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William Hagmann

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Ihor Kopka; Linus S Lin; James P Jewell; Thomas J Lanza; Tung M Fong; Chun-Pyn Shen; Zhege J Lao; Sookhee Ha; Laurie G Castonguay; Lex Van der Ploeg; Mark T Goulet; William K Hagmann
Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant.
Wu Du; James P Jewell; Linus S Lin; Vincent J Colandrea; Jing Chen Xiao; Julie Lao; Chun-Pyn Shen; Thomas J Bateman; Vijay B G Reddy; Sookhee N Ha; Shrenik K Shah; Tung M Fong; Jeffrey J Hale; William K Hagmann
Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists.
Kelly M Treonze; Kenneth Alves; Paul Fischer; William K Hagmann; Donald Hora; Alison Kulick; Ken Vakerich; Nicholas D Smith; Russell Lingham; Salony Maniar; Thomas S Reger; Jasmine Zunic; Benito Munoz; Peppi Prasit; Donald Nicholson; Qian Si; Keith Judd; Susan Nicolich; Patricia Kellerhouse; Donald Thompson; Richard A Mumford
Characterization of alpha(4)beta(1) (CD49d/CD29) on equine leukocytes: potential utility of a potent alpha(4)beta(1) (CD49d/CD29) receptor antagonist in the treatment of equine heaves (recurrent airway obstruction).

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All Publications

2010: Ihor Kopka; Linus S Lin; James P Jewell; Thomas J Lanza; Tung M Fong; Chun-Pyn Shen; Zhege J Lao; Sookhee Ha; Laurie G Castonguay; Lex Van der Ploeg; Mark T Goulet; William K Hagmann
Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant.
Bioorganic & medicinal chemistry letters 2010;20(16):4757-61.
2009: Wu Du; James P Jewell; Linus S Lin; Vincent J Colandrea; Jing Chen Xiao; Julie Lao; Chun-Pyn Shen; Thomas J Bateman; Vijay B G Reddy; Sookhee N Ha; Shrenik K Shah; Tung M Fong; Jeffrey J Hale; William K Hagmann
Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists.
Bioorganic & medicinal chemistry letters 2009;19(17):5195-9.
2009: Kelly M Treonze; Kenneth Alves; Paul Fischer; William K Hagmann; Donald Hora; Alison Kulick; Ken Vakerich; Nicholas D Smith; Russell Lingham; Salony Maniar; Thomas S Reger; Jasmine Zunic; Benito Munoz; Peppi Prasit; Donald Nicholson; Qian Si; Keith Judd; Susan Nicolich; Patricia Kellerhouse; Donald Thompson; Richard A Mumford
Characterization of alpha(4)beta(1) (CD49d/CD29) on equine leukocytes: potential utility of a potent alpha(4)beta(1) (CD49d/CD29) receptor antagonist in the treatment of equine heaves (recurrent airway obstruction).
Veterinary immunology and immunopathology 2009;130(1-2):79-87.
2009: Terence G Hamill; Linus S Lin; William K Hagmann; Ping Liu; James P Jewell; Sandra Sanabria; Waisi Eng; Christine Ryan; Tung M Fong; Brett Connolly; Amy Vanko; Richard Hargreaves; Mark T Goulet; H Donald Burns
PET imaging studies in rhesus monkey with the cannabinoid-1 (CB1) receptor ligand [11C]CB-119.
Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging 2009;11(4):246-52.
2009: Linus S Lin; Thomas J Lanza; James P Jewell; Ping Liu; Carrie Jones; Gerard R Kieczykowski; Kelly Treonze; Qian Si; Salony Manior; Gloria C Koo; Xinchun Tong; Junying Wang; Anne Schuelke; James V Pivnichny; Regina Wang; Conrad E Raab; Stella Vincent; Philip Davies; Malcolm MacCoss; Richard A Mumford; William K Hagmann
Discovery of N-{N-[(3-cyanophenyl)sulfonyl]-4(R)-cyclobutylamino-(L)-prolyl}-4-[(3',5'-dichloroisonicotinoyl) amino]-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4.
