Cyclic peptide RD808 reduces myocardial injury induced by β1-adrenoreceptor autoantibodies

Dong, Yu; Zhang, Shangyue; Xu, Wenli; Xu, Jiahui; Zhang, Yi; Zhang, Suli; Wu, Ye; Yu, Hefen; Cao, Ning; Liu, Huirong; Wang, Wen

doi:10.1007/s00380-018-1321-3

Cited by 7 publications

(6 citation statements)

References 40 publications

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“…In addition, some peptides that are beneficial to cardiovascular disease are being tested in animals. For example, infusion of vasoactive intestinal peptide increased the concentration of myocardial vasoactive intestinal peptide and reversed existing myocardial fibrosis in rats 311 , and cyclopeptide RD808 neutralized the β 1adrenergic receptor, attenuating myocardial injury induced by the β 1 -adrenergic receptor in mice 312 . The central adrenocorticotropin-releasing factor (CRF)-related peptide system is currently attracting increasing attention as a target for the prevention of cardiovascular disease 313 .…”

Section: Current Development and Application Of Therapeutic Peptides ...mentioning

confidence: 99%

Therapeutic peptides: current applications and future directions

Wang

Zhang

et al. 2022

Sig Transduct Target Ther

927

595

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Peptide drug development has made great progress in the last decade thanks to new production, modification, and analytic technologies. Peptides have been produced and modified using both chemical and biological methods, together with novel design and delivery strategies, which have helped to overcome the inherent drawbacks of peptides and have allowed the continued advancement of this field. A wide variety of natural and modified peptides have been obtained and studied, covering multiple therapeutic areas. This review summarizes the efforts and achievements in peptide drug discovery, production, and modification, and their current applications. We also discuss the value and challenges associated with future developments in therapeutic peptides.

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Section: Current Development and Application Of Therapeutic Peptides ...mentioning

confidence: 99%

Therapeutic peptides: current applications and future directions

Wang

Zhang

et al. 2022

Sig Transduct Target Ther

927

595

View full text Add to dashboard Cite

show abstract

“…In rodent experiments, a cyclic peptide corresponding to β1-AR ECL2 prevented the development of chronic heart failure caused by autoantibodies to β1-AR [432,443]. A cardioprotective effect on myocardial injury in mice was also demonstrated for another cyclic peptide, RD808, also corresponding to ECL2 of β1-AR [444].…”

Section: Allosteric Regulators Of β-Adrenergic Receptorsmentioning

confidence: 88%

Allosteric Regulation of G-Protein-Coupled Receptors: From Diversity of Molecular Mechanisms to Multiple Allosteric Sites and Their Ligands

Ao¹

2023

Preprint

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A separate group consists of compounds that are able to simultaneously interact with both orthosteric and allosteric sites, which are classified as bitopic GPCR ligands [74, 76-81]. They have two pharmacophores, one of which binds with high affinity to the orthosteric site, while the other, with lower affinity, binds to the allosteric site. If these sites are spatially separated in the receptor, then the pharmacophores in the bitopic ligand must be connected with a flexible linker, the length of which exactly corresponds to the distance between the orthosteric and allosteric sites. At the same time, it is important that the linker does not significantly affect the conformational rearrangements in the receptor caused by its activation by orthosteric and (or) allosteric agonists [74, 79].

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“…In the experiments with rodents, a cyclic peptide corresponding to β 1 -AR ECL2 prevented the development of chronic heart failure caused by autoantibodies to β 1 -AR [ 433 , 444 ]. A cardioprotective effect on myocardial injury in mice was demonstrated for another cyclic peptide, RD808, also corresponding to ECL2 of β1-AR [ 445 ].…”

Section: Allosteric Regulators Of β-Adrenergic Receptorsmentioning

confidence: 99%

Allosteric Regulation of G-Protein-Coupled Receptors: From Diversity of Molecular Mechanisms to Multiple Allosteric Sites and Their Ligands

2023

IJMS

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Allosteric regulation is critical for the functioning of G protein-coupled receptors (GPCRs) and their signaling pathways. Endogenous allosteric regulators of GPCRs are simple ions, various biomolecules, and protein components of GPCR signaling (G proteins and β-arrestins). The stability and functional activity of GPCR complexes is also due to multicenter allosteric interactions between protomers. The complexity of allosteric effects caused by numerous regulators differing in structure, availability, and mechanisms of action predetermines the multiplicity and different topology of allosteric sites in GPCRs. These sites can be localized in extracellular loops; inside the transmembrane tunnel and in its upper and lower vestibules; in cytoplasmic loops; and on the outer, membrane-contacting surface of the transmembrane domain. They are involved in the regulation of basal and orthosteric agonist-stimulated receptor activity, biased agonism, GPCR-complex formation, and endocytosis. They are targets for a large number of synthetic allosteric regulators and modulators, including those constructed using molecular docking. The review is devoted to the principles and mechanisms of GPCRs allosteric regulation, the multiplicity of allosteric sites and their topology, and the endogenous and synthetic allosteric regulators, including autoantibodies and pepducins. The allosteric regulation of chemokine receptors, proteinase-activated receptors, thyroid-stimulating and luteinizing hormone receptors, and beta-adrenergic receptors are described in more detail.

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Cyclic peptide RD808 reduces myocardial injury induced by β1-adrenoreceptor autoantibodies

Cited by 7 publications

References 40 publications

Therapeutic peptides: current applications and future directions

Therapeutic peptides: current applications and future directions

Allosteric Regulation of G-Protein-Coupled Receptors: From Diversity of Molecular Mechanisms to Multiple Allosteric Sites and Their Ligands

Allosteric Regulation of G-Protein-Coupled Receptors: From Diversity of Molecular Mechanisms to Multiple Allosteric Sites and Their Ligands

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