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Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors

Ashton, Wallace T ; Dong, Hong ; Sisco, Rosemary M ; Doss, George A ; Leiting, Barbara ; Patel, Reshma A ; Wu, Joseph K ; Marsilio, Frank ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 23 February 2004, Vol.14(4), pp.859-863 [Peer Reviewed Journal]

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Dipeptidyl peptidase IV inhibitors derived from β-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole

Ashton, Wallace T ; Sisco, Rosemary M ; Dong, Hong ; Lyons, Kathryn A ; He, Huaibing ; Doss, George A ; Leiting, Barbara ; Patel, Reshma A ; Wu, Joseph K ; Marsilio, Frank ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2005, Vol.15(9), pp.2253-2258 [Peer Reviewed Journal]

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Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis

Becker, Joseph W ; Rotonda, Jennifer ; Soisson, Stephen M ; Aspiotis, Renee ; Bayly, Christopher ; Francoeur, Sébastien ; Gallant, Michel ; Garcia-Calvo, Marga ; Giroux, Andre ; Grimm, Erich ; Han, Yongxin ; Mckay, Dan ; Nicholson, Donald W ; Peterson, Erin ; Renaud, Johanne ; Roy, Sophie ; Thornberry, Nancy ; Zamboni, Robert

Journal of medicinal chemistry, 06 May 2004, Vol.47(10), pp.2466-74 [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 ; Sinharoy, Ranabir ; Pocai, Alessandro ; Kelly, Theresa ; Scapin, Giovanna ; Pryor, Kelly ; Wu, Joseph ; Eiermann, George ; Xu, Shiyao ; Zhang, Xiaoping ; Tatosian, Daniel ; Weber, Ann ; Thornberry, Nancy ; Carr, Richard

Endocrinology, Diabetes & Metabolism, Jan 2018, Vol.1(1) [Peer Reviewed Journal]

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(3 R)-4-[(3 R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

Biftu, Tesfaye ; Feng, Dennis ; Qian, Xiaoxia ; Liang, Gui-Bai ; Kieczykowski, Gerard ; Eiermann, George ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathy ; Petrov, Aleksandr ; Sinha-Roy, Ranabir ; Zhang, Bei ; Scapin, Giovanna ; Patel, Sangita ; Gao, Ying-Duo ; Singh, Suresh ; Wu, Joseph ; Zhang, Xiaoping ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(1), pp.49-52 [Peer Reviewed Journal]

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Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin

Biftu, Tesfaye ; Scapin, Giovanna ; Singh, Suresh ; Feng, Dennis ; Becker, Joe W ; Eiermann, George ; He, Huaibing ; Lyons, Kathy ; Patel, Sangita ; Petrov, Aleksandr ; Sinha-Roy, Ranabir ; Zhang, Bei ; Wu, Joseph ; Zhang, Xiaoping ; Doss, George A ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(12), pp.3384-3387 [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, Sangita ; Doss, George ; Petrov, Aleksandr ; Wu, Joseph ; Xu, Shiyao Sherrie ; Sewall, Charles ; Zhang, Xiaoping ; Zhang, Bei ; Thornberry, Nancy A ; Weber, Ann E

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

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Substituted piperazines as novel dipeptidyl peptidase IV inhibitors

Brockunier, Linda L ; He, Jiafang ; Colwell, Lawrence F ; Habulihaz, Bahanu ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathryn A ; Marsilio, Frank ; Patel, Reshma A ; Teffera, Yohannes ; Wu, Joseph K ; Thornberry, Nancy A ; Weber, Ann E ; Parmee, Emma R

Bioorganic & Medicinal Chemistry Letters, 2004, Vol.14(18), pp.4763-4766 [Peer Reviewed Journal]

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Glucagon-like peptide 1-based drugs and pancreatic safety

Brodovicz, Kimberly G ; Engel, Samuel S ; Thornberry, Nancy A

JAMA internal medicine, 28 October 2013, Vol.173(19), pp.1842-3 [Peer Reviewed Journal]

