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33 Results  for Everything (Includes Articles)

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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 ; Gonzalez Trotter, Dinko ; Feng, Danqing ; Xu, Shiyao ; Eiermann, George ; Holahan, Marie A ; Rubins, Daniel ; Conarello, Stacey ; Niu, Xiaoda ; Souza, Sandra C ; Miller, Corin ; Liu

Science (New York, N.Y.), 04 August 2017, Vol.357(6350), pp.507-511 [Peer Reviewed Journal]

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Hit-to-Lead Optimization and Discovery of 5-((5-(1,1'-Biphenyl-4-yl)-6-chloro-1H-benzodimidazol-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

Journal of medicinal chemistry, 09 November 2017, Vol.60(21), pp.9040-9052 [Peer Reviewed Journal]

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Discovery of a novel glucagon receptor antagonist N-(4-{(1S)-1-3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-ylethyl}phenyl)carbonyl-β-alanine (MK-0893) for the treatment of type II diabetes

Xiong, Yusheng ; Guo, Jian ; Candelore, Mari R ; Liang, Rui ; Miller, Corey ; Dallas-Yang, Qing ; Jiang, Guoqiang ; Mccann, Peggy E ; Qureshi, Sajjad A ; Tong, Xinchun ; Xu, Shiyao Sherrie ; Shang, Jackie ; Vincent, Stella H ; Tota, Laurie M ; Wright, Michael J ; Yang, Xiaodong ; Zhang, Bei B ; Tata, James R ; Parmee, Emma R

Journal of medicinal chemistry, 12 July 2012, Vol.55(13), pp.6137-48 [Peer Reviewed Journal]

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Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes

Biftu, Tesfaye ; Sinha-Roy, Ranabir ; Chen, Ping ; Qian, Xiaoxia ; Feng, Dennis ; Kuethe, Jeffrey T ; Scapin, Giovanna ; Gao, Ying Duo ; Yan, Youwei ; Krueger, Davida ; Bak, Annette ; Eiermann, George ; He, Jiafang ; Cox, Jason ; Hicks, Jacqueline ; Lyons, Kathy ; He, Huaibing ; Salituro, Gino ; Tong, Sharon ; Patel

Journal of medicinal chemistry, 24 April 2014, Vol.57(8), pp.3205-12 [Peer Reviewed Journal]

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AMP010014A09 in Sus Scrofa Encodes an Analog of G Protein-Coupled Receptor 109A, Which Mediates the Anti-Inflammatory Effects of Beta-Hydroxybutyric Acid

Chen, Guangxin ; Fu, Shoupeng ; Feng, Wenqian ; Huang, Bingxu ; Xu, Shiyao ; Wang, Wei ; Liu, Juxiong

Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology, 2017, Vol.42(4), pp.1420-1430 [Peer Reviewed Journal]

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AG and UAG induce β-casein expression via activation of ERK1/2 and AKT pathways

Li, Sunan ; Liu, Juxiong ; Lv, Qingkang ; Zhang, Chuan ; Xu, Shiyao ; Yang, Dongxue ; Huang, Bingxu ; Zeng, Yalong ; Gao, Yingjie ; Wang, Wei

Journal of molecular endocrinology, April 2016, Vol.56(3), pp.213-25 [Peer Reviewed Journal]

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Licochalcone A Prevents the Loss of Dopaminergic Neurons by Inhibiting Microglial Activation in Lipopolysaccharide (LPS)-Induced Parkinson’s Disease Models

Huang, Bingxu ; Liu, Juxiong ; Chen, Ju ; Yang, Dongxue ; Chen, Guangxin ; Xu, Shiyao ; Zeng, Yalong ; Yan, Xuan ; Wang, Wei ; Liu, Dianfeng ; Fu, Shoupeng

International Journal of Molecular Sciences, 2017, Vol.18(10), p.2043 [Peer Reviewed Journal]

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The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors

Cox, Jason M ; Chu, Hong D ; Kuethe, Jeffrey T ; Gao, Ying-Duo ; Scapin, Giovanna ; Eiermann, George ; He, Huaibing ; Li, Xiaohua ; Lyons, Kathryn A ; Metzger, Joseph ; Petrov, Aleksandr ; Wu, Joseph K ; Xu, Shiyao ; Sinha-Roy, Ranabir ; Weber, Ann E ; Biftu, Tesfaye

Bioorganic & Medicinal Chemistry Letters, 01 June 2016, Vol.26(11), pp.2622-2626 [Peer Reviewed Journal]

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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.

