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Nancy Thornberry

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Xiaoyan Nina Li; Christopher B Newgard; Aleksandr Petrov; Nancy A Thornberry; Michael Wagner; Yusheng Xiong; Bei B Zhang; George Eiermann; Maria L Garcia; Lan Ge; James Herrington; Hans E Hohmeier; Andrew D Howard; Mette V Jensen; Gregory J Kaczorowski; Yun-Ping Zhou
The role of voltage-gated potassium channels Kv2.1 and Kv2.2 in the regulation of insulin and somatostatin release from pancreatic islets.
Jonathan W Day; Richard Dimarchi; George J Eiermann; Mark D Erion; Vasily Gelfanov; Jas Gidda; Donald J Marsh; Ranabir SinhaRoy; David Smiley; Nancy A Thornberry; Matthias H Tschöp; Paul E Carrington; Gary G Chicchi; Alessandro Pocai
Optimization of co-agonism at GLP-1 and glucagon receptors to safely maximize weight reduction in DIO-rodents.
Yue Feng; Xiao-Ming Guan; Kirstine Juhl; Jing Li; Joseph M Metzger; Marc L Reitman; Nancy A Thornberry; Bei B Zhang; Yonghua Zhu; Yun-Ping Zhou
Bombesin receptor subtype-3 (BRS-3) regulates glucose-stimulated insulin secretion in pancreatic islets across multiple species.

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All Publications

2013: Xiaoyan Nina Li; Christopher B Newgard; Aleksandr Petrov; Nancy A Thornberry; Michael Wagner; Yusheng Xiong; Bei B Zhang; George Eiermann; Maria L Garcia; Lan Ge; James Herrington; Hans E Hohmeier; Andrew D Howard; Mette V Jensen; Gregory J Kaczorowski; Yun-Ping Zhou
The role of voltage-gated potassium channels Kv2.1 and Kv2.2 in the regulation of insulin and somatostatin release from pancreatic islets.
The Journal of pharmacology and experimental therapeutics 2013;344(2):407-16.
2012: Jonathan W Day; Richard Dimarchi; George J Eiermann; Mark D Erion; Vasily Gelfanov; Jas Gidda; Donald J Marsh; Ranabir SinhaRoy; David Smiley; Nancy A Thornberry; Matthias H Tschöp; Paul E Carrington; Gary G Chicchi; Alessandro Pocai
Optimization of co-agonism at GLP-1 and glucagon receptors to safely maximize weight reduction in DIO-rodents.
Biopolymers 2012;98(5):443-50.
2011: Yue Feng; Xiao-Ming Guan; Kirstine Juhl; Jing Li; Joseph M Metzger; Marc L Reitman; Nancy A Thornberry; Bei B Zhang; Yonghua Zhu; Yun-Ping Zhou
Bombesin receptor subtype-3 (BRS-3) regulates glucose-stimulated insulin secretion in pancreatic islets across multiple species.
Endocrinology 2011;152(11):4106-15.
2011: Ping Chen; Charles G Caldwell; Wallace T Ashton; Joseph K Wu; Huaibing He; Kathryn A Lyons; Nancy A Thornberry; Ann E Weber
Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors.
Bioorganic & medicinal chemistry letters 2011;21(6):1880-6.
2010: Elizabeth Migoya; R Bergeron; J L Miller; R N K Snyder; Michael Tanen; Deborah Hilliard; B Weiss; P Larson; M Gutierrez; Guoqiang Jiang; Franklin Liu; K A Pryor; J Yao; Lan Zhu; Jens J Holst; C Deacon; Gary A Herman; Nancy A Thornberry; John M Amatruda; D Williams-Herman; John A Wagner; R SinhaRoy
Dipeptidyl peptidase-4 inhibitors administered in combination with metformin result in an additive increase in the plasma concentration of active GLP-1.
Clinical pharmacology and therapeutics 2010;88(6):801-8.
2010: Changyou Zhou; Cheng Tang; Eric Chang; Min Ge; Songnian Lin; Eric Cline; Carina P Tan; Yue Feng; Yun-Ping Zhou; George J Eiermann; Aleksandr Petrov; Gino M Salituro; Peter Meinke; Ralph T Mosley; Taro E Akiyama; Monica Einstein; Sanjeev Kumar; Joel P Berger; Andrew D Howard; Nancy A Thornberry; Sander G Mills; Lihu Yang
Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.
Bioorganic & medicinal chemistry letters 2010;20(3):1298-301.
2009: James Mu; Aleksandr Petrov; George J Eiermann; John Woods; Yun-Ping Zhou; Zhihua Li; Emanuel Zycband; Yue Feng; Lan Zhu; Ranabir Sinha Roy; Andrew D Howard; Cai Li; Nancy A Thornberry; Bei B Zhang
Inhibition of DPP-4 with sitagliptin improves glycemic control and restores islet cell mass and function in a rodent model of type 2 diabetes.
European journal of pharmacology 2009;623(1-3):148-54.
