1995
DOI: 10.1021/bi00039a010 View full text |Buy / Rent full text
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Abstract: The cholesteryl ester transfer protein-catalyzed cholesteryl ester transfer is inhibited by two compounds identified by a large-scale screening of cholesterol backbone-containing molecules. Kinetic analysis shows that U-95,594, an amino steroid, inhibits competitively the cholesteryl ester transfer protein-catalyzed transfer of both cholesteryl esters and triglycerides, as well from high-density lipoproteins as from synthetic microemulsions. In contrast, U-617, an organomercurial derivative of cholesterol, inh… Show more

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“…Consequently, cysteine 13 has been proposed to be near the neutral lipid binding site for CETP. U-95,594 (22), an amino steroid, demonstrated kinetic aspects of a competitive inhibitor, consistent with its structural similarities to CE. Similarly, a nonsteroid inhibitor, SC-795 (31), was shown to block CE binding to CETP.…”
Section: Inhibition Of Cetp By Torcetrapib Is Reversiblementioning
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“…Consequently, cysteine 13 has been proposed to be near the neutral lipid binding site for CETP. U-95,594 (22), an amino steroid, demonstrated kinetic aspects of a competitive inhibitor, consistent with its structural similarities to CE. Similarly, a nonsteroid inhibitor, SC-795 (31), was shown to block CE binding to CETP.…”
Section: Inhibition Of Cetp By Torcetrapib Is Reversiblementioning
“…Both reversible agents were proposed as competitive inhibitors of CETP, although they also inhibited TG transfer. Interestingly, U-617, an organomercurial derivative of cholesterol, was shown to inhibit CE transfer but not TG transfer (22). Additional reports that a number of synthetic compounds, as well as antibodies and their fragments, inhibit CE and TG transfer selectively are consistent with the idea that different lipids may rely on different sites on CETP for binding and transfer (35).…”
Section: Inhibition Of Cetp By Torcetrapib Is Reversiblementioning
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“…Epps e colaboradores 16 estudaram a cinética de inibição in vitro de dois derivados de colesterol (U-617 e U-95594) sobre CETP (Figura 6). Apesar da grande semelhança estrutural desses dois compostos, seus mecanismos de inibição diferem drasticamente.…”
Section: Agentes Modificadores De Cisteína (Dalcetrapib Jtt-705)unclassified