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Structure-based, multi-targeted drug discovery approach to eicosanoid inhibition: Dual inhibitors of mPGES-1 and 5-lipoxygenase activating protein (FLAP).
Ho JD, Lee MR, Rauch CT, Aznavour K, Park JS, Luz JG, Antonysamy S, Condon B, Maletic M, Zhang A, Hickey MJ, Hughes NE, Chandrasekhar S, Sloan AV, Gooding K, Harvey A, Yu XP, Kahl SD, Norman BH. Ho JD, et al. Among authors: lee mr. Biochim Biophys Acta Gen Subj. 2021 Feb;1865(2):129800. doi: 10.1016/j.bbagen.2020.129800. Epub 2020 Nov 25. Biochim Biophys Acta Gen Subj. 2021. PMID: 33246032
Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics.
Luz JG, Antonysamy S, Kuklish SL, Condon B, Lee MR, Allison D, Yu XP, Chandrasekhar S, Backer R, Zhang A, Russell M, Chang SS, Harvey A, Sloan AV, Fisher MJ. Luz JG, et al. Among authors: lee mr. J Med Chem. 2015 Jun 11;58(11):4727-37. doi: 10.1021/acs.jmedchem.5b00330. Epub 2015 May 20. J Med Chem. 2015. PMID: 25961169
Structural basis for GPR40 allosteric agonism and incretin stimulation.
Ho JD, Chau B, Rodgers L, Lu F, Wilbur KL, Otto KA, Chen Y, Song M, Riley JP, Yang HC, Reynolds NA, Kahl SD, Lewis AP, Groshong C, Madsen RE, Conners K, Lineswala JP, Gheyi T, Saflor MD, Lee MR, Benach J, Baker KA, Montrose-Rafizadeh C, Genin MJ, Miller AR, Hamdouchi C. Ho JD, et al. Among authors: lee mr. Nat Commun. 2018 Apr 25;9(1):1645. doi: 10.1038/s41467-017-01240-w. Nat Commun. 2018. PMID: 29695780 Free PMC article.
Discovery of N-(6-Fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide (LSN 3213128), a Potent and Selective Nonclassical Antifolate Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase (AICARFT) Inhibitor Effective at Tumor Suppression in a Cancer Xenograft Model.
Fales KR, Njoroge FG, Brooks HB, Thibodeaux S, Torrado A, Si C, Toth JL, Mc Cowan JR, Roth KD, Thrasher KJ, Frimpong K, Lee MR, Dally RD, Shepherd TA, Durham TB, Margolis BJ, Wu Z, Wang Y, Atwell S, Wang J, Hui YH, Meier TI, Konicek SA, Geeganage S. Fales KR, et al. Among authors: lee mr. J Med Chem. 2017 Dec 14;60(23):9599-9616. doi: 10.1021/acs.jmedchem.7b01046. Epub 2017 Nov 9. J Med Chem. 2017. PMID: 29072452
Discovery of 5-(1H-indol-5-yl)-1,3,4-thiadiazol-2-amines as potent PIM inhibitors.
Wu B, Wang HL, Cee VJ, Lanman BA, Nixey T, Pettus L, Reed AB, Wurz RP, Guerrero N, Sastri C, Winston J, Lipford JR, Lee MR, Mohr C, Andrews KL, Tasker AS. Wu B, et al. Among authors: lee mr. Bioorg Med Chem Lett. 2015 Feb 15;25(4):775-80. doi: 10.1016/j.bmcl.2014.12.091. Epub 2015 Jan 7. Bioorg Med Chem Lett. 2015. PMID: 25616902
Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2.
Ashton KS, St Jean DJ Jr, Poon SF, Lee MR, Allen JG, Zhang S, Lofgren JA, Zhang X, Fotsch C, Hungate R. Ashton KS, et al. Among authors: lee mr. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5191-6. doi: 10.1016/j.bmcl.2011.07.056. Epub 2011 Jul 23. Bioorg Med Chem Lett. 2011. PMID: 21824779
Discovery of imidazopyridazines as potent Pim-1/2 kinase inhibitors.
Wurz RP, Sastri C, D'Amico DC, Herberich B, Jackson CLM, Pettus LH, Tasker AS, Wu B, Guerrero N, Lipford JR, Winston JT, Yang Y, Wang P, Nguyen Y, Andrews KL, Huang X, Lee MR, Mohr C, Zhang JD, Reid DL, Xu Y, Zhou Y, Wang HL. Wurz RP, et al. Among authors: lee mr. Bioorg Med Chem Lett. 2016 Nov 15;26(22):5580-5590. doi: 10.1016/j.bmcl.2016.09.067. Epub 2016 Oct 1. Bioorg Med Chem Lett. 2016. PMID: 27769621
Discovery of Selective Small Molecule Degraders of BRAF-V600E.
Han XR, Chen L, Wei Y, Yu W, Chen Y, Zhang C, Jiao B, Shi T, Sun L, Zhang C, Xu Y, Lee MR, Luo Y, Plewe MB, Wang J. Han XR, et al. Among authors: lee mr. J Med Chem. 2020 Apr 23;63(8):4069-4080. doi: 10.1021/acs.jmedchem.9b02083. Epub 2020 Apr 10. J Med Chem. 2020. PMID: 32223235
The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors.
Wang HL, Cee VJ, Chavez F Jr, Lanman BA, Reed AB, Wu B, Guerrero N, Lipford JR, Sastri C, Winston J, Andrews KL, Huang X, Lee MR, Mohr C, Xu Y, Zhou Y, Tasker AS. Wang HL, et al. Among authors: lee mr. Bioorg Med Chem Lett. 2015 Feb 15;25(4):834-40. doi: 10.1016/j.bmcl.2014.12.068. Epub 2014 Dec 30. Bioorg Med Chem Lett. 2015. PMID: 25597005
Characterization of a novel AICARFT inhibitor which potently elevates ZMP and has anti-tumor activity in murine models.
Brooks HB, Meier TI, Geeganage S, Fales KR, Thrasher KJ, Konicek SA, Spencer CD, Thibodeaux S, Foreman RT, Hui YH, Roth KD, Qian YW, Wang T, Luo S, Torrado A, Si C, Toth JL, Mc Cowan JR, Frimpong K, Lee MR, Dally RD, Shepherd TA, Durham TB, Wang Y, Wu Z, Iversen PW, Njoroge FG. Brooks HB, et al. Among authors: lee mr. Sci Rep. 2018 Oct 18;8(1):15458. doi: 10.1038/s41598-018-33453-4. Sci Rep. 2018. PMID: 30337562 Free PMC article.
1,262 results