Endocrinology, Diabetes & Metabolism, January 2018, Vol.1(1), pp.n/a-n/a [Peer Reviewed Journal]

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Discovery of N-Aryl-2-acylindole human glucagon receptor antagonists

Sinz, Christopher ; Bittner, Amy ; Brady, Ed ; Candelore, Mari ; Dallas-Yang, Qing ; Ding, Victor ; Jiang, Guoqiang ; Lin, Zhen ; Qureshi, Sajjad ; Salituro, Gino ; Saperstein, Richard ; Shang, Jackie ; Szalkowski, Deborah ; Tota, Laurie ; Vincent, Stella ; Wright, Michael ; Xu, Shiyao ; Yang, Xiaodong ; Zhang, Bei ; Tata, James

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(23), pp.7124-7130 [Peer Reviewed Journal]

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Structure–activity-relationship of amide and sulfonamide analogs of omarigliptin

Chen, Ping ; Feng, Dennis ; Qian, Xiaoxia ; Apgar, James ; Wilkening, Robert ; Kuethe, Jeffrey T ; Gao, Ying-Duo ; Scapin, Giovanna ; Cox, Jason ; Doss, George ; Eiermann, George ; He, Huaibing ; Li, Xiaohua ; Lyons, Kathryn A ; Metzger, Joseph ; Petrov, Aleksandr ; Wu, Joseph K ; Xu, Shiyao ; Weber, Ann E ; Yan, Youwei

Bioorganic & Medicinal Chemistry Letters, 15 December 2015, Vol.25(24), pp.5767-5771 [Peer Reviewed Journal]

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Discovery of cyclic guanidines as potent, orally active, human glucagon receptor antagonists

Sinz, Christopher ; Chang, Jiang ; Lins, Ashley Rouse ; Brady, Ed ; Candelore, Mari ; Dallas-Yang, Qing ; Ding, Victor ; Jiang, Guoqiang ; Lin, Zhen ; Mock, Steven ; Qureshi, Sajjad ; Salituro, Gino ; Saperstein, Richard ; Shang, Jackie ; Szalkowski, Deborah ; Tota, Laurie ; Vincent, Stella ; Wright, Michael ; Xu, Shiyao ; Yang, Xiaodong

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(23), pp.7131-7136 [Peer Reviewed Journal]

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Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (2R,3S,5R)-2-(2,5-difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine (23)

Biftu, Tesfaye ; Qian, Xiaoxia ; Chen, Ping ; Feng, Dennis ; Scapin, Giovanna ; Gao, Ying-Duo ; Cox, Jason ; Sinha Roy, Ranabir ; Eiermann, George ; He, Huabing ; Lyons, Kathy ; Salituro, Gino ; Patel, Sangita ; Petrov, Alexander ; Xu, Feng ; Xu, Shiyao Sherrie ; Zhang, Bei ; Caldwell, Charles ; Wu, Joseph K ; Lyons, Kathy

Bioorganic & Medicinal Chemistry Letters, 01 October 2013, Vol.23(19), pp.5361-5366 [Peer Reviewed Journal]

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14
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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

ACS medicinal chemistry letters, 11 January 2018, Vol.9(1), pp.39-44 [Peer Reviewed Journal]

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15
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Corrigendum to “Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(4,6-dihydropyrrolo[3,4-c]pyrazol-5-(1H)-yl)tetrahydro-2H-pyran-3-amine (23)” [Bioorg. Med. Chem. Lett. 23 (2013) 5361–5366]

Biftu, Tesfaye ; Qian, Xiaoxia ; Chen, Ping ; Feng, Dennis ; Scapin, Giovanna ; Gao, Ying-Duo ; Cox, Jason ; Roy, Ranabir Sinha ; Eiermann, George ; He, Huabing ; Lyons, Kathy ; Salituro, Gino ; Patel, Sangita ; Petrov, Alexander ; Xu, Feng ; Xu, Shiyao Sherrie ; Zhang, Bei ; Caldwell, Charles ; Wu, Joseph K ; Lyons, Kathy

Bioorganic & Medicinal Chemistry Letters, 01 June 2014, Vol.24(11), pp.2590-2590 [Peer Reviewed Journal]

