Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities
Jurica, Elizabeth A., Wu, Ximao, Williams, Kristin N., Haque, Lauren E., Rampulla, Richard A., Mathur, Arvind, Zhou, Min, Cao, Gary, Cai, Hong, Wang, Tao, Liu, Heng, Xu, Carrie, Kunselman, Lori K., Antrilli, Thomas M., Hicks, Michael B., Sun, Qin, Dierks, Elizabeth A., Apedo, Atsu, Moore, Douglas B., Foster, Kimberly A., Cvijic, Mary Ellen, Panemangalore, Reshma, Khandelwal, Purnima, Wilkes, Jason J., Zinker, Bradley A., Robertson, Donald G., Janovitz, Evan B., Galella, Michael, Li, Yi-Xin, Li, Julia, Ramar, Thangeswaran, Jalagam, Prasada Rao, Jayaram, Ramya, Whaley, Jean M., Barrish, Joel C., Robl, Jeffrey A., Ewing, William R., Ellsworth, Bruce A.
Published in Bioorganic & medicinal chemistry (01.05.2023)
Published in Bioorganic & medicinal chemistry (01.05.2023)
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Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists
Shi, Jun, Gu, Zhengxiang, Jurica, Elizabeth Anne, Wu, Ximao, Haque, Lauren E, Williams, Kristin N, Hernandez, Andres S, Hong, Zhenqiu, Gao, Qi, Dabros, Marta, Davulcu, Akin H, Mathur, Arvind, Rampulla, Richard A, Gupta, Arun Kumar, Jayaram, Ramya, Apedo, Atsu, Moore, Douglas B, Liu, Heng, Kunselman, Lori K, Brady, Edward J, Wilkes, Jason J, Zinker, Bradley A, Cai, Hong, Shu, Yue-Zhong, Sun, Qin, Dierks, Elizabeth A, Foster, Kimberly A, Xu, Carrie, Wang, Tao, Panemangalore, Reshma, Cvijic, Mary Ellen, Xie, Chunshan, Cao, Gary G, Zhou, Min, Krupinski, John, Whaley, Jean M, Robl, Jeffrey A, Ewing, William R, Ellsworth, Bruce Alan
Published in Journal of medicinal chemistry (08.02.2018)
Published in Journal of medicinal chemistry (08.02.2018)
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Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode
Jurica, Elizabeth A, Wu, Ximao, Williams, Kristin N, Hernandez, Andres S, Nirschl, David S, Rampulla, Richard A, Mathur, Arvind, Zhou, Min, Cao, Gary, Xie, Chunshan, Jacob, Biji, Cai, Hong, Wang, Tao, Murphy, Brian J, Liu, Heng, Xu, Carrie, Kunselman, Lori K, Hicks, Michael B, Sun, Qin, Schnur, Dora M, Sitkoff, Doree F, Dierks, Elizabeth A, Apedo, Atsu, Moore, Douglas B, Foster, Kimberly A, Cvijic, Mary Ellen, Panemangalore, Reshma, Flynn, Neil A, Maxwell, Brad D, Hong, Yang, Tian, Yuan, Wilkes, Jason J, Zinker, Bradley A, Whaley, Jean M, Barrish, Joel C, Robl, Jeffrey A, Ewing, William R, Ellsworth, Bruce A
Published in Journal of medicinal chemistry (23.02.2017)
Published in Journal of medicinal chemistry (23.02.2017)
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Inducible Sbds deletion impairs bone marrow niche capacity to engraft donor bone marrow after transplantation
Zha, Ji, Kunselman, Lori K., Xie, Hongbo M., Ennis, Brian, Shah, Yash B., Qin, Xia, Fan, Jian-Meng, Babushok, Daria V., Olson, Timothy S.
