PMID- 20000459
OWN - NLM
STAT- MEDLINE
DCOM- 20100520
LR  - 20220129
IS  - 1520-4812 (Electronic)
IS  - 1043-1802 (Linking)
VI  - 21
IP  - 1
DP  - 2010 Jan
TI  - Modification of thiol functionalized aptamers by conjugation of synthetic 
      polymers.
PG  - 169-74
LID - 10.1021/bc900397s [doi]
AB  - Aptamers are known for their short in vivo circulating half-life and rapid renal 
      clearance. Their conjugation to poly(ethylene glycol) (PEG) is a way to improve 
      their residence in the body. Two aptamers (AptD and AptF), having a disulfide 
      protected thiol modification on the 3' end, have been conjugated to maleimide 
      activated PEGs of various molecular weights and structures (linear PEG20; 
      branched PEG20 and 40; PolyPEG17, 40, and 60 kDa). The high yield coupling 
      (70-80% in most of the cases) could be achieved using immobilized 
      tris[2-carboxyethyl]phosphine hydrochloride (TCEP) as reducing agent at pH 4. The 
      affinity of PEGylated AptD for its target was reduced by conjugation to linear 
      PEG20 and branched PEG40, but not to branched PEG20 and PolyPEGs. This work 
      demonstrates an alternative approach to PEGylation of aptamers, and that the 
      effect of PEG on the affinity for the target varies according to the structure 
      and conformation of the synthetic polymer.
FAU - Da Pieve, Chiara
AU  - Da Pieve C
AD  - Department of Chemistry and Analytical Sciences, The Open University, Milton 
      Keynes, UK. c.dapieve@open.ac.uk
FAU - Williams, Paul
AU  - Williams P
FAU - Haddleton, David M
AU  - Haddleton DM
FAU - Palmer, Richard M J
AU  - Palmer RM
FAU - Missailidis, Sotiris
AU  - Missailidis S
LA  - eng
GR  - 2005MAY11/BCN_/Breast Cancer Now/United Kingdom
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - Bioconjug Chem
JT  - Bioconjugate chemistry
JID - 9010319
RN  - 0 (Aptamers, Nucleotide)
RN  - 0 (Drug Carriers)
RN  - 0 (Maleimides)
RN  - 0 (Mucin-1)
RN  - 0 (Phosphines)
RN  - 0 (Sulfhydryl Compounds)
RN  - 22OAC2MO2S (tris(2-carboxyethyl)phosphine)
RN  - 2519R1UGP8 (maleimide)
RN  - 3WJQ0SDW1A (Polyethylene Glycols)
SB  - IM
MH  - Aptamers, Nucleotide/*chemistry/genetics/metabolism/pharmacokinetics
MH  - Binding Sites
MH  - Drug Carriers/*chemistry
MH  - Half-Life
MH  - Hydrogen-Ion Concentration
MH  - Kinetics
MH  - Maleimides/chemistry
MH  - Molecular Weight
MH  - Mucin-1/genetics
MH  - Phosphines/chemistry
MH  - Polyethylene Glycols/*chemistry
MH  - Spectrometry, Fluorescence
MH  - Sulfhydryl Compounds/*chemistry
EDAT- 2009/12/17 06:00
MHDA- 2010/05/21 06:00
CRDT- 2009/12/17 06:00
PHST- 2009/12/17 06:00 [entrez]
PHST- 2009/12/17 06:00 [pubmed]
PHST- 2010/05/21 06:00 [medline]
AID - 10.1021/bc900397s [doi]
PST - ppublish
SO  - Bioconjug Chem. 2010 Jan;21(1):169-74. doi: 10.1021/bc900397s.