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Structure-Based Rationale for Interleukin 5 Receptor Antagonism

Current Pharmaceutical Design, 2008
Human interleukin 5 (IL5) is the major hematopoietin that stimulates the proliferation, migration and activation of eosinophils and is implicated in the pathogenesis of inflammatory and other myeloproliferative diseases. IL5 functions through the signaling of a common receptor subunit beta (beta c), in a receptor activation process that requires ...
Tetsuya, Ishino   +3 more
openaire   +2 more sources

Recruitment pharmacophore for interleukin 5 receptor α antagonism

Peptide Science, 2006
AbstractInterleukin‐5 receptor α is a therapeutic target for hypereosinophilic diseases including allergic inflammations and asthma. The cyclic peptide AF17121 (Ac‐VDE[CWRIIASHTWFC]AEE‐CONH2) has been identified as a submicromolar inhibitor of interleukin 5 (IL5)‐interleukin 5 receptor α (IL5Rα) interaction from a random peptide screen.
Madhushree, Bhattacharya   +6 more
openaire   +2 more sources

Biological and Molecular Characteristics of Interleukin-5 and its Receptor

International Reviews of Immunology, 1998
Interleukin-5 (IL5) is a T cell-derived cytokine involved in the pathogenesis of atopic diseases. It specifically controls the production, the activation and the localization of Eosinophils. The Eosinophils are the major cause of tissue damage resulting in the symptoms of asthma and related allergic disorders.
S, Karlen   +5 more
openaire   +2 more sources

The Interleukin-5 Receptor

1995
Abstract The nucleotide sequence of the human IL-5Ra cDNA (GenBank accession numbers M75914, M96651, M96652, X61176, X61177, X61178, and X62156) predicts a polypeptide of 420 amino acids (Fig. 1) (Tavernier et al. 1991, 1992; Murata et al. 1992).
openaire   +1 more source

Characterization of YM-90709 as a novel antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor

International Immunopharmacology, 2002
Interleukin-5 (IL-5) plays an important role in the activation of eosinophils in allergic inflammation including asthma and atopic dermatitis. A newly synthesized compound, YM-90709, 2,3-dimethoxy-6,6-dimethyl-5,6-dihydrobenzo[7,8]indolizino [2,3-b]quinoxaline, is reported here to inhibit the binding of IL-5 to its receptor on peripheral human ...
Tatsuaki, Morokata   +2 more
openaire   +2 more sources

Analysis of interleukin 5 receptors on murine eosinophils: A comparison with receptors on B13 cells

Cytokine, 1991
The interleukin 5 receptor (IL-5R) on murine eosinophils and a mouse B cell line (B13) was investigated using iodinated murine IL-5 produced in the baculovirus system. Electrophoretic analysis of this recombinant protein identified a range of bands Mr 26,000 to 32,000 resulting from differential glycosylation. The specific activity and binding kinetics
S C, Barry   +3 more
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Functional analysis of the interleukin-5 receptor antagonist peptide, AF18748

Cytokine, 2004
AF18748 is a dimeric peptide of 2 x 19 amino acids that specifically binds to the alpha-chain of the human IL-5 receptor (IL-5R), preventing binding of IL-5 and acting as a receptor antagonist. However, the peptide acts by inducing alpha-chain dimerization, and we therefore set out to investigate whether this peptide would have any residual agonist ...
Marcela, Rosas   +5 more
openaire   +2 more sources

Characterization of the murine interleukin 5 receptor by using a monoclonal antibody

International Immunology, 1990
Murine interleukin 5 (IL-5), a lymphokine produced by helper T cells, is involved in the regulation of growth and differentiation of B cells and other hematopoietic cells. The receptor for IL-5 has been identified as two cross-linked complexes on T88-M cells (a murine IL-5-dependent early B cell line).
N, Yamaguchi   +7 more
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Expression of the murine interleukin-5 receptor on Xenopus laevis oocytes

Biochemical and Biophysical Research Communications, 1990
In this study we describe the use of Xenopus laevis oocytes for the detection of mRNA coding for a murine interleukin-5 (mI15) receptor. When injected with sucrose gradient fractionated polyA+ RNA derived from the murine 115-dependent pre B cell line B13, these oocytes could specifically bind 35S-methionine labeled mI15.
R, Devos   +5 more
openaire   +2 more sources

Molecular characterization of the β chain of the murine interleukin 5 receptor

International Immunology, 1991
Interleukin 5 (IL-5) is a multifunctional cytokine that regulates the proliferation and differentiation of hematopoietic cells including B cells and eosinophils. The murine IL-5 acts on target cells via an IL-5 specific high-affinity receptor (Kd approximately 150 pM) that has been proposed to be composed of at least two membrane polypeptide chains ...
S, Mita   +6 more
openaire   +2 more sources

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