Journal of medicinal chemistry 2009;52(11):3449-52.
2009: Petr Vachal; Joan M Fletcher; Tung M Fong; Cathy C R-R Huang; Julie Lao; Jing Chen Xiao; Chun-Pyn Shen; Alison M Strack; Lauren P Shearman; Sloan Stribling; Richard Z Chen; Andrea Frassetto; Xinchun Tong; Junying Wang; Richard G Ball; Nancy N Tsou; Gerard J Hickey; Donald Thompson; TD Faidley; Susan Nicolich; Joana Achanfuo-Yeboah; Donald F Hora; Jeffrey J Hale; William K Hagmann
1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity.
Journal of medicinal chemistry 2009;52(8):2550-8.
2008: Jing Chen Xiao; James P Jewell; Linus S Lin; William K Hagmann; Tung M Fong; Chun-Pyn Shen
Similar in vitro pharmacology of human cannabinoid CB1 receptor variants expressed in CHO cells.
Brain research 2008;1238():36-43.
2008: William K Hagmann
The many roles for fluorine in medicinal chemistry.
Journal of medicinal chemistry 2008;51(15):4359-69.
2008: Linus S Lin; Sookhee Ha; Richard G Ball; Nancy N Tsou; Laurie A Castonguay; George A Doss; Tung M Fong; Chun-Pyn Shen; Jing Chen Xiao; Mark T Goulet; William K Hagmann
Conformational analysis and receptor docking of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (taranabant, MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist.
Journal of medicinal chemistry 2008;51(7):2108-14.
2008: Linda L Chang; Ginger X Yang; Ermengilda McCauley; Richard A Mumford; John A Schmidt; William K Hagmann
Constraining the amide bond in N-sulfonylated dipeptide VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2008;18(5):1688-91.
2008: Wei Tang; Ralph A Stearns; Qing Chen; K Bleasby; Yohannes Teffera; Adria Colletti; M Hafey; Raymond Evers; Dennis C Dean; Plato A Magriotis; Thomas J Lanza; Linus S Lin; William K Hagmann; Thomas A Baillie
Importance of mechanistic drug metabolism studies in support of drug discovery: A case study with an N -sulfonylated dipeptide VLA-4 antagonist in rats.
Xenobiotica; the fate of foreign compounds in biological systems 2008;38(2):223-37.
2008: Lauren P Shearman; D Sloan Stribling; Ramon E Camacho; Kimberly Rosko; Junying Wang; Sharon Tong; Yue Feng; Donald J Marsh; Hong Yu; Xiaoming Guan; Stephanie K Spann; Douglas J MacNeil; Tung M Fong; Joseph M Metzger; Mark T Goulet; William K Hagmann; Christopher W Plummer; Paul E Finke; Sander G Mills; Shrenik K Shah; Quang Truong; Lex H T Van Der Ploeg; D Euan MacIntyre; Alison M Strack
Characterization of a novel and selective cannabinoid CB1 receptor inverse agonist, Imidazole 24b, in rodents.
European journal of pharmacology 2008;579(1-3):215-24.
2007: Ping Liu; Linus S Lin; Terence G Hamill; James P Jewell; Thomas J Lanza; Raymond E Gibson; Stephen M Krause; Christine Ryan; Waisi Eng; Sandra Sanabria; Xinchun Tong; Junying Wang; Dorothy A Levorse; Karen Owens; Tung M Fong; Chun-Pyn Shen; Julie Lao; Sanjeev Kumar; Wenji Yin; Joseph F Payack; Shawn A Springfield; Richard Hargreaves; H Donald Burns; Mark T Goulet; William K Hagmann
Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use.
Journal of medicinal chemistry 2007;50(15):3427-30.