2009: Maria Alba; D Sheng; Y Guan; D Williams-Herman; P Larson; J R Sachs; Nancy A Thornberry; Gary A Herman; Keith D Kaufman; B J Goldstein
Sitagliptin 100 mg daily effect on DPP-4 inhibition and compound-specific glycemic improvement.
Current medical research and opinion 2009;25(10):2507-14.
2009: Alessandro Pocai; Paul E Carrington; Jennifer R Adams; Michael Wright; George J Eiermann; Lan Zhu; Xiaobing Du; Aleksandr Petrov; Michael E Lassman; Guoqiang Jiang; Franklin Liu; Corey Miller; Laurie M Tota; Gaochao Zhou; Xiaoping Zhang; Michael M Sountis; Alessia Santoprete; Elena Capito'; Gary G Chicchi; Nancy A Thornberry; Elisabetta Bianchi; Antonello Pessi; Donald J Marsh; Ranabir SinhaRoy
Glucagon-like peptide 1/glucagon receptor dual agonism reverses obesity in mice.
Diabetes 2009;58(10):2258-66.
2009: Nancy A Thornberry; Baptist Gallwitz
Mechanism of action of inhibitors of dipeptidyl-peptidase-4 (DPP-4).
Best practice & research. Clinical endocrinology & metabolism 2009;23(4):479-86.
2009: Scott D Edmondson; Anthony Mastracchio; Jason M. Cox; George J Eiermann; Huaibing He; Kathryn A Lyons; Reshma A Patel; Sangita B Patel; Aleksandr Petrov; Giovanna Scapin; Joseph K Wu; Shiyao Xu; Bing Zhu; Nancy A Thornberry; Ranabir Sinha Roy; Ann E Weber
Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors.
Bioorganic & medicinal chemistry letters 2009;19(15):4097-101.
2008: Sarah M Ronnebaum; Mette Jensen; Hans E Hohmeier; Shawn C Burgess; Yun-Ping Zhou; Su Qian; Douglas MacNeil; Andrew Howard; Nancy A Thornberry; Olga Ilkayeva; Danhong Lu; A Dean Sherry; Christopher B Newgard
Silencing of cytosolic or mitochondrial isoforms of malic enzyme has no effect on glucose-stimulated insulin secretion from rodent islets.
The Journal of biological chemistry 2008;283(43):28909-17.
2008: Carina P Tan; Yue Feng; Yun-Ping Zhou; George J Eiermann; Aleksandr Petrov; Changyou Zhou; Songnian Lin; Gino Salituro; Peter Meinke; Ralph T Mosley; Taro E Akiyama; Monica Einstein; Sanjeev Kumar; Joel P Berger; Sander G Mills; Nancy A Thornberry; Lihu Yang; Andrew D Howard
Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice.
Diabetes 2008;57(8):2211-9.
2008: Gui-Bai Liang; Xiaoxia Qian; Szalkowski Deborah; Suresh Singh; Ying-Duo Gao; Giovanna Scapin; Sangita Patel; Barbara Leiting; Reshma Patel; Joseph Wu; Xiaoping Zhang; Nancy A Thornberry; Ann E Weber
Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design.
Bioorganic & medicinal chemistry letters 2008;18(13):3706-10.
2008: Scott D Edmondson; Lan Wei; Jinyou Xu; Jackie Shang; Shiyao Xu; Jianmei Pang; Ashok Chaudhary; Dennis C Dean; Huaibing He; Barbara Leiting; Kathryn A Lyons; Reshma A Patel; Sangita B Patel; Giovanna Scapin; Joseph K Wu; Maria G Beconi; Nancy A Thornberry; Ann E Weber
Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(7):2409-13.
2008: Dooseop Kim; Jennifer E Kowalchick; Linda L Brockunier; Emma R Parmee; George J Eiermann; Michael H Fisher; Huaibing He; Barbara Leiting; Kathryn Lyons; Giovanna Scapin; Sangita B Patel; Aleksandr Petrov; KellyAnn D Pryor; Ranabir Sinha Roy; Joseph K Wu; Xiaoping Zhang; Matthew J Wyvratt; Bei B Zhang; Lan Zhu; Nancy A Thornberry; Ann E Weber
Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines.
Journal of medicinal chemistry 2008;51(3):589-602.
2008: Weizhen Wu; Jin Shang; Yue Feng; Chris Thompson; Jing Li; John Ryan Thompson; Euan D MacIntyre; Nancy A Thornberry; Kevin Chapman; Yun-Ping Zhou; Andrew D Howard; Jing Li
Identification of glucose-dependant insulin secretion targets in pancreatic beta cells by combining defined-mechanism compound library screening and siRNA gene silencing.
Journal of biomolecular screening 2008;13(2):128-34.
2007: Ping Chen; Charles G Caldwell; Robert J Mathvink; Barbara Leiting; Frank Marsilio; Reshma A Patel; Joseph K Wu; Huaibing He; Kathryn A Lyons; Nancy A Thornberry; Ann E Weber
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
Bioorganic & medicinal chemistry letters 2007;17(21):5853-7.
2007: David E Kaelin; Abigail L Smenton; George J Eiermann; Huaibing He; Barbara Leiting; Kathryn A Lyons; Reshma A Patel; Sangita B Patel; Aleksandr Petrov; Giovanna Scapin; Joseph K Wu; Nancy A Thornberry; Ann E Weber; Joseph L Duffy
4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV.