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16
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Improvement of hERG-ROMK index of spirocyclic ROMK inhibitors through scaffold optimization and incorporation of novel pharmacophores

Dong, Shuzhi ; Vangelder, Kelsey ; Shi, Zhi-Cai ; Yu, Yang ; Wu, Zhicai ; Ferguson, Ron ; Guo, Zack Zhiqiang ; Tang, Haifeng ; Frie, Jessica ; Fu, Qinghong ; Gu, Xin ; Priest, Birgit T ; Thomas-Fowlkes, Brande ; Weinglass, Adam ; Margulis, Michael ; Liu, Jessica ; Pai, Lee-Yuh ; Hampton, Caryn ; Haimbach, Robin E ; Owens, Karen ; Tong, Vincent ; Xu, Shiyao ; Hu, Mengwei ; Zingaro, Gloria J ; Morissette, Pierre ; Ehrhart, Juliann ; Roy, Sophie ; Sullivan, Kathleen ; Pasternak, Alexander

Bioorganic & Medicinal Chemistry Letters, 01 June 2017, Vol.27(11), pp.2559-2566 [Peer Reviewed Journal]

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17
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Transport of the dipeptidyl peptidase-4 inhibitor sitagliptin by human organic anion transporter 3, organic anion transporting polypeptide 4C1, and multidrug resistance P-glycoprotein

Chu, Xiao-Yan ; Bleasby, Kelly ; Yabut, Jocelyn ; Cai, Xiaoxin ; Chan, Grace Hoyee ; Hafey, Michael J ; Xu, Shiyao ; Bergman, Arthur J ; Braun, Matthew P ; Dean, Dennis C ; Evers, Raymond

The Journal of pharmacology and experimental therapeutics, May 2007, Vol.321(2), pp.673-83 [Peer Reviewed Journal]

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18
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Effect of clofibrate administration on the esterification and deesterification of steroid hormones by liver and extrahepatic tissues in rats

Xu, Shiyao ; Zhu, Bao Ting ; Conney, Allan H

Biochemical Pharmacology, 2002, Vol.63(5), pp.985-992 [Peer Reviewed Journal]

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19
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Characterization of the human mucin 5AC promoter and its regulation by the histone acetyltransferase P300

Xu, Shiyao ; Hui, Yu ; Shu, Jin ; Qian, Jun ; Li, Ling

International journal of molecular medicine, March 2019, Vol.43(3), pp.1263-1270 [Peer Reviewed Journal]

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20
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Characterization of 1'-hydroxymidazolam glucuronidation in human liver microsomes

Zhu, Bing ; Bush, David ; Doss, George A ; Vincent, Stella ; Franklin, Ronald B ; Xu, Shiyao

Drug metabolism and disposition: the biological fate of chemicals, February 2008, Vol.36(2), pp.331-8 [Peer Reviewed Journal]

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21
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(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-1,2,4triazolo1,5-a-pyridin-6-ylphenyl)butanamide: a selective alpha-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

Journal of medicinal chemistry, 15 June 2006, Vol.49(12), pp.3614-27 [Peer Reviewed Journal]

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22
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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

PloS one, 2019, Vol.14(2), pp.e0211568 [Peer Reviewed Journal]

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23
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Effect of 2,3,7,8-tetrachlorodibenzo- p-dioxin administration and high-fat diet on the body weight and hepatic estrogen metabolism in female C3H/HeN mice

Zhu, Bao Ting ; Gallo, Michael A ; Burger, Conney W ; Meeker, Robert J ; Cai, May Xiaoxin ; Xu, Shiyao ; Conney, Allan H

Toxicology and Applied Pharmacology, 2008, Vol.226(2), pp.107-118 [Peer Reviewed Journal]

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24
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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

Bioorganic & Medicinal Chemistry Letters, 01 August 2009, Vol.19(15), pp.4097-4101 [Peer Reviewed Journal]

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25
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Exploring the tissue tropism of pseudorabies virus based on miRNA level analysis

Fan, Yi ; Zhu, Ling ; Sun, Xiangang ; Lyu, Wenting ; Xu, Lei ; Yin, Yue ; Zhao, Jun ; Huang, Jianbo ; Den, Yichao ; Jiang, Zhiyi ; Xu, Shiyao ; Mao, Xiyu ; Xu, Zhiwen

