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Page 1
Identification of potent inhibitors of the sortilin-progranulin interaction.
Stachel SJ, Ginnetti AT, Johnson SA, Cramer P, Wang Y, Bukhtiyarova M, Krosky D, Stump C, Hurzy DM, Schlegel KA, Cooke AJ, Allen S, O'Donnell G, Ziebell M, Parthasarathy G, Getty KL, Ho T, Ou Y, Jovanovska A, Carroll SS, Pausch M, Lumb K, Mosser SD, Voleti B, Klein DJ, Soisson SM, Zerbinatti C, Coleman PJ. Stachel SJ, et al. Among authors: klein dj. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127403. doi: 10.1016/j.bmcl.2020.127403. Epub 2020 Jul 15. Bioorg Med Chem Lett. 2020. PMID: 32738972
Structure of the bacterial deacetylase LpxC bound to the nucleotide reaction product reveals mechanisms of oxyanion stabilization and proton transfer.
Clayton GM, Klein DJ, Rickert KW, Patel SB, Kornienko M, Zugay-Murphy J, Reid JC, Tummala S, Sharma S, Singh SB, Miesel L, Lumb KJ, Soisson SM. Clayton GM, et al. Among authors: klein dj. J Biol Chem. 2013 Nov 22;288(47):34073-34080. doi: 10.1074/jbc.M113.513028. Epub 2013 Oct 9. J Biol Chem. 2013. PMID: 24108127 Free PMC article.
Discovery of 2-Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV-1 Integrase Strand Transfer Inhibitors.
Raheem IT, Walji AM, Klein D, Sanders JM, Powell DA, Abeywickrema P, Barbe G, Bennet A, Childers K, Christensen M, Clas SD, Dubost D, Embrey M, Grobler J, Hafey MJ, Hartingh TJ, Hazuda DJ, Kuethe JT, McCabe Dunn J, Miller MD, Moore KP, Nolting A, Pajkovic N, Patel S, Peng Z, Rada V, Rearden P, Schreier JD, Sisko J, Steele TG, Truchon JF, Wai J, Xu M, Coleman PJ. Raheem IT, et al. Among authors: klein d. J Med Chem. 2015 Oct 22;58(20):8154-65. doi: 10.1021/acs.jmedchem.5b01037. Epub 2015 Oct 8. J Med Chem. 2015. PMID: 26397965
Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
Stachel SJ, Zerbinatti C, Rudd MT, Cosden M, Suon S, Nanda KK, Wessner K, DiMuzio J, Maxwell J, Wu Z, Uslaner JM, Michener MS, Szczerba P, Brnardic E, Rada V, Kim Y, Meissner R, Wuelfing P, Yuan Y, Ballard J, Holahan M, Klein DJ, Lu J, Fradera X, Parthasarathy G, Uebele VN, Chen Z, Li Y, Li J, Cooke AJ, Bennett DJ, Bilodeau MT, Renger J. Stachel SJ, et al. Among authors: klein dj. J Med Chem. 2016 Apr 14;59(7):3489-98. doi: 10.1021/acs.jmedchem.6b00176. Epub 2016 Apr 1. J Med Chem. 2016. PMID: 27011007
Discovery and optimization of 2-pyridinone aminal integrase strand transfer inhibitors for the treatment of HIV.
Schreier JD, Embrey MW, Raheem IT, Barbe G, Campeau LC, Dubost D, McCabe Dunn J, Grobler J, Hartingh TJ, Hazuda DJ, Klein D, Miller MD, Moore KP, Nguyen N, Pajkovic N, Powell DA, Rada V, Sanders JM, Sisko J, Steele TG, Wai J, Walji A, Xu M, Coleman PJ. Schreier JD, et al. Among authors: klein d. Bioorg Med Chem Lett. 2017 May 1;27(9):2038-2046. doi: 10.1016/j.bmcl.2017.02.039. Epub 2017 Feb 20. Bioorg Med Chem Lett. 2017. PMID: 28285916
Discovery of a Distinct Chemical and Mechanistic Class of Allosteric HIV-1 Integrase Inhibitors with Antiretroviral Activity.
Burlein C, Wang C, Xu M, Bhatt T, Stahlhut M, Ou Y, Adam GC, Heath J, Klein DJ, Sanders J, Narayan K, Abeywickrema P, Heo MR, Carroll SS, Grobler JA, Sharma S, Diamond TL, Converso A, Krosky DJ. Burlein C, et al. Among authors: klein dj. ACS Chem Biol. 2017 Nov 17;12(11):2858-2865. doi: 10.1021/acschembio.7b00550. Epub 2017 Oct 19. ACS Chem Biol. 2017. PMID: 29024587
Discovery of ethyl ketone-based HDACs 1, 2, and 3 selective inhibitors for HIV latency reactivation.
Yu W, Liu J, Yu Y, Zhang V, Clausen D, Kelly J, Wolkenberg S, Beshore D, Duffy JL, Chung CC, Myers RW, Klein DJ, Fells J, Holloway K, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski J. Yu W, et al. Among authors: klein dj. Bioorg Med Chem Lett. 2020 Jul 1;30(13):127197. doi: 10.1016/j.bmcl.2020.127197. Epub 2020 Apr 15. Bioorg Med Chem Lett. 2020. PMID: 32331932
Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance.
Liu J, Kelly J, Yu W, Clausen D, Yu Y, Kim H, Duffy JL, Chung CC, Myers RW, Carroll S, Klein DJ, Fells J, Holloway MK, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski JA. Liu J, et al. Among authors: klein dj. ACS Med Chem Lett. 2020 Jun 22;11(7):1476-1483. doi: 10.1021/acsmedchemlett.0c00302. eCollection 2020 Jul 9. ACS Med Chem Lett. 2020. PMID: 32676157 Free PMC article.
Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir.
Clausen DJ, Liu J, Yu W, Duffy JL, Chung CC, Myers RW, Klein DJ, Fells J, Holloway K, Wu J, Wu G, Howell BJ, Barnard RJO, Kozlowski J. Clausen DJ, et al. Among authors: klein dj. Bioorg Med Chem Lett. 2020 Sep 1;30(17):127367. doi: 10.1016/j.bmcl.2020.127367. Epub 2020 Jun 26. Bioorg Med Chem Lett. 2020. PMID: 32738976
368 results