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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.
Structural basis for selective small molecule kinase inhibition of activated c-Met.
Rickert KW, Patel SB, Allison TJ, Byrne NJ, Darke PL, Ford RE, Guerin DJ, Hall DL, Kornienko M, Lu J, Munshi SK, Reid JC, Shipman JM, Stanton EF, Wilson KJ, Young JR, Soisson SM, Lumb KJ. Rickert KW, et al. Among authors: lu j. J Biol Chem. 2011 Apr 1;286(13):11218-25. doi: 10.1074/jbc.M110.204404. Epub 2011 Jan 18. J Biol Chem. 2011. PMID: 21247903 Free PMC article.
Discovery of kibdelomycin, a potent new class of bacterial type II topoisomerase inhibitor by chemical-genetic profiling in Staphylococcus aureus.
Phillips JW, Goetz MA, Smith SK, Zink DL, Polishook J, Onishi R, Salowe S, Wiltsie J, Allocco J, Sigmund J, Dorso K, Lee S, Skwish S, de la Cruz M, Martín J, Vicente F, Genilloud O, Lu J, Painter RE, Young K, Overbye K, Donald RG, Singh SB. Phillips JW, et al. Among authors: lu j. Chem Biol. 2011 Aug 26;18(8):955-65. doi: 10.1016/j.chembiol.2011.06.011. Chem Biol. 2011. PMID: 21867911
Restoring methicillin-resistant Staphylococcus aureus susceptibility to β-lactam antibiotics.
Tan CM, Therien AG, Lu J, Lee SH, Caron A, Gill CJ, Lebeau-Jacob C, Benton-Perdomo L, Monteiro JM, Pereira PM, Elsen NL, Wu J, Deschamps K, Petcu M, Wong S, Daigneault E, Kramer S, Liang L, Maxwell E, Claveau D, Vaillancourt J, Skorey K, Tam J, Wang H, Meredith TC, Sillaots S, Wang-Jarantow L, Ramtohul Y, Langlois E, Landry F, Reid JC, Parthasarathy G, Sharma S, Baryshnikova A, Lumb KJ, Pinho MG, Soisson SM, Roemer T. Tan CM, et al. Among authors: lu j. Sci Transl Med. 2012 Mar 21;4(126):126ra35. doi: 10.1126/scitranslmed.3003592. Sci Transl Med. 2012. PMID: 22440737
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
Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40.
Lu J, Byrne N, Wang J, Bricogne G, Brown FK, Chobanian HR, Colletti SL, Di Salvo J, Thomas-Fowlkes B, Guo Y, Hall DL, Hadix J, Hastings NB, Hermes JD, Ho T, Howard AD, Josien H, Kornienko M, Lumb KJ, Miller MW, Patel SB, Pio B, Plummer CW, Sherborne BS, Sheth P, Souza S, Tummala S, Vonrhein C, Webb M, Allen SJ, Johnston JM, Weinglass AB, Sharma S, Soisson SM. Lu J, et al. Nat Struct Mol Biol. 2017 Jul;24(7):570-577. doi: 10.1038/nsmb.3417. Epub 2017 Jun 5. Nat Struct Mol Biol. 2017. PMID: 28581512
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
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 A, 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. 2021 Feb 18;28(2):243. doi: 10.1016/j.chembiol.2021.01.019. Cell Chem Biol. 2021. PMID: 33607006 Free article. No abstract available.
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