Published in Blood advances (11.01.2022)
Published in Blood advances (11.01.2022)
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Discovery of an Oxybenzylglycine Based Peroxisome Proliferator Activated Receptor α Selective Agonist 2-((3-((2-(4-Chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic Acid (BMS-687453)
Li, Jun, Kennedy, Lawrence J, Shi, Yan, Tao, Shiwei, Ye, Xiang-Yang, Chen, Stephanie Y, Wang, Ying, Hernández, Andrés S, Wang, Wei, Devasthale, Pratik V, Chen, Sean, Lai, Zhi, Zhang, Hao, Wu, Shung, Smirk, Rebecca A, Bolton, Scott A, Ryono, Denis E, Zhang, Huiping, Lim, Ngiap-Kie, Chen, Bang-Chi, Locke, Kenneth T, O’Malley, Kevin M, Zhang, Litao, Srivastava, Rai Ajit, Miao, Bowman, Meyers, Daniel S, Monshizadegan, Hossain, Search, Debra, Grimm, Denise, Zhang, Rongan, Harrity, Thomas, Kunselman, Lori K, Cap, Michael, Kadiyala, Pathanjali, Hosagrahara, Vinayak, Zhang, Lisa, Xu, Carrie, Li, Yi-Xin, Muckelbauer, Jodi K, Chang, Chiehying, An, Yongmi, Krystek, Stanley R, Blanar, Michael A, Zahler, Robert, Mukherjee, Ranjan, Cheng, Peter T. W, Tino, Joseph A
Published in Journal of medicinal chemistry (08.04.2010)
Published in Journal of medicinal chemistry (08.04.2010)
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Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11β-hydroxydehydrogenase 1 (11β-HSD1)
Wu, Shung C., Yoon, David, Chin, Janice, van Kirk, Katy, Seethala, Ramakrishna, Golla, Rajasree, He, Bin, Harrity, Thomas, Kunselman, Lori K., Morgan, Nathan N., Ponticiello, Randolph P., Taylor, Joseph R., Zebo, Rachel, Harper, Timothy W., Li, Wenying, Wang, Mengmeng, Zhang, Lisa, Sleczka, Bogdan G., Nayeem, Akbar, Sheriff, Steven, Camac, Daniel M., Morin, Paul E., Everlof, John G., Li, Yi-Xin, Ferraro, Cheryl A., Kieltyka, Kasia, Shou, Wilson, Vath, Marianne B., Zvyaga, Tatyana A., Gordon, David A., Robl, Jeffrey A.
Published in Bioorganic & medicinal chemistry letters (15.11.2011)
Published in Bioorganic & medicinal chemistry letters (15.11.2011)
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Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARα Selective Agonist
Shi, Yan, Li, Jun, Kennedy, Lawrence J, Tao, Shiwei, Hernández, Andrés S, Lai, Zhi, Chen, Sean, Wong, Henry, Zhu, Juliang, Trehan, Ashok, Lim, Ngiap-Kie, Zhang, Huiping, Chen, Bang-Chi, Locke, Kenneth T, O’Malley, Kevin M, Zhang, Litao, Srivastava, Rai Ajit, Miao, Bowman, Meyers, Daniel S, Monshizadegan, Hossain, Search, Debra, Grimm, Denise, Zhang, Rongan, Harrity, Thomas, Kunselman, Lori K, Cap, Michael, Muckelbauer, Jodi, Chang, Chiehying, Krystek, Stanley R, Li, Yi-Xin, Hosagrahara, Vinayak, Zhang, Lisa, Kadiyala, Pathanjali, Xu, Carrie, Blanar, Michael A, Zahler, Robert, Mukherjee, Ranjan, Cheng, Peter T. W, Tino, Joseph A
Published in ACS medicinal chemistry letters (09.06.2016)
Published in ACS medicinal chemistry letters (09.06.2016)
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A Novel Series of Highly Potent Benzimidazole-Based Microsomal Triglyceride Transfer Protein Inhibitors
Robl, Jeffrey A, Sulsky, Richard, Sun, Chong-Qing, Simpkins, Ligaya M, Wang, Tammy, Dickson, John K, Chen, Ying, Magnin, David R, Taunk, Prakash, Slusarchyk, William A, Biller, Scott A, Lan, Shih-Jung, Connolly, Fergal, Kunselman, Lori K, Sabrah, Talal, Jamil, Haris, Gordon, David, Harrity, Thomas W, Wetterau, John R
Published in Journal of medicinal chemistry (15.03.2001)
Published in Journal of medicinal chemistry (15.03.2001)
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Orally Active Squalene Synthase Inhibitors: Bis((acyloxy)alkyl) Prodrugs of the α-Phosphonosulfonic Acid Moiety
Dickson, John K, Biller, Scott A, Magnin, David R, Petrillo, Edward W, Hillyer, John W, Hsieh, Dolly C, Lan, Shih-Jung, Rinehart, J. Kent, Gregg, Richard E, Harrity, Thomas W, Jolibois, Kern G, Kalinowski, Stephen S, Kunselman, Lori K, Mookhtiar, Kasim A, Ciosek, Carl P
Published in Journal of medicinal chemistry (02.02.1996)
Published in Journal of medicinal chemistry (02.02.1996)
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Enantioselective Synthesis of α-Phosphono Sulfonate Squalene Synthase Inhibitors: Chiral Recognition in the Interactions of an α-Phosphono Sulfonate Inhibitor with Squalene Synthase
