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Host Defence Cryptides from Human Apolipoproteins: Applications in Medicinal Chemistry

[ Vol. 20 , Issue. 14 ]

Author(s):

Rosa Gaglione, Elio Pizzo, Eugenio Notomista, Cesar de la Fuente-Nunez and Angela Arciello*   Pages 1324 - 1337 ( 14 )

Abstract:


Several eukaryotic proteins with defined physiological roles may act as precursors of cryptic bioactive peptides released upon protein cleavage by the host and/or bacterial proteases. Based on this, the term “cryptome” has been used to define the unique portion of the proteome encompassing proteins with the ability to generate bioactive peptides (cryptides) and proteins (crypteins) upon proteolytic cleavage. Hence, the cryptome represents a source of peptides with potential pharmacological interest. Among eukaryotic precursor proteins, human apolipoproteins play an important role, since promising bioactive peptides have been identified and characterized from apolipoproteins E, B, and A-I sequences. Human apolipoproteins derived peptides have been shown to exhibit antibacterial, anti-biofilm, antiviral, anti-inflammatory, anti-atherogenic, antioxidant, or anticancer activities in in vitro assays and, in some cases, also in in vivo experiments on animal models. The most interesting Host Defence Peptides (HDPs) identified thus far in human apolipoproteins are described here with a focus on their biological activities applicable to biomedicine. Altogether, reported evidence clearly indicates that cryptic peptides represent promising templates for the generation of new drugs and therapeutics against infectious diseases.

Keywords:

Host defence peptides, Human apolipoproteins, Bioactive cryptides, Synergistic effects, Bacterial biofilm, Combinatorial therapy.

Affiliation:

Department of Chemical Sciences, University of Naples Federico II, 80126 Naples, Department of Biology, University of Naples Federico II, 80126 Naples, Department of Biology, University of Naples Federico II, 80126 Naples, Machine Biology Group, Departments of Psychiatry and Microbiology, Institute for Biomedical Informatics, Institute for Translational Medicine and Therapeutics, Perelman School of Medicine, and Department of Bioengineering, University of Pennsylvania, Philadelphia, Pennsylvania, Department of Chemical Sciences, University of Naples Federico II, 80126 Naples



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