2007: H Donald Burns; Koen Van Laere; Sandra Sanabria; Terence G Hamill; Guy Bormans; Waisi Eng; Ray Gibson; Christine Ryan; Brett Connolly; Shil Patel; Stephen Krause; Amy Vanko; Anne Van Hecken; Patrick Dupont; Inge De Lepeleire; Paul L Rothenberg; S Aubrey Stoch; Josee Cote; William K Hagmann; James P Jewell; Linus S Lin; Ping Liu; Mark T Goulet; Keith M Gottesdiener; John A Wagner; Jan de Hoon; Luc Mortelmans; Tung M Fong; Richard Hargreaves
[18F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptor.
Proceedings of the National Academy of Sciences of the United States of America 2007;104(23):9800-5.
2007: Tung M Fong; Xiao-Ming Guan; Donald J Marsh; Chun-Pyn Shen; D Sloan Stribling; Kimberly Rosko; Julie Lao; Hong Yu; Yue Feng; Jing Chen Xiao; Lex H T Van Der Ploeg; Mark T Goulet; William K Hagmann; Linus S Lin; Thomas J Lanza; James P Jewell; Ping Liu; Shrenik K Shah; Hongbo Qi; Xinchun Tong; Junying Wang; Suoyu S Xu; Barbara Francis; Alison M Strack; D Euan MacIntyre; Lauren P Shearman
Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents.
The Journal of pharmacology and experimental therapeutics 2007;321(3):1013-22.
2007: Helen E Armstrong; Amy Galka; Linus S Lin; Thomas J Lanza; James P Jewell; Shrenik K Shah; Ravindra N Guthikonda; Quang Truong; Linda L Chang; Grace Quaker; Vincent J Colandrea; Xinchun Tong; Junying Wang; Sherry Xu; Tung M Fong; Chun-Pyn Shen; Julie Lao; Jing Chen; Lauren P Shearman; D Sloan Stribling; Kimberly Rosko; Alison M Strack; Sookhee Ha; Lex H T Van Der Ploeg; Mark T Goulet; William K Hagmann
Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.
Bioorganic & medicinal chemistry letters 2007;17(8):2184-7.
2007: Linda L Chang; Quang Truong; George A Doss; Malcolm MacCoss; Kathryn Lyons; Ermengilda McCauley; Richard A Mumford; Gail Forrest; Stella Vincent; John A Schmidt; William K Hagmann
Highly constrained bicyclic VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2007;17(3):597-601.
2006: Linus S Lin; Thomas J Lanza; James P Jewell; Ping Liu; Shrenik K Shah; Hongbo Qi; Xinchun Tong; Junying Wang; Suoyu S Xu; Tung M Fong; Chun-Pyn Shen; Julie Lao; Jing Chen Xiao; Lauren P Shearman; D Sloan Stribling; Kimberly Rosko; Alison M Strack; Donald J Marsh; Yue Feng; Sanjeev Kumar; Koppara Samuel; Wenji Yin; Lex H T Van Der Ploeg; Mark T Goulet; William K Hagmann
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.
Journal of medicinal chemistry 2006;49(26):7584-7.
2006: Chun-Pyn Shen; Jing Chen Xiao; Helen Armstrong; William K Hagmann; Tung M Fong
F200A substitution in the third transmembrane helix of human cannabinoid CB1 receptor converts AM2233 from receptor agonist to inverse agonist.
European journal of pharmacology 2006;531(1-3):41-6.
2004: K Shankaran; Karla L Donnelly; Shrenik K Shah; Charles G Caldwell; Ping Chen; William K Hagmann; Malcolm MacCoss; John L Humes; Stephen G Pacholok; Theresa M Kelly; Stephan K Grant; Kenny K Wong
Synthesis of analogs of (1,4)-3- and 5-imino oxazepane, thiazepane, and diazepane as inhibitors of nitric oxide synthases.
Bioorganic & medicinal chemistry letters 2004;14(23):5907-11.
2004: Linus S Lin; Thomas J Lanza; Laurie A Castonguay; Theodore M Kamenecka; Ermengilda McCauley; Gail Van Riper; Linda A Egger; Richard A Mumford; Xinchun Tong; Malcolm MacCoss; John A Schmidt; William K Hagmann
Bioisosteric replacement of anilide with benzoxazole: potent and orally bioavailable antagonists of VLA-4.
