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Your search keyword '"Pai, Lee-Yuh"' showing total 4 results
Start Over Author "Pai, Lee-Yuh" Journal journal of medicinal chemistry
4 results on '"Pai, Lee-Yuh"'

1. Discovery of MK-8153, a Potent and Selective ROMK Inhibitor and Novel Diuretic/Natriuretic

Author

Jiang, Jinlong, primary, Ding, Fa-Xiang, additional, Zhou, Xiaoyan, additional, Bateman, Thomas J., additional, Dong, Shuzhi, additional, Gu, Xin, additional, Keh deJesus, Reynalda, additional, Pio, Barbara, additional, Tang, Haifeng, additional, Chobanian, Harry R., additional, Levorse, Dorothy, additional, Hu, Mengwei, additional, Thomas-Fowlkes, Brande, additional, Margulis, Michael, additional, Koehler, Martin, additional, Weinglass, Adam, additional, Gibson, Jack, additional, Houle, Kevin, additional, Yudkovitz, Joel, additional, Hampton, Caryn, additional, Pai, Lee-Yuh, additional, Samuel, Koppara, additional, Cutarelli, Timothy, additional, Sullivan, Kathleen, additional, Parmee, Emma R., additional, Davies, Ian, additional, and Pasternak, Alexander, additional

Published
2021
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2. Discovery of a Highly Potent, Selective, and Bioavailable Soluble Epoxide Hydrolase Inhibitor with Excellent Ex Vivo Target Engagement

Author

Shen, Hong C., primary, Ding, Fa-Xiang, additional, Wang, Siyi, additional, Deng, Qiaolin, additional, Zhang, Xiaoping, additional, Chen, Yuli, additional, Zhou, Gaochao, additional, Xu, Suoyu, additional, Chen, Hsuan-shen, additional, Tong, Xinchun, additional, Tong, Vincent, additional, Mitra, Kaushik, additional, Kumar, Sanjeev, additional, Tsai, Christine, additional, Stevenson, Andra S., additional, Pai, Lee-Yuh, additional, Alonso-Galicia, Magdalena, additional, Chen, Xiaoli, additional, Soisson, Stephen M., additional, Roy, Sophie, additional, Zhang, Bei, additional, Tata, James R., additional, Berger, Joel P., additional, and Colletti, Steven L., additional

Published
2009
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3. Estrogen Receptor Ligands. II. Discovery of Benzoxathiins as Potent, Selective Estrogen Receptor α Modulators

Author

Kim, Seongkon, primary, Wu, Jane Y., additional, Birzin, Elizabeth T., additional, Frisch, Katalin, additional, Chan, Wanda, additional, Pai, Lee-Yuh, additional, Yang, Yi Tien, additional, Mosley, Ralph T., additional, Fitzgerald, Paula M. D., additional, Sharma, Nandini, additional, Dahllund, Johanna, additional, Thorsell, Ann-Gerd, additional, DiNinno, Frank, additional, Rohrer, Susan P., additional, Schaeffer, James M., additional, and Hammond, Milton L., additional

Published
2004
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4. Estrogen receptor ligands. II. Discovery of benzoxathiins as potent, selective estrogen receptor alpha modulators.

Author

Kim S, Wu JY, Birzin ET, Frisch K, Chan W, Pai LY, Yang YT, Mosley RT, Fitzgerald PM, Sharma N, Dahllund J, Thorsell AG, DiNinno F, Rohrer SP, Schaeffer JM, and Hammond ML

Subjects
Animals, Binding Sites, Binding, Competitive, Cell Line, Crystallography, X-Ray, Estrogen Receptor alpha, Estrogen Receptor beta, Female, Humans, Ligands, Models, Molecular, Molecular Conformation, Organ Size drug effects, Oxathiins chemistry, Oxathiins pharmacology, Receptors, Estrogen drug effects, Receptors, Estrogen metabolism, Selective Estrogen Receptor Modulators chemistry, Selective Estrogen Receptor Modulators pharmacology, Stereoisomerism, Structure-Activity Relationship, Transcriptional Activation, Uterus drug effects, Oxathiins chemical synthesis, Selective Estrogen Receptor Modulators chemical synthesis
Abstract

The discovery and synthesis of dihydrobenzoxathiins as potent, ERalpha subtype selective ligands are described. The most active analogue, 4-D, was found to be 50-fold selective in a competitive binding assay and 100-fold selective in a transactivation assay in HEK-293 cells. The alpha selectivity was postulated to lie in the interaction of the sulfur atom of the benzoxathiin ring with the two discriminating residues in the binding pocket of the receptor isoforms.

Published
2004
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