cyclisation increases the stability of the sea anemone peptide apetx2 but decreases its activity at acid-sensing ion channel 3cyclisation增加稳定的海葵肽apetx2但减少酸感性离子通道活动3.pdfVIP
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cyclisation increases the stability of the sea anemone peptide apetx2 but decreases its activity at acid-sensing ion channel 3cyclisation增加稳定的海葵肽apetx2但减少酸感性离子通道活动3
Mar. Drugs 2012, 10, 1511-1527; doi:10.3390/m OPEN ACCESS Marine Drugs ISSN 1660-3397 /journal/marinedrugs Article Cyclisation Increases the Stability of the Sea Anemone Peptide APETx2 but Decreases Its Activity at Acid-Sensing Ion Channel 3 Jonas E. Jensen, Mehdi Mobli, Andreas Brust, Paul F. Alewood, Glenn F. King * and Lachlan D. Rash * The University of Queensland, Institute for Molecular Bioscience, Brisbane, QLD 4072, Australia; E-Mails: eklund_jensen@ (J.E.J.); m.mobli@.au (M.M.); a.brust@.au (A.B.); p.alewood@.au (P.F.A.) * Authors to whom correspondence should be addressed; E-Mails: l.rash@.au (L.D.R.); glenn.king@.au (G.F.K.); Tel.: +61-7-3346-2985 (L.D.R.); +61-7-3346-2025 (G.F.K.); Fax: +61-7-3346-2090 (L.D.R.); +61-7-3346-2101 (G.F.K.). Received: 30 May 2012; in revised form: 14 June 2012 / Accepted: 6 July 2012 / Published: 16 July 2012 Abstract: APETx2 is a peptide isolated from the sea anemone Anthopleura elegantissima . It is the most potent and selective inhibitor of acid-sensing ion channel 3 (ASIC3) and it is currently in preclinical studies as a novel analgesic for the treatment of chronic inflammatory pain. As a peptide it faces many challenges in the drug development process, including the potential lack of stability often associated with therapeutic peptides. In this study we determined the susceptibili
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