Bioorganic & medicinal chemistry letters 2004;14(9):2331-4.
2004: Theodore M Kamenecka; You-Jung Park; Linus S Lin; Stephen E de Laszlo; Ermengilda McCauley; Gail Van Riper; Linda A Egger; Usha Kidambi; Richard A Mumford; Sharon Tong; Wei Tang; Adria Colletti; Yohannes Teffera; Ralph A Stearns; Malcolm MacCoss; John A Schmidt; William K Hagmann
Amidines as amide bond replacements in VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2004;14(9):2323-6.
2004: William K Hagmann
The discovery and potential of N-sulfonylated dipeptide VLA-4 antagonists.
Current topics in medicinal chemistry 2004;4(14):1461-71.
2003: Linda A Egger; Jin Cao; Christine McCallum; Usha Kidambi; Gail Van Riper; Ermengilda McCauley; Richard A Mumford; Thomas J Lanza; Linus S Lin; Stephen E de Laszlo; David N Young; Ginger Yang; Dennis C Dean; Conrad E Raab; Michael A Wallace; Allen Jones; William K Hagmann; John A Schmidt; R Blake Pepinsky; Daniel M Scott; Wen-Cherng Lee; Mark Cornebise; Patricia A Detmers
A small molecule alpha4beta1/alpha4beta7 antagonist differentiates between the low-affinity states of alpha4beta1 and alpha4beta7: characterization of divalent cation dependence.
The Journal of pharmacology and experimental therapeutics 2003;306(3):903-13.
2003: George A Doherty; Ginger X Yang; Edite Borges; Sharon Tong; Ermengilda McCauley; Kelly M Treonz; Gail Van Riper; Stephen G Pacholok; Qian Si; Gloria C Koo; Kashmira Shah; Richard A Mumford; William K Hagmann
N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2003;13(11):1891-5.
2003: Gloria C Koo; Kashmira Shah; Gloria J F Ding; Jianying Xiao; Richard Wnek; George Doherty; Xin Chun Tong; R Blake Pepinsky; Ko-Chung Lin; William K Hagmann; Douglas W Kawka; Irwin I Singer
A small molecule very late antigen-4 antagonist can inhibit ovalbumin-induced lung inflammation.
American journal of respiratory and critical care medicine 2003;167(10):1400-9.
2003: Ginger X Yang; William K Hagmann
VLA-4 antagonists: potent inhibitors of lymphocyte migration.
Medicinal research reviews 2003;23(3):369-92.
2003: Clare E Gutteridge; Stephen E de Laszlo; Theodore M Kamenecka; Ermengilda McCauley; Gail Van Riper; Richard A Mumford; Usha Kidambi; Linda A Egger; Sharon Tong; William K Hagmann
N-(3-phenylsulfonyl-3-piperidinoyl)-phenylalanine derivatives as potent, selective VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2003;13(5):885-90.
2003: Koppara Samuel; Wenji Yin; Ralph A Stearns; Yui S Tang; Ashok G Chaudhary; James P Jewell; Thomas J Lanza; Linus S Lin; William K Hagmann; David C Evans; Sanjeev Kumar
Addressing the metabolic activation potential of new leads in drug discovery: a case study using ion trap mass spectrometry and tritium labeling techniques.
Journal of mass spectrometry : JMS 2003;38(2):211-21.
2002: Ihor E Kopka; Linus S Lin; Richard A Mumford; Thomas J Lanza; Plato A Magriotis; David Young; Stephen E DeLaszlo; Malcolm MacCoss; Sander G Mills; Gail Van Riper; Ermengilda McCauley; Kathryn Lyons; Stella Vincent; Linda A Egger; Usha Kidambi; Ralph A Stearns; Adria Colletti; Yohannes Teffera; Sharon Tong; Karen Owens; Dorothy A Levorse; John A Schmidt; William K Hagmann
Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2002;12(17):2415-8.