Lawrence, R. Michael, Biller, Scott A, Dickson, John K, Logan, Janette V. H, Magnin, David R, Sulsky, Richard B, DiMarco, John D, Gougoutas, Jack Z, Beyer, Barbara D, Taylor, Susan C, Lan, Shih-Jung, Ciosek, Carl P, Harrity, Thomas W, Jolibois, Kern G, Kunselman, Lori K, Slusarchyk, Dorothy A
Published in Journal of the American Chemical Society (20.11.1996)
Published in Journal of the American Chemical Society (20.11.1996)
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1,1-Bisphosphonate Squalene Synthase Inhibitors: Interplay Between the Isoprenoid Subunit and the Diphosphate Surrogate
Magnin, David R, Dickson, John K, Logan, Janette V, Lawrence, R. Michael, Chen, Ying, Sulsky, Richard B, Ciosek, Carl P, Biller, Scott A, Harrity, Thomas W, Jolibois, Kern G, Kunselman, Lori K, Rich, Lois C, Slusarchyk, Dorothy A
Published in Journal of medicinal chemistry (01.07.1995)
Published in Journal of medicinal chemistry (01.07.1995)
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An MTP Inhibitor that Normalizes Atherogenic Lipoprotein Levels in WHHL Rabbits
Wetterau, John R., Gregg, Richard E., Harrity, Thomas W., Arbeeny, Cynthia, Cap, Michael, Connolly, Fergal, Chu, Ching-Hsuen, George, Rocco J., Gordon, David A., Jamil, Haris, Jolibois, Kern G., Kunselman, Lori K., Lan, Shih-Jung, Maccagnan, Thomas J., Ricci, Beverly, Yan, Mujing, Young, Douglas, Chen, Ying, Fryszman, Olga M., Janette V. H. Logan, Musial, Christa L., Poss, Michael A., Robl, Jeffrey A., Simpkins, Ligaya M., Slusarchyk, William A., Sulsky, Richard, Taunk, Prakash, Magnin, David R., Tino, Joseph A., Lawrence, R. Michael, Dickson, John K., Biller, Scott A.
Published in Science (American Association for the Advancement of Science) (23.10.1998)
Published in Science (American Association for the Advancement of Science) (23.10.1998)
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Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11I super(2)-hydroxydehydrogenase 1 (11I super(2)-HSD1)
Wu, Shung C, Yoon, David, Chin, Janice, Van Kirk, Katy, Seethala, Ramakrishna, Golla, Rajasree, He, Bin, Harrity, Thomas, Kunselman, Lori K, Morgan, Nathan N, Ponticiello, Randolph P, Taylor, Joseph R, Zebo, Rachel, Harper, Timothy W, Li, Wenying, Wang, Mengmeng, Zhang, Lisa, Sleczka, Bogdan G, Nayeem, Akbar, Sheriff, Steven, Camac, Daniel M, Morin, Paul E, Everlof, John G, Li, Yi-Xin, Ferraro, Cheryl A, Kieltyka, Kasia, Shou, Wilson, Vath, Marianne B, Zvyaga, Tatyana A, Gordon, David A, Robl, Jeffrey A
Published in Bioorganic & medicinal chemistry letters (15.11.2011)
Published in Bioorganic & medicinal chemistry letters (15.11.2011)
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Journal Article
Discovery of an Oxybenzylglycine Based Peroxisome Proliferator Activated Receptor [alpha] Selective Agonist 2-((3-((2-(4-Chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic Acid (BMS-687453)
Li, Jun, Kennedy, Lawrence J., Shi, Yan, Tao, Shiwei, Ye, Xiang-Yang, Chen, Stephanie Y., Wang, Ying, Hernndez, Andrs S., Wang, Wei, Devasthale, Pratik V., Chen, Sean, Lai, Zhi, Zhang, Hao, Wu, Shung, Smirk, Rebecca A., Bolton, Scott A., Ryono, Denis E., Zhang, Huiping, Lim, Ngiap-Kie, Chen, Bang-Chi, Locke, Kenneth T., OMalley, Kevin M., Zhang, Litao, Srivastava, Rai Ajit, Miao, Bowman, Meyers, Daniel S., Monshizadegan, Hossain, Search, Debra, Grimm, Denise, Zhang, Rongan, Harrity, Thomas, Kunselman, Lori K., Cap, Michael, Kadiyala, Pathanjali, Hosagrahara, Vinayak, Zhang, Lisa, Xu, Carrie, Li, Yi-Xin, Muckelbauer, Jodi K., Chang, Chiehying, An, Yongmi, Krystek, Stanley R., Blanar, Michael A., Zahler, Robert, Mukherjee, Ranjan, Cheng, Peter T.W., Tino, Joseph A.
Published in Journal of medicinal chemistry (12.04.2010)
Published in Journal of medicinal chemistry (12.04.2010)
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Lipophilic 1,1-bisphosphonates are potent squalene synthase inhibitors and orally active cholesterol lowering agents in vivo
Ciosek, C P, Magnin, D R, Harrity, T W, Logan, J V, Dickson, J K, Gordon, E M, Hamilton, K A, Jolibois, K G, Kunselman, L K, Lawrence, R M
Published in The Journal of biological chemistry (25.11.1993)
Published in The Journal of biological chemistry (25.11.1993)
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