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Pharmaceuticals 2011, 4(9), 1248-1280;

RFamide Peptides: Structure, Function, Mechanisms and Pharmaceutical Potential

Institute of Biochemistry, Leipzig University, Brüderstraße 34, 04103 Leipzig, Germany
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Received: 29 August 2011 / Revised: 9 September 2011 / Accepted: 15 September 2011 / Published: 21 September 2011
(This article belongs to the Special Issue Peptidomimetics)
Full-Text   |   PDF [601 KB, uploaded 21 September 2011]


Different neuropeptides, all containing a common carboxy-terminal RFamide sequence, have been characterized as ligands of the RFamide peptide receptor family. Currently, five subgroups have been characterized with respect to their N-terminal sequence and hence cover a wide pattern of biological functions, like important neuroendocrine, behavioral, sensory and automatic functions. The RFamide peptide receptor family represents a multiligand/multireceptor system, as many ligands are recognized by several GPCR subtypes within one family. Multireceptor systems are often susceptible to cross-reactions, as their numerous ligands are frequently closely related. In this review we focus on recent results in the field of structure-activity studies as well as mutational exploration of crucial positions within this GPCR system. The review summarizes the reported peptide analogs and recently developed small molecule ligands (agonists and antagonists) to highlight the current understanding of the pharmacophoric elements, required for affinity and activity at the receptor family. Furthermore, we address the biological functions of the ligands and give an overview on their involvement in physiological processes. We provide insights in the knowledge for the design of highly selective ligands for single receptor subtypes to minimize cross-talk and to eliminate effects from interactions within the GPCR system. This will support the drug development of members of the RFamide family. View Full-Text
Keywords: RFamide; neuropeptide FF; kisspeptin; prolactin-releasing peptide; QRFP RFamide; neuropeptide FF; kisspeptin; prolactin-releasing peptide; QRFP
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Findeisen, M.; Rathmann, D.; Beck-Sickinger, A.G. RFamide Peptides: Structure, Function, Mechanisms and Pharmaceutical Potential. Pharmaceuticals 2011, 4, 1248-1280.

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