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Rui-Qin Liu
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Network (preview)
28
Decicco, Carl
25
Covington, Maryanne
23
Duan, James J-W
23
Newton, Robert
22
Trzaskos, James
16
Qian, Mingxin
15
Christ, David
11
Magolda, Ronald
10
Vaddi, Kris
10
Wasserman, Zelda
10
Xue, Chu-Biao
9
Tortorella, Micky
8
Wexler, Ruth
7
Roderick, John
7
Pratta, Michael
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All Publications
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2008: Lu Zhonghui; Ott Gregory R; Anand Rajan; Liu Rui-Qin; Covington Maryanne B; Vaddi Krishna; Qian Mingxin; Newton Robert C; Christ David D; Trzaskos James; Duan James J-W
Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents.
Bioorganic & medicinal chemistry letters 2008;18(6):1958-62.
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2008: Ott Gregory R; Asakawa Naoyuki; Lu Zhonghui; Anand Rajan; Liu Rui-Qin; Covington Maryanne B; Vaddi Krishna; Qian Mingxin; Newton Robert C; Christ David D; Trzaskos James M; Duan James J-W
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents.
Bioorganic & medicinal chemistry letters 2008;18(5):1577-82.
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2008: Ott Gregory R; Asakawa Naoyuki; Liu Rui-Qin; Covington Maryanne B; Qian Mingxin; Vaddi Krishna; Newton Robert C; Trzaskos James M; Christ David D; Galya Laurine; Scholz Thomas; Marshall Will; Duan James J-W
Alpha,Beta-cyclic-beta-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bioorganic & medicinal chemistry letters 2008;18(4):1288-92.
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2008: Ott Gregory R; Asakawa Naoyuki; Lu Zhonghui; Liu Rui-Qin; Covington Maryanne B; Vaddi Krishna; Qian Mingxin; Newton Robert C; Christ David D; Traskos James M; Decicco Carl P; Duan James J-W
Alpha,beta-cyclic-beta-benzamido hydroxamic acids: novel templates for the design, synthesis, and evaluation of selective inhibitors of TNF-alpha converting enzyme (TACE).
Bioorganic & medicinal chemistry letters 2008;18(2):694-9.
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2008: Duan James J-W; Chen Lihua; Lu Zhonghui; Xue Chu-Biao; Liu Rui-Qin; Covington Maryanne B; Qian Mingxin; Wasserman Zelda R; Vaddi Krishna; Christ David D; Trzaskos James M; Newton Robert C; Decicco Carl P
Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(1):241-6.
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2007: Qian Mingxin; Bai Stephen A; Brogdon Bernice; Wu Jing-Tao; Liu Rui-Qin; Covington Maryanne B; Vaddi Kris; Newton Robert C; Fossler Michael J; Garner C Edwin; Deng Yuzhong; Maduskuie Thomas; Trzaskos James; Duan James J-W; Decicco Carl P; Christ David D
Pharmacokinetics and pharmacodynamics of DPC 333 ((2R)-2-((3R)-3-amino-3{4-[2-methyl-4-quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide)), a potent and selective inhibitor of tumor necrosis factor alpha-converting enzyme in rodents, dogs, chimpanzees, and humans.
Drug metabolism and disposition: the biological fate of chemicals 2007;35(10):1916-25.
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2007: Gilmore John L; King Bryan W; Asakawa Naoyuki; Harrison Kimberly; Tebben Andrew; Sheppeck James E; Liu Rui-Qin; Covington Maryanne; Duan James J-W
Synthesis and structure-activity relationship of a novel, non-hydroxamate series of TNF-alpha converting enzyme inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(16):4678-82.
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2007: Sheppeck James E; Gilmore John L; Tebben Andrew; Xue Chu-Biao; Liu Rui-Qin; Decicco Carl P; Duan James J-W
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bioorganic & medicinal chemistry letters 2007;17(10):2769-74.
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2007: Carter Percy H; Liu Rui-Qin; Foster William R; Tamasi Joseph A; Tebben Andrew J; Favata Margaret; Staal Ada; Cvijic Mary Ellen; French Michele H; Dell Vanessa; Apanovitch Donald; Lei Ming; Zhao Qihong; Cunningham Mark; Decicco Carl P; Trzaskos James M; Feyen Jean H M
Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe.
Proceedings of the National Academy of Sciences of the United States of America 2007;104(16):6846-51.