Bioorganic & medicinal chemistry letters 2007;17(21):5806-11.
2007: Jennifer E Kowalchick; Barbara Leiting; KellyAnn D Pryor; Frank Marsilio; Joseph K Wu; Huaibing He; Kathryn A Lyons; George J Eiermann; Aleksandr Petrov; Giovanna Scapin; Reshma A Patel; Nancy A Thornberry; Ann E Weber; Dooseop Kim
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(21):5934-9.
2007: Jason M. Cox; Bart Harper; Anthony Mastracchio; Barbara Leiting; Ranabir Sinha Roy; Reshma A Patel; Joseph K Wu; Kathryn A Lyons; Huaibing He; Shiyao Xu; Bing Zhu; Nancy A Thornberry; Ann E Weber; Scott D Edmondson
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(16):4579-83.
2007: Ying-Duo Gao; Dennis Feng; Robert P Sheridan; Giovanna Scapin; Sangita B Patel; Joseph K Wu; Xiaoping Zhang; Ranabir Sinha Roy; Nancy A Thornberry; Ann E Weber; Szalkowski Deborah
Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(14):3877-9.
2007: Dooseop Kim; Jennifer E Kowalchick; Scott D Edmondson; Anthony Mastracchio; Jinyou Xu; George J Eiermann; Barbara Leiting; Joseph K Wu; KellyAnn D Pryor; Reshma A Patel; Huaibing He; Kathryn A Lyons; Nancy A Thornberry; Ann E Weber
Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).
Bioorganic & medicinal chemistry letters 2007;17(12):3373-7.
2007: Szalkowski Deborah; Giovanna Scapin; Suresh Singh; Dennis Feng; Joseph W Becker; George J Eiermann; Huaibing He; Kathryn Lyons; Sangita Patel; Aleksandr Petrov; Ranabir Sinha Roy; Bei Zhang; Joseph Wu; Xiaoping Zhang; George A Doss; Nancy A Thornberry; Ann E Weber
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.
Bioorganic & medicinal chemistry letters 2007;17(12):3384-7.
2007: Joseph L Duffy; Brian A Kirk; Liping Wang; George J Eiermann; Huaibing He; Barbara Leiting; Kathryn A Lyons; Reshma A Patel; Sangita B Patel; Aleksandr Petrov; Giovanna Scapin; Joseph K Wu; Nancy A Thornberry; Ann E Weber
4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV.
Bioorganic & medicinal chemistry letters 2007;17(10):2879-85.
2007: Gui-Bai Liang; Xiaoxia Qian; Dennis Feng; Szalkowski Deborah; George J Eiermann; Huaibing He; Barbara Leiting; Kathryn Lyons; Aleksandr Petrov; Ranabir Sinha Roy; Bei Zhang; Joseph Wu; Xiaoping Zhang; Nancy A Thornberry; Ann E Weber
Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes.
Bioorganic & medicinal chemistry letters 2007;17(7):1903-7.
2007: Livia Casciola-Rosen; Margarita Garcia-Calvo; Herbert G Bull; Joseph W Becker; Tonie Hines; Nancy A Thornberry; Antony Rosen
Mouse and human granzyme B have distinct tetrapeptide specificities and abilities to recruit the bid pathway.
The Journal of biological chemistry 2007;282(7):4545-52.
2007: Nancy A Thornberry; Ann E Weber
Discovery of JANUVIA (Sitagliptin), a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Current topics in medicinal chemistry 2007;7(6):557-68.
2007: Szalkowski Deborah; Dennis Feng; Xiaoxia Qian; Gui-Bai Liang; Gerard Kieczykowski; George J Eiermann; Huaibing He; Barbara Leiting; Kathryn Lyons; Aleksandr Petrov; Ranabir Sinha Roy; Bei Zhang; Giovanna Scapin; Sangita Patel; Ying-Duo Gao; Suresh Singh; Joseph Wu; Xiaoping Zhang; Nancy A Thornberry; Ann E Weber
(3R)-4-[(3R)-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.
Bioorganic & medicinal chemistry letters 2007;17(1):49-52.
2006: Jinyou Xu; Lan Wei; Robert J Mathvink; Scott D Edmondson; George J Eiermann; Huaibing He; Joseph F Leone; Barbara Leiting; Kathryn A Lyons; Frank Marsilio; Reshma A Patel; Sangita B Patel; Aleksandr Petrov; Giovanna Scapin; Joseph K Wu; Nancy A Thornberry; Ann E Weber
Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(20):5373-7.
2006: Scott D Edmondson; Anthony Mastracchio; Robert J Mathvink; Jiafang He; Bart Harper; You-Jung Park; Maria G Beconi; Jerry Di Salvo; George J Eiermann; Huaibing He; Barbara Leiting; Joseph F Leone; Dorothy A Levorse; Kathryn Lyons; Reshma A Patel; Sangita B Patel; Aleksandr Petrov; Giovanna Scapin; Jackie Shang; Ranabir Sinha Roy; Aaron Smith; Joseph K Wu; Shiyao Xu; Bing Zhu; Nancy A Thornberry; Ann E Weber
(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 alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Journal of medicinal chemistry 2006;49(12):3614-27.
