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1
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High pressure gel-permeation assay for the proteolysis of human aggrecan by human stromelysin-1: Kinetic constants for aggrecan hydrolysis

Poe, Martin ; Stein, Ross L ; Wu, Joseph K

Archives of Biochemistry and Biophysics, 1992, Vol.298(2), pp.757-759 [Peer Reviewed Journal]

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Synthesis and evaluation of [(1 R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1 R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines 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, 2011, Vol.21(6), pp.1880-1886 [Peer Reviewed Journal]

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Unanticipated Inhibition of the Metallo-β-lactamase from Bacteroides f ragilis by 4-Morpholineethanesulfonic Acid (MES):  A Crystallographic Study at 1.85-Å Resolution ‡
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Unanticipated Inhibition of the Metallo-β-lactamase from Bacteroides f ragilis by 4-Morpholineethanesulfonic Acid (MES):  A Crystallographic Study at 1.85-Å Resolution ‡

Fitzgerald, Paula M. D. ; Wu, Joseph K. ; Toney, Jeffrey H.

Biochemistry, 05/1998, Vol.37(19), pp.6791-6800 [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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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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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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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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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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9
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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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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

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

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11
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Soluble Penicillin-Binding Protein 2a: β-Lactam Binding and Inhibition by Non-β-Lactams Using a 96-Well Format

Toney, Jeffrey H ; Hammond, Gail G ; Leiting, Barbara ; Pryor, Kellyann D ; Wu, Joseph K ; Cuca, Gregory C ; Pompliano, David L

Analytical Biochemistry, 01 January 1998, Vol.255(1), pp.113-119 [Peer Reviewed Journal]

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12
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Renin cleavage of a human kidney renin substrate analogous to human angiotensinogen, H-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu-Val-Ile-His-Ser-OH, that is human renin specific and is resistant to cathepsin D

Poe, Martin ; Wu, Joseph K ; Lin, Tsau-Yen ; Hoogsteen, Karst ; Bull, Herbert G ; Slater, Eve E

Analytical Biochemistry, 1984, Vol.140(2), pp.459-467 [Peer Reviewed Journal]

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13
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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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14
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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

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

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15
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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

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

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16
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CTL lysis: there is a hyperbolic relation of killing rate to exocytosable granzyme A for highly cytotoxic murine cytotoxic T lymphocytes

Poe, Martin ; Wu, Joseph K ; Talento, Althea ; Koo, Gloria C

Journal of Immunological Methods, 1996, Vol.192(1), pp.37-41 [Peer Reviewed Journal]

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17
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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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18
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The enzymatic activity of human cytotoxic T-lymphocyte granzyme a and cytolysis mediated by cytotoxic T-lymphocytes are potently inhibited by a synthetic antiprotease, FUT-175

Poe, Martin ; Wu, Joseph K ; Blake, J.T ; Zweerink, H.J ; Sigal, N.H

Archives of Biochemistry and Biophysics, 1991, Vol.284(1), pp.215-218 [Peer Reviewed Journal]

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19
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High-Yield Expression, Purification, and Characterization of Active, SolubleBacteroides fragilisMetallo-β-Lactamase, CcrA

Toney, Jeffrey H ; Wu, Joseph K ; Overbye, Karen M ; Thompson, Chris M ; Pompliano, David L

Protein Expression and Purification, April 1997, Vol.9(3), pp.355-362 [Peer Reviewed Journal]

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20
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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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21
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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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22
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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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23
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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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24
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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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25
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Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors

Xu, Jinyou ; Wei, Lan ; Mathvink, Robert ; He, Jiafang ; Park, You-Jung ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathryn A ; Marsilio, Frank ; Patel, Reshma A ; Wu, Joseph K ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 16 May 2005, Vol.15(10), pp.2533-2536 [Peer Reviewed Journal]

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26
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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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27
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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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28
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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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29
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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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30
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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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31
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Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors

Xu, Jinyou ; Wei, Lan ; Mathvink, Robert ; Edmondson, Scott D ; Mastracchio, Anthony ; Eiermann, George J ; He, Huaibing ; Leone, Joseph F ; Leiting, Barbara ; Lyons, Kathryn A ; Marsilio, Frank ; Patel, Reshma A ; Petrov, Aleksandr ; Wu, Joseph K ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(5), pp.1346-1349 [Peer Reviewed Journal]

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32
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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

Bioorganic & Medicinal Chemistry Letters, 2006, Vol.16(20), pp.5373-5377 [Peer Reviewed Journal]

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33
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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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34
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Discovery of potent and selective β-homophenylalanine based dipeptidyl peptidase IV inhibitors

Xu, Jinyou ; Ok, Hyun O ; Gonzalez, Edward J ; Colwell, Lawrence F ; Habulihaz, Bahanu ; He, Huaibing ; Leiting, Barbara ; Lyons, Kathryn A ; Marsilio, Frank ; Patel, Reshma A ; Wu, Joseph K ; Thornberry, Nancy A ; Weber, Ann E ; Parmee, Emma R

Bioorganic & Medicinal Chemistry Letters, 2004, Vol.14(18), pp.4759-4762 [Peer Reviewed Journal]

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35
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4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors

Parmee, Emma R ; He, Jiafang ; Mastracchio, Anthony ; Edmondson, Scott D ; Colwell, Larry ; Eiermann, George ; Feeney, William P ; Habulihaz, Bahanu ; He, Huaibing ; Kilburn, Ruth ; Leiting, Barbara ; Lyons, Kathryn ; Marsilio, Frank ; Patel, Reshma A ; Petrov, Aleksandr ; Di Salvo, Jerry ; Wu, Joseph K ; Thornberry, Nancy A ; Weber, Ann E

Bioorganic & Medicinal Chemistry Letters, 2004, Vol.14(1), pp.43-46 [Peer Reviewed Journal]

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