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2007: Chen Xiao-Tao; Ghavimi Bahman; Corbett Ronald L; Xue Chu-Biao; Liu Rui-Qin; Covington Maryanne B; Qian Mingxin; Vaddi Krishna G; Christ David D; Hartman Karl D; Ribadeneira Maria D; Trzaskos James M; Newton Robert C; Decicco Carl P; Duan James J-W
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(7):1865-70.
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2007: Sheppeck James E; Gilmore John L; Yang Anle; Chen Xiao-Tao; Xue Chu-Biao; Roderick John; Liu Rui-Qin; Covington Maryanne B; Decicco Carl P; Duan James J-W
Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bioorganic & medicinal chemistry letters 2007;17(5):1413-7.
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2007: Barnett Joshua M; McCollum Gary W; Fowler Jessica A; Duan James J-W; Kay Jesse D; Liu Rui-Qin; Bingaman David P; Penn John S
Pharmacologic and genetic manipulation of MMP-2 and -9 affects retinal neovascularization in rodent models of OIR.
Investigative ophthalmology & visual science 2007;48(2):907-15.
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2007: Duan James J-W; Chen Lihua; Lu Zhonghui; Jiang Bin; Asakawa Naoyuki; Sheppeck James E; Liu Rui-Qin; Covington Maryanne B; Pitts William; Kim Soong-Hoon; Decicco Carl P
Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bioorganic & medicinal chemistry letters 2007;17(1):266-71.
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2006: Gilmore John L; King Bryan W; Harris Cathy; Maduskuie Thomas; Mercer Stephen E; Liu Rui-Qin; Covington Maryanne B; Qian Mingxin; Ribadeneria Maria D; Vaddi Krishna; Trzaskos James M; Newton Robert C; Decicco Carl P; Duan James J-W
Synthesis and structure-activity relationship of a novel, achiral series of TNF-alpha converting enzyme inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(10):2699-704.
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2006: Thompson Lorin A; Liauw Ann Y; Ramanjulu Mercy M; Kasireddy-Polam Padmaja; Mercer Stephen E; Maduskuie Thomas P; Glicksman Marcie; Roach Arthur H; Meredith Jere E; Liu Rui-Qin; Combs Andrew P; Higaki Jeffrey N; Cordell Barbara; Seiffert Dietmar; Zaczek Robert C; Robertson David W; Olson Richard E
Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(9):2357-63.
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2006: Cherney Robert J; King Bryan W; Gilmore John L; Liu Rui-Qin; Covington Maryanne B; Duan James J-W; Decicco Carl P
Conversion of potent MMP inhibitors into selective TACE inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(4):1028-31.
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2005: Duan James J-W; Lu Zhonghui; Wasserman Zelda R; Liu Rui-Qin; Covington Maryanne B; Decicco Carl P
Non-hydroxamate 5-phenylpyrimidine-2,4,6-trione derivatives as selective inhibitors of tumor necrosis factor-alpha converting enzyme.
Bioorganic & medicinal chemistry letters 2005;15(12):2970-3.
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2004: Xue Chu-Biao; Chen Xiao-Tao; He Xiaohua; Roderick John; Corbett Ronald L; Ghavimi Bahman; Liu Rui-Qin; Covington Maryanne B; Qian Mingxin; Ribadeneira Maria D; Vaddi Krishna; Trzaskos James; Newton Robert C; Duan James J-W; Decicco Carl P
Synthesis and structure-activity relationship of a novel sulfone series of TNF-alpha converting enzyme inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(17):4453-9.
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2004: Cherney Robert J; Mo Ruowei; Meyer Dayton T; Hardman Karl D; Liu Rui-Qin; Covington Maryanne B; Qian Mingxin; Wasserman Zelda R; Christ David D; Trzaskos James M; Newton Robert C; Decicco Carl P
Sultam hydroxamates as novel matrix metalloproteinase inhibitors.
Journal of medicinal chemistry 2004;47(12):2981-3.
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2004: Wang Xinkang; Feuerstein Giora Z; Xu Lin; Wang Hugh; Schumacher William A; Ogletree Martin L; Taub Rebecca; Duan James J-W; Decicco Carl P; Liu Rui-Qin
Inhibition of tumor necrosis factor-alpha-converting enzyme by a selective antagonist protects brain from focal ischemic injury in rats.
Molecular pharmacology 2004;65(4):890-6.
