Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Kevin J. Milliner"'
Characterisation of the lipoprotein structure in the St. Thomas’ Mixed Hyperlipidaemic (SMHL) rabbit
Autor:
G. Martin Benson, Baukje de Roos, Christopher J. Packard, Muriel J. Caslake, Kevin J. Milliner, Keith E. Suckling
Publikováno v:
Atherosclerosis. 181:63-68
Familial combined hyperlipidaemia (FCHL) is a complex genetic disorder of unknown aetiology. Study of this human condition over many decades has been hampered by likely genetic heterogeneity. In order to find better phenotypic markers, we have charac
Autor:
V.Ann Lewis, Ian Stansfield, Kevin J. Milliner, Ivan Leo Pinto, Jackie C. Bloomer, Steven J. Stanway, Stephen A. Smith, Josie A. Blackie, Colin J. Theobald, Beverley Hammond, Hung Yuan Cheng, Colin A. Leach, Maxine A. Taylor, Robert J. Ife, Richard L. Elliott, Deirdre Mary Bernadette Hickey, Murray J. B. Brown, Caroline M. Whittaker, Kitty Moores, Colin H. Macphee
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:2603-2606
The introduction of a functionalised amido substituent into a series of 1-(biphenylmethylacetamido)-pyrimidones has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A(2) with sub-nanomolar potency and very encouraging
Autor:
Deirdre M. B. Hickey, Ian Stansfield, Leach Colin Andrew, Caroline M. Whittaker, Ivan Leo Pinto, Stephen A. Smith, Stephen Christopher Martin Fell, Sean Thomas Flynn, Kitty Moores, Helen F. Boyd, Colin J. Theobald, David G. Tew, Roderick A. Porter, Robert John Ife, Kevin J. Milliner, Colin H. Macphee, D. Anthony Rawlings
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2557-2561
From two related series of 2-(alkylthio)-pyrimidones, a novel series of 1-((amidolinked)-alkyl)-pyrimidones has been designed as nanomolar inhibitors of human lipoprotein-associated phopholipase A 2 . These compounds show greatly enhanced activity in
Autor:
Martin Jones, Colin J. Theobald, Leach Colin Andrew, Sean Thomas Flynn, Deirdre M. B. Hickey, Ian Stansfield, David G. Tew, Brian Peter Slingsby, Helen F. Boyd, Stephen A. Smith, Kevin J. Milliner, Colin H. Macphee, Robert John Ife, D. Anthony Rawlings
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:395-398
Starting from two weakly active hits from high throughput screening, a novel series of 2-(alkylthio)-pyrimidin-4-ones with high potency and selectivity for lipoprotein-associated phospholipase A2 has been designed. In contrast to previously known inh
Autor:
David G. Tew, Simon Q.J. Rice, Tomi Häkkinen, Kari Karkola, Lisa Patel, Jukka Luoma, Mikko Hiltunen, Colin H. Macphee, Kevin J. Milliner, Seppo Ylä-Herttuala
Publikováno v:
Arteriosclerosis, Thrombosis, and Vascular Biology. 19:2909-2917
Abstract —We studied the expression of lipoprotein-associated phospholipase A 2 (Lp-PLA 2 ), an enzyme capable of hydrolyzing platelet-activating factor (PAF), PAF-like phospholipids, and polar-modified phosphatidylcholines, in human and rabbit ath
Autor:
Helen F. Boyd, Deirdre M. B. Hickey, Kitty Moores, Kevin J. Milliner, Colin H. Macphee, Dash Dhanak, Keith E. Suckling, Leach Colin Andrew, Rebecca A. Patterson, Robert John Ife, David S. Leake, David G. Tew
Publikováno v:
Biochemical Journal. 338:479-487
A novel and potent azetidinone inhibitor of the lipoprotein-associated phospholipase A2 (Lp-PLA2), i.e. platelet-activating factor acetylhydrolase, is described for the first time. This inhibitor, SB-222657 (Ki = 40±3 nM, kobs/[I] = 6.6×105 M-1·s-
Autor:
V.Ann Lewis, Colin A. Leach, Colin H. Macphee, Kitty Moores, Murray J. B. Brown, Ivan Leo Pinto, Stephen A. Smith, Robert J. Ife, Ian Stansfield, Steven J. Stanway, Jackie C. Bloomer, Kevin J. Milliner, Maxine A. Taylor, Deirdre Mary Bernadette Hickey, Beverley Hammond, Hung Yuan Cheng, Colin J. Theobald, Josie A. Blackie
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(6)
Modification of the pyrimidone 5-substituent in clinical candidate SB-435495 has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A 2 with sub-nanomolar potency. Cyclopentyl fused derivative 21 , SB-480848, showed an e
Autor:
Josie A, Blackie, Jackie C, Bloomer, Murray J B, Brown, Hung-Yuan, Cheng, Richard L, Elliott, Beverley, Hammond, Deirdre M B, Hickey, Robert J, Ife, Colin A, Leach, V Ann, Lewis, Colin H, Macphee, Kevin J, Milliner, Kitty E, Moores, Ivan L, Pinto, Stephen A, Smith, Ian G, Stansfield, Steven J, Stanway, Maxine A, Taylor, Colin J, Theobald, Caroline M, Whittaker
Publikováno v:
Bioorganicmedicinal chemistry letters. 12(18)
The introduction of a functionalised amido substituent into a series of 1-(biphenylmethylacetamido)-pyrimidones has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A(2) with sub-nanomolar potency and very encouraging
Autor:
Helen F. Boyd, Stephen Christopher Martin Fell, Stephen A. Smith, Deirdre Mary Bernadette Hickey, Colin A. Leach, Colin J. Theobald, Colin H. Macphee, Caroline M. Whittaker, D. Anthony Rawlings, Ivan Leo Pinto, Ian Stansfield, Steven J. Stanway, Kevin J. Milliner, Robert J. Ife
Publikováno v:
Bioorganicmedicinal chemistry letters. 12(1)
A series of 1-(biphenylmethylamidoalkyl)-pyrimidones has been designed as nanomolar inhibitors of recombinant lipoprotein-associated phospholipase A 2 with high potency in whole human plasma. 5-(Pyrazolylmethyl) derivative 16 and 5-(methoxypyrimidiny
Autor:
Maxine A. Taylor, Robert J. Ife, Colin H. Macphee, Kevin J. Milliner, Ivan Leo Pinto, Jackie C. Bloomer, Steven J. Stanway, Colin A. Leach, D. Anthony Rawlings, Stephen A. Smith, Ian Stansfield, Caroline M. Whittaker, Helen F. Boyd, Colin J. Theobald, Deirdre Mary Bernadette Hickey
Publikováno v:
Bioorganicmedicinal chemistry letters. 11(14)
The lipophilic 1-substituent in a series of 1-((amidolinked)-alkyl)-pyrimidones, inhibitors of recombinant lipoprotein-associated phospholipase A 2 , has been modified to give inhibitors of high potency in human plasma and enhanced physicochemical pr