Kun Liu
Merck & Co.
28 Papers
242 Citations
Kun Liu is an academic researcher from Merck & Co.. The author has contributed to research in topics: Peroxisome proliferator-activated receptor & Amide. The author has an hindex of 13, co-authored 28 publications.
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Papers
Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.
Harold G. Selnick,J. Fred Hess,Cuyue Tang,Kun Liu,Joel B. Schachter,Jeanine E. Ballard,Jacob Marcus,Daniel J. Klein,Xiaohai Wang,Michelle Pearson,Mary J. Savage,Ramesh Kaul,Tong-Shuang Li,David J. Vocadlo,Yuanxi Zhou,Yongbao Zhu,Changwei Mu,Yaode Wang,Wei Zhongyong,Chang Bai,Joseph L. Duffy,Ernest J. McEachern +21 more
TL;DR: The medicinal chemistry and pharmacological studies that led to the identification of (3aR,5S,6S,7R, 7aR)-5-(difluoromethyl)-2-(ethylamino)-3a,6,7,7a-tetrahydro-5H-pyrano[3,2-d]thiazole- 6,7-diol 42 (MK-8719) are described.
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Selective PPARγ modulators with improved pharmacological profiles
Kun Liu,Black Regina M,John J. Acton,Ralph T. Mosley,Sheryl D. Debenham,Ramon Abola,Meng Yang,Richard Tschirret-Guth,Lawrence F. Colwell,Cherrie Liu,Margaret Wu,Chuanlin F. Wang,Karen L. MacNaul,Margaret E. McCann,David E. Moller,Joel P. Berger,Peter T. Meinke,A. Brian Jones,Harold B. Wood +18 more
TL;DR: In vivo, these SPPARγMs result in potent glucose lowering in db/db mice and attenuate increases in heart weight and brown adipose tissue that is typically observed in rats upon treatment with PPARγ full agonists.
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Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic Acid (MK-0533): A Novel Selective Peroxisome Proliferator-Activated Receptor γ Modulator for the Treatment of Type 2 Diabetes Mellitus with a Reduced Potential to Increase Plasma and Extracellular Fluid Volume
John J. Acton,Taro E. Akiyama,Ching H. Chang,Lawrence F. Colwell,Sheryl D. Debenham,Thomas W. Doebber,Monica Einstein,Kun Liu,Margaret E. McCann,David E. Moller,Eric S. Muise,Yugen Tan,John R. Thompson,Kenny K. Wong,Margaret Wu,Libo Xu,Peter T. Meinke,Joel P. Berger,Harold B. Wood +18 more
TL;DR: Compound 6 exhibited comparable efficacy to rosiglitazone and pioglitaz one in vivo, however, with regard to the induction of untoward events, 6 displayed no cardiac hypertrophy, attenuated increases in brown adipose tissue, minimal increases in plasma volume, and no increases in extracellular fluid volume in vivo.
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Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.
Hongjun Zhang,Kun Liu,Qinglin Pu,Abdelghani Achab,Michael J. Ardolino,Mangeng Cheng,Yongqi Deng,Amy C. Doty,Heidi Ferguson,Xavier Fradera,Ian Knemeyer,Ravi Kurukulasuriya,Yu-hong Lam,Charles A. Lesburg,Theodore A. Martinot,Meredeth A. McGowan,J. Richard Miller,Karin M. Otte,Purakattle J Biju,Nunzio Sciammetta,Nicolas Solban,Wensheng Yu,H. Zhou,Xiao Wang,David Jonathan Bennett,Yongxin Han +25 more
TL;DR: The discovery of a class of IDO1 heme-binding inhibitors featuring a unique amino-cyclobutarene motif, which was discovered through SBDD from a known and weakly active inhibitor, rendering it a potential drug candidate.
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Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides.
Libo Xu,Amy K. Farthing,James F. Dropinski,Peter T. Meinke,Christine McCallum,Penny Sue Leavitt,Emily Hickey,Lawrence F. Colwell,John F. Barrett,Kun Liu +9 more
TL;DR: Novel water-soluble amide analogs were synthesized from nocathiacin I through the formation of the carboxylic acid intermediate followed by coupling to primary or secondary amines to identify compounds with potent antibacterial activity and adequate water solubility.
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