BMC microbiology, 11 June 2019, Vol.19(1), pp.125 [Peer Reviewed Journal]

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26
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Different Biochemical Properties of Nuclear and Microsomal Estrone-3-Sulfatases: Evidence for the Presence of a Nuclear Isozyme

Zhu, Bao Ting ; Fu, Jia-Huey ; Xu, Shiyao ; Kauffman, Frederick C ; Conney, Allan H

Biochemical and Biophysical Research Communications, 08 May 1998, Vol.246(1), pp.45-49 [Peer Reviewed Journal]

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27
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Strong inhibition of estrone-3-sulfatase activity by pregnenolone 16α-carbonitrile but not by several analogs lacking a 16α-nitrile group

Zhu, Bao Ting ; Kosh, Joseph W ; Fu, Jia-Huey ; Cai, May Xiaoxin ; Xu, Shiyao ; Conney, Allan H

Steroids, 2000, Vol.65(9), pp.521-527 [Peer Reviewed Journal]

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28
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Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors

Cox, Jason M ; Harper, Bart ; Mastracchio, Anthony ; Leiting, Barbara ; Sinha Roy, Ranabir ; Patel, Reshma A ; Wu, Joseph K ; Lyons, Kathryn A ; He, Huaibing ; Xu, Shiyao ; Zhu, Bing ; Thornberry, Nancy A ; Weber, Ann E ; Edmondson, Scott D

Bioorganic & Medicinal Chemistry Letters, 15 August 2007, Vol.17(16), pp.4579-4583 [Peer Reviewed Journal]

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29
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Metabolic activation of fluoropyrrolidine dipeptidyl peptidase-IV inhibitors by rat liver microsomes

Xu, Shiyao ; Zhu, Bing ; Teffera, Yohannes ; Pan, Deborah E ; Caldwell, Charles G ; Doss, George ; Stearns, Ralph A ; Evans, David C ; Beconi, Maria G

Drug metabolism and disposition: the biological fate of chemicals, January 2005, Vol.33(1), pp.121-30 [Peer Reviewed Journal]

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30
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Impact of renal impairment and human organic anion transporter inhibition on pharmacokinetics, safety, and tolerability of relebactam combined with imipenem and cilastatin PK of relebactam and imipenem/cilastatin

Bhagunde, Pratik ; Colon-Gonzalez, Francheska ; Liu, Yang ; Wu, Jin ; Xu, Shiyao Sherrie ; Garrett, Graigory ; Jumes, Patricia ; Lasseter, Kenneth ; Marbury, Thomas ; Rizk, Matthew L ; Lala, Mallika ; Rhee, Elizabeth G ; Butterton, Joan R ; Boundy, Keith

British journal of clinical pharmacology, 19 December 2019 [Peer Reviewed Journal]

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31
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Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors

Edmondson, Scott D ; Wei, Lan ; Xu, Jinyou ; Shang, Jackie ; Xu, Shiyao ; Pang, Jianmei ; Chaudhary, Ashok ; Dean, Dennis C ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathryn A ; Patel, Reshma A ; Patel, Sangita B ; Scapin, Giovanna ; Wu, Joseph K ; Beconi, Maria G ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2008, Vol.18(7), pp.2409-2413 [Peer Reviewed Journal]

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32
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Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor 14Csitagliptin in humans

Vincent, Stella H ; Reed, James R ; Bergman, Arthur J ; Elmore, Charles S ; Zhu, Bing ; Xu, Shiyao ; Ebel, David ; Larson, Patrick ; Zeng, Wei ; Chen, Li ; Dilzer, Stacy ; Lasseter, Kenneth ; Gottesdiener, Keith ; Wagner, John A ; Herman, Gary A

Drug metabolism and disposition: the biological fate of chemicals, April 2007, Vol.35(4), pp.533-8 [Peer Reviewed Journal]

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33
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Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs

Beconi, Maria G ; Reed, James R ; Teffera, Yohannes ; Xia, Yuan-Qing ; Kochansky, Christopher J ; Liu, David Q ; Xu, Shiyao ; Elmore, Charles S ; Ciccotto, Suzanne ; Hora, Donald F ; Stearns, Ralph A ; Vincent, Stella H

Drug metabolism and disposition: the biological fate of chemicals, April 2007, Vol.35(4), pp.525-32 [Peer Reviewed Journal]

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