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The identification of a novel lead class for phosphodiesterase 2 inhibition by fragment-based drug design.
Forster AB, Abeywickrema P, Bunda J, Cox CD, Cabalu TD, Egbertson M, Fay J, Getty K, Hall D, Kornienko M, Lu J, Parthasarathy G, Reid J, Sharma S, Shipe WD, Smith SM, Soisson S, Stachel SJ, Su HP, Wang D, Berger R. Forster AB, et al. Among authors: lu j. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5167-5171. doi: 10.1016/j.bmcl.2017.10.054. Epub 2017 Oct 23. Bioorg Med Chem Lett. 2017. PMID: 29113762
Structure-Guided Design and Procognitive Assessment of a Potent and Selective Phosphodiesterase 2A Inhibitor.
Stachel SJ, Berger R, Nomland AB, Ginnetti AT, Paone DV, Wang D, Puri V, Lange H, Drott J, Lu J, Marcus J, Dwyer MP, Suon S, Uslaner JM, Smith SM. Stachel SJ, et al. Among authors: lu j. ACS Med Chem Lett. 2018 Jul 26;9(8):815-820. doi: 10.1021/acsmedchemlett.8b00214. eCollection 2018 Aug 9. ACS Med Chem Lett. 2018. PMID: 30128073 Free PMC article.
Lead optimization of cathepsin K inhibitors for the treatment of Osteoarthritis.
Ginnetti AT, Paone DV, Nanda KK, Li J, Busuek M, Johnson SA, Lu J, Soisson SM, Robinson R, Fisher J, Webber A, Wesolowski G, Ma B, Duong L, Carroll S, Burgey CS, Stachel SJ. Ginnetti AT, et al. Among authors: lu j. Bioorg Med Chem Lett. 2022 Oct 15;74:128927. doi: 10.1016/j.bmcl.2022.128927. Epub 2022 Aug 6. Bioorg Med Chem Lett. 2022. PMID: 35944849
Tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of left-hand-side moiety (Part-2).
Singh SB, Kaelin DE, Wu J, Miesel L, Tan CM, Black T, Nargund R, Meinke PT, Olsen DB, Lagrutta A, Lu J, Patel S, Rickert KW, Smith RF, Soisson S, Sherer E, Joyce LA, Wei C, Peng X, Wang X, Fukuda H, Kishii R, Takei M, Takano H, Shibasaki M, Yajima M, Nishimura A, Shibata T, Fukuda Y. Singh SB, et al. Among authors: lu j. Bioorg Med Chem Lett. 2015 May 1;25(9):1831-5. doi: 10.1016/j.bmcl.2015.03.044. Epub 2015 Mar 24. Bioorg Med Chem Lett. 2015. PMID: 25851938
Chondroitin sulfate promotes activation of cathepsin K.
Lemaire PA, Huang L, Zhuo Y, Lu J, Bahnck C, Stachel SJ, Carroll SS, Duong LT. Lemaire PA, et al. Among authors: lu j. J Biol Chem. 2014 Aug 1;289(31):21562-72. doi: 10.1074/jbc.M114.559898. Epub 2014 Jun 23. J Biol Chem. 2014. PMID: 24958728 Free PMC article.
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: lu j. 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
From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9.
Petrilli WL, Adam GC, Erdmann RS, Abeywickrema P, Agnani V, Ai X, Baysarowich J, Byrne N, Caldwell JP, Chang W, DiNunzio E, Feng Z, Ford R, Ha S, Huang Y, Hubbard B, Johnston JM, Kavana M, Lisnock JM, Liang R, Lu J, Lu Z, Meng J, Orth P, Palyha O, Parthasarathy G, Salowe SP, Sharma S, Shipman J, Soisson SM, Strack AM, Youm H, Zhao K, Zink DL, Zokian H, Addona GH, Akinsanya K, Tata JR, Xiong Y, Imbriglio JE. Petrilli WL, et al. Among authors: lu j, lu z. Cell Chem Biol. 2020 Jan 16;27(1):32-40.e3. doi: 10.1016/j.chembiol.2019.10.002. Epub 2019 Oct 22. Cell Chem Biol. 2020. PMID: 31653597 Free article.
Discovery of MK-7655, a β-lactamase inhibitor for combination with Primaxin®.
Blizzard TA, Chen H, Kim S, Wu J, Bodner R, Gude C, Imbriglio J, Young K, Park YW, Ogawa A, Raghoobar S, Hairston N, Painter RE, Wisniewski D, Scapin G, Fitzgerald P, Sharma N, Lu J, Ha S, Hermes J, Hammond ML. Blizzard TA, et al. Among authors: lu j. Bioorg Med Chem Lett. 2014 Feb 1;24(3):780-5. doi: 10.1016/j.bmcl.2013.12.101. Epub 2014 Jan 3. Bioorg Med Chem Lett. 2014. PMID: 24433862
Side chain SAR of bicyclic beta-lactamase inhibitors (BLIs). 1. Discovery of a class C BLI for combination with imipinem.
Blizzard TA, Chen H, Kim S, Wu J, Young K, Park YW, Ogawa A, Raghoobar S, Painter RE, Hairston N, Lee SH, Misura A, Felcetto T, Fitzgerald P, Sharma N, Lu J, Ha S, Hickey E, Hermes J, Hammond ML. Blizzard TA, et al. Among authors: lu j. Bioorg Med Chem Lett. 2010 Feb 1;20(3):918-21. doi: 10.1016/j.bmcl.2009.12.069. Epub 2009 Dec 23. Bioorg Med Chem Lett. 2010. PMID: 20044254
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