18(7):3332.
ILB® resolves inflammatory scarring and promotes functional tissue repair.
Hill LJ, Botfield HF, Begum G, Qureshi O, Vigneswara V, Masood I, Barnes NM, Bruce L, Logan A. ILB® resolves inflammatory scarring and promotes functional tissue repair. NPJ Regen Med. 2021;6:3.
The future of phenotypic drug discovery.
Berg EL. The future of phenotypic drug discovery. Cell Chemical Biology. 2021;28(3):424-430.
Chapter 2: Development and Validation of Disease Assays for Phenotypic Screening.
Berg EL, Denker SP, O’Mahony A. Chapter 2: Development and Validation of Disease Assays for Phenotypic Screening. In: Phenotypic Drug Discovery.; 2020:20-36.
Tapinarof Is a Natural AhR Agonist that Resolves Skin Inflammation in Mice and Humans.
Smith SH, Jayawickreme C, Rickard DJ, Nicodeme E, Bui T, Simmons C, Coquery CM, Neil J, Pryor WM, Mayhew D, Rajpal DK, Creech K, Furst S, Lee J, Wu D, Rastinejad F, Willson TM, Viviani F, Morris DC, Moore JT, Cote-Sierra J. Tapinarof Is a Natural AhR Agonist that Resolves Skin Inflammation in Mice and Humans. J Invest Dermatol. 2017;137(10):2110-2119.
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.
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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.
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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.
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Efficacy of the highly selective focal adhesion kinase inhibitor BI 853520 in adenocarcinoma xenograft models is linked to a mesenchymal tumor phenotype.
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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.
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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.
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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.
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A novel framework for predicting in vivo toxicities from in vitro data using optimal methods for dense and sparse matrix reordering and logistic regression.
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Discovery of dual inhibitors of the immune cell PI3Ks p110δ and p110γ: a prototype for new anti-inflammatory drugs.
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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.
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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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