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2004: Tortorella Micky D; Arner Elizabeth C; Hills Robert; Easton Alan; Korte-Sarfaty Jennifer; Fok Kam; Wittwer Arthur J; Liu Rui-Qin; Malfait Anne-Marie
Alpha2-macroglobulin is a novel substrate for ADAMTS-4 and ADAMTS-5 and represents an endogenous inhibitor of these enzymes.
The Journal of biological chemistry 2004;279(17):17554-61.
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2003: Xue Chu-Biao; He Xiaohua; Roderick John; Corbett Ronald L; Duan James J-W; Liu Rui-Qin; Covington Maryanne B; Qian Mingxin; Ribadeneira Maria D; Vaddi Krishna; Christ David D; Newton Robert C; Trzaskos James M; Magolda Ronald L; Wexler Ruth R; Decicco Carl P
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization.
Bioorganic & medicinal chemistry letters 2003;13(24):4299-304.
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2003: Xue Chu-Biao; He Xiaohua; Roderick John; Corbett Ronald L; Duan James J-W; Liu Rui-Qin; Covington Maryanne B; Newton Robert C; Trzaskos James M; Magolda Ronald L; Wexler Ruth R; Decicco Carl P
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.
Bioorganic & medicinal chemistry letters 2003;13(24):4293-7.
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2003: Pratta Michael A; Yao Wenqing; Decicco Carl; Tortorella Micky D; Liu Riu-Qin; Copeland Robert A; Magolda Ronald; Newton Robert C; Trzaskos James M; Arner Elizabeth C
Aggrecan protects cartilage collagen from proteolytic cleavage.
The Journal of biological chemistry 2003;278(46):45539-45.
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2003: Duan James J-W; Lu Zhonghui; Xue Chu-Biao; He Xiaohua; Seng Jennifer L; Roderick John J; Wasserman Zelda R; Liu Rui-Qin; Covington Maryanne B; Magolda Ronald L; Newton Robert C; Trzaskos James M; Decicco Carl P
Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bioorganic & medicinal chemistry letters 2003;13(12):2035-40.
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2003: Cherney Robert J; Duan James J-W; Voss Matthew E; Chen Lihua; Wang Li; Meyer Dayton T; Wasserman Zelda R; Hardman Karl D; Liu Rui-Qin; Covington Maryanne B; Qian Mingxin; Mandlekar Sandhya; Christ David D; Trzaskos James M; Newton Robert C; Magolda Ronald L; Wexler Ruth R; Decicco Carl P
Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors.
Journal of medicinal chemistry 2003;46(10):1811-23.
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2003: Cherney Robert J; Mo Ruowei; Meyer Dayton T; Wang Li; Yao Wenqing; Wasserman Zelda R; Liu Rui-Qin; Covington Maryanne B; Tortorella Micky D; Arner Elizabeth C; Qian Mingxin; Christ David D; Trzaskos James M; Newton Robert C; Magolda Ron L; Decicco Carl P
Potent and selective aggrecanase inhibitors containing cyclic P1 substituents.
Bioorganic & medicinal chemistry letters 2003;13(7):1297-300.
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2003: Miller Jeffery A; Liu Rui-Qin; Davis Gary L; Pratta Michael A; Trzaskos James M; Copeland Robert A
A microplate assay specific for the enzyme aggrecanase.
Analytical biochemistry 2003;314(2):260-5.
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2003: Voss Matthew E; Carter Percy H; Tebben Andrew J; Scherle Peggy A; Brown Gregory D; Thompson Lorin A; Xu Meizhong; Lo Yvonne C; Yang Gengjie; Liu Rui-Qin; Strzemienski Paul; Everlof J Gerry; Trzaskos James M; Decicco Carl P
Both 5-arylidene-2-thioxodihydropyrimidine-4,6(1H,5H)-diones and 3-thioxo-2,3-dihydro-1H-imidazo[1,5-a]indol-1-ones are light-dependent tumor necrosis factor-alpha antagonists.
Bioorganic & medicinal chemistry letters 2003;13(3):533-8.
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2003: Pratta Michael A; Scherle Peggy A; Yang Gengjie; Liu Rui-Qin; Newton Robert C
Induction of aggrecanase 1 (ADAM-TS4) by interleukin-1 occurs through activation of constitutively produced protein.
Arthritis and rheumatism 2003;48(1):119-33.
