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DGKα/ζ inhibitors combine with PD-1 checkpoint therapy to promote T cell-mediated antitumor immunity.
Wichroski M, Benci J, Liu SQ, Chupak L, Fang J, Cao C, Wang C, Onorato J, Qiu H, Shan Y, Banas D, Powles R, Locke G, Witt A, Stromko C, Qi H, Zheng X, Martin S, Ding M, Gentles R, Meanwell N, Velaparthi U, Olson R, Wee S, Tenney D, Parker CG, Cravatt BF, Lawrence M, Borzilleri R, Lees E. Wichroski M, et al. Among authors: olson r. Sci Transl Med. 2023 Oct 25;15(719):eadh1892. doi: 10.1126/scitranslmed.adh1892. Epub 2023 Oct 25. Sci Transl Med. 2023. PMID: 37878674
Development of New Benzenesulfonamides As Potent and Selective Nav1.7 Inhibitors for the Treatment of Pain.
Wu YJ, Guernon J, Shi J, Ditta J, Robbins KJ, Rajamani R, Easton A, Newton A, Bourin C, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Bristow LJ, Meanwell NA, Olson R, Thompson LA, Dzierba C. Wu YJ, et al. Among authors: olson r. J Med Chem. 2017 Mar 23;60(6):2513-2525. doi: 10.1021/acs.jmedchem.6b01918. Epub 2017 Mar 10. J Med Chem. 2017. PMID: 28234467
Discovery of morpholine-based aryl sulfonamides as Nav1.7 inhibitors.
Wu YJ, Guernon J, McClure A, Venables B, Rajamani R, Robbins KJ, Knox RJ, Matchett M, Pieschl RL, Herrington J, Bristow LJ, Meanwell NA, Olson R, Thompson LA, Dzierba C. Wu YJ, et al. Among authors: olson r. Bioorg Med Chem Lett. 2018 Mar 1;28(5):958-962. doi: 10.1016/j.bmcl.2018.01.035. Epub 2018 Feb 1. Bioorg Med Chem Lett. 2018. PMID: 29439904
Discovery of non-zwitterionic aryl sulfonamides as Nav1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation.
Wu YJ, Guernon J, McClure A, Luo G, Rajamani R, Ng A, Easton A, Newton A, Bourin C, Parker D, Mosure K, Barnaby O, Soars MG, Knox RJ, Matchett M, Pieschl R, Herrington J, Chen P, Sivarao DV, Bristow LJ, Meanwell NA, Bronson J, Olson R, Thompson LA, Dzierba C. Wu YJ, et al. Among authors: olson r. Bioorg Med Chem. 2017 Oct 15;25(20):5490-5505. doi: 10.1016/j.bmc.2017.08.012. Epub 2017 Aug 9. Bioorg Med Chem. 2017. PMID: 28818462
Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors.
Gavai AV, Quesnelle C, Norris D, Han WC, Gill P, Shan W, Balog A, Chen K, Tebben A, Rampulla R, Wu DR, Zhang Y, Mathur A, White R, Rose A, Wang H, Yang Z, Ranasinghe A, D'Arienzo C, Guarino V, Xiao L, Su C, Everlof G, Arora V, Shen DR, Cvijic ME, Menard K, Wen ML, Meredith J, Trainor G, Lombardo LJ, Olson R, Baran PS, Hunt JT, Vite GD, Fischer BS, Westhouse RA, Lee FY. Gavai AV, et al. Among authors: olson r. ACS Med Chem Lett. 2015 Mar 11;6(5):523-7. doi: 10.1021/acsmedchemlett.5b00001. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005526 Free PMC article.
BMS-986163, a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder.
Marcin LR, Warrier J, Thangathirupathy S, Shi J, Karageorge GN, Pearce BC, Ng A, Park H, Kempson J, Li J, Zhang H, Mathur A, Reddy AB, Nagaraju G, Tonukunuru G, Gupta GVRKM, Kamble M, Mannoori R, Cheruku S, Jogi S, Gulia J, Bastia T, Sanmathi C, Aher J, Kallem R, Srikumar BN, Vijaya KK, Naidu PS, Paschapur M, Kalidindi N, Vikramadithyan R, Ramarao M, Denton R, Molski T, Shields E, Subramanian M, Zhuo X, Nophsker M, Simmermacher J, Sinz M, Albright C, Bristow LJ, Islam I, Bronson JJ, Olson RE, King D, Thompson LA, Macor JE. Marcin LR, et al. Among authors: olson re. ACS Med Chem Lett. 2018 Apr 13;9(5):472-477. doi: 10.1021/acsmedchemlett.8b00080. eCollection 2018 May 10. ACS Med Chem Lett. 2018. PMID: 29795762 Free PMC article.
Identification and characterization of a MAPT-targeting locked nucleic acid antisense oligonucleotide therapeutic for tauopathies.
Easton A, Jensen ML, Wang C, Hagedorn PH, Li Y, Weed M, Meredith JE, Guss V, Jones K, Gill M, Krause C, Brown JM, Hunihan L, Natale J, Fernandes A, Lu Y, Polino J, Bookbinder M, Cadelina G, Benitex Y, Sane R, Morrison J, Drexler D, Mercer SE, Bon C, Pandya NJ, Jagasia R, Ou Yang TH, Distler T, Grüninger F, Meldgaard M, Terrigno M, Macor JE, Albright CF, Loy J, Hoeg AM, Olson RE, Cacace AM. Easton A, et al. Among authors: olson re. Mol Ther Nucleic Acids. 2022 Aug 4;29:625-642. doi: 10.1016/j.omtn.2022.07.027. eCollection 2022 Sep 13. Mol Ther Nucleic Acids. 2022. PMID: 36090761 Free PMC article.
Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481.
Boy KM, Guernon JM, Zuev DS, Xu L, Zhang Y, Shi J, Marcin LR, Higgins MA, Wu YJ, Krishnananthan S, Li J, Trehan A, Smith D, Toyn JH, Meredith JE, Burton CR, Kimura SR, Zvyaga T, Zhuo X, Lentz KA, Grace JE, Denton R, Morrison JS, Mathur A, Albright CF, Ahlijanian MK, Olson RE, Thompson LA, Macor JE. Boy KM, et al. Among authors: olson re. ACS Med Chem Lett. 2019 Feb 17;10(3):312-317. doi: 10.1021/acsmedchemlett.8b00541. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891132 Free PMC article.
Effects of BMS-902483, an α7 nicotinic acetylcholine receptor partial agonist, on cognition and sensory gating in relation to receptor occupancy in rodents.
Pieschl RL, Miller R, Jones KM, Post-Munson DJ, Chen P, Newberry K, Benitex Y, Molski T, Morgan D, McDonald IM, Macor JE, Olson RE, Asaka Y, Digavalli S, Easton A, Herrington J, Westphal RS, Lodge NJ, Zaczek R, Bristow LJ, Li YW. Pieschl RL, et al. Among authors: olson re. Eur J Pharmacol. 2017 Jul 15;807:1-11. doi: 10.1016/j.ejphar.2017.04.024. Epub 2017 Apr 22. Eur J Pharmacol. 2017. PMID: 28438647
2,106 results