2006: James Mu; John Woods; Yun-Ping Zhou; Ranabir Sinha Roy; Zhihua Li; Emanuel Zycband; Yue Feng; Lan Zhu; Cai Li; Andrew D Howard; David E Moller; Nancy A Thornberry; Bei B Zhang
Chronic inhibition of dipeptidyl peptidase-4 with a sitagliptin analog preserves pancreatic beta-cell mass and function in a rodent model of type 2 diabetes.
Diabetes 2006;55(6):1695-704.
2006: Jinyou Xu; Lan Wei; Robert J Mathvink; Scott D Edmondson; Anthony Mastracchio; George J Eiermann; Huaibing He; Joseph F Leone; Barbara Leiting; Kathryn A Lyons; Frank Marsilio; Reshma A Patel; Aleksandr Petrov; Joseph K Wu; Nancy A Thornberry; Ann E Weber
Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(5):1346-9.
2005: George R Lankas; Barbara Leiting; Ranabir Sinha Roy; George J Eiermann; Maria G Beconi; Szalkowski Deborah; Chi-Chung Chan; Scott D Edmondson; William P Feeney; Huaibing He; Dawn E Ippolito; Dooseop Kim; Kathryn A Lyons; Hyun O Ok; Reshma A Patel; Aleksandr N Petrov; Kelly Ann Pryor; Xiaoxia Qian; Leah Reigle; Andrea Woods; Joseph K Wu; Dennis Zaller; Xiaoping Zhang; Lan Zhu; Ann E Weber; Nancy A Thornberry
Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9.
Diabetes 2005;54(10):2988-94.
2005: Christophe Mellon; Renee Aspiotis; Cameron W Black; Christopher I Bayly; Erich L Grimm; André Giroux; Yongxin Han; Elise Isabel; Daniel J McKay; Donald W Nicholson; Dita M Rasper; Sophie Roy; John Tam; Nancy A Thornberry; John P Vaillancourt; Steven Xanthoudakis; Robert Zamboni
Lipophilic versus hydrogen-bonding effect in P3 on potency and selectivity of valine aspartyl ketones as caspase 3 inhibitors.
Bioorganic & medicinal chemistry letters 2005;15(17):3886-90.
2005: Scott D Edmondson; Anthony Mastracchio; Joseph L Duffy; George J Eiermann; Huaibing He; Ida Ita; Barbara Leiting; Joseph F Leone; Kathryn A Lyons; Amanda M Makarewicz; Reshma A Patel; Aleksandr Petrov; Joseph K Wu; Nancy A Thornberry; Ann E Weber
Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.
Bioorganic & medicinal chemistry letters 2005;15(12):3048-52.
2005: Margarita Garcia-Calvo; JeanMarie Lisnock; Herbert G Bull; Brian E Hawes; Duane A Burnett; Matthew P Braun; James H Crona; Harry R Davis; Dennis C Dean; Patricia A Detmers; Michael P Graziano; Meredith Hughes; D Euan MacIntyre; Anthony Ogawa; Kim A O'neill; Sai Prasad N Iyer; Diane E Shevell; Marsha M Smith; Yui S Tang; Amanda M Makarewicz; Feroze Ujjainwalla; Scott W Altmann; Kevin Chapman; Nancy A Thornberry
The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1).
Proceedings of the National Academy of Sciences of the United States of America 2005;102(23):8132-7.
2005: Jinyou Xu; Lan Wei; Robert J Mathvink; Jiafang He; You-Jung Park; Huaibing He; Barbara Leiting; Kathryn A Lyons; Frank Marsilio; Reshma A Patel; Joseph K Wu; Nancy A Thornberry; Ann E Weber
Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.
Bioorganic & medicinal chemistry letters 2005;15(10):2533-6.
2005: Wallace T Ashton; Rosemary M Sisco; Hong Dong; Kathryn A Lyons; Huaibing He; George A Doss; Barbara Leiting; Reshma A Patel; Joseph K Wu; Frank Marsilio; Nancy A Thornberry; Ann E Weber
Dipeptidyl peptidase IV inhibitors derived from beta-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole.
Bioorganic & medicinal chemistry letters 2005;15(9):2253-8.
2005: Dooseop Kim; Liping Wang; Maria G Beconi; George J Eiermann; Michael H Fisher; Huaibing He; Gerard J Hickey; Jennifer E Kowalchick; Barbara Leiting; Kathryn Lyons; Frank Marsilio; Margaret E McCann; Reshma A Patel; Aleksandr Petrov; Giovanna Scapin; Sangita B Patel; Ranabir Sinha Roy; Joseph K Wu; Matthew J Wyvratt; Bei B Zhang; Lan Zhu; Nancy A Thornberry; Ann E Weber
(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.
Journal of medicinal chemistry 2005;48(1):141-51.
