Synthesis and LTB4 receptor antagonist activities of the naturally occurring LTB4 receptor antagonist leucettamine A and related analogs

1993 ◽  
Vol 36 (22) ◽  
pp. 3333-3340 ◽  
Author(s):  
Jeffrey C. Boehm ◽  
John G. Gleason ◽  
Israil Pendrak ◽  
Henry M. Sarau ◽  
Dulcie B. Schmidt ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Naturally Occurring ◽  
Ltb4 Receptor

The guinea pig as a suitable species for the characterization of the LTB4 receptor antagonist ZK 158252

1998 ◽  
Vol 16 ◽  
pp. S211
Author(s):  
Claudia Giesen ◽  
Bernd Buchmann ◽  
Roland Ekerdt ◽  
Wolfgang Fröhlich ◽  
Josef Heindl ◽  
...  
Keyword(s):  
Guinea Pig ◽  
Receptor Antagonist ◽  
Ltb4 Receptor

Cross-linking of the beta-glucan receptor on human monocytes results in interleukin-1 receptor antagonist but not interleukin-1 production

Blood ◽  
1993 ◽  
Vol 82 (12) ◽  
pp. 3695-3700 ◽  
Author(s):  
DD Poutsiaka ◽  
M Mengozzi ◽  
E Vannier ◽  
B Sinha ◽  
CA Dinarello
Keyword(s):  
Receptor Antagonist ◽  
Mononuclear Cells ◽  
Human Peripheral Blood ◽  
Interleukin 1 ◽  
Beta Glucan ◽  
Peripheral Blood Mononuclear ◽  
Naturally Occurring ◽  
Beta Glucans ◽  
Or Gene ◽  
Plastic Surfaces

Abstract The beta-glucan receptor, found on monocytes and neutrophils, binds glucose polymers derived from fungi. Ligands for the receptor have various immunomodulatory effects, including increased microbicidal killing activity. We have investigated the effect of beta-glucans on the production of interleukin-1 (IL-1) and its naturally occurring inhibitor, the IL-1 receptor antagonist (IL-1Ra). Particulate beta- glucan induced IL-1Ra production from human peripheral blood mononuclear cells (PBMC) but did not stimulate IL-1 beta synthesis or gene expression in these same cells. Monomeric (soluble) beta-glucan did not induce IL-1Ra production. However, when preincubated with PBMC, monomeric beta-glucan significantly (P <.01) reduced particulate beta- glucan induction of IL-1Ra by 40%, suggesting that crosslinking of beta- glucan receptors is required for induction of IL-1Ra. In support of this, monomeric beta-glucan immobilized on plastic surfaces stimulated IL-1Ra production. Vitamin D3, which increases the functional capacity of beta-glucan receptors, increased IL-1Ra production induced by particulate beta-glucan, whereas dexamethasone suppressed IL-1Ra synthesis. Because of their differential effects on cytokine production, beta-glucans may be used to therapeutic advantage in the diseases in which IL-1 is implicated.

scholarly journals TGF-β type 2 receptor–mediated modulation of the IL-36 family can be therapeutically targeted in osteoarthritis

2019 ◽  
Vol 11 (491) ◽  
pp. eaan2585 ◽  
Author(s):  
Tieshi Li ◽  
Susan Chubinskaya ◽  
Alessandra Esposito ◽  
Xin Jin ◽  
Lidia Tagliafierro ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Therapeutic Agent ◽  
Human Tissues ◽  
Human Cartilage ◽  
Joint Development ◽  
Naturally Occurring ◽  
Oa Chondrocytes ◽  
Disease Modifying ◽  
Surgical Conditions