2002: Theodore M Kamenecka; Thomas J Lanza; Stephen E de Laszlo; Bing Li; Ermengilda McCauley; Gail Van Riper; Linda A Egger; Usha Kidambi; Richard A Mumford; Sharon Tong; Malcolm MacCoss; John A Schmidt; William K Hagmann
N-aryl-prolyl-dipeptides as potent antagonists of VLA-4.
Bioorganic & medicinal chemistry letters 2002;12(16):2205-8.
2002: Bing Li; Stephen E de Laszlo; Theodore M Kamenecka; Ihor E Kopka; Philippe L Durette; Thomas J Lanza; Malcolm MacCoss; Sharon Tong; Richard A Mumford; Ermengilda McCauley; Gail Van Riper; John A Schmidt; William K Hagmann
N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2002;12(16):2141-4.
2002: Linda A Egger; Usha Kidambi; Jin Cao; Gail Van Riper; Ermengilda McCauley; Richard A Mumford; Suzanne E Amo; Russell Lingham; Thomas J Lanza; Linus S Lin; Stephen E de Laszlo; David N Young; Ihor E Kopka; Sharon Tong; Bill Pikounis; Evelyn Benson; Sarah Warwood; Robert Bargatze; William K Hagmann; John A Schmidt; Patricia A Detmers
Alpha(4)beta(7)/alpha(4)beta(1) dual integrin antagonists block alpha(4)beta(7)-dependent adhesion under shear flow.
The Journal of pharmacology and experimental therapeutics 2002;302(1):153-62.
2002: R Blake Pepinsky; Richard A Mumford; Ling Ling Chen; Diane R Leone; Suzanne E Amo; Gail Van Riper; Adrian Whitty; Brian M Dolinski; Roy R Lobb; Dennis C Dean; Linda L Chang; Conrad E Raab; Qian Si; William K Hagmann; Russell Lingham
Comparative assessment of the ligand and metal ion binding properties of integrins alpha9beta1 and alpha4beta1.
Biochemistry 2002;41(22):7125-41.
2002: George A Doherty; Ginger X Yang; Edite Borges; Linda L Chang; Malcolm MacCoss; Sharon Tong; Usha Kidambi; Linda A Egger; Ermengilda McCauley; Gail Van Riper; Richard A Mumford; John A Schmidt; William K Hagmann
Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2002;12(11):1501-5.
2002: Ginger X Yang; Linda L Chang; Quang Truong; George A Doherty; Plato A Magriotis; Stephen E de Laszlo; Bing Li; Malcolm MacCoss; Usha Kidambi; Linda A Egger; Ermengilda McCauley; Gail Van Riper; Richard A Mumford; John A Schmidt; William K Hagmann
N-Tetrahydrofuroyl-(L)-phenylalanine derivatives as potent VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2002;12(11):1497-500.
2002: George A Doherty; Theodore M Kamenecka; Ermengilda McCauley; Gail Van Riper; Richard A Mumford; Sharon Tong; William K Hagmann
N-aryl 2,6-dimethoxybiphenylalanine analogues as VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2002;12(5):729-31.
2002: Stephen E de Laszlo; Bing Li; Ermengilda McCauley; Gail Van Riper; William K Hagmann
Identification of unique VLA-4 antagonists from a combinatorial library.
Bioorganic & medicinal chemistry letters 2002;12(4):685-8.
2002: Ihor E Kopka; David N Young; Linus S Lin; Richard A Mumford; Plato A Magriotis; Malcolm MacCoss; Sander G Mills; Gail Van Riper; Ermengilda McCauley; Linda E Egger; Usha Kidambi; John A Schmidt; Kathryn Lyons; Ralph A Stearns; Stella Vincent; Adria Colletti; Zhen Wang; Sharon Tong; Junying Wang; Song Zheng; Karen Owens; Dorothy A Levorse; William K Hagmann
Substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl-phenylalanine analogues as potent VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2002;12(4):637-40.
