Gregory, Laura S., Kelly, Wendy L., Reid, Robert R., Fairlie, David P., Forwood, Mark R.
Epidemiological evidence and in vitro data suggest that COX-2 is a key regulator of accelerated remodeling. Accelerated states of osteoblast and osteoclast activity are regulated by prostaglandins in...
Gregory, Laura S., Kelly, Wendy L., Reid, Robert R., Fairlie, David P., Forwood, Mark R.
Epidemiological evidence and in vitro data suggest that COX-2 is a key regulator of accelerated remodeling. Accelerated states of osteoblast and osteoclast activity are regulated by prostaglandins in...
Levick, Scott, Loch, David, Rolfe, Barbara, Reid, Robert C., Fairlie, David P., Taylor, Stephan M., ...
The development of fibrosis in the chronically hypertensive heart is associated with infiltration of inflammatory cells and cardiac hypertrophy. In this study, an inhibitor of the proinflammatory...
Modular alpha-helical mimetics with antiviral activity against respiratory syncitial virus (2006)
Shepherd, Nicholas E., Hoang, Huy N., Desai, Vishal S., Letouze, Eric, Young, Paul R., Fairlie, David P.
A 13-residue peptide sequence from a respiratory syncitial virus fusion protein was constrained in an alpha-helical conformation by fusing two back-to-back cyclic alpha-turn mimetics. The resulting...
Gregory, Laura S., Kelly, Wendy L., Reid, Robert R., Fairlie, David P., Forwood, Mark R.
Epidemiological evidence and in vitro data suggest that COX-2 is a key regulator of accelerated remodeling. Accelerated states of osteoblast and osteoclast activity are regulated by prostaglandins in...
Keith J. Chappell, Tessa A. Nall, Martin J. Stoermer, Ning-Xia Fang, David P. Fairlie, ...
A series of papers that have been published since our 2001 paper (above) has built on our understanding of flavivirus protease specificity. We have expanded our studies to incorporate West Nile virus...
Keith J. Chappell, Tessa A. Nall, Martin J. Stoermer, Ning-Xia Fang, David P. Fairlie, ...
A series of papers that have been published since our 2001 paper (above) has built on our understanding of flavivirus protease specificity. We have expanded our studies to incorporate West Nile virus...
Chappell, Keith J., Nall, Tessa A., Stoermer, Martin J., Fang, Ning-Xia, Tyndall, Joel D. A., Fairlie, David P., ...
The flavivirus West Nile virus (WNV) has spread rapidly throughout the world in recent years causing fever, meningitis, encephalitis, and fatalities. Because the viral protease NS2B/NS3 is essential...
Renee L. Beyer, Huy N. Hoang, Trevor G. Appleton, David P. Fairlie
This paper showed that overlapping metal clips induces strong helicity in a short peptide in water.
Alpha-Turn Mimetics: Short Peptide -Helices Composed of Cyclic Metallopentapeptide Modules (2004)
Michael J. Kelso, Renée L. Beyer, Huy N. Hoang, Ami S. Lakdawala, James P. Snyder, Warren V. Oliver, ...
Interfering with protein-protein binding is the mode of action of many existing drugs and is a potential mechanistic target in the design of new drugs. Small molecule peptidomimetics are potential...
Renee L. Beyer, Huy N. Hoang, Trevor G. Appleton, David P. Fairlie
This paper showed that overlapping metal clips induces strong helicity in a short peptide in water.
Reid, Robert C., Pattenden, Lenard K., Tyndall, Joel D. A., Martin, Jennifer L., Walsh, Terry, Fairlie, David P.
A major problem in de novo design of enzyme inhibitors is the unpredictability of the induced fit, with the shape of both ligand and enzyme changing cooperatively and unpredictably in response to...
Van Den Brenk, Anna L., Tyndall, Joel D. A., Cusack, Rodney M., Jones, Alun, Fairlie, David P., Gahan, Lawrence R., ...
Patellamide D (patH(4)) is a cyclic octapeptide isolated from the ascidian Lissoclinum patella. The peptide possesses a 24-azacrown-8 macrocyclic structure containing two oxazoline and two thiazole...
Alpha-Turn Mimetics: Short Peptide -Helices Composed of Cyclic Metallopentapeptide Modules (2004)
Michael J. Kelso, Renée L. Beyer, Huy N. Hoang, Ami S. Lakdawala, James P. Snyder, Warren V. Oliver, ...
Interfering with protein-protein binding is the mode of action of many existing drugs and is a potential mechanistic target in the design of new drugs. Small molecule peptidomimetics are potential...
Tumor cell-specific cytotoxicity by targeting cell cycle checkpoints (2003)
Robyn Warrener, Heather Beamish, Andrew Burgess, Nigel J. Waterhouse, Nichole Giles, David P. Fairlie, ...
Warrener and Beamish are joint first authors on this paper. In this paper we demonstrate that the selective targeting of cell cycle checkpoint by chemotherapeutic agents increases the efficacy of the...
Cycloadditions of isobenzofuran to a constrained template bearing neighboring dienophiles (2003)
Stoermer, Martin J., Weerasuria, K. D. V., Fairlie, David P.
A high yielding synthesis of the pentacyclic diene ± dione 1 has enabled investigation of its reactivity as a double dienophile in Diels ±Alder [4 2] cycloadditions with isobenzofuran, leading to...
