Search Results - "Perregaux, David G."

The specificity of JAK3 kinase inhibitors by Changelian, Paul S., Moshinsky, Deborah, Kuhn, Cyrille F., Flanagan, Mark E., Munchhof, Michael J., Harris, Thomas M., Whipple, David A., Doty, Jonathan L., Sun, Jianmin, Kent, Craig R., Magnuson, Kelly S., Perregaux, David G., Sawyer, Perry S., Kudlacz, Elizabeth M.

“…PF-956980 is a selective inhibitor of JAK3, related in structure to CP-690550, a compound being evaluated in clinical trials for rheumatoid arthritis and…”
Get full text

Identification and characterization of a novel class of interleukin-1 post-translational processing inhibitors by Perregaux, D G, McNiff, P, Laliberte, R, Hawryluk, N, Peurano, H, Stam, E, Eggler, J, Griffiths, R, Dombroski, M A, Gabel, C A

“…Lipopolysaccharide (LPS)-activated monocytes and macrophages produce large quantities of pro-interleukin (IL)-1beta but externalize little mature cytokine…”
Get more information

Analysis of the role of the HIF hydroxylase family members in erythropoiesis by Fisher, Timothy S., Lira, Paul D., Stock, Jeffrey L., Perregaux, David G., Brissette, William H., Ozolinš, Terence R.S., Li, Baiyong

“…HIF (hypoxia-inducible factor) hydroxylases have been implicated in EPO (erythropoietin) production and erythropoiesis. Here we examined the role of each of…”
Get full text

Antimicrobial peptides initiate IL-1 beta posttranslational processing: a novel role beyond innate immunity by Perregaux, David G, Bhavsar, Kanan, Contillo, Len, Shi, Jishu, Gabel, Christopher A

“…Human monocytes stimulated with LPS produce large quantities of prointerleukin-1beta, but little of this cytokine product is released extracellularly as the…”
Get full text

Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X7 receptor by Subramanyam, Chakrapani, Duplantier, Allen J., Dombroski, Mark A., Chang, Shang-Poa, Gabel, Christopher A., Whitney-Pickett, Carrie, Perregaux, David G., Labasi, Jeff M., Yoon, Kwansik, Shepard, Richard M., Fisher, Michael

“…The discovery, of a series of 2-Cl-5-heteroaryl-benzamide antagonists of the P2X7 receptor via parallel medicinal chemistry is described. Initial analogs…”
Get full text

Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X₇ receptor antagonists leading to the discovery of the clinical candidate CE-224,535 by Duplantier, Allen J, Dombroski, Mark A, Subramanyam, Chakrapani, Beaulieu, Aimee M, Chang, Shang-Poa, Gabel, Christopher A, Jordan, Crystal, Kalgutkar, Amit S, Kraus, Kenneth G, Labasi, Jeff M, Mussari, Christopher, Perregaux, David G, Shepard, Rick, Taylor, Timothy J, Trevena, Kristen A, Whitney-Pickett, Carrie, Yoon, Kwansik

“…High throughput screening (HTS) of our compound file provided an attractive lead compound with modest P2X₇ receptor antagonist potency and high selectivity…”
Get full text

Altered Cytokine Production in Mice Lacking P2X7Receptors by Solle, Mike, Labasi, Jeff, Perregaux, David G., Stam, Ethan, Petrushova, Nina, Koller, Beverly H., Griffiths, Richard J., Gabel, Christopher A.

“…The P2X7 receptor (P2X7R) is an ATP-gated ion channel expressed by monocytes and macrophages. To directly address the role of this receptor in interleukin…”
Get full text

Human monocyte ATP-induced IL-1 beta posttranslational processing is a dynamic process dependent on in vitro growth conditions by Laliberte, Ronald E., Perregaux, David G., McNiff, Patricia, Gabel, Christopher A.

“…Despite a large production capacity, freshly isolated lipopolysaccharide (LPS)‐activated human monocytes release only a small percentage of their newly…”
Get full text

Interleukin-1β posttranslational processing-exploration of P2X7 receptor involvement by Perregaux, David G., Labasi, Jeff, Laliberte, Ron, Stam, Ethan, Solle, Mike, Koller, Bev, Griffiths, Richard, Gabel, Christopher A.

“…Cultured monocytes and macrophages stimulated with LPS produce large quantities of prointerleukin (IL)‐1β, but release little mature cytokine to the medium…”
Get full text

Correlation of polymorphic variation in the promoter region of the interleukin‐1β gene with secretion of interleukin‐1β protein by Hall, Stephanie K., Perregaux, David G., Gabel, Christopher A., Woodworth, Thasia, Durham, L. Kathryn, Huizinga, T. W. F., Breedveld, F. C., Seymour, Albert B.