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Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors

Caldwell, Charles G ; Chen, Ping ; He, Jiafang ; Parmee, Emma R ; Leiting, Barbara ; Marsilio, Frank ; Patel, Reshma A ; Wu, Joseph K ; Eiermann, George J ; Petrov, Aleksandr ; He, Huaibing ; Lyons, Kathryn A ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 08 March 2004, Vol.14(5), pp.1265-1268 [Peer Reviewed Journal]

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Mouse and human granzyme B have distinct tetrapeptide specificities and abilities to recruit the bid pathway

Casciola-Rosen, Livia ; Garcia-Calvo, Margarita ; Bull, Herbert G ; Becker, Joseph W ; Hines, Tonie ; Thornberry, Nancy A ; Rosen, Antony

The Journal of biological chemistry, 16 February 2007, Vol.282(7), pp.4545-52 [Peer Reviewed Journal]

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Synthesis and evaluation of (1R)-1-amino-2-(2,5-difluorophenyl)ethylcyclohexanes and 4-(1R)-1-amino-2-(2,5-difluorophenyl)ethylpiperidines as DPP-4 inhibitors

Chen, Ping ; Caldwell, Charles G ; Ashton, Wallace ; Wu, Joseph K ; He, Huaibing ; Lyons, Kathryn A ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & medicinal chemistry letters, 15 March 2011, Vol.21(6), pp.1880-6 [Peer Reviewed Journal]

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Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes

Chen, Ping ; Caldwell, Charles G ; Mathvink, Robert J ; Leiting, Barbara ; Marsilio, Frank ; Patel, Reshma A ; Wu, Joseph K ; He, Huaibing ; Lyons, Kathryn A ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(21), pp.5853-5857 [Peer Reviewed Journal]

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Mice lacking dipeptidyl peptidase IV are protected against obesity and insulin resistance

Conarello, Stacey L ; Li, Zhihua ; Ronan, John ; Roy, Ranabir Sinha ; Zhu, Lan ; Jiang, Guoqiang ; Liu, Franklin ; Woods, John ; Zycband, Emanuel ; Moller, David E ; Thornberry, Nancy A ; Zhang, Bei B

Proceedings of the National Academy of Sciences of the United States of America, 27 May 2003, Vol.100(11), pp.6825-30 [Peer Reviewed Journal]

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15
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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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Optimization of co-agonism at GLP-1 and glucagon receptors to safely maximize weight reduction in DIO-rodents

Day, Jonathan W ; Gelfanov, Vasily ; Smiley, David ; Carrington, Paul E ; Eiermann, George ; Chicchi, Gary ; Erion, Mark D ; Gidda, Jas ; Thornberry, Nancy A ; Tschöp, Matthias H ; Marsh, Donald J ; Sinharoy, Ranabir ; Dimarchi, Richard ; Pocai, Alessandro

Biopolymers, 2012, Vol.98(5), pp.443-50 [Peer Reviewed Journal]

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Enzymatic activity of the Staphylococcus aureus SplB serine protease is induced by substrates containing the sequence Trp-Glu-Leu-Gln

Dubin, Grzegorz ; Stec-Niemczyk, Justyna ; Kisielewska, Magdalena ; Pustelny, Katarzyna ; Popowicz, Grzegorz M ; Bista, Michal ; Kantyka, Tomasz ; Boulware, Kevin T ; Stennicke, Henning R ; Czarna, Anna ; Phopaisarn, Mullika ; Daugherty, Patrick S ; Thøgersen, Ida B ; Enghild, Jan J ; Thornberry, Nancy ; Dubin, Adam ; Potempa, Jan

Journal of molecular biology, 30 May 2008, Vol.379(2), pp.343-56 [Peer Reviewed Journal]

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18
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4-Aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV

Duffy, Joseph L ; Kirk, Brian A ; Wang, Liping ; Eiermann, George J ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathryn A ; Patel, Reshma A ; Patel, Sangita B ; Petrov, Alexsandr ; Scapin, Giovanna ; Wu, Joseph K ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(10), pp.2879-2885 [Peer Reviewed Journal]

