Pharmacological AMPK activation induces transcriptional responses congruent to exercise in skeletal and cardiac muscle, adipose tissues and liver
Muise, Eric S, Guan, Hong-Ping, Liu, Jinqi, Nawrocki, Andrea R, Yang, Xiaodong, Wang, Chuanlin, Rodríguez, Carlos G, Zhou, Dan, Gorski, Judith N, Kurtz, Marc M, Feng, Danqing, Leavitt, Kenneth J, Wei, Lan, Wilkening, Robert R, Apgar, James M, Xu, Shiyao, Lu, Ku, Feng, Wen, Li, Ying, He, Huaibing, Previs, Stephen F, Shen, Xiaolan, van Heek, Margaret, Souza, Sandra C, Rosenbach, Mark J, Biftu, Tesfaye, Erion, Mark D, Kelley, David E, Kemp, Daniel M, Myers, Robert W, Sebhat, Iyassu K
Published in PloS one (27.02.2019)
Published in PloS one (27.02.2019)
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Discovery of MK-8722: A Systemic, Direct Pan-Activator of AMP-Activated Protein Kinase
Feng, Danqing, Biftu, Tesfaye, Romero, F. Anthony, Kekec, Ahmet, Dropinski, James, Kassick, Andrew, Xu, Shiyao, Kurtz, Marc M, Gollapudi, Anantha, Shao, Qing, Yang, Xiaodong, Lu, Ku, Zhou, Gaochao, Kemp, Daniel, Myers, Robert W, Guan, Hong-Ping, Trujillo, Maria E, Li, Cai, Weber, Ann, Sebhat, Iyassu K
Published in ACS medicinal chemistry letters (11.01.2018)
Published in ACS medicinal chemistry letters (11.01.2018)
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Molecular Profiling Reveals a Common Metabolic Signature of Tissue Fibrosis
Zhang, Ji, Muise, Eric S., Han, Seongah, Kutchukian, Peter S., Costet, Philippe, Zhu, Yonghua, Kan, Yanqing, Zhou, Haihong, Shah, Vinit, Huang, Yongcheng, Saigal, Ashmita, Akiyama, Taro E., Shen, Xiao-Lan, Cai, Tian-Quan, Shah, Kashmira, Carballo-Jane, Ester, Zycband, Emanuel, Yi, Lan, Tian, Ye, Chen, Ying, Imbriglio, Jason, Smith, Elizabeth, Devito, Kristine, Conway, James, Ma, Li-Jun, Hoek, Maarten, Sebhat, Iyassu K., Peier, Andrea M., Talukdar, Saswata, McLaren, David G., Previs, Stephen F., Jensen, Kristian K., Pinto, Shirly
Published in Cell reports. Medicine (21.07.2020)
Published in Cell reports. Medicine (21.07.2020)
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Small molecule ligands of the human melanocortin-4 receptor
Ujjainwalla, Feroze, Sebhat, Iyassu K
Published in Current topics in medicinal chemistry (01.06.2007)
Published in Current topics in medicinal chemistry (01.06.2007)
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Design and Pharmacology of N-[(3R)-1,2,3,4-Tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a Potent, Selective, Melanocortin Subtype-4 Receptor Agonist
Sebhat, Iyassu K, Martin, William J, Ye, Zhixiong, Barakat, Khaled, Mosley, Ralph T, Johnston, David B. R, Bakshi, Raman, Palucki, Brenda, Weinberg, David H, MacNeil, Tanya, Kalyani, Rubana N, Tang, Rui, Stearns, Ralph A, Miller, Randy R, Tamvakopoulos, Constantin, Strack, Alison M, McGowan, Erin, Cashen, Doreen E, Drisko, Jennifer E, Hom, Gary J, Howard, Andrew D, MacIntyre, D. Euan, van der Ploeg, Lex H. T, Patchett, Arthur A, Nargund, Ravi P
Published in Journal of medicinal chemistry (10.10.2002)
Published in Journal of medicinal chemistry (10.10.2002)
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Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy
Myers, Robert W., Guan, Hong-Ping, Ehrhart, Juliann, Petrov, Aleksandr, Prahalada, Srinivasa, Tozzo, Effie, Yang, Xiaodong, Kurtz, Marc M., Trujillo, Maria, Trotter, Dinko Gonzalez, Feng, Danqing, Xu, Shiyao, Eiermann, George, Holahan, Marie A., Rubins, Daniel, Conarello, Stacey, Niu, Xiaoda, Souza, Sandra C., Miller, Corin, Liu, Jinqi, Lu, Ku, Feng, Wen, Li, Ying, Painter, Ronald E., Milligan, James A., He, Huaibing, Liu, Franklin, Ogawa, Aimie, Wisniewski, Douglas, Rohm, Rory J., Wang, Liyang, Bunzel, Michelle, Qian, Ying, Zhu, Wei, Wang, Hongwu, Bennet, Bindu, Scheuch, Lisa LaFranco, Fernandez, Guillermo E., Li, Cai, Klimas, Michael, Zhou, Gaochao, van Heek, Margaret, Biftu, Tesfaye, Weber, Ann, Kelley, David E., Thornberry, Nancy, Erion, Mark D., Kemp, Daniel M., Sebhat, Iyassu K.
Published in Science (American Association for the Advancement of Science) (04.08.2017)
Published in Science (American Association for the Advancement of Science) (04.08.2017)
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Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity
Sebhat, Iyassu K, Franklin, Christopher, Lo, Michael M.-C, Chen, David, Jewell, James P, Miller, Randy, Pang, Jianmei, Palyha, Oksana, Kan, Yanqing, Kelly, Theresa M, Guan, Xiao-Ming, Marsh, Donald J, Kosinski, Jennifer A, Metzger, Joseph M, Lyons, Kathryn, Dragovic, Jasminka, Guzzo, Peter R, Henderson, Alan J, Reitman, Marc L, Nargund, Ravi P, Wyvratt, Matthew J, Lin, Linus S
Published in ACS medicinal chemistry letters (13.01.2011)
Published in ACS medicinal chemistry letters (13.01.2011)
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PAN-AMPK Activation Improves Renal Function in a Rat Model of Progressive Diabetic Nephropathy
Zhou, Xiaoyan, Muise, Eric S, Haimbach, Robin, Sebhat, Iyassu K, Zhu, Yonghua, Liu, Franklin, Souza, Sandra C, Kan, Yanqing, Pinto, Shirly, Kelley, David E, Hoek, Maarten
Published in The Journal of pharmacology and experimental therapeutics (01.10.2019)
Published in The Journal of pharmacology and experimental therapeutics (01.10.2019)
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Hit-to-Lead Optimization and Discovery of 5‑((5-([1,1′-Biphenyl]-4-yl)-6-chloro‑1H‑benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase
Lan, Ping, Romero, F. Anthony, Wodka, Dariusz, Kassick, Andrew J, Dang, Qun, Gibson, Tony, Cashion, Daniel, Zhou, Gaochao, Chen, Yuli, Zhang, Xiaoping, Zhang, Aihua, Li, Ying, Trujillo, Maria E, Shao, Qing, Wu, Margaret, Xu, Shiyao, He, Huaibing, MacKenna, Deidre, Staunton, Jocelyn, Chapman, Kevin T, Weber, Ann, Sebhat, Iyassu K, Makara, Gergely M
Published in Journal of medicinal chemistry (09.11.2017)
Published in Journal of medicinal chemistry (09.11.2017)
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Discovery and activity of (1 R,4 S,6 R)- N-[(1 R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist
Ye, Zhixiong, Guo, Liangqin, Barakat, Khaled J., Pollard, Patrick G., Palucki, Brenda L., Sebhat, Iyassu K., Bakshi, Raman K., Tang, Rui, Kalyani, Rubana N., Vongs, Aurawan, Chen, Airu S., Chen, Howard Y., Rosenblum, Charles I., MacNeil, Tanya, Weinberg, David H., Peng, Qianping, Tamvakopoulos, Constantin, Miller, Randy R., Stearns, Ralph A., Cashen, Doreen E., Martin, William J., Metzger, Joseph M., Strack, Alison M., MacIntyre, D. Euan, Van der Ploeg, Lex H.T., Patchett, Arthur A., Wyvratt, Matthew J., Nargund, Ravi P.
Published in Bioorganic & medicinal chemistry letters (01.08.2005)
Published in Bioorganic & medicinal chemistry letters (01.08.2005)
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Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity
He, Shuwen, Ye, Zhixiong, Dobbelaar, Peter H., Bakshi, Raman K., Hong, Qingmei, Dellureficio, James P., Sebhat, Iyassu K., Guo, Liangqin, Liu, Jian, Jian, Tianying, Lai, Yingjie, Franklin, Christopher L., Reibarkh, Mikhail, Holmes, Mark A., Weinberg, David H., MacNeil, Tanya, Tang, Rui, Tamvakopoulos, Constantin, Peng, Qianping, Miller, Randy R., Stearns, Ralph A., Chen, Howard Y., Chen, Airu S., Strack, Alison M., Fong, Tung M., Wyvratt, Matthew J., Nargund, Ravi P.
Published in Bioorganic & medicinal chemistry letters (15.11.2010)
Published in Bioorganic & medicinal chemistry letters (15.11.2010)
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Synthesis and SAR of heterocyclic carboxylic acid isosteres based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity
Hadden, Mark, Goodman, Allan, Guo, Cheng, Guzzo, Peter R., Henderson, Alan J., Pattamana, Kevin, Ruenz, Megan, Sargent, Bruce J., Swenson, Brian, Yet, Larry, Liu, Jian, He, Shuwen, Sebhat, Iyassu K., Lin, Linus S., Tamvakopoulos, Constantin, Peng, Qianping, Kan, Yanqing, Palyha, Oksana, Kelly, Theresa M., Guan, Xiao-Ming, Metzger, Joseph M., Reitman, Marc L., Nargund, Ravi P.
Published in Bioorganic & medicinal chemistry letters (01.05.2010)
Published in Bioorganic & medicinal chemistry letters (01.05.2010)
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Journal Article
Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity
Liu, Jian, He, Shuwen, Jian, Tianying, Dobbelaar, Peter H., Sebhat, Iyassu K., Lin, Linus S., Goodman, Allan, Guo, Cheng, Guzzo, Peter R., Hadden, Mark, Henderson, Alan J., Pattamana, Kevin, Ruenz, Megan, Sargent, Bruce J, Swenson, Brian, Yet, Larry, Tamvakopoulos, Constantin, Peng, Qianping, Pan, Jie, Kan, Yanqing, Palyha, Oksana, Kelly, Theresa M., Guan, Xiao-Ming, Howard, Andrew D., Marsh, Donald J., Metzger, Joseph M., Reitman, Marc L., Wyvratt, Matthew J., Nargund, Ravi P.
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
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A new class of prolylcarboxypeptidase inhibitors, Part 1: Discovery and evaluation
Graham, Thomas H., Liu, Wensheng, Verras, Andreas, Sebhat, Iyassu K., Xiong, Yusheng, Bleasby, Kelly, Bhatt, Urmi R., Chen, Qing, Garcia-Calvo, Margarita, Geissler, Wayne M., Gorski, Judith N., He, Huaibing, Lassman, Michael E., Lisnock, JeanMarie, Li, Xiaohua, Shen, Zhu, Tong, Xinchun, Tung, Elaine C., Wiltsie, Judyann, Xiao, Jianying, Xie, Dan, Xu, Suoyu, Hale, Jeffrey J., Pinto, Shirly, Shen, Dong-Ming
Published in Bioorganic & medicinal chemistry letters (15.04.2012)
Published in Bioorganic & medicinal chemistry letters (15.04.2012)
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Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists
He, Shuwen, Dobbelaar, Peter H., Liu, Jian, Jian, Tianying, Sebhat, Iyassu K., Lin, Linus S., Goodman, Allan, Guo, Cheng, Guzzo, Peter R., Hadden, Mark, Henderson, Alan J., Ruenz, Megan, Sargent, Bruce J., Yet, Larry, Kelly, Theresa M., Palyha, Oksana, Kan, Yanqing, Pan, Jie, Chen, Howard, Marsh, Donald J., Shearman, Lauren P., Strack, Alison M., Metzger, Joseph M., Feighner, Scott D., Tan, Carina, Howard, Andrew D., Tamvakopoulos, Constantin, Peng, Qianping, Guan, Xiao-Ming, Reitman, Marc L., Patchett, Arthur A., Wyvratt, Matthew J., Nargund, Ravi P.
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
Published in Bioorganic & medicinal chemistry letters (15.03.2010)
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Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist
Hong, Qingmei, Bakshi, Raman K., Palucki, Brenda L., Park, Min K., Ye, Zhixiong, He, Shuwen, Pollard, Patrick G., Sebhat, Iyassu K., Liu, Jian, Guo, Liangqin, Cashen, Doreen E., Martin, William J., Weinberg, David H., MacNeil, Tanya, Tang, Rui, Tamvakopoulos, Constantin, Peng, Qianping, Miller, Randy R., Stearns, Ralph A., Chen, Howard Y., Chen, Airu S., Strack, Alison M., Fong, Tung M., MacIntyre, D. Euan, Wyvratt, Matthew J., Nargund, Ravi P.
Published in Bioorganic & medicinal chemistry letters (15.04.2011)
Published in Bioorganic & medicinal chemistry letters (15.04.2011)
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Journal Article
Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist
He, Shuwen, Ye, Zhixiong, Dobbelaar, Peter H., Sebhat, Iyassu K., Guo, Liangqin, Liu, Jian, Jian, Tianying, Lai, Yingjie, Franklin, Christopher L., Bakshi, Raman K., Dellureficio, James P., Hong, Qingmei, Tsou, Nancy N., Ball, Richard G., Cashen, Doreen E., Martin, William J., Weinberg, David H., MacNeil, Tanya, Tang, Rui, Tamvakopoulos, Constantin, Peng, Qianping, Miller, Randy R., Stearns, Ralph A., Chen, Howard Y., Chen, Airu S., Strack, Alison M., Fong, Tung M., MacIntyre, D. Euan, Wyvratt, Matthew J., Nargund, Ravi P.
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
Published in Bioorganic & medicinal chemistry letters (01.04.2010)
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Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity
He, Shuwen, Ye, Zhixiong, Dobbelaar, Peter H., Sebhat, Iyassu K., Guo, Liangqin, Liu, Jian, Jian, Tianying, Lai, Yingjie, Franklin, Christopher L., Bakshi, Raman K., Dellureficio, James P., Hong, Qingmei, Weinberg, David H., MacNeil, Tanya, Tang, Rui, Strack, Alison M., Tamvakopoulos, Constantin, Peng, Qianping, Miller, Randy R., Stearns, Ralph A., Chen, Howard Y., Chen, Airu S., Fong, Tung M., Wyvratt, Matthew J., Nargund, Ravi P.
Published in Bioorganic & medicinal chemistry letters (01.08.2010)
Published in Bioorganic & medicinal chemistry letters (01.08.2010)
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Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists
LIANGQIN GUO, ZHIXIONG YE, TSOU, Nancy N, BALL, Richard G, WEINBERG, David H, MACNEIL, Tanya, RUI TANG, TAMVAKOPOULOS, Constantin, QIANPING PENG, CHEN, Howard Y, CHEN, Airu S, MARTIN, William J, JIAN LIU, EUAN MACINTYRE, D, STRACK, Alison M, FONG, Tung M, WYVRATT, Matthew J, NARGUND, Ravi P, SHUWEN HE, BAKSHI, Raman K, SEBHAT, Iyassu K, DOBBELAAR, Peter H, QINGMEI HONG, TIANYING JIAN, DELLUREFICIO, James P
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
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