Hairpin ODN-based ligands as potential inhibitors of HMGB1 cytokine activity
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Hairpin ODN-based ligands as potential inhibitors of HMGB1 cytokine activity (467 views)

Musumeci D, Roviello GN, Montesarchio D, Sapio R, Valente M, Anr V, Bucci EM

Rsc Adv (ISSN: 2046-2069, 2046-2069electronic), 2013; 3(30): 12176-12184.

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Paper type: Journal Article,

Impact factor: 3.708, 5-year impact factor: 3.708

Url: http://www.scopus.com/inward/record.url?eid=2-s2.0-84881523430&partnerID=40&md5=e5083493c20f9c665f62871ad3952f20

Keywords: Cytokine Activity, Enzymatic Stability, High-Mobility Groups, Hydrodynamic Volumes, Inflammatory Disease, Nuclear Proteins, Pharmacokinetic Properties, Potential Inhibitors, Bioactivity, Biosynthesis, Ethylene Glycol, Optimization, Plasma Stability, Polyols, Ligands,

Affiliations:
*** IBB - CNR ***

Dipartimento di Scienze Chimiche, Università di Napoli Federico II, Complesso Universitario di Monte, via Cintia 21, Sant'Angelo, Napoli I-80126, Italy
Istituto di Biostrutture e Bioimmagini-CNR, via Mezzocannone 16, I-80134 Napoli, Italy
Bionucleon Srl, via Ribes 5, I-10010 Colleretto Giacosa (TO), Italy


References:
Not available.
Hairpin ODN-based ligands as potential inhibitors of HMGB1 cytokine activity

We here report the design, synthesis, and biological activity of a kinked hairpin-loop DNA acting at low nM concentrations as a strong inhibitor of HMGB1 (High-Mobility Group Box-1), a nuclear protein with cytokine activity in a number of inflammatory diseases. Lead compound optimization has been realized by inserting different oligo-ethylene glycol spacers at the 5′-end and loop positions of the natural hairpin DNA, in order to improve its enzymatic stability and structuring capability, as well as its overall pharmacokinetic properties. Thermal stability data as well as activity assays proved that the ODN which contained two hexa-ethylene glycol spacers, one at the 5′-end and the other in the loop, was the best candidate to inhibit HMGB1. Plasma stability assays and hydrodynamic volume measurements afforded further encouraging results in view of future in vivo evaluation of the optimized ligand. This journal is © The Royal Society of Chemistry 2013.
Hairpin ODN-based ligands as potential inhibitors of HMGB1 cytokine activity

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Hairpin ODN-based ligands as potential inhibitors of HMGB1 cytokine activity

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5 Records (5 excluding Abstracts).
Total impact factor: 20.077 (20.077 excluding Abstracts).
Total 5 year impact factor: 16.136 (16.136 excluding Abstracts).

Last modified by Marco Comerci on Sunday 12 July 2020, 13:14:55
467 views. Last view on Tuesday 29 August 2023, 9:26:39