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Ligands for C3a and C5a Receptors [PDF]

, 2023
Prolonged activation of the complement system of blood proteins in response to infection or tissue injury can lead to inflammatory diseases. This thesis investigates the potency, selectivity and structures of reported and rationally designed new ligands for human complement receptors C3aR and C5aR, towards development of new therapeutic agents. Chapter
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Amino acids 327-350 of the human C5a-receptor are not essential for [125I]C5a binding in COS cells and signal transduction inXenopusoocytes [PDF]

FEBS Letters, 1994
The anaphylatoxic peptide C5a is an important inflammatory mediator of the complement system. We have generated human C5a-receptor (hC5aR) mutants with truncation of its cytosolic carboxyl-terminus (C-terminus). Both mutants were analysed for C5a-binding
Ulrich Martin, Joerg Koehl
exaly   +2 more sources

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Role of C5a and C5a Receptor in Sepsis

2006
In experimental sepsis (after cecal ligation and puncture, CLP) there is convincing evidence of complement activation, as there is in human sepsis. In addition, in sepsis involving rodents and humans, blood neutrophils have lost innate immune functions (chemotaxis, phagocytosis, the ability to produce H2O2).
F. S. Zetoune, P. A. Ward, M. S. Huber-Lang   +2 more
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Human T Cells Express the C5a Receptor and Are Chemoattracted to C5a

The Journal of Immunology, 1999
Abstract The anaphylatoxin C5a is a potent mediator of inflammation that exerts a broad range of activity on cells of the myeloid lineage. In this study, we present the first evidence that human T cells express the C5a receptor (C5aR) and are chemotactic to C5a.
S, Nataf, N, Davoust, R S, Ames, S R, Barnum   +3 more
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Modeling Molecular Mechanisms of Binding of the Anaphylatoxin C5a to the C5a Receptor

Biochemistry, 2008
This study presents the 3D model of the complex between the anaphylatoxin C5a and its specific receptor, C5aR. This is the first 3D model of a G-protein-coupled receptor (GPCR) complex with a peptide ligand deduced by a molecular modeling procedure analyzing various conformational possibilities of the extracellular loops and the N-terminal segment of ...
Gregory V, Nikiforovich, Garland R, Marshall, Thomas J, Baranski   +2 more
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The chemotactic receptor for human C5a anaphylatoxin

Nature, 1991
Host defence and inflammatory responses are controlled and amplified by receptor-mediated events often initiated by a chemotactic factor that directs the approach of phagocytic cells. Complement receptors CR1 and CR3 are responsible for the phagocytic and adhesive properties of neutrophils, whereas the C5a receptor mediates the pro-inflammatory and ...
N P, Gerard, C, Gerard
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Analysis of C5a receptor by monoclonal antibody

Journal of Immunological Methods, 1995
We prepared a mouse monoclonal antibody (mAb), termed 4C8, to the human C5a receptor (C5aR, CD88) by fusing spleen cells from mice immunized with mouse Ltk- cells transfected with cDNA of human C5aR (Ltk-/C5aR) to the mouse myeloma cell line P3U1. This mAb belonging to the IgM kappa subclass, detected a 43 kDa band on cell lysates of Ltk-/C5aR by ...
H, Watanabe, M, Kuraya, R, Kasukawa, H, Yanagisawa, M, Yanagisawa, T, Fujita   +5 more
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Distribution of Rat C5a Anaphylatoxin Receptor

Microbiology and Immunology, 2002
AbstractThe anaphylatoxin, complement 5a (C5a), plays a key role in mediating various inflammatory reactions following complement activation. Several investigators have reported that C5a receptor (C5aR) is expressed in non‐myeloid cells under certain conditions or in different cell lines.
Hiroyasu, Akatsu, Masayoshi, Abe, Takashi, Miwa, Hisashi, Tateyama, Seiji, Maeda, Noriko, Okada, Kiyohide, Kojima, Hidechika, Okada   +7 more
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The Alternative C5a Receptor Function

2012
When acute inflammatory states are induced by treatment with chemical mediators in C5-deficient mice, neutrophil influxes are commonly decreased. Therefore, the neutrophil C5a receptor (C5aR) is believed to be a member of the pro-inflammatory receptors.
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C5a receptor antagonists.

Current pharmaceutical design, 1999
The anaphylatoxin C5a is an extremely potent proinflammatory peptide produced during activation of the complement system. The structure of C5a includes a core region (N-terminal residues 1-63) consisting of four, antiparallel alpha-helices held together by three disulfide linkages and a structured C-terminal tail (residues 64-74).
T C, Pellas, L P, Wennogle
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