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Discovery of Novel TLR7 Agonists as Systemic Agent for Combination With aPD1 for Use in Immuno-oncology.
Poudel YB, He L, Cox M, Zhang Q, Johnson WL, Cong Q, Cheng H, Chowdari NS, Tarby C, Donnell AF, Broekema M, O'Malley DP, Zhang Y, A M Subbaiah M, Kumar BV, Subramani L, Wang B, Li YX, Sivaprakasam P, Critton D, Mulligan D, Sandhu B, Xie C, Ramakrishnan R, Nagar J, Dudhgaonkar S, Oderinde MS, Murtaza A, Schieven GL, Mathur A, Gavai AV, Vite G, Gangwar S. Poudel YB, et al. Among authors: he l. ACS Med Chem Lett. 2024 Jan 8;15(2):181-188. doi: 10.1021/acsmedchemlett.3c00455. eCollection 2024 Feb 8. ACS Med Chem Lett. 2024. PMID: 38352830
Identification and Optimization of Small Molecule Pyrazolopyrimidine TLR7 Agonists for Applications in Immuno-oncology.
He L, Zhang MY, Cox M, Zhang Q, Donnell AF, Zhang Y, Tarby C, Gill P, Subbaiah MAM, Ramar T, Reddy M, Puttapaka V, Li YX, Sivaprakasam P, Critton D, Mulligan D, Xie C, Ramakrishnan R, Nagar J, Dudhgaonkar S, Murtaza A, Oderinde MS, Schieven GL, Mathur A, Gavai AV, Vite G, Gangwar S, Poudel YB. He L, et al. ACS Med Chem Lett. 2024 Jan 9;15(2):189-196. doi: 10.1021/acsmedchemlett.3c00456. eCollection 2024 Feb 8. ACS Med Chem Lett. 2024. PMID: 38352849
Modulation of cofilin phosphorylation by inhibition of the Lim family kinases.
He L, Seitz SP, Trainor GL, Tortolani D, Vaccaro W, Poss M, Tarby CM, Tokarski JS, Penhallow B, Hung CY, Attar R, Lin TA. He L, et al. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5995-8. doi: 10.1016/j.bmcl.2012.07.002. Epub 2012 Jul 21. Bioorg Med Chem Lett. 2012. PMID: 22902653
Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.
Gilligan PJ, Clarke T, He L, Lelas S, Li YW, Heman K, Fitzgerald L, Miller K, Zhang G, Marshall A, Krause C, McElroy JF, Ward K, Zeller K, Wong H, Bai S, Saye J, Grossman S, Zaczek R, Arneric SP, Hartig P, Robertson D, Trainor G. Gilligan PJ, et al. Among authors: he l. J Med Chem. 2009 May 14;52(9):3084-92. doi: 10.1021/jm900025h. J Med Chem. 2009. PMID: 19361209
8-(4-Methoxyphenyl)pyrazolo[1,5-a]-1,3,5-triazines: selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists.
Gilligan PJ, He L, Clarke T, Tivitmahaisoon P, Lelas S, Li YW, Heman K, Fitzgerald L, Miller K, Zhang G, Marshall A, Krause C, McElroy J, Ward K, Shen H, Wong H, Grossman S, Nemeth G, Zaczek R, Arneric SP, Hartig P, Robertson DW, Trainor G. Gilligan PJ, et al. Among authors: he l. J Med Chem. 2009 May 14;52(9):3073-83. doi: 10.1021/jm9000242. J Med Chem. 2009. PMID: 19361210
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.
Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Sang X, Frennesson DB, Struzynski C, Seitz SP, He L, Carboni JM, Li A, Greer AF, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Lee FY, Sinz M, Kim S, Vyas D. Zimmermann K, et al. Among authors: he l. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1744-8. doi: 10.1016/j.bmcl.2010.01.087. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20153189
Identification of a nonkinase target mediating cytotoxicity of novel kinase inhibitors.
Ross-Macdonald P, de Silva H, Guo Q, Xiao H, Hung CY, Penhallow B, Markwalder J, He L, Attar RM, Lin TA, Seitz S, Tilford C, Wardwell-Swanson J, Jackson D. Ross-Macdonald P, et al. Among authors: he l. Mol Cancer Ther. 2008 Nov;7(11):3490-8. doi: 10.1158/1535-7163.MCT-08-0826. Mol Cancer Ther. 2008. PMID: 19001433
Non-peptide corticotropin-releasing hormone antagonists: syntheses and structure-activity relationships of 2-anilinopyrimidines and -triazines.
Arvanitis AG, Gilligan PJ, Chorvat RJ, Cheeseman RS, Christos TE, Bakthavatchalam R, Beck JP, Cocuzza AJ, Hobbs FW, Wilde RG, Arnold C, Chidester D, Curry M, He L, Hollis A, Klaczkiewicz J, Krenitsky PJ, Rescinito JP, Scholfield E, Culp S, De Souza EB, Fitzgerald L, Grigoriadis D, Tam SW, Shen HL, et al. Arvanitis AG, et al. Among authors: he l. J Med Chem. 1999 Mar 11;42(5):805-18. doi: 10.1021/jm980222w. J Med Chem. 1999. PMID: 10072679
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