2004: Scott D Edmondson; Anthony Mastracchio; Maria G Beconi; Lawrence F Colwell; Bahanu Habulihaz; Huaibing He; Sanjeev Kumar; Barbara Leiting; Kathryn A Lyons; Ann Mao; Frank Marsilio; Reshma A Patel; Joseph K Wu; Lan Zhu; Nancy A Thornberry; Ann E Weber; Emma R Parmee
Potent and selective proline derived dipeptidyl peptidase IV inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(20):5151-5.
2004: Linda L Brockunier; Jiafang He; Lawrence F Colwell; Bahanu Habulihaz; Huaibing He; Barbara Leiting; Kathryn A Lyons; Frank Marsilio; Reshma A Patel; Yohannes Teffera; Joseph K Wu; Nancy A Thornberry; Ann E Weber; Emma R Parmee
Substituted piperazines as novel dipeptidyl peptidase IV inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(18):4763-6.
2004: Jinyou Xu; Hyun O Ok; Edward J Gonzalez; Lawrence F Colwell; Bahanu Habulihaz; Huaibing He; Barbara Leiting; Kathryn A Lyons; Frank Marsilio; Reshma A Patel; Joseph K Wu; Nancy A Thornberry; Ann E Weber; Emma R Parmee
Discovery of potent and selective beta-homophenylalanine based dipeptidyl peptidase IV inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(18):4759-62.
2004: Joseph W Becker; Jennifer Rotonda; Stephen M Soisson; Renee Aspiotis; Christopher I Bayly; Sébastien Francoeur; Michel Gallant; Marga Garcia-Calvo; André Giroux; Erich L Grimm; Yongxin Han; Dan McKay; Donald W Nicholson; Erin Peterson; Johanne Renaud; Sophie Roy; Nancy A Thornberry; Robert Zamboni
Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis.
Journal of medicinal chemistry 2004;47(10):2466-74.
2004: Charles G Caldwell; Ping Chen; Jiafang He; Emma R Parmee; Barbara Leiting; Frank Marsilio; Reshma A Patel; Joseph K Wu; George J Eiermann; Aleksandr Petrov; Huaibing He; Kathryn A Lyons; Nancy A Thornberry; Ann E Weber
Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(5):1265-8.
2004: Wallace T Ashton; Hong Dong; Rosemary M Sisco; George A Doss; Barbara Leiting; Reshma A Patel; Joseph K Wu; Frank Marsilio; Nancy A Thornberry; Ann E Weber
Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(4):859-63.
2004: Yongxin Han; André Giroux; Erich L Grimm; Renee Aspiotis; Sébastien Francoeur; Christopher I Bayly; Daniel J McKay; Sophie Roy; Steven Xanthoudakis; John P Vaillancourt; Dita M Rasper; John Tam; Paul Tawa; Nancy A Thornberry; Erin P Paterson; Margarita Garcia-Calvo; Joseph W Becker; Jennifer Rotonda; Donald W Nicholson; Robert Zamboni
Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(3):805-8.
2004: Emma R Parmee; Jiafang He; Anthony Mastracchio; Scott D Edmondson; Lawrence F Colwell; George J Eiermann; William P Feeney; Bahanu Habulihaz; Huaibing He; Ruth Kilburn; Barbara Leiting; Kathryn Lyons; Frank Marsilio; Reshma A Patel; Aleksandr Petrov; Jerry Di Salvo; Joseph K Wu; Nancy A Thornberry; Ann E Weber
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(1):43-6.
2003: Alexei F Kisselev; Margarita Garcia-Calvo; Herman S Overkleeft; Erin Peterson; Michael Pennington; Hidde L Ploegh; Nancy A Thornberry; Alfred L Goldberg
The caspase-like sites of proteasomes, their substrate specificity, new inhibitors and substrates, and allosteric interactions with the trypsin-like sites.
The Journal of biological chemistry 2003;278(38):35869-77.
2003: Elise Isabel; W Cameron Black; Christopher I Bayly; Erich L Grimm; Marc K Janes; Daniel J McKay; Donald W Nicholson; Dita M Rasper; Johanne Renaud; Sophie Roy; John Tam; Nancy A Thornberry; John P Vaillancourt; Steven Xanthoudakis; Robert Zamboni
Nicotinyl aspartyl ketones as inhibitors of caspase-3.
Bioorganic & medicinal chemistry letters 2003;13(13):2137-40.
2003: Lan Zhu; Constantin Tamvakopoulos; Dan Xie; Jasminka Dragovic; Xiaolan Shen; Judy Fenyk-Melody; Keith Schmidt; Ansuman Bagchi; Patrick R Griffin; Nancy A Thornberry; Ranabir Sinha Roy
The role of dipeptidyl peptidase IV in the cleavage of glucagon family peptides: in vivo metabolism of pituitary adenylate cyclase activating polypeptide-(1-38).
The Journal of biological chemistry 2003;278(25):22418-23.
2003: Stacey L Conarello; Zhihua Li; John Ronan; Ranabir Sinha Roy; Lan Zhu; Guoqiang Jiang; Franklin Liu; John Woods; Emanuel Zycband; David E Moller; Nancy A Thornberry; Bei B Zhang
Mice lacking dipeptidyl peptidase IV are protected against obesity and insulin resistance.
