PMID- 16083440
OWN - NLM
STAT- MEDLINE
DCOM- 20051011
LR  - 20131121
IS  - 1397-002X (Print)
IS  - 1397-002X (Linking)
VI  - 66
IP  - 3
DP  - 2005 Sep
TI  - [Ala12]MCD peptide: a lead peptide to inhibitors of immunoglobulin E binding to 
      mast cell receptors.
PG  - 132-7
AB  - An effort was made to discover mast cell degranulating (MCD) peptide analogs that 
      bind with high affinity to mast cell receptors without triggering secretion of 
      histamine or other mediators of the allergic reaction initiated by immunoglobulin 
      E (IgE) after mast cell activation. Such compounds could serve as inhibitors of 
      IgE binding to mast cell receptors. An alanine scan of MCD peptide reported 
      previously showed that the analog [Ala12]MCD was 120-fold less potent in 
      histamine-releasing activity and fivefold more potent in binding affinity to mast 
      cell receptors than the parent MCD peptide. Because this analog showed marginal 
      intrinsic activity and good binding affinity it was subsequently tested in the 
      present study as an IgE inhibitor. In contrast to MCD peptide, [Ala12]MCD showed 
      a 50% inhibition of IgE binding to the Fc epsilon RI alpha mast cell receptor by 
      using rat basophilic leukemia (RBL-2H3) mast cells and fluorescence polarization. 
      Furthermore, in a beta-hexosaminidase secretory assay, the peptide also showed a 
      50% inhibition of the secretion of this enzyme caused by IgE. An attempt was made 
      to relate structural changes and biologic differences between the [Ala12]MCD 
      analog and the parent MCD peptide. The present results show that [Ala12]MCD may 
      provide a base for designing agents to prevent IgE/Fc epsilon RI alpha 
      interactions and, consequently, allergic conditions.
FAU - Buku, A
AU  - Buku A
AD  - Department of Physiology and Biophysics, Mount Sinai School of Medicine, New 
      York, NY 10029, USA. angeliki.buku@mssm.edu
FAU - Condie, B A
AU  - Condie BA
FAU - Price, J A
AU  - Price JA
FAU - Mezei, M
AU  - Mezei M
LA  - eng
PT  - Journal Article
PL  - Denmark
TA  - J Pept Res
JT  - The journal of peptide research : official journal of the American Peptide 
      Society
JID - 9707067
RN  - 0 (Peptides)
RN  - 0 (Receptors, Cell Surface)
RN  - 32908-73-9 (mast cell degranulating peptide)
RN  - 37341-29-0 (Immunoglobulin E)
RN  - EC 3.2.1.52 (beta-N-Acetylhexosaminidases)
RN  - OF5P57N2ZX (Alanine)
SB  - IM
MH  - Alanine/*chemistry
MH  - Amino Acid Substitution
MH  - Animals
MH  - Immunoglobulin E/*metabolism
MH  - Mast Cells/drug effects/*metabolism
MH  - Models, Molecular
MH  - Monte Carlo Method
MH  - Peptides/chemical synthesis/chemistry/*metabolism
MH  - Protein Binding
MH  - Rats
MH  - Receptors, Cell Surface/*metabolism
MH  - Tumor Cells, Cultured
MH  - beta-N-Acetylhexosaminidases/analysis
EDAT- 2005/08/09 09:00
MHDA- 2005/10/12 09:00
CRDT- 2005/08/09 09:00
PHST- 2005/08/09 09:00 [pubmed]
PHST- 2005/10/12 09:00 [medline]
PHST- 2005/08/09 09:00 [entrez]
AID - JPP281 [pii]
AID - 10.1111/j.1399-3011.2005.00281.x [doi]
PST - ppublish
SO  - J Pept Res. 2005 Sep;66(3):132-7. doi: 10.1111/j.1399-3011.2005.00281.x.