2002: Linus S Lin; Ihor E Kopka; Richard A Mumford; Plato A Magriotis; Thomas J Lanza; Philippe L Durette; Theodore M Kamenecka; David N Young; Stephen E de Laszlo; Ermengilda McCauley; Gail Van Riper; Usha Kidambi; Linda A Egger; Xinchun Tong; Kathryn Lyons; Stella Vincent; Ralph A Stearns; Adria Colletti; Yohannes Teffera; Judy Fenyk-Melody; John A Schmidt; Malcolm MacCoss; William K Hagmann
The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.
Bioorganic & medicinal chemistry letters 2002;12(4):611-4.
2002: Linda L Chang; Quang Truong; Richard A Mumford; Linda A Egger; Usha Kidambi; Kathryn Lyons; Ermengilda McCauley; Gail Van Riper; Stella Vincent; John A Schmidt; Malcolm MacCoss; William K Hagmann
The discovery of small molecule carbamates as potent dual alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.
Bioorganic & medicinal chemistry letters 2002;12(2):159-63.
2002: Linus S Lin; Thomas J Lanza; Ermengilda McCauley; Gail Van Riper; Usha Kidambi; Jin Cao; Linda A Egger; Richard A Mumford; John A Schmidt; Malcolm MacCoss; William K Hagmann
Specific and dual antagonists of alpha(4)beta(1) and alpha(4)beta(7) integrins.
Bioorganic & medicinal chemistry letters 2002;12(2):133-6.
2002: Stan Spence; Christine Vetter; William K Hagmann; Gail Van Riper; Hollis Williams; Richard A Mumford; Thomas J Lanza; Linus S Lin; John A Schmidt
Effects of VLA-4 antagonists in rat whole embryo culture.
Teratology 2002;65(1):26-37.
2001: Linda L Chang; K L Sidler; Margaret A Cascieri; Stephen E de Laszlo; G Koch; Bing Li; Malcolm MacCoss; N Mantlo; S O'Keefe; Margaret Pang; AM Rolando; William K Hagmann
Substituted imidazoles as glucagon receptor antagonists.
Bioorganic & medicinal chemistry letters 2001;11(18):2549-53.
2000: William K Hagmann; Charles G Caldwell; Ping Chen; Philippe L Durette; C K Esser; Thomas J Lanza; Ihor E Kopka; Ravindra N Guthikonda; Shrenik K Shah; Malcolm MacCoss; Renee M Chabin; D Fletcher; Stephan K Grant; Barbara G Green; John L Humes; Theresa M Kelly; Silvi Luell; Roger Meurer; VL Moore; Stephen G Pacholok; T Pavia; H R Williams; Kenny K Wong
Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.
Bioorganic & medicinal chemistry letters 2000;10(17):1975-8.
1999: Margaret A Cascieri; Greg E Koch; E Ber; Sharon Sadowski; D Louizides; Stephen E de Laszlo; C Hacker; William K Hagmann; Malcolm MacCoss; Gary G Chicchi; Pasquale P Vicario
Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor.
The Journal of biological chemistry 1999;274(13):8694-7.
1999: Stephen E de Laszlo; C Hacker; Bing Li; Dooseop Kim; Malcolm MacCoss; N Mantlo; James V Pivnichny; Lawrence F Colwell; Greg E Koch; Margaret A Cascieri; William K Hagmann
Potent, orally absorbed glucagon receptor antagonists.
Bioorganic & medicinal chemistry letters 1999;9(5):641-6.
1997: C K Esser; R L Bugianesi; Charles G Caldwell; Kevin Chapman; Philippe L Durette; N N Girotra; Ihor E Kopka; Thomas J Lanza; Dorothy A Levorse; Malcolm MacCoss; Karen Owens; M M Ponpipom; J P Simeone; R K Harrison; L Niedzwiecki; Joseph W Becker; A I Marcy; M G Axel; A J Christen; J McDonnell; VL Moore; J M Olszewski; C Saphos; Denise visco; William K Hagmann
Inhibition of stromelysin-1 (MMP-3) by P1'-biphenylylethyl carboxyalkyl dipeptides.
Journal of medicinal chemistry 1997;40(6):1026-40.
