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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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Pharmacological activity of C3a and C3a receptor ligands

2023
The complement system is an integral component of the innate immune response to infection and injury. The anaphylatoxins, C3a and C5a, are produced upon activation of the classical, alternative or mannan-binding lectin complement pathways. C5a is a potent pro-inflammatory mediator and overactivation or underegulation of C5a is implicated in the ...
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Reevaluation of the C3a active site using short synthetic C3a analogues

European Journal of Immunology, 1990
AbstractIn 1980 the C‐terminal pentapeptide LGLAR (C3a 73–77) was described (Caporale, L. H. et al. J. Biol. Chem. 1980. 255: 10758) as the minimal sequence inducing a C3a‐specific activity. We have synthesized C3a‐analogue peptides connected to non‐peptidic acyl residues known to potentiate biological activity.
J, Köhl, M, Casaretto, M, Gier, G, Karwath, C, Gietz, W, Bautsch, D, Saunders, D, Bitter-Suermann   +7 more
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Anaphylatoxins: C3a and C5a

1978
Publisher Summary This chapter discusses the structural and functional characterization of anaphylatoxins, spasmogenic substances released during complement activation. These low molecular weight peptide fragments of C3 and C5 elicit a variety of cellular responses, which implies that they play a significant role in inflammation and acute allergic ...
T E, Hugli, H J, Müller-Eberhard
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Anti-C3a, Anti-C3B (Anti-B) and Their Reaction with the Anaphylatoxic Fragment C3a

The Journal of Immunology, 1973
Abstract Specific antisera against the third human complement component (C3) and its fragments (C3a, C3c and C3d) were raised in rabbits. The reactions of anti-C3B (anti-B) with the anaphylatoxic fragment C3a were investigated by means of line electrophoresis, agglutination inhibition and Prausnitz-Küstner type reactions.
J L, Molenaar, A, ten Velde, K W, Pondman   +2 more
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Modulation of C3a Activity: Internalization of the Human C3a Receptor and its Inhibition by C5a

The Journal of Immunology, 1999
Abstract The C3a receptor (C3aR) is expressed on most human peripheral blood leukocytes with the exception of resting lymphocytes, implying a much higher pathophysiological relevance of the anaphylatoxin C3a as a proinflammatory mediator than previously thought.
B, Settmacher, D, Bock, H, Saad, S, Gärtner, C, Rheinheimer, J, Köhl, W, Bautsch, A, Klos   +7 more
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Complement C3a and C3a Receptor Activation Mediates Podocyte Injuries in the Mechanism of Primary Membranous Nephropathy

Journal of the American Society of Nephrology, 2022
Background The complement system is highly activated in primary membranous nephropathy (MN). Identifying the complement components that damage podocytes has important therapeutic implications. This study investigated the role of C3a and the C3a receptor (C3aR) in the pathogenesis of MN.
Shuang Gao, Zhao Cui, Ming-hui Zhao
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Development of a simple radioimmunoassay for human C3a

Inflammation, 1988
A radioimmunoassay was devised for the human complement cleavage product, C3a, using charcoal separation and selective precipitation of interfering substances. When compared with the commercially available immunoassay now marketed, the assay reported here was somewhat simpler to perform; furthermore, it overcame delivery and availability problems in ...
H R, Lamche, E, Paul, G, Schlag, H, Redl, D E, Hammerschmidt   +4 more
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C3a receptor on dibutyryl-cAMP-differentiated U937 cells and human neutrophils: The human C3a receptor characterized by functional responses and 125I-C3a binding

Biochemistry, 1992
The anaphylatoxic peptide C3a is part of a basic immunological defense mechanism, the complement system. Research on the human C3a receptor and signal transduction is hampered by the lack of a suitable human cell or cell line. We screened tumor cell lines and human blood cells for a C3a-dependent increase in cytosolic Ca2+ ([Ca2+]i) and analyzed this ...
A, Klos, S, Bank, C, Gietz, W, Bautsch, J, Köhl, M, Burg, T, Kretzschmar   +6 more
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Effective inhibition of C3a‐mediated pro‐inflammatory response by a human C3a‐specific protein binder

Biotechnology and Bioengineering, 2020
AbstractComplement component 3a (C3a) plays a crucial role in the immune response and host defense, but it is also involved in pro‐inflammatory responses, causing many inflammatory disorders. Blockade of C3a has been regarded as a potent therapeutic strategy for inflammatory diseases.
Yoo‐Kyoung Sohn, Sumin Son, Yoonjoo Choi, Da‐Eun Hwang, Hyo‐Deok Seo, Joong‐jae Lee, Hak‐Sung Kim   +6 more
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