title: Antagonists of IL-1R: a patent evaluation (WO2012122985).
abstract: IL-1 is a master cytokine that plays a pivotal role in local and systemic inflammation and is involved in the host response to both physiological and pathological stimuli. The recent development of biological compounds targeting IL-1 activity in vivo has revealed the contribution of this cytokine to a large number of human inflammatory and autoimmune diseases. Nevertheless, these currently used drugs display some disadvantages that limit their use in several IL-1-driven diseases, urging for the identification of more powerful agents. The present article describes the identification of new small peptides displaying IL-1 inhibitory activity and covered by the patent WO2012122985. The experimental work in support of the patent's claims is also discussed. Specific attention is paid to the comparison with the original compound from which the peptides were originated: the IL-1 receptor antagonist (IL-1RA) protein. The potential advantages brought about by the present invention as well as the limits documented by the experimental results shown in the patent are also discussed.
authors.affiliation: University of Rome Tor Vergata, Department of Biomedicine and Prevention, 00133 Rome, Italy. claudio.sette@uniroma2.it
authors.forename: Claudio
authors.initials: C
authors.lastname: Sette
mesh_terms: D000818:Animals; D001327:Autoimmune Diseases / Q000188:drug therapy / Q000503:physiopathology; D015195:Drug Design; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000503:physiopathology; D007375:Interleukin-1 / Q000378:metabolism*; D058990:Molecular Targeted Therapy; D010330:Patents as Topic; D010455:Peptides / Q000494:pharmacology; D017472:Receptors, Interleukin-1 / Q000037:antagonists & inhibitors*
chemical_list: D007375:Interleukin-1; D010455:Peptides; D017472:Receptors, Interleukin-1