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19
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Potent and selective proline derived dipeptidyl peptidase IV inhibitors

Edmondson, Scott D ; Mastracchio, Anthony ; Beconi, Maria ; Colwell, Lawrence F ; Habulihaz, Bahanu ; He, Huaibing ; Kumar, Sanjeev ; Leiting, Barbara ; Lyons, Kathryn A ; Mao, Ann ; Marsilio, Frank ; Patel, Reshma A ; Wu, Joseph K ; Zhu, Lan ; Thornberry, Nancy A ; Weber, Ann E ; Parmee, Emma R

Bioorganic & Medicinal Chemistry Letters, 18 October 2004, Vol.14(20), pp.5151-5155 [Peer Reviewed Journal]

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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.4097-101 [Peer Reviewed Journal]

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21
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Discovery of potent and selective orally bioavailable β-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors

Edmondson, Scott D ; Mastracchio, Anthony ; Duffy, Joseph L ; Eiermann, George J ; He, Huaibing ; Ita, Ida ; Leiting, Barbara ; Leone, Joseph F ; Lyons, Kathryn A ; Makarewicz, Amanda M ; Patel, Reshma A ; Petrov, Aleksandr ; Wu, Joseph K ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2005, Vol.15(12), pp.3048-3052 [Peer Reviewed Journal]

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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, Ranabir Sinha ; Smith, Aaron ; Wu, Joseph K ; Xu, Shiyao ; Zhu, Bing ; Thornberry, Nancy A ; Weber, Ann E

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

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23
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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, 01 April 2008, Vol.18(7), pp.2409-13 [Peer Reviewed Journal]

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Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors

Gao, Ying-Duo ; Feng, Dennis ; Sheridan, Robert P ; Scapin, Giovanna ; Patel, Sangita B ; Wu, Joseph K ; Zhang, Xiaoping ; Sinha-Roy, Ranabir ; Thornberry, Nancy A ; Weber, Ann E ; Biftu, Tesfaye

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(14), pp.3877-3879 [Peer Reviewed Journal]

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25
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The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1)

Garcia-Calvo, Margarita ; Lisnock, Jeanmarie ; Bull, Herbert G ; Hawes, Brian E ; Burnett, Duane A ; Braun, Matthew P ; Crona, James H ; Davis, Harry R ; Dean, Dennis C ; Detmers, Patricia A ; Graziano, Michael P ; Hughes, Meredith ; Macintyre, D Euan ; Ogawa, Anthony ; O'Neill, Kim A ; Iyer, Sai Prasad N ; Shevell, Diane E ; Smith, Marsha M ; Tang, Yui S ; Makarewicz, Amanda M ; Ujjainwalla, Feroze ; Altmann, Scott W ; Chapman, Kevin T ; Thornberry, Nancy A

Proceedings of the National Academy of Sciences of the United States of America, 07 June 2005, Vol.102(23), pp.8132-7 [Peer Reviewed Journal]

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26
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Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors

Han, Yongxin ; Giroux, André ; Grimm, Erich L ; Aspiotis, Renée ; Francoeur, Sébastien ; Bayly, Christopher I ; Mckay, Daniel J ; Roy, Sophie ; Xanthoudakis, Steve ; Vaillancourt, John P ; Rasper, Dita M ; Tam, John ; Tawa, Paul ; Thornberry, Nancy A ; Paterson, Erin P ; Garcia-Calvo, Margarita ; Becker, Joseph W ; Rotonda, Jennifer ; Nicholson, Donald W ; Zamboni, Robert J

Bioorganic & Medicinal Chemistry Letters, 2004, Vol.14(3), pp.805-808 [Peer Reviewed Journal]

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27
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Nicotinyl aspartyl ketones as inhibitors of caspase-3

