Publications & References -

Functional selectivity of adenosine receptor ligands.
Verzijl, D., and Ijzerman, A.P.. Functional selectivity of adenosine receptor ligands. Purinergic Signal 2011 7, 171-192. PMID: 21544511
Host protein Ku70 binds and protects HIV-1 integrase from proteasomal degradation and is required for HIV replication.
Zheng Y, Ao Z, Wang B, Jayappa KD, Yao X.. Host protein Ku70 binds and protects HIV-1 integrase from proteasomal degradation and is required for HIV replication.. J Biol Chem. 2011 May 20;286(20):17722-35. Epub 2011 Mar 29.. PMID:21454661
Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers.
Gao, Z.G., Verzijl, D., Zweemer, A., Ye, K., Goblyos, A., Ijzerman, A.P., and Jacobson, K.A.. Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers. Biochem Pharmacol 2011 82, 658-668.
Discovery of novel small molecule activators of β-catenin signaling
Verkaar F, van der Stelt M, Blankesteijn WM, van der Doelen AA, Zaman GJ. Discovery of novel small molecule activators of β-catenin signaling. PLoS One. 2011 Apr 29;6(4):e19185. PMID:21559429
N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.
Banala AK, Levy BA, Khatri SS, Furman CA, Roof, RA, Mishra Y, Griffin SA, Sibley DR, Luedtke RR, and Newman AH. N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity. J Med Chem 54(10):3581-94. PMID:21495689
Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy.
Allen JA, Yost JM, Setola V, Chen X, Sassano MF, Chen M, Peterson S, Yadav PN, Huang XP, Feng B, Jensen NH, Che X, Bai X, Frye SV, Wetsel WC, Caron MG, Javitch JA, Roth BL, Jin J. Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy. Proc Natl Acad Sci USA 108(45):18488-93. PMID:22025698
Teaching old receptors new tricks: biasing seven-transmembrane receptors.
Rajagopal S, Rajagopal K, Lefkowitz RJ.. Teaching old receptors new tricks: biasing seven-transmembrane receptors.. Nat Rev Drug Discov. 2010 May;9(5):373-86.. PMID:20431569
Distinct metabolism of cyclic adenosine monophosphate in regulatory and helper CD4+ T cells.
Bazhin AV, Kahnert S, Kimpfler S, Schadendorf D, Umansky V.. Distinct metabolism of cyclic adenosine monophosphate in regulatory and helper CD4+ T cells.. Mol Immunol. 2010 Jan;47(4):678-84. Epub 2009 Nov 24.. PMID:19939455
Chemical validation of phosphodiesterase C as a chemotherapeutic target in Trypanosoma cruzi, the etiological agent of Chagas' disease.
King-Keller S, Li M, Smith A, Zheng S, Kaur G, Yang X, Wang B, Docampo R.. Chemical validation of phosphodiesterase C as a chemotherapeutic target in Trypanosoma cruzi, the etiological agent of Chagas' disease.. Antimicrob Agents Chemother. 2010 Sep;54(9):3738-45. Epub 2010 Jul 12.. PMID:20625148
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
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
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
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
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
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
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
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
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
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
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

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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 181-184 (of 184)

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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

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

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Publications & References