Proceedings of the National Academy of Sciences of the United States of America 2003;100(11):6825-30.
2003: Barbara Leiting; KellyAnn D Pryor; Joseph K Wu; Frank Marsilio; Reshma A Patel; Charles S Craik; Jonathan A Ellman; Richard T Cummings; Nancy A Thornberry
Catalytic properties and inhibition of proline-specific dipeptidyl peptidases II, IV and VII.
The Biochemical journal 2003;371(Pt 2):525-32.
2003: Donald W Nicholson; Nancy A Thornberry
Apoptosis. Life and death decisions.
Science (New York, N.Y.) 2003;299(5604):214-5.
2002: Christopher A Willoughby; Herbert G Bull; Margarita Garcia-Calvo; Joanne Jiang; Kevin Chapman; Nancy A Thornberry
Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis.
Bioorganic & medicinal chemistry letters 2002;12(16):2197-200.
2001: Felipe Andrade; Herbert G Bull; Nancy A Thornberry; Gary Ketner; Livia Casciola-Rosen; Antony Rosen
Adenovirus L4-100K assembly protein is a granzyme B substrate that potently inhibits granzyme B-mediated cell death.
Immunity 2001;14(6):751-61.
2001: Sophie Roy; Christopher I Bayly; Yves Gareau; Vicky Houtzager; Stacia Kargman; S L Keen; K Rowland; I M Seiden; Nancy A Thornberry; Donald W Nicholson
Maintenance of caspase-3 proenzyme dormancy by an intrinsic "safety catch" regulatory tripeptide.
Proceedings of the National Academy of Sciences of the United States of America 2001;98(11):6132-7.
2001: Jennifer Rotonda; Margarita Garcia-Calvo; Herbert G Bull; Wayne M Geissler; Brian McKeever; Christopher A Willoughby; Nancy A Thornberry; Joseph W Becker
The three-dimensional structure of human granzyme B compared to caspase-3, key mediators of cell death with cleavage specificity for aspartic acid in P1.
Chemistry & biology 2001;8(4):357-68.
2000: Shin Jung Kang; S Wang; H Hara; EP Peterson; Shobu Namura; Sepideh Amin-Hanjani; Zhihong Huang; A Srinivasan; K J Tomaselli; Nancy A Thornberry; Michael A Moskowitz; Junying Yuan
Dual role of caspase-11 in mediating activation of caspase-1 and caspase-3 under pathological conditions.
The Journal of cell biology 2000;149(3):613-22.
2000: M Mancini; Carolyn E Machamer; S Roy; Donald W Nicholson; Nancy A Thornberry; Livia Casciola-Rosen; Antony Rosen
Caspase-2 is localized at the Golgi complex and cleaves golgin-160 during apoptosis.
The Journal of cell biology 2000;149(3):603-12.
2000: Nancy A Thornberry; Kevin Chapman; Donald W Nicholson
Determination of caspase specificities using a peptide combinatorial library.
Methods in enzymology 2000;322():100-10.
1999: François G Gervais; D Xu; George S Robertson; John P Vaillancourt; Y Zhu; J Huang; A LeBlanc; D Smith; M Rigby; Mark S Shearman; E E Clarke; Hui Zheng; L H Van Der Ploeg; Salvatore C Ruffolo; Nancy A Thornberry; Steven Xanthoudakis; Robert Zamboni; Sophie Roy; Donald W Nicholson
Involvement of caspases in proteolytic cleavage of Alzheimer's amyloid-beta precursor protein and amyloidogenic A beta peptide formation.
Cell 1999;97(3):395-406.
1999: Margarita Garcia-Calvo; EP Peterson; Dita M Rasper; John P Vaillancourt; Robert Zamboni; Donald W Nicholson; Nancy A Thornberry
Purification and catalytic properties of human caspase family members.
Cell death and differentiation 1999;6(4):362-9.
1998: Margarita Garcia-Calvo; EP Peterson; Barbara Leiting; R Ruel; Donald W Nicholson; Nancy A Thornberry
Inhibition of human caspases by peptide-based and macromolecular inhibitors.
The Journal of biological chemistry 1998;273(49):32608-13.
1998: Jennifer L Harris; EP Peterson; Dorothy Hudig; Nancy A Thornberry; Charles S Craik
Definition and redesign of the extended substrate specificity of granzyme B.
The Journal of biological chemistry 1998;273(42):27364-73.
1998: Nancy A Thornberry; Y Lazebnik
Caspases: enemies within.
Science (New York, N.Y.) 1998;281(5381):1312-6.
1998: François G Gervais; Nancy A Thornberry; Salvatore C Ruffolo; Donald W Nicholson; Sophie Roy
Caspases cleave focal adhesion kinase during apoptosis to generate a FRNK-like polypeptide.
The Journal of biological chemistry 1998;273(27):17102-8.
1998: Nancy A Thornberry
Caspases: key mediators of apoptosis.
Chemistry & biology 1998;5(5):R97-103.
