This panel provides drug-protein interaction and their ADRs along with references
| Toxicity |
Interacting Protein |
Mechanism |
Reference |
| Central Adiposity | Cellular retinoic acid-binding protein 1 (P29762) | Protease inhibitors inhibit CRABP-1-modified@ and cytochrome P450 3A-mediated synthesis of cis-9-retinoic acid@ a key activator of the retinoid X receptor@which leads to central adiposity. [ ADR Type 1 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
|
| Central Adiposity | Cytochrome P450 3A43 (Q9HB55) | Protease inhibitors inhibit CRABP-1-modified@ and cytochrome P450 3A-mediated synthesis of cis-9-retinoic acid@ a key activator of the retinoid X receptor@which leads to central adiposity. [ ADR Type 1 