Document Detail


Cobalt(III)-induced hexamerization of PEGylated insulin.
MedLine Citation:
PMID:  21835194     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Insulin conjugates in which the B1Phe residue has been chemically modified often exhibit a reduced tendency to associate into hexamers due to weakened interactions between subunits. The purpose of this study was to prepare a hexamer formulation for such insulin conjugates by using Co(III) as a coordinating metal ion. PEGylated insulin in which monomethoxypoly(ethylene glycol) (mPEG, M(r) 5000 or 20,000) had been site-specifically attached to B1Phe was chosen as a model conjugate. Hexamerization of mPEG-insulin upon H(2)O(2)-mediated oxidation of Co(II) was kinetically and quantitatively analysed by visible spectrometry and size-exclusion HPLC. Co(III) mPEG-insulin hexamers thus obtained were extremely stable, existing mostly as a hexameric form even at nanomolar concentrations. A remarkable increase in hydrodynamic volumes was observed for Co(III) mPEG(20k)-insulin hexamers (1600kDa), as well as Co(III) mPEG(5k)-insulin hexamers (300kDa). Our results demonstrate the potential benefits of Co(III) hexamer formulation for weakly associating insulin conjugates in the treatment of diabetes.
Authors:
Sung In Lim; Myung Hyun Jang; Dae Jin Kim; Sung Min Bae; Se Chang Kwon
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-8-3
Journal Detail:
Title:  International journal of biological macromolecules     Volume:  -     ISSN:  1879-0003     ISO Abbreviation:  -     Publication Date:  2011 Aug 
Date Detail:
Created Date:  2011-8-12     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7909578     Medline TA:  Int J Biol Macromol     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 Elsevier B.V. All rights reserved.
Affiliation:
Research Center, Hanmi Pharm. Co., Ltd., 377-1 Yeongcheon-ri, Dongtan-myeon, Hwaseong-si, Gyeonggi-do 445-813, Republic of Korea.
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