1998: Dita M Rasper; John P Vaillancourt; Shinji Hadano; Vicky Houtzager; I Seiden; S L Keen; Paul Tawa; Steven Xanthoudakis; Jamal Nasir; Duane W Martindale; BF Koop; EP Peterson; Nancy A Thornberry; J Huang; D P MacPherson; SC Black; Felicita Hornung; Michael J Lenardo; Michael R Hayden; Sophie Roy; Donald W Nicholson
Cell death attenuation by 'Usurpin', a mammalian DED-caspase homologue that precludes caspase-8 recruitment and activation by the CD-95 (Fas, APO-1) receptor complex.
Cell death and differentiation 1998;5(4):271-88.
1998: Felipe Andrade; S Roy; D Nicholson; Nancy A Thornberry; Antony Rosen; Livia Casciola-Rosen
Granzyme B directly and efficiently cleaves several downstream caspase substrates: implications for CTL-induced apoptosis.
Immunity 1998;8(4):451-60.
1998: M Mancini; Donald W Nicholson; S Roy; Nancy A Thornberry; EP Peterson; Livia Casciola-Rosen; Antony Rosen
The caspase-3 precursor has a cytosolic and mitochondrial distribution: implications for apoptotic signaling.
The Journal of cell biology 1998;140(6):1485-95.
1998: D M Sanghavi; M Thelen; Nancy A Thornberry; Livia Casciola-Rosen; Antony Rosen
Caspase-mediated proteolysis during apoptosis: insights from apoptotic neutrophils.
FEBS letters 1998;422(2):179-84.
1997: Donald W Nicholson; Nancy A Thornberry
Caspases: killer proteases.
Trends in biochemical sciences 1997;22(8):299-306.
1997: Nancy A Thornberry; Thomas A Rano; EP Peterson; Dita M Rasper; T Timkey; Margarita Garcia-Calvo; Vicky Houtzager; P A Nordstrom; Sophie Roy; John P Vaillancourt; Kevin Chapman; Donald W Nicholson
A combinatorial approach defines specificities of members of the caspase family and granzyme B. Functional relationships established for key mediators of apoptosis.
The Journal of biological chemistry 1997;272(29):17907-11.
1997: Thomas A Rano; T Timkey; EP Peterson; Jennifer Rotonda; Donald W Nicholson; Joseph W Becker; Kevin Chapman; Nancy A Thornberry
A combinatorial approach for determining protease specificities: application to interleukin-1beta converting enzyme (ICE).
Chemistry & biology 1997;4(2):149-55.
1997: Nancy A Thornberry
The caspase family of cysteine proteases.
British medical bulletin 1997;53(3):478-90.
1997: Nancy A Thornberry; Antony Rosen; Donald W Nicholson
Control of apoptosis by proteases.
Advances in pharmacology (San Diego, Calif.) 1997;41():155-77.
1996: E S Alnemri; D J Livingston; Donald W Nicholson; G Salvesen; Nancy A Thornberry; W W Wong; J Yuan
Human ICE/CED-3 protease nomenclature.
Cell 1996;87(2):171.
1996: Y Paul Goldberg; Donald W Nicholson; Dita M Rasper; M A Kalchman; H B Koide; Graham Kyrenia Rona; M Bromm; P Kazemi-Esfarjani; Nancy A Thornberry; John P Vaillancourt; Michael R Hayden
Cleavage of huntingtin by apopain, a proapoptotic cysteine protease, is modulated by the polyglutamine tract.
Nature genetics 1996;13(4):442-9.
1996: Jennifer Rotonda; Donald W Nicholson; K M Fazil; M Gallant; Y Gareau; M Labelle; EP Peterson; Dita M Rasper; R Ruel; John P Vaillancourt; Nancy A Thornberry; Joseph W Becker
The three-dimensional structure of apopain/CPP32, a key mediator of apoptosis.
Nature structural biology 1996;3(7):619-25.
1996: Livia Casciola-Rosen; Donald W Nicholson; T Chong; K R Rowan; Nancy A Thornberry; D K Miller; Antony Rosen
Apopain/CPP32 cleaves proteins that are essential for cellular repair: a fundamental principle of apoptotic death.
The Journal of experimental medicine 1996;183(5):1957-64.
1996: J Schlegel; I Peters; Sten Orrenius; D K Miller; Nancy A Thornberry; T T Yamin; Donald W Nicholson
CPP32/apopain is a key interleukin 1 beta converting enzyme-like protease involved in Fas-mediated apoptosis.
The Journal of biological chemistry 1996;271(4):1841-4.
1995: Donald W Nicholson; A Ali; Nancy A Thornberry; John P Vaillancourt; C K Ding; M Gallant; Y Gareau; P R Griffin; M Labelle; Y A Lazebnik
Identification and inhibition of the ICE/CED-3 protease necessary for mammalian apoptosis.
Nature 1995;376(6535):37-43.
1995: Andrew D Howard; Oksana C Palyha; P R Griffin; EP Peterson; A B Lenny; G J Ding; David J Pickup; Nancy A Thornberry; J A Schmidt; M J Tocci
Human IL-1 beta processing and secretion in recombinant baculovirus-infected Sf9 cells is blocked by the cowpox virus serpin crmA.
