Publications & References -

A 1536-well cAMP assay for Gs- and Gi-coupled receptors using enzyme fragmentation complementation.
Weber M, Ferrer M, Zheng W, Inglese J, Strulovici B, Kunapuli P.. A 1536-well cAMP assay for Gs- and Gi-coupled receptors using enzyme fragmentation complementation.. Assay Drug Dev Technol. 2004 Feb;2(1):39-49.. PMID:15090209
Identifying orphan G protein coupled receptors in drug discovery
John Dunlop, Richard M Eglen. Identifying orphan G protein coupled receptors in drug discovery. Drug Discovery Today: Technologies. 2004 Sep;1(1):61-68.. DOI:10.1016/j.ddtec.2004.06.004
cAMP detection methods in HTS: selecting the best from the rest.
Williams C.. cAMP detection methods in HTS: selecting the best from the rest.. Nat Rev Drug Discov. 2004 Feb;3(2):125-35.. PMID:15040577
High throughput screening technologies for direct cyclic AMP measurement.
Gabriel D, Vernier M, Pfeifer MJ, Dasen B, Tenaillon L, Bouhelal R.. High throughput screening technologies for direct cyclic AMP measurement.. Assay Drug Dev Technol. 2003 Apr;1(2):291-303.. PMID:15090194
A homogeneous enzyme fragment complementation cyclic AMP screen for GPCR agonists.
Golla R, Seethala R.. A homogeneous enzyme fragment complementation cyclic AMP screen for GPCR agonists.. J Biomol Screen. 2002 Dec;7(6):515-25.. PMID:14599349
A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays.
Zhang JH, Chung TD, Oldenburg KR.. A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays.. J Biomol Screen. 1999;4(2):67-73.. PMID:10838414
Fluorescent and bioluminescent protein-fragment complementation assays in the study of G protein-coupled receptor oligomerization and signaling.
Vidi PA, Watts VJ.. Fluorescent and bioluminescent protein-fragment complementation assays in the study of G protein-coupled receptor oligomerization and signaling.. Mol Pharmacol. 2009 Apr;75(4):733-9. Epub 2009 Jan 13.. PMID:19141658
Signal transduction of the CB1 cannabinoid receptor.
Turu G, Hunyady L.. Signal transduction of the CB1 cannabinoid receptor.. J Mol Endocrinol. 2010 Feb;44(2):75-85. Epub 2009 Jul 20.. PMID:19620237
Review: Hydroxyoctadecadienoic acids: novel regulators of macrophage differentiation and atherogenesis
R. Lee Kennedy, Venkat Vangavet, Bernhard T. Baune. Review: Hydroxyoctadecadienoic acids: novel regulators of macrophage differentiation and atherogenesis. Therapeutic Advances in Endocrinology and Metabolism June 2010 vol. 1 no. 2 51-60 . DOI:10.1177/2042018810375656
Review: Free fatty acid receptors: emerging targets for treatment of diabetes and its complications
R. Lee Kennedy, Venkat Vangavet, Ghassan Jarrod, Venkatesh Shashidhar, Bernhard T. Baune. Review: Free fatty acid receptors: emerging targets for treatment of diabetes and its complications. Therapeutic Advances in Endocrinology and Metabolism October 2010 vol. 1 no. 4 165-175 . doi:10.1177/2042018810381066
Molecular Interactions Between The Human Muscarinic M3 And ß2 Receptors: Evidence For Heterodimerization.
Paola Casarosa, PhD., Ines Kollak, MSc.. Molecular Interactions Between The Human Muscarinic M3 And ß2 Receptors: Evidence For Heterodimerization.. American Journal of Respiratory and Critical Care Medicine Vol 181. pp. A6368, (2010).
Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits beta-arrestin without activating G proteins.
Rosethorne EM and Charlton SJ. Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits beta-arrestin without activating G proteins. Mol Pharmacol 79(4):749-57. PMID:21134907
Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance.
Violin JD, DeWire SM, Yamashita D, Rominger DH, Nguyen L, Schiller K, Whalen EJ, Gowen M, Lark MW.. Selectively engaging β-arrestins at the angiotensin II type 1 receptor reduces blood pressure and increases cardiac performance.. J Pharmacol Exp Ther. 2010 Dec;335(3):572-9. PMID:20801892
The E92K melanocortin 1 receptor mutant induces cAMP production and arrestin recruitment but not ERK activity indicating biased constitutive signaling.
Benned-Jensen T, Mokrosinski J, and Rosenkilde MM. The E92K melanocortin 1 receptor mutant induces cAMP production and arrestin recruitment but not ERK activity indicating biased constitutive signaling. PLoS One. 2011;6(9):e24644. PMID:21931793
Beta-arrestins and cell signaling.
DeWire SM, Ahn S, Lefkowitz RJ, Shenoy SK.. Beta-arrestins and cell signaling.. Annu Rev Physiol. 2007;69:483-510.. PMID:17305471
Beta-arrestin-biased agonism at the beta2-adrenergic receptor.
Drake MT, Violin JD, Whalen EJ, Wisler JW, Shenoy SK, Lefkowitz RJ. Beta-arrestin-biased agonism at the beta2-adrenergic receptor. J Biol Chem. 2008 Feb 29;283(9):5669-76. PMID:18086673
Beta-arrestin-biased ligands at seven-transmembrane receptors.
Violin JD, Lefkowitz RJ.. Beta-arrestin-biased ligands at seven-transmembrane receptors.. Trends Pharmacol Sci. 2007 Aug;28(8):416-22. Epub 2007 Jul 20.. PMID:17644195
Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor.
de Kruijf P, van Heteren J, Lim HD, Conti PG, van der Lee MM, Bosch L, Ho KK, Auld D, Ohlmeyer M, Smit MJ, et al. Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor. J Pharmacol Exp Ther 329(2):783-90. PMID:19190236
Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation.
Ma L, Seager MA, Wittmann M, Jacobson M, Bickel D, Burno M, Jones K, Graufelds VK, Xu G, Pearson M, McCampbell A, Gaspar R, Shughrue P, Danziger A, Regan C, Flick R, Pascarella D, Garson S, Doran S, Kreatsoulas C, Veng L, Lindsley CW, Shipe W, Kuduk S, Sur C, Kinney G, Seabrook GR, Ray WJ.. Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation.. Proc Natl Acad Sci U S A. 2009 Sep 15;106(37):15950-5. Epub 2009 Aug 26.. PMID:19717450
Decoding functional metabolomics with docosahexaenoyl ethanolamide (DHEA) identifies novel bioactive signals.
Yang R, Fredman G, Krishnamoorthy S, Agrawal N, Irimia D, Piomelli D, Serhan CN. Decoding functional metabolomics with docosahexaenoyl ethanolamide (DHEA) identifies novel bioactive signals. J Biol Chem. 2011 Sep 9;286(36):31532-41. PMID:21757729

Displaying results 281-300 (of 349)

|< < 9 10 11 12 13 14 15 16 17 18 > >|

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 181-186 (of 186)

|< < 1 2 3 4 5 6 7 8 9 10 > >|

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

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

resource type

Publications & References