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Page 1
Lipid Tales: Optimizing Arylomycin Membrane Anchors.
Koehler MFT, Chen YC, Chen Y, Chen Y, Crawford JJ, Durk MR, Garland K, Hanan EJ, Higuchi RI, Hu H, Ly CQ, Paraselli PG, Roberts TC, Schwarz JB, Smith PA, Yu Z, Heise CE. Koehler MFT, et al. Among authors: schwarz jb. ACS Med Chem Lett. 2023 Oct 11;14(11):1524-1530. doi: 10.1021/acsmedchemlett.3c00327. eCollection 2023 Nov 9. ACS Med Chem Lett. 2023. PMID: 37974942
Optimized arylomycins are a new class of Gram-negative antibiotics.
Smith PA, Koehler MFT, Girgis HS, Yan D, Chen Y, Chen Y, Crawford JJ, Durk MR, Higuchi RI, Kang J, Murray J, Paraselli P, Park S, Phung W, Quinn JG, Roberts TC, Rougé L, Schwarz JB, Skippington E, Wai J, Xu M, Yu Z, Zhang H, Tan MW, Heise CE. Smith PA, et al. Among authors: schwarz jb. Nature. 2018 Sep;561(7722):189-194. doi: 10.1038/s41586-018-0483-6. Epub 2018 Sep 12. Nature. 2018. PMID: 30209367
GluN2A-Selective Pyridopyrimidinone Series of NMDAR Positive Allosteric Modulators with an Improved in Vivo Profile.
Villemure E, Volgraf M, Jiang Y, Wu G, Ly CQ, Yuen PW, Lu A, Luo X, Liu M, Zhang S, Lupardus PJ, Wallweber HJ, Liederer BM, Deshmukh G, Plise E, Tay S, Wang TM, Hanson JE, Hackos DH, Scearce-Levie K, Schwarz JB, Sellers BD. Villemure E, et al. Among authors: schwarz jb. ACS Med Chem Lett. 2016 Oct 31;8(1):84-89. doi: 10.1021/acsmedchemlett.6b00388. eCollection 2017 Jan 12. ACS Med Chem Lett. 2016. PMID: 28105280 Free PMC article.
Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1α Inhibitory Activity.
Beveridge RE, Wallweber HA, Ashkenazi A, Beresini M, Clark KR, Gibbons P, Ghiro E, Kaufman S, Larivée A, Leblanc M, Leclerc JP, Lemire A, Ly C, Rudolph J, Schwarz JB, Srivastava S, Wang W, Zhao L, Braun MG. Beveridge RE, et al. Among authors: schwarz jb. ACS Med Chem Lett. 2020 Oct 16;11(12):2389-2396. doi: 10.1021/acsmedchemlett.0c00344. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335661 Free PMC article.
Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design.
Volgraf M, Sellers BD, Jiang Y, Wu G, Ly CQ, Villemure E, Pastor RM, Yuen PW, Lu A, Luo X, Liu M, Zhang S, Sun L, Fu Y, Lupardus PJ, Wallweber HJ, Liederer BM, Deshmukh G, Plise E, Tay S, Reynen P, Herrington J, Gustafson A, Liu Y, Dirksen A, Dietz MG, Liu Y, Wang TM, Hanson JE, Hackos D, Scearce-Levie K, Schwarz JB. Volgraf M, et al. Among authors: schwarz jb. J Med Chem. 2016 Mar 24;59(6):2760-79. doi: 10.1021/acs.jmedchem.5b02010. Epub 2016 Mar 8. J Med Chem. 2016. PMID: 26919761
A novel NMDA receptor positive allosteric modulator that acts via the transmembrane domain.
Wang TM, Brown BM, Deng L, Sellers BD, Lupardus PJ, Wallweber HJA, Gustafson A, Wong E, Volgraf M, Schwarz JB, Hackos DH, Hanson JE. Wang TM, et al. Among authors: schwarz jb. Neuropharmacology. 2017 Jul 15;121:204-218. doi: 10.1016/j.neuropharm.2017.04.041. Epub 2017 Apr 27. Neuropharmacology. 2017. PMID: 28457974 Free article.
Positive Allosteric Modulators of GluN2A-Containing NMDARs with Distinct Modes of Action and Impacts on Circuit Function.
Hackos DH, Lupardus PJ, Grand T, Chen Y, Wang TM, Reynen P, Gustafson A, Wallweber HJ, Volgraf M, Sellers BD, Schwarz JB, Paoletti P, Sheng M, Zhou Q, Hanson JE. Hackos DH, et al. Among authors: schwarz jb. Neuron. 2016 Mar 2;89(5):983-99. doi: 10.1016/j.neuron.2016.01.016. Epub 2016 Feb 11. Neuron. 2016. PMID: 26875626 Free article.
GluN2A NMDA Receptor Enhancement Improves Brain Oscillations, Synchrony, and Cognitive Functions in Dravet Syndrome and Alzheimer's Disease Models.
Hanson JE, Ma K, Elstrott J, Weber M, Saillet S, Khan AS, Simms J, Liu B, Kim TA, Yu GQ, Chen Y, Wang TM, Jiang Z, Liederer BM, Deshmukh G, Solanoy H, Chan C, Sellers BD, Volgraf M, Schwarz JB, Hackos DH, Weimer RM, Sheng M, Gill TM, Scearce-Levie K, Palop JJ. Hanson JE, et al. Among authors: schwarz jb. Cell Rep. 2020 Jan 14;30(2):381-396.e4. doi: 10.1016/j.celrep.2019.12.030. Cell Rep. 2020. PMID: 31940483 Free PMC article.
Novel, Selective Inhibitors of USP7 Uncover Multiple Mechanisms of Antitumor Activity In Vitro and In Vivo.
Ohol YM, Sun MT, Cutler G, Leger PR, Hu DX, Biannic B, Rana P, Cho C, Jacobson S, Wong ST, Sanchez J, Shah N, Pookot D, Abraham B, Young K, Suthram S, Marshall LA, Bradford D, Kozon N, Han X, Okano A, Maung J, Colas C, Schwarz J, Wustrow D, Brockstedt DG, Kassner PD. Ohol YM, et al. Mol Cancer Ther. 2020 Oct;19(10):1970-1980. doi: 10.1158/1535-7163.MCT-20-0184. Epub 2020 Aug 11. Mol Cancer Ther. 2020. PMID: 32788207
Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model.
Braun MG, Ashkenazi A, Beveridge RE, Castanedo G, Wallweber HA, Beresini MH, Clark KR, De Bruyn T, Fu L, Gibbons P, Jiang F, Kaufman S, Kan D, Kiefer JR, Leclerc JP, Lemire A, Ly C, Segal E, Sims J, Wang W, Wei W, Zhao L, Schwarz JB, Rudolph J. Braun MG, et al. Among authors: schwarz jb. J Med Chem. 2024 May 15. doi: 10.1021/acs.jmedchem.3c02425. Online ahead of print. J Med Chem. 2024. PMID: 38748820
35 results