Document Detail


The LC/MS analysis of glycation of IgG molecules in sucrose containing formulations.
MedLine Citation:
PMID:  17621682     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Glycation of a recombinant monoclonal IgG2 molecule, in sucrose containing liquid formulations, was studied using reversed-phase LC/MS analysis of the intact IgG, the F(ab')2 fragments and after complete tryptic digestion. The extent of glycation in sucrose containing formulations was monitored at different temperatures over a period of 21 months using the Hexose index (Hex(I)). Hex(I) represents the average number of hexose molecules per molecule of IgG and was calculated by using the intensity values of peaks corresponding to hexose isoforms in the deconvoluted mass spectra. The rate of glycation in mildly acidic sucrose containing formulations was proportional to the incubation temperature. No glycation was observed in sucrose containing formulations incubated at 4 degrees C even after 18 months. However, when the same formulations were incubated at 37 degrees C glycation was observed after just 1 month. The glycation sites were mapped to 10 lysine residues distributed throughout the molecule. The amino terminal end of the light chain was also shown to contain glycation. The surface accessibility of the lysine side chain could influence its susceptibility to glycation.
Authors:
Himanshu S Gadgil; Pavel V Bondarenko; Gary Pipes; Doug Rehder; Arnold McAuley; Natalie Perico; Tom Dillon; Margaret Ricci; Michael Treuheit
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  96     ISSN:  0022-3549     ISO Abbreviation:  J Pharm Sci     Publication Date:  2007 Oct 
Date Detail:
Created Date:  2007-09-03     Completed Date:  2007-11-09     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  2607-21     Citation Subset:  IM    
Copyright Information:
(c) 2007 Wiley-Liss, Inc.
Affiliation:
Department of Pharmaceutics, Amgen Inc., 1201 Amgen Court West, Seattle, Washington 99119-3105, USA. hgadgil@amgen.com
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MeSH Terms
Descriptor/Qualifier:
Antibodies, Monoclonal / chemistry*
Chemistry, Pharmaceutical
Chromatography, Liquid*
Excipients / chemistry*
Glycosylation
Hydrogen-Ion Concentration
Immunoglobulin Fab Fragments / chemistry
Immunoglobulin G / chemistry*
Lysine / chemistry
Models, Molecular
Peptide Mapping*
Protein Conformation
Protein Denaturation
Recombinant Proteins / chemistry
Spectrometry, Mass, Electrospray Ionization*
Sucrose / chemistry*
Technology, Pharmaceutical / methods*
Temperature
Time Factors
Trypsin
Chemical
Reg. No./Substance:
0/Antibodies, Monoclonal; 0/Excipients; 0/Immunoglobulin Fab Fragments; 0/Immunoglobulin G; 0/Recombinant Proteins; 56-87-1/Lysine; 57-50-1/Sucrose; EC 3.4.21.4/Trypsin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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