Isabel, Elise ; Black, W.Cameron ; Bayly, Christopher I ; Grimm, Erich L ; Janes, Marc K ; Mckay, Daniel J ; Nicholson, Donald W ; Rasper, Dita M ; Renaud, Johanne ; Roy, Sophie ; Tam, John ; Thornberry, Nancy A ; Vaillancourt, John P ; Xanthoudakis, Steven ; Zamboni, Robert

Bioorganic & Medicinal Chemistry Letters, 2003, Vol.13(13), pp.2137-2140 [Peer Reviewed Journal]

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4-Arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV

Kaelin, David E ; Smenton, Abigail L ; Eiermann, George J ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathryn A ; Patel, Reshma A ; Patel, Sangita B ; Petrov, Alexsandr ; Scapin, Giovanna ; Wu, Joseph K ; Thornberry, Nancy A ; Weber, Ann E ; Duffy, Joseph L

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(21), pp.5806-5811 [Peer Reviewed Journal]

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29
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Dual Role of Caspase-11 in Mediating Activation of Caspase-1 and Caspase-3 under Pathological Conditions

Kang, Shin-Jung ; Wang, Suyue ; Hara, Hideaki ; Peterson, Erin P ; Namura, Shobu ; Amin-Hanjani, Sepideh ; Huang, Zhihong ; Srinivasan, Anu ; Tomaselli, Kevin J ; Thornberry, Nancy A ; Moskowitz, Michael A ; Yuan, Junying

The Journal of Cell Biology, 2000, Vol.149(3), p.613-622 [Peer Reviewed Journal]

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30
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Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-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

Journal of medicinal chemistry, 14 February 2008, Vol.51(3), pp.589-602 [Peer Reviewed Journal]

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31
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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

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(12), pp.3373-3377 [Peer Reviewed Journal]

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(2R)-4-oxo-4-3-(trifluoromethyl)-5,6-dihydro1,2,4triazolo4,3-apyrazin-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

Journal of medicinal chemistry, 13 January 2005, Vol.48(1), pp.141-51 [Peer Reviewed Journal]

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33
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The caspase-like sites of proteasomes, their substrate specificity, new inhibitors and substrates, and allosteric interactions with the trypsin-like sites

Kisselev, Alexei F ; Garcia-Calvo, Margarita ; Overkleeft, Herman S ; Peterson, Erin ; Pennington, Michael W ; Ploegh, Hidde L ; Thornberry, Nancy A ; Goldberg, Alfred L

The Journal of biological chemistry, 19 September 2003, Vol.278(38), pp.35869-77 [Peer Reviewed Journal]

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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

Bioorganic & Medicinal Chemistry Letters, 2007, Vol.17(21), pp.5934-5939 [Peer Reviewed Journal]

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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 ; Roy, Ranabir Sinha ; Eiermann, George J ; Beconi, Maria G ; Biftu, Tesfaye ; Chan, Chi-Chung ; Edmondson, Scott ; Feeney, William P ; He, Huaibing ; Ippolito, Dawn E ; Kim, Dooseop ; Lyons, Kathryn A ; Ok, Hyun O ; Patel, Reshma A ; Petrov, Aleksandr N ; Pryor, Kelly Ann ; Qian, Xiaoxia ; Reigle, Leah ; Woods, Andrea ; Wu, Joseph K ; Zaller, Dennis ; Zhang, Xiaoping ; Zhu, Lan ; Weber, Ann E ; Thornberry, Nancy A

Diabetes, October 2005, Vol.54(10), pp.2988-94 [Peer Reviewed Journal]

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Catalytic properties and inhibition of proline-specific dipeptidyl peptidases II, IV and VII

Leiting, Barbara ; Pryor, Kellyann D ; Wu, Joseph K ; Marsilio, Frank ; Patel, Reshma A ; Craik, Charles S ; Ellman, Jonathan A ; Cummings, Richard T ; Thornberry, Nancy A

The Biochemical journal, 15 April 2003, Vol.371(Pt 2), pp.525-32 [Peer Reviewed Journal]

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