Mechanisms that govern the shift from joint homeostasis to osteoarthritis (OA) remain unknown. Here, we identify a pathway used for joint development and homeostasis, and its role in OA. Using a combination of transgenic, pharmacological, and surgical conditions in mouse and human tissues, we found that TGF-β signaling promotes joint homeostasis through regulation of the IL-36 family. We identified IL-36 receptor antagonist (IL-36 in mice and IL-36RN in humans) as a potential disease-modifying OA drug. Specifically, OA development was associated with IL-36α up-regulation and IL-36Ra down-regulation in mice with tissue-specific postnatally induced ablation of Tgfbr2, mice treated with a TGF-β signaling inhibitor, mice with posttraumatic OA, and aging mice with naturally occurring OA. In human cartilage, OA severity was associated with decreased TGFBR2 and IL-36RN, whereas IL-36α increased. Functionally, intra-articular treatment with IL-36Ra attenuated OA development in mice, and IL-36RN reduced MMP13 in human OA chondrocytes. These findings highlight the relevance of TGFBR2–IL-36 interplay in joint homeostasis and IL-36RN as a potential therapeutic agent for OA.

The analysis of IL-1 beta and its naturally occurring inhibitors in multiple sclerosis: The elevation of IL-1 receptor antagonist and IL-1 receptor type II after steroid therapy

2009 ◽  
Vol 207 (1-2) ◽  
pp. 101-106 ◽  
Author(s):  
Irena Dujmovic ◽  
Katia Mangano ◽  
Tatjana Pekmezovic ◽  
Cinzia Quattrocchi ◽  
Sarlota Mesaros ◽  
...  
Keyword(s):  
Multiple Sclerosis ◽  
Receptor Antagonist ◽  
Steroid Therapy ◽  
Receptor Type ◽  
Type Ii ◽  
Naturally Occurring

Fibronectin modulates expression of interleukin-1 beta and its receptor antagonist in human mononuclear cells

1996 ◽  
Vol 271 (1) ◽  
pp. L61-L69 ◽  
Author(s):  
K. L. Graves ◽  
J. Roman
Keyword(s):  
Receptor Antagonist ◽  
Type I Collagen ◽  
Mononuclear Cells ◽  
Human Peripheral Blood ◽  
Interleukin 1 ◽  
Type I ◽  
Peripheral Blood Mononuclear ◽  
Human Mononuclear Cells ◽  
Naturally Occurring ◽  
Dose Dependent

Identification of factors that regulate production of proinflammatory cytokines may provide insight into mechanisms governing lung inflammation. One potential regulatory factor highly expressed in inflamed tissues is fibronectin (FN). To determine the potential effects of FN on interleukin (IL)-1 beta production, we exposed human peripheral blood mononuclear cells to soluble FN. This treatment resulted in the accumulation of IL-1 beta mRNA and enhancement of IL-1 beta protein synthesis and secretion. This effect was dose dependent and appeared to be mediated by the integrin alpha 5 beta 1. Treatment with FN also increased production of IL-1 receptor antagonist (IL-1ra), a naturally occurring inhibitor of IL-1 function. However, the stimulatory effect of FN on IL-1ra production was abolished by costimulation with type I collagen. We conclude that the increased deposition of FN in injured tissues may enhance the expression of IL-1 beta mRNA and augment the production and release of IL-1 beta protein by mononuclear cells. Differential expression of IL-1 beta and IL-1ra resulting in a high IL-1 beta-to-IL-1ra ratio in response to mixed matrices containing FN and type I collagen may be an important regulatory point in inflammation.

Yangambin: A New Naturally-Occurring Platelet-Activating Factor Receptor Antagonist: Binding andIn VitroFunctional Studies

Planta Medica ◽  
1995 ◽  
Vol 61 (02) ◽  
pp. 101-105 ◽  
Author(s):  
Hugo Castro-Faria-Neto ◽  
Patricía Bozza ◽  
Hermenegildo Cruz ◽  
Cláudia Silva ◽  
Flávio Violante ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Platelet Activating Factor ◽  
Naturally Occurring ◽  
Antagonist Binding ◽  
Platelet Activating Factor Receptor
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