New peptide analogues of β-secretase inhibitor OM 99-2 modified in P3 position

2009 ◽  
Author(s):  
Ivan Ivanov ◽  
Lyubomir Vezenkov ◽  
Dantcho Danalev
Keyword(s):  
Secretase Inhibitor ◽  
Peptide Analogues

IMMUNOGENICITY OF HEPATITIS B SURFACE ANTIGEN SYNTHETIC PEPTIDE ANALOGUES

1987 ◽  
pp. 565-568
Author(s):  
B. Lammek ◽  
G. Kupryszewski ◽  
U. Ragnarsson ◽  
H. Świderska ◽  
M. Jastrzebska ◽  
...  
Keyword(s):  
Hepatitis B ◽  
Surface Antigen ◽  
Synthetic Peptide ◽  
Hepatitis B Surface Antigen ◽  
Peptide Analogues

Positive charge modifications alter the ability of XIP to inhibit the plasma membrane calcium pump

1996 ◽  
Vol 271 (3) ◽  
pp. C736-C741 ◽  
Author(s):  
W. Xu ◽  
C. Gatto ◽  
M. A. Milanick
Keyword(s):  
Plasma Membrane ◽  
Positive Charge ◽  
Calcium Pump ◽  
Inhibitory Peptide ◽  
Ca Pump ◽  
Contact Points ◽  
Plasma Membrane Calcium Pump ◽  
Peptide Analogues ◽  
Positively Charged

Exchange inhibitory peptide (XIP; RRLLFYKYVYKRYRAGKQRG) is the shortest peptide that inhibits the plasma membrane Ca pump at high Ca (A. Enyedi, T. Vorherr, P. James, D. J. McCormick, A. G. Filoteo, E. Carafoli, and J. T. Penniston, J. Biol. Chem. 264: 12313-12321, 1989). Sulfosuccinimidyl acetate (SNA)-modified XIP does not inhibit the Ca pump; SNA neutralizes the positive charge on Lys at positions 7, 11, and 17. Peptide 2CK-XIP (RRLLFYRYVYRCYCAGRQKG) inhibits the pump, but the iodoacetamido-modified peptide does not inhibit. Three peptide analogues, in which 7, 11, and 17 were Ala, Cys, or Lys, inhibited about as well as XIP. SNA modification of these analogues (each with 1 Lys) did not inhibit. SNA modification of 2CK-XIP results in a peptide that does not inhibit; thus position 19 is important. Our results suggest that it is critical that position 19 be positively charged, that positions 7, 11, and 17 are important contact points between XIP and the Ca pump (with at least one positively charged), and that, whereas it is not essential that residues 12 and 14 be positive, they cannot be negative.

P1-180 Reduction in a-beta(1-40) and A-beta(1-42) in CSF and plasma in the beagle dog following acute oral dosing of the gamma secretase inhibitor, LY450139

2004 ◽  
Vol 25 ◽  
pp. S147 ◽  
Author(s):  
Paul A. Hyslop ◽  
Patrick C. May ◽  
James E. Audia ◽  
David O. Calligaro ◽  
Carl L. McMillian ◽  
...  
Keyword(s):  
Gamma Secretase ◽  
Oral Dosing ◽  
Beagle Dog ◽  
Secretase Inhibitor ◽  
Gamma Secretase Inhibitor

scholarly journals Intermittent Oral Coadministration of a Gamma Secretase Inhibitor with Dexamethasone Mitigates Intestinal Goblet Cell Hyperplasia in Rats

2013 ◽  
Vol 42 (2) ◽  
pp. 422-434 ◽  
Author(s):  
Shirley A. Aguirre ◽  
Ling Liu ◽  
Natilie A. Hosea ◽  
Wesley Scott ◽  
Jeffrey R. May ◽  
...  
Keyword(s):  
Goblet Cell ◽  
Gamma Secretase ◽  
Cell Hyperplasia ◽  
Goblet Cell Hyperplasia ◽  
Secretase Inhibitor ◽  
Gamma Secretase Inhibitor
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