Synthesis and sst(2) binding profiles of new [Tyr(3)]octreotate analogs.
One of the main objectives of our current work is the development of new somatostatin analogs that would retain the general characteristics of [Tyr(3)]octreotate (Tate) while showing potential for clinical application. In this respect, study of their interaction with the sst(2) is crucial in providing preliminary structure-activity relationships data. In the present work we report on the synthesis and the preliminary biological evaluation of a total of 15 new structurally modified [Tyr(3)]octreotate analogs. The binding affinities were determined during competition binding assays in sst(2)-positive rat acinar pancreatic AR4-2J cell membranes using [(125)I-Tyr(3)]octreotide as the radioligand.
Petrou
Christos
C
Department of Pharmacy, Laboratory of Pharmacognosy and Chemistry of Natural Products, University of Patras, Hellas, Greece.
Magafa
Vassiliki
V
Nikolopoulou
Anastasia
A
Pairas
George
G
Nock
Berthold
B
Maina
Theodosia
T
Cordopatis
Paul
P
D000818:Animals; D001667:Binding, Competitive; D045744:Cell Line, Tumor; D010456:Peptides, Cyclic / Q000737:chemistry / Q000378:metabolism*; D051381:Rats; D013004:Somatostatin / Q000031:analogs & derivatives / Q000378:metabolism*; D013329:Structure-Activity Relationship
D010456:Peptides, Cyclic; C470036:octreotate, Tyr(3)-; D013004:Somatostatin