Tumor cell-specific cytotoxicity by targeting cell cycle checkpoints (2003)
Robyn Warrener, Heather Beamish, Andrew Burgess, Nigel J. Waterhouse, Nichole Giles, David P. Fairlie, ...
Warrener and Beamish are joint first authors on this paper. In this paper we demonstrate that the selective targeting of cell cycle checkpoint by chemotherapeutic agents increases the efficacy of the...
Reid, Robert C., Abbenante, Giovanni, Taylor, Stephen M., Fairlie, David P.
Relatively few cyclic peptides have reached the pharmaceutical marketplace during the past decade, most produced through fermentation rather than made synthetically. Generally, this class of...
Donmienne Leung, Kate Schroder, Helen White, Ning-Xia Fang, Martin J. Stoermer, Giovanni Abbenante, ...
Our paper describes the expression and purification of the first active recombinant flavivirus protease suitable for in vitro assays. We used this assay to probe substrate specificity and develop the...
Leung, Donmienne, Schroder, Kate, White, Helen, Fang, Ning-Xia, Stoermer, Martin J., Abbenante, Giovanni, ...
Qiu, Ling, Burgess, Andrew, Fairlie, David P., Leonard, Helen, Parsons, Peter G., Gabrielli, Brian G.
Important aspects of cell cycle regulation are the checkpoints, which respond to a variety of cellular stresses to inhibit cell cycle progression and act as protective mechanisms to ensure genomic...
Andrews, Katherine T., Fairlie, David P., Madala, Praveen K., Ray, John, Wyatt, David M., Hilton, Petrina M., ...
Parasite resistance to antimalarial drugs is a serious threat to human health, and novel agents that act on enzymes essential for parasite metabolism, such as proteases, are attractive targets for...
Qiu, Ling, Burgess, Andrew, Fairlie, David P., Leonard, Helen, Parsons, Peter G., Gabrielli, Brian G.
Important aspects of cell cycle regulation are the checkpoints, which respond to a variety of cellular stresses to inhibit cell cycle progression and act as protective mechanisms to ensure genomic...
Andrews, Katherine T., Fairlie, David P., Madala, Praveen K., Ray, John, Wyatt, David M., Hilton, Petrina M., ...
Parasite resistance to antimalarial drugs is a serious threat to human health, and novel agents that act on enzymes essential for parasite metabolism, such as proteases, are attractive targets for...
Effects of a new C5a receptor antagonist on C5a- and endotoxin- induced neutropenia in the rat
Short, Anna, Wong, Allan K, Finch, Angela M, Haaima, Gerald, Shiels, Ian A, Fairlie, David P, ...
A new C5a receptor antagonist, the cyclic peptide Phe-[Orn-Pro-D-cyclohexylalanine-Trp-Arg], (F-[OPdChaWR]), was tested for its ability to antagonize the neutropenic effects of both C5a and endotoxin...
Pharmacological characterization of antagonists of the C5a receptor
Paczkowski, Natalii J, Finch, Angela M, Whitmore, Jacqueline B, Short, Anna J, Wong, Allan K, Monk, Peter N, ...
Potent and highly selective small molecule antagonists have recently been developed by us for C5a receptors (C5aR) on human polymorphonuclear leukocytes (PMN). In this study we compared a new cyclic...
Strachan, Anna J, Shiels, Ian A, Reid, Robert C, Fairlie, David P, Taylor, Stephen M
Initiation of a peritoneal Arthus reaction by deposition of immune-complexes results in vascular leakage, polymorphonuclear leukocyte (PMN) infiltration, and tumour necrosis factor α (TNFα) and...
Arumugam, Thiruma V, Arnold, Naomi, Proctor, Lavinia M, Newman, Michelle, Reid, Robert C, Hansford, Karl A, ...
A new group IIa sPLA2 inhibitor was compared with selective inhibitors of COX-1, COX-2 and an LTC4 antagonist for effects on local and remote tissue injuries following ischaemia and reperfusion (I/R)...
Proctor, Lavinia M, Arumugam, Thiruma V, Shiels, Ian, Reid, Robert C, Fairlie, David P, Taylor, Stephen M
Complement activation is implicated in the pathogenesis of intestinal ischaemia–reperfusion injury (I/R), although the relative importance of individual complement components is unclear. A C3a...
Arumugam, Thiruma V., Tang, Sung-Chun, Lathia, Justin D., Cheng, Aiwu, Mughal, Mohamed R., Chigurupati, Srinivasulu, ...
Stroke is among the three leading causes of death worldwide and the most frequent cause of permanent disability. Brain ischemia induces an inflammatory response involving activated complement...
Donmienne Leung, Kate Schroder, Helen White, Ning-Xia Fang, Martin J. Stoermer, Giovanni Abbenante, ...
Our paper describes the expression and purification of the first active recombinant flavivirus protease suitable for in vitro assays. We used this assay to probe substrate specificity and develop the...
Seow, W. Kim, Nakamura, Kazuhiro, Sugimura, Yukio, Sugimoto, Yukihiro, Yamada, Yasuyuki, Fairlie, David P., ...
Synthesis of IL-1β and TNFα by human monocytesmacrophages was significantly inhibited by eleven bisbenzylisoquinolines and one half-molecule (benzylisoquinoline), with IC50 values in the μM range....