1996: J M Olszewski; V L Moore; J McDonnell; H Williams; C A Saphos; Barbara G Green; W B Knight; Kevin Chapman; William K Hagmann; C P Dorn; Jeffrey J Hale; R A Mumford
Proteoglycan-degrading activity of human stromelysin-1 and leukocyte elastase in rabbit joints. Quantitation of proteoglycan and a stromelysin-induced HABR fragment of aggrecan in synovial fluid and cartilage.
Connective tissue research 1996;33(4):291-9.
1996: P R Gooley; J F O'Connell; A I Marcy; G C Cuca; M G Axel; C G Caldwell; William K Hagmann; Joseph W Becker
Comparison of the structure of human recombinant short form stromelysin by multidimensional heteronuclear NMR and X-ray crystallography.
Journal of biomolecular NMR 1996;7(1):8-28.
1995: L J Bonassar; K A Jeffries; E H Frank; V L Moore; Michael W Lark; Ellen K Bayne; J McDonnell; J Olszewski; William K Hagmann; K Chapman
In vivo effects of stromelysin on the composition and physical properties of rabbit articular cartilage in the presence and absence of a synthetic inhibitor.
Arthritis and rheumatism 1995;38(11):1678-86.
1995: Joseph W Becker; A I Marcy; L L Rokosz; M G Axel; J J Burbaum; P M Fitzgerald; Patricia M Cameron; C K Esser; William K Hagmann; Jeffrey Donald Hermes
Stromelysin-1: three-dimensional structure of the inhibited catalytic domain and of the C-truncated proenzyme.
Protein science : a publication of the Protein Society 1995;4(10):1966-76.
1995: Ellen K Bayne; K L MacNaul; S A Donatelli; A Christen; P R Griffin; L A Hoerrner; JR Calaycay; Julia Ayala; K Chapman; William K Hagmann
Use of an antibody against the matrix metalloproteinase-generated aggrecan neoepitope FVDIPEN-COOH to assess the effects of stromelysin in a rabbit model of cartilage degradation.
Arthritis and rheumatism 1995;38(10):1400-9.
1994: L J Bonassar; C G Paguio; E H Frank; K A Jeffries; V L Moore; Michael W Lark; C G Caldwell; William K Hagmann; Alan J Grodzinsky
Effects of matrix metalloproteinases on cartilage biophysical properties in vitro and in vivo.
Annals of the New York Academy of Sciences 1994;732():439-43.
1994: M Izquierdo-Martin; Kevin Chapman; William K Hagmann; R L Stein
Studies on the kinetic and chemical mechanism of inhibition of stromelysin by an N-(carboxyalkyl)dipeptide.
Biochemistry 1994;33(6):1356-65.
1994: P R Gooley; J F O'Connell; A I Marcy; G C Cuca; S P Salowe; B L Bush; Jeffrey Donald Hermes; C K Esser; William K Hagmann; J P Springer
The NMR structure of the inhibited catalytic domain of human stromelysin-1.
Nature structural biology 1994;1(2):111-8.
1993: P R Gooley; B A Johnson; A I Marcy; G C Cuca; S P Salowe; William K Hagmann; C K Esser; J P Springer
Secondary structure and zinc ligation of human recombinant short-form stromelysin by multidimensional heteronuclear NMR.
Biochemistry 1993;32(48):13098-108.
1993: J B Doherty; S K Shah; P E Finke; C P Dorn; William K Hagmann; Jeffrey J Hale; A L Kissinger; K R Thompson; K Brause; G O Chandler
Chemical, biochemical, pharmacokinetic, and biological properties of L-680,833: a potent, orally active monocyclic beta-lactam inhibitor of human polymorphonuclear leukocyte elastase.
Proceedings of the National Academy of Sciences of the United States of America 1993;90(18):8727-31.
1993: R Chabin; Barbara G Green; P Gale; A L Maycock; H Weston; C P Dorn; P E Finke; William K Hagmann; Jeffrey J Hale; Malcolm MacCoss
Mechanism of inhibition of human leucocyte elastase by monocyclic beta-lactams.