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2002: Duan James J-W; Chen Lihua; Wasserman Zelda R; Lu Zhonghui; Liu Rui-Qin; Covington Maryanne B; Qian Mingxin; Hardman Karl D; Magolda Ronald L; Newton Robert C; Christ David D; Wexler Ruth R; Decicco Carl P
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
Journal of medicinal chemistry 2002;45(23):4954-7.
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2002: Tortorella Micky D; Liu Rui-Qin; Burn Timothy; Newton Robert C; Arner Elizabeth
Characterization of human aggrecanase 2 (ADAM-TS5): substrate specificity studies and comparison with aggrecanase 1 (ADAM-TS4).
Matrix biology : journal of the International Society for Matrix Biology 2002;21(6):499-511.
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2002: Malfait Anne-Marie; Liu Rui-Qin; Ijiri Kosei; Komiya Setsuro; Tortorella Micky D
Inhibition of ADAM-TS4 and ADAM-TS5 prevents aggrecan degradation in osteoarthritic cartilage.
The Journal of biological chemistry 2002;277(25):22201-8.
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2002: Yao Wenqing; Chao Michael; Wasserman Zelda R; Liu Rui Qin; Covington Maryanne B; Newton Robert; Christ David; Wexler Ruth R; Decicco Carl P
Potent P1' biphenylmethyl substituted aggrecanase inhibitors.
Bioorganic & medicinal chemistry letters 2002;12(1):101-4.
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2001: Carter P H; Scherle P A; Muckelbauer J K; Voss M E; Liu R Q; Thompson L A; Tebben A J; Solomon K A; Lo Y C; Li Z; Strzemienski P; Yang G; Falahatpisheh N; Xu M; Wu Z; Farrow N A; Ramnarayan K; Wang J; Rideout D; Yalamoori V; Domaille P; Underwood D J; Trzaskos J M; Friedman S M; Newton R C; Decicco C P;
Photochemically enhanced binding of small molecules to the tumor necrosis factor receptor-1 inhibits the binding of TNF-alpha.
Proceedings of the National Academy of Sciences of the United States of America 2001;98(21):11879-84.
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2001: Xue C B; He X; Corbett R L; Roderick J; Wasserman Z R; Liu R Q; Jaffee B D; Covington M B; Qian M; Trzaskos J M; Newton R C; Magolda R L; Wexler R R; Decicco C P
Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release.
Journal of medicinal chemistry 2001;44(21):3351-4.
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2001: Yao W; Wasserman Z R; Chao M; Reddy G; Shi E; Liu R Q; Covington M B; Arner E C; Pratta M A; Tortorella M; Magolda R L; Newton R; Qian M; Ribadeneira M D; Christ D; Wexler R R; Decicco C P
Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors.
Journal of medicinal chemistry 2001;44(21):3347-50.
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2001: Xue C B; Voss M E; Nelson D J; Duan J J; Cherney R J; Jacobson I C; He X; Roderick J; Chen L; Corbett R L; Wang L; Meyer D T; Kennedy K; DeGradodagger W F; Hardman K D; Teleha C A; Jaffee B D; Liu R Q; Copeland R A; Covington M B; Christ D D; Trzaskos J M; Newton R C; Magolda R L; Wexler R R; Decicco C P
Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo.
Journal of medicinal chemistry 2001;44(16):2636-60.
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2000: Tortorella M; Pratta M; Liu R Q; Abbaszade I; Ross H; Burn T; Arner E
The thrombospondin motif of aggrecanase-1 (ADAMTS-4) is critical for aggrecan substrate recognition and cleavage.
The Journal of biological chemistry 2000;275(33):25791-7.
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2000: Tortorella M D; Pratta M; Liu R Q; Austin J; Ross O H; Abbaszade I; Burn T; Arner E
Sites of aggrecan cleavage by recombinant human aggrecanase-1 (ADAMTS-4).
The Journal of biological chemistry 2000;275(24):18566-73.
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1999: Abbaszade I; Liu R Q; Yang F; Rosenfeld S A; Ross O H; Link J R; Ellis D M; Tortorella M D; Pratta M A; Hollis J M; Wynn R; Duke J L; George H J; Hillman M C; Murphy K; Wiswall B H; Copeland R A; Decicco C P; Bruckner R; Nagase H; Itoh Y; Newton R C; Magolda R L; Trzaskos J M; Burn T C
Cloning and characterization of ADAMTS11, an aggrecanase from the ADAMTS family.
The Journal of biological chemistry 1999;274(33):23443-50.
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