“…Objective Significant variation in interleukin‐1β (IL‐1β) protein secretion between subjects has been observed when using a lipopolysaccharide…”
Get full text

Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X 7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535 by Duplantier, Allen J., Dombroski, Mark A., Subramanyam, Chakrapani, Beaulieu, Aimee M., Chang, Shang-Poa, Gabel, Christopher A., Jordan, Crystal, Kalgutkar, Amit S., Kraus, Kenneth G., Labasi, Jeff M., Mussari, Christopher, Perregaux, David G., Shepard, Rick, Taylor, Timothy J., Trevena, Kristen A., Whitney-Pickett, Carrie, Yoon, Kwansik

“…High throughput screening (HTS) of our compound file provided an attractive lead compound with modest P2X 7 receptor antagonist potency and high selectivity…”
Get full text

Glutathione S-Transferase Omega 1-1 Is a Target of Cytokine Release Inhibitory Drugs and May Be Responsible for Their Effect on Interleukin-1 beta Posttranslational Processing by Laliberte, R E, Perregaux, D G, Hoth, L R, Rosner, P J, Jordan, C K, Peese, K M, Eggler, J, Dombroski, MA, Geoghegan, K F, Gabel, CA

“…Stimulus-induced posttranslational processing of human monocyte interleukin-1 beta (IL-1 beta ) is accompanied by major changes to the intracellular ionic…”
Get full text

ATP acts as an agonist to promote stimulus-induced secretion of IL-1 beta and IL-18 in human blood by Perregaux, D G, McNiff, P, Laliberte, R, Conklyn, M, Gabel, C A

“…Cultured monocytes and macrophages stimulated with LPS produce large quantities of proIL-1beta, but release little mature cytokine to the medium. The…”
Get full text

Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X sub(7 receptor) by Subramanyam, Chakrapani, Duplantier, Allen J, Dombroski, Mark A, Chang, Shang-Poa, Gabel, Christopher A, Whitney-Pickett, Carrie, Perregaux, David G, Labasi, Jeff M, Yoon, Kwansik, Shepard, Richard M, Fisher, Michael

“…The discovery, of a series of 2-Cl-5-heteroaryl-benzamide antagonists of the P2X sub(7 receptor via parallel medicinal chemistry is described. Initial analogs…”
Get full text

Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X sub(7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535) by Duplantier, Allen J, Dombroski, Mark A, Subramanyam, Chakrapani, Beaulieu, Aimee M, Chang, Shang-Poa, Gabel, Christopher A, Jordan, Crystal, Kalgutkar, Amit S, Kraus, Kenneth G, Labasi, Jeff M, Mussari, Christopher, Perregaux, David G, Shepard, Rick, Taylor, Timothy J, Trevena, Kristen A, Whitney-Pickett, Carrie, Yoon, Kwansik

“…High throughput screening (HTS) of our compound file provided an attractive lead compound with modest P2X sub(7 receptor antagonist potency and high…”
Get full text

Post-translational processing of murine IL-1: evidence that ATP-induced release of IL-1 alpha and IL-1 beta occurs via a similar mechanism by Perregaux, D G, Gabel, C A

“…In response to LPS, peritoneal macrophages produce IL-1, but, for the most part, newly synthesized cytokine molecules remain cell associated. Externalization…”
Get full text

Human monocyte interleukin-1 beta posttranslational processing. Evidence of a volume-regulated response by Perregaux, D G, Laliberte, R E, Gabel, CA

“…Interleukin (IL)-1 beta produced by monocytes and macrophages is not released via the normal secretory apparatus, and prior to its release, this cytokine must…”
Get full text

Glutathione s-transferase omega 1-1 is a target of cytokine release inhibitory drugs and may be responsible for their effect on interleukin-1beta posttranslational processing by Laliberte, Ronald E, Perregaux, David G, Hoth, Lise R, Rosner, Philip J, Jordan, Crystal K, Peese, Kevin M, Eggler, James F, Dombroski, Mark A, Geoghegan, Kieran F, Gabel, Christopher A

“…Stimulus-induced posttranslational processing of human monocyte interleukin-1beta (IL-1beta) is accompanied by major changes to the intracellular ionic…”
Get full text

Glutathione S-Transferase Omega 1-1 Is a Target of Cytokine Release Inhibitory Drugs and May Be Responsible for Their Effect on Interleukin-1β Posttranslational Processing by Ronald E. Laliberte, David G. Perregaux, Lise R. Hoth, Philip J. Rosner, Crystal K. Jordan, Kevin M. Peese, James. F. Eggler, Mark A. Dombroski, Kieran F. Geoghegan, Christopher A. Gabel

“…Stimulus-induced posttranslational processing of human monocyte interleukin-1β (IL-1β) is accompanied by major changes to the intracellular ionic…”
Get full text

Glutathione S-Transferase Omega 1-1 Is a Target of Cytokine Release Inhibitory Drugs and May Be Responsible for Their Effect on Interleukin-1औ Posttranslational Processing by Laliberte, Ronald E., Perregaux, David G., Hoth, Lise R., Rosner, Philip J., Jordan, Crystal K., Peese, Kevin M., Eggler, James.F., Dombroski, Mark A., Geoghegan, Kieran F., Gabel, Christopher A.

“…Stimulus-induced posttranslational processing of human monocyte interleukin-1औ (IL-1औ) is accompanied by major changes to the intracellular ionic environment,…”
Get full text