Biochemistry 1993;32(34):8970-80.
1993: William K Hagmann; A L Kissinger; S K Shah; P E Finke; C P Dorn; K A Brause; B M Ashe; H Weston; A L Maycock; W B Knight
Orally active beta-lactam inhibitors of human leukocyte elastase. 2. Effect of C-4 substitution.
Journal of medicinal chemistry 1993;36(6):771-7.
1992: S K Shah; C P Dorn; P E Finke; Jeffrey J Hale; William K Hagmann; K A Brause; G O Chandler; A L Kissinger; B M Ashe; H Weston
Orally active beta-lactam inhibitors of human leukocyte elastase-1. Activity of 3,3-diethyl-2-azetidinones.
Journal of medicinal chemistry 1992;35(21):3745-54.
1992: W B Knight; A L Maycock; Barbara G Green; B M Ashe; P Gale; H Weston; P E Finke; William K Hagmann; S K Shah; J B Doherty
Mechanism of inhibition of human leukocyte elastase by two cephalosporin derivatives.
Biochemistry 1992;31(21):4980-6.
1992: S P Salowe; A I Marcy; G C Cuca; C K Smith; Ihor Kopka; William K Hagmann; Jeffrey Donald Hermes
Characterization of zinc-binding sites in human stromelysin-1: stoichiometry of the catalytic domain and identification of a cysteine ligand in the proenzyme.
Biochemistry 1992;31(19):4535-40.
1992: T J Lanza; P L Durette; T Rollins; Salvatore J Siciliano; D N Cianciarulo; S V Kobayashi; C G Caldwell; Martin S Springer; William K Hagmann
Substituted 4,6-diaminoquinolines as inhibitors of C5a receptor binding.
Journal of medicinal chemistry 1992;35(2):252-8.
1991: A I Marcy; L L Eiberger; R Harrison; H K Chan; N I Hutchinson; William K Hagmann; Patricia M Cameron; D A Boulton; Jeffrey Donald Hermes
Human fibroblast stromelysin catalytic domain: expression, purification, and characterization of a C-terminally truncated form.
Biochemistry 1991;30(26):6476-83.
1991: Barbara G Green; H Weston; B M Ashe; J Doherty; P Finke; William K Hagmann; Michael W Lark; J Mao; A Maycock; V Moore
PMN elastases: a comparison of the specificity of human isozymes and the enzyme from other species toward substrates and inhibitors.
Archives of biochemistry and biophysics 1991;286(1):284-92.
1990: D S Fletcher; D G Osinga; K M Hand; P S Dellea; B M Ashe; R A Mumford; P Davies; William K Hagmann; P E Finke; J B Doherty
A comparison of alpha 1-proteinase inhibitor methoxysuccinyl-Ala-Ala-Pro-Val-chloromethylketone and specific beta-lactam inhibitors in an acute model of human polymorphonuclear leukocyte elastase-induced lung hemorrhage in the hamster.
The American review of respiratory disease 1990;141(3):672-7.
1990: R W Egan; William K Hagmann; P H Gale
Naphthalenes as inhibitors of myeloperoxidase: direct and indirect mechanisms of inhibition.
Agents and actions 1990;29(3-4):266-76.
1990: M M Ponpipom; William K Hagmann; L A O'Grady; J J Jackson; D D Wood; H J Zweerink
Glycolipids as host resistance stimulators.
Journal of medicinal chemistry 1990;33(2):861-7.
1990: William K Hagmann; M M Ponpipom; J J Jackson; D D Wood; R C Boltz; H J Zweerink
Steroidal glycolipid, L-644,257, is a potent enhancer of nonspecific host resistance.
International journal of immunopharmacology 1990;12(2):241-6.
1986: William K Hagmann; C P Dorn; R A Frankshun; L A O'Grady; P J Bailey; A Rackham; H W Dougherty
Synthesis and antiinflammatory/analgesic activities of 11H-dibenzo[b, e,][1,4]dioxepinacetic acids.
Journal of medicinal chemistry 1986;29(8):1436-41.