oxldl binding

Oxidized low-density lipoprotien (oxLDL) particles contain low molecular weight species which are cytotoxic and pro-atherogenic. Many of these substances were recently isolated and purified from oxLDL, and identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position. 1-(Palmitoyl)-2-(5-oxovaleroyl)-phosphatidylcholine, or POV-PC, is one of the oxLDL species derived from 2-arachidonoyl or eicosapentanoyl phospholipids. POV-PC confers CD36 scavenger receptor binding affinity more potently than any hydroperoxy PC species, and may be one of the more important structural determinants of oxLDL. Treatment of cultured endothelial cells with POV-PC stimulates monocyte binding, stimulates intracellular cAMP production, and strongly inhibits the LPS-induced binding of neutrophils.

Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species which are cytotoxic and pro-atherogenic. Many of these substances were recently isolated and purified from oxLDL, and identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position. KDdiA-PC is one of the most potent CD36 ligands among the oxLDL species. KDdiA-PC confers CD-36 scavenger receptor binding affinity to LDL at a frequency of only two to three KDdiA-PC molecules/LDL particle, and may be one of the more important structural determinants of oxLDL.

BI-0115 is a selective small molecule inhibitor of LOX-1 that blocks cellular uptake of oxLDL. It binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain. The structure of LOX-1 bound to BI-0115 shows that inte

Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species which promote the differentiation of monocytes via the nuclear receptor PPARγ. One of these substances was recently isolated and purified from oxLDL, and identified as azelaoyl PAF. Azelaoyl PAF is a potent PPARγ agonist which competes for the thiazolidinedione binding site. Azelaoyl PAF is more potent than 15-deoxy-δ12,14-prostaglandin J2, and equipotent with rosiglitazone as a ligand for this receptor.

Oxidized low-density lipoprotien (oxLDL) particles contain low molecular weight species which are cytotoxic and pro-atherogenic. Many of these substances were recently isolated and purified from oxLDL, and identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position. 1-(Palmitoyl)-2-(5-keto-6-octene-dioyl) phosphatidylcholine, or KOdiA-PC, is one of the most potent CD36 ligands among the oxLDL species. KOdiA-PC confers CD36 scavenger receptor binding affinity to LDL at a frequency of only 2 to 3 KOdiA-PC molecules/LDL particle, and may be one of the more important structural determinants of oxLDL.