Journal of immunology (Baltimore, Md. : 1950) 1995;154(5):2321-32.
1995: Daniel S Fletcher; L Agarwal; Kevin Chapman; J Chin; L A Egger; G Limjuco; Silvi Luell; D E MacIntyre; EP Peterson; Nancy A Thornberry
A synthetic inhibitor of interleukin-1 beta converting enzyme prevents endotoxin-induced interleukin-1 beta production in vitro and in vivo.
Journal of interferon & cytokine research : the official journal of the International Society for Interferon and Cytokine Research 1995;15(3):243-8.
1995: Nancy A Thornberry; S M Molineaux
Interleukin-1 beta converting enzyme: a novel cysteine protease required for IL-1 beta production and implicated in programmed cell death.
Protein science : a publication of the Protein Society 1995;4(1):3-12.
1994: T Komiyama; Caroline A Ray; David J Pickup; Andrew D Howard; Nancy A Thornberry; EP Peterson; G Salvesen
Inhibition of interleukin-1 beta converting enzyme by the cowpox virus serpin CrmA. An example of cross-class inhibition.
The Journal of biological chemistry 1994;269(30):19331-7.
1994: Nancy A Thornberry; EP Peterson; J J Zhao; Andrew D Howard; P R Griffin; Kevin Chapman
Inactivation of interleukin-1 beta converting enzyme by peptide (acyloxy)methyl ketones.
Biochemistry 1994;33(13):3934-40.
1994: Nancy A Thornberry
Interleukin-1 beta converting enzyme.
Methods in enzymology 1994;244():615-31.
1993: D K Miller; JR Calaycay; Kevin Chapman; Andrew D Howard; M J Kostura; S M Molineaux; Nancy A Thornberry
The IL-1 beta converting enzyme as a therapeutic target.
Annals of the New York Academy of Sciences 1993;696():133-48.
1992: Nancy A Thornberry; H G Bull; JR Calaycay; Kevin Chapman; Andrew D Howard; M J Kostura; D K Miller; S M Molineaux; J R Weidner; John G Aunins
A novel heterodimeric cysteine protease is required for interleukin-1 beta processing in monocytes.
Nature 1992;356(6372):768-74.
1991: Nancy A Thornberry; H G Bull; D Taub; K E Wilson; G Giménez-Gallego; A Rosegay; D D Soderman; Arthur A Patchett
Mechanism-based inactivation of alanine racemase by 3-halovinylglycines.
The Journal of biological chemistry 1991;266(32):21657-65.
1991: Andrew D Howard; M J Kostura; Nancy A Thornberry; G J Ding; G Limjuco; J Weidner; J P Salley; K A Hogquist; D D Chaplin; R A Mumford
IL-1-converting enzyme requires aspartic acid residues for processing of the IL-1 beta precursor at two distinct sites and does not cleave 31-kDa IL-1 alpha.
Journal of immunology (Baltimore, Md. : 1950) 1991;147(9):2964-9.
1989: C Dunwiddie; Nancy A Thornberry; H G Bull; Mohinder K Sardana; P A Friedman; J W Jacobs; E Simpson
Antistasin, a leech-derived inhibitor of factor Xa. Kinetic analysis of enzyme inhibition and identification of the reactive site.
The Journal of biological chemistry 1989;264(28):16694-9.
1988: Arthur A Patchett; D Taub; B Weissberger; M E Valiant; H Gadebusch; Nancy A Thornberry; H G Bull
Antibacterial activities of fluorovinyl- and chlorovinylglycine and several derived dipeptides.
Antimicrobial agents and chemotherapy 1988;32(3):319-23.
1988: C A Rouzer; Nancy A Thornberry; H G Bull
Kinetic effects of ATP and two cellular stimulatory components on human leukocyte 5-lipoxygenase.
Annals of the New York Academy of Sciences 1988;524():1-11.
1985: H G Bull; Nancy A Thornberry; E H Cordes
Purification of angiotensin-converting enzyme from rabbit lung and human plasma by affinity chromatography.
The Journal of biological chemistry 1985;260(5):2963-72.
1985: H G Bull; Nancy A Thornberry; M H Cordes; Arthur A Patchett; E H Cordes
Inhibition of rabbit lung angiotensin-converting enzyme by N alpha-[(S)-1-carboxy-3-phenylpropyl]L-alanyl-L-proline and N alpha-[(S)-1-carboxy-3-phenylpropyl]L-lysyl-L-proline.
The Journal of biological chemistry 1985;260(5):2952-62.
1984: M A Cascieri; H G Bull; R A Mumford; Arthur A Patchett; Nancy A Thornberry; T Liang
Carboxyl-terminal tripeptidyl hydrolysis of substance P by purified rabbit lung angiotensin-converting enzyme and the potentiation of substance P activity in vivo by captopril and MK-422.
Molecular pharmacology 1984;25(2):287-93.
1982: H A El-Dorry; H G Bull; K Iwata; Nancy A Thornberry; E H Cordes; R L Soffer
Molecular and catalytic properties of rabbit testicular dipeptidyl carboxypeptidase.
The Journal of biological chemistry 1982;257(23):14128-33.