Synthesis and biological evaluation of PEG-tirofiban conjugates.
We have conjugated tirofiban, an antagonist of the GPIIb/IIIa integrin receptor, to PEG, and shown that these polymers effectively inhibit platelet aggregation. This inhibition decreased with the size of the polymer. Our goal was to develop new cryoprotective agents to store frozen platelets. Surprisingly, tirofiban-conjugated PEG did not exhibit any protection.
Désaubry
Laurent
L
UMR 7175 LC1, Université Louis Pasteur, CNRS, Faculté de Pharmacie, 67401 Illkirch, France. desaubry@chimie.u-strasbg.fr
Riché
Stéphanie
S
Laeuffer
Patricia
P
Cazenave
Jean-Pierre
JP
D003094:Collagen / Q000494:pharmacology; D003451:Cryoprotective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D005615:Freezing; D006801:Humans; D056913:Mediator Complex Subunit 1; D015394:Molecular Structure; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000037:antagonists & inhibitors; D011092:Polyethylene Glycols / Q000138:chemical synthesis* / Q000494:pharmacology*; D011108:Polymers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D000077466:Tirofiban; D014157:Transcription Factors / Q000037:antagonists & inhibitors; D014443:Tyrosine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D003451:Cryoprotective Agents; C538855:MED1 protein, human; D056913:Mediator Complex Subunit 1; D010975:Platelet Aggregation Inhibitors; D019039:Platelet Glycoprotein GPIIb-IIIa Complex; D011108:Polymers; D014157:Transcription Factors; D011092:Polyethylene Glycols; D014443:Tyrosine; D003094:Collagen; D000077466:Tirofiban