Selective Small-Molecule Agonists of G Protein–Coupled Receptor 40 Promote Glucose-Dependent Insulin Secretion and Reduce Blood Glucose in Mice
Tan, Carina P, Feng, Yue, Zhou, Yun-Ping, Eiermann, George J, Petrov, Aleksandr, Zhou, Changyou, Lin, Songnian, Salituro, Gino, Meinke, Peter, Mosley, Ralph, Akiyama, Taro E, Einstein, Monica, Kumar, Sanjeev, Berger, Joel P, Mills, Sander G, Thornberry, Nancy A, Yang, Lihu, Howard, Andrew D
Published in Diabetes (New York, N.Y.) (01.08.2008)
Published in Diabetes (New York, N.Y.) (01.08.2008)
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Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists
Zhou, Changyou, Tang, Cheng, Chang, Eric, Ge, Min, Lin, Songnian, Cline, Eric, Tan, Carina P., Feng, Yue, Zhou, Yun-Ping, Eiermann, George J., Petrov, Aleksandr, Salituro, Gino, Meinke, Peter, Mosley, Ralph, Akiyama, Taro E., Einstein, Monica, Kumar, Sanjeev, Berger, Joel, Howard, Andrew D., Thornberry, Nancy, Mills, Sander G., Yang, Lihu
Published in Bioorganic & medicinal chemistry letters (01.02.2010)
Published in Bioorganic & medicinal chemistry letters (01.02.2010)
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Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors
Xu, Jinyou, Wei, Lan, Mathvink, Robert J., Edmondson, Scott D., Eiermann, George J., He, Huaibing, Leone, Joseph F., Leiting, Barbara, Lyons, Kathryn A., Marsilio, Frank, Patel, Reshma A., Patel, Sangita B., Petrov, Aleksandr, Scapin, Giovanna, Wu, Joseph K., Thornberry, Nancy A., Weber, Ann E.
Published in Bioorganic & medicinal chemistry letters (15.10.2006)
Published in Bioorganic & medicinal chemistry letters (15.10.2006)
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Differential effects of oxyntomodulin and GLP-1 on glucose metabolism
Du, Xiaobing, Kosinski, Jennifer R, Lao, Julie, Shen, Xiaolan, Petrov, Aleksandr, Chicchi, Gary G, Eiermann, George J, Pocai, Alessandro
Published in American journal of physiology: endocrinology and metabolism (15.07.2012)
Published in American journal of physiology: endocrinology and metabolism (15.07.2012)
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Inhibition of DPP-4 with sitagliptin improves glycemic control and restores islet cell mass and function in a rodent model of type 2 diabetes
Mu, James, Petrov, Aleksandr, Eiermann, George J., Woods, John, Zhou, Yun-Ping, Li, Zhihua, Zycband, Emanuel, Feng, Yue, Zhu, Lan, Roy, Ranabir Sinha, Howard, Andrew D., Li, Cai, Thornberry, Nancy A., Zhang, Bei B.
Published in European journal of pharmacology (25.11.2009)
Published in European journal of pharmacology (25.11.2009)
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Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes : Potential importance of selectivity over dipeptidyl peptidases 8 and 9
LANKAS, George R, LEITING, Barbara, IPPOLITO, Dawn E, KIM, Dooseop, LYONS, Kathryn A, OK, Hyun O, PATEL, Reshma A, PETROV, Aleksandr N, PRYOR, Kelly Ann, XIAOXIA QIAN, REIGLE, Leah, WOODS, Andrea, ROY, Ranabir Sinha, WU, Joseph K, ZALLER, Dennis, XIAOPING ZHANG, LAN ZHU, WEBER, Ann E, THORNBERRY, Nancy A, EIERMANN, George J, BECONI, Maria G, BIFTU, Tesfaye, CHAN, Chi-Chung, EDMONDSON, Scott, FEENEY, William P, HUAIBING HE
Published in Diabetes (New York, N.Y.) (01.10.2005)
Published in Diabetes (New York, N.Y.) (01.10.2005)
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Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus
Xu, Jiayi, Lin, Songnian, Myers, Robert W., Addona, George, Berger, Joel P., Campbell, Brian, Chen, Hsuan-shen, Chen, Zhesheng, Eiermann, George J., Elowe, Nadine H., Farrer, Brian T., Feng, Wen, Fu, Qinghong, Kats-Kagan, Roman, Kavana, Michael, Malkani, Sunita, McMasters, Daniel R., Mitra, Kaushik, Pachanski, Michele J., Tong, Xinchun, Trujillo, Maria E., Xu, Libo, Zhang, Bei, Zhang, Fengqi, Zhang, Rui, Parmee, Emma R.
Published in Bioorganic & medicinal chemistry letters (01.05.2017)
Published in Bioorganic & medicinal chemistry letters (01.05.2017)
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Quantifying rates of glucose production in vivo following an intraperitoneal tracer bolus
Wang, Sheng-Ping, Zhou, Dan, Yao, Zuliang, Satapati, Santhosh, Chen, Ying, Daurio, Natalie A, Petrov, Aleksandr, Shen, Xiaolan, Metzger, Daniel, Yin, Wu, Nawrocki, Andrea R, Eiermann, George J, Hwa, Joyce, Fancourt, Craig, Miller, Corin, Herath, Kithsiri, Roddy, Thomas P, Slipetz, Deborah, Erion, Mark D, Previs, Stephen F, Kelley, David E
Published in American journal of physiology: endocrinology and metabolism (01.12.2016)
Published in American journal of physiology: endocrinology and metabolism (01.12.2016)
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A comparative study of the binding properties, dipeptidyl peptidase‐4 (DPP‐4) inhibitory activity and glucose‐lowering efficacy of the DPP‐4 inhibitors alogliptin, linagliptin, saxagliptin, sitagliptin and vildagliptin in mice
Berger, Joel P., SinhaRoy, Ranabir, Pocai, Alessandro, Kelly, Theresa M., Scapin, Giovanna, Gao, Ying‐Duo, Pryor, Kelly Ann D., Wu, Joseph K., Eiermann, George J., Xu, Shiyao S., Zhang, Xiaoping, Tatosian, Daniel A., Weber, Ann E., Thornberry, Nancy A., Carr, Richard D.
Published in Endocrinology, diabetes & metabolism (01.01.2018)
Published in Endocrinology, diabetes & metabolism (01.01.2018)
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Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus
Xu, Jiayi, Lin, Songnian, Myers, Robert W., Trujillo, Maria E., Pachanski, Michele J., Malkani, Sunita, Chen, Hsuan-shen, Chen, Zhesheng, Campbell, Brian, Eiermann, George J., Elowe, Nadine, Farrer, Brian T., Feng, Wen, Fu, Qinghong, Kats-Kagan, Roman, Kavana, Michael, McMasters, Daniel R., Mitra, Kaushik, Tong, Xinchun, Xu, Libo, Zhang, Fengqi, Zhang, Rui, Addona, George H., Berger, Joel P., Zhang, Bei, Parmee, Emma R.
Published in Bioorganic & medicinal chemistry letters (01.05.2017)
Published in Bioorganic & medicinal chemistry letters (01.05.2017)
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(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]- pyridin-6-ylphenyl)butanamide: A Selective α-Amino Amide Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
Edmondson, Scott D, Mastracchio, Anthony, Mathvink, Robert J, He, Jiafang, Harper, Bart, Park, You-Jung, Beconi, Maria, Di Salvo, Jerry, Eiermann, George J, He, Huaibing, Leiting, Barbara, Leone, Joseph F, Levorse, Dorothy A, Lyons, Kathryn, Patel, Reshma A, Patel, Sangita B, Petrov, Aleksandr, Scapin, Giovanna, Shang, Jackie, Roy, Ranabir Sinha, Smith, Aaron, Wu, Joseph K, Xu, Shiyao, Zhu, Bing, Thornberry, Nancy A, Weber, Ann E
Published in Journal of medicinal chemistry (15.06.2006)
Published in Journal of medicinal chemistry (15.06.2006)
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SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists
He, Shuwen, Dobbelaar, Peter H., Guo, Liangqin, Ye, Zhixiong, Liu, Jian, Jian, Tianying, Truong, Quang, Shah, Shrenik K., Du, Wu, Qi, Hongbo, Bakshi, Raman K., Hong, Qingmei, Dellureficio, James D., Sherer, Edward, Pasternak, Alexander, Feng, Zhe, Reibarkh, Mikhail, Lin, Melissa, Samuel, Koppara, Reddy, Vijay B., Mitelman, Stan, Tong, Sharon X., Chicchi, Gary G., Tsao, Kwei-Lan, Trusca, Dorina, Wu, Margaret, Shao, Qing, Trujillo, Maria E., Fernandez, Guillermo, Nelson, Donald, Bunting, Patricia, Kerr, Janet, Fitzgerald, Patrick, Morissette, Pierre, Volksdorf, Sylvia, Eiermann, George J., Li, Cai, Zhang, Bei B., Howard, Andrew D., Zhou, Yun-Ping, Nargund, Ravi P., Hagmann, William K.
Published in Bioorganic & medicinal chemistry letters (15.03.2016)
Published in Bioorganic & medicinal chemistry letters (15.03.2016)
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3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists
Walsh, Shawn P., Severino, Alexandra, Zhou, Changyou, He, Jiafang, Liang, Gui-Bai, Tan, Carina P., Cao, Jin, Eiermann, George J., Xu, Ling, Salituro, Gino, Howard, Andrew D., Mills, Sander G., Yang, Lihu
Published in Bioorganic & medicinal chemistry letters (01.06.2011)
Published in Bioorganic & medicinal chemistry letters (01.06.2011)
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Discovery of Potent and Selective Dipeptidyl Peptidase IV Inhibitors Derived from β-Aminoamides Bearing Subsituted Triazolopiperazines
Kim, Dooseop, Kowalchick, Jennifer E, Brockunier, Linda L, Parmee, Emma R, Eiermann, George J, Fisher, Michael H, He, Huaibing, Leiting, Barbara, Lyons, Kathryn, Scapin, Giovanna, Patel, Sangita B, Petrov, Aleksandr, Pryor, KellyAnn D, Roy, Ranabir Sinha, Wu, Joseph K, Zhang, Xiaoping, Wyvratt, Matthew J, Zhang, Bei B, Zhu, Lan, Thornberry, Nancy A, Weber, Ann E
Published in Journal of medicinal chemistry (14.02.2008)
Published in Journal of medicinal chemistry (14.02.2008)
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Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes
Guo, Liangqin, Parker, Dann L, Zang, Yi, Sweis, Ramzi F, Liu, Weiguo, Sherer, Edward C, Buist, Nicole, Terebetski, Jenna, Kelly, Terri, Bugianesi, Randal, Priest, Birgit T, Dingley, Karen H, Li, Xiaofang, Mitelman, Stan, Salituro, Gino, Trujillo, Maria E, Pachanski, Michele, Kirkland, Melissa, Powles, Mary Ann, Eiermann, George J, Feng, Yue, Shang, Jin, Howard, Andrew D, Ujjainwalla, Feroze, Sinz, Christopher J, Debenham, John S, Edmondson, Scott D, Nargund, Ravi P, Hagmann, William K, Li, Derun
Published in ACS medicinal chemistry letters (08.12.2016)
Published in ACS medicinal chemistry letters (08.12.2016)
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(2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes
Kim, Dooseop, Wang, Liping, Beconi, Maria, Eiermann, George J, Fisher, Michael H, He, Huaibing, Hickey, Gerard J, Kowalchick, Jennifer E, Leiting, Barbara, Lyons, Kathryn, Marsilio, Frank, McCann, Margaret E, Patel, Reshma A, Petrov, Aleksandr, Scapin, Giovanna, Patel, Sangita B, Roy, Ranabir Sinha, Wu, Joseph K, Wyvratt, Matthew J, Zhang, Bei B, Zhu, Lan, Thornberry, Nancy A, Weber, Ann E
Published in Journal of medicinal chemistry (13.01.2005)
Published in Journal of medicinal chemistry (13.01.2005)
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Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: Close analogs of JANUVIA™ (sitagliptin phosphate)
Kim, Dooseop, Kowalchick, Jennifer E., Edmondson, Scott D., Mastracchio, Anthony, Xu, Jinyou, Eiermann, George J., Leiting, Barbara, Wu, Joseph K., Pryor, KellyAnn D., Patel, Reshma A., He, Huaibing, Lyons, Kathryn A., Thornberry, Nancy A., Weber, Ann E.
Published in Bioorganic & medicinal chemistry letters (15.06.2007)
Published in Bioorganic & medicinal chemistry letters (15.06.2007)
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Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes
Shah, Shrenik K, He, Shuwen, Guo, Liangqin, Truong, Quang, Qi, Hongbo, Du, Wu, Lai, Zhong, Liu, Jian, Jian, Tianying, Hong, Qingmei, Dobbelaar, Peter, Ye, Zhixiong, Sherer, Edward, Feng, Zhe, Yu, Yang, Wong, Frederick, Samuel, Koppara, Madiera, Maria, Karanam, Bindhu V, Reddy, Vijay B, Mitelman, Stan, Tong, Sharon X, Chicchi, Gary G, Tsao, Kwei-Lan, Trusca, Dorina, Feng, Yue, Wu, Margaret, Shao, Qing, Trujillo, Maria E, Eiermann, George J, Li, Cai, Pachanski, Michele, Fernandez, Guillermo, Nelson, Donald, Bunting, Patricia, Morissette, Pierre, Volksdorf, Sylvia, Kerr, Janet, Zhang, Bei B, Howard, Andrew D, Zhou, Yun-Ping, Pasternak, Alexander, Nargund, Ravi P, Hagmann, William K
Published in ACS medicinal chemistry letters (14.05.2015)
Published in ACS medicinal chemistry letters (14.05.2015)
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Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors
Edmondson, Scott D., Mastracchio, Anthony, Cox, Jason M., Eiermann, George J., He, Huaibing, Lyons, Kathryn A., Patel, Reshma A., Patel, Sangita B., Petrov, Aleksandr, Scapin, Giovanna, Wu, Joseph K., Xu, Shiyao, Zhu, Bing, Thornberry, Nancy A., Roy, Ranabir Sinha, Weber, Ann E.
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
Published in Bioorganic & medicinal chemistry letters (01.08.2009)
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Design, synthesis, and biological evaluation of triazolopiperazine-based β-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors
Kowalchick, Jennifer E., Leiting, Barbara, Pryor, KellyAnn D., Marsilio, Frank, Wu, Joseph K., He, Huaibing, Lyons, Kathryn A., Eiermann, George J., Petrov, Aleksandr, Scapin, Giovanna, Patel, Reshma A., Thornberry, Nancy A., Weber, Ann E., Kim, Dooseop
Published in Bioorganic & medicinal chemistry letters (01.11.2007)
Published in Bioorganic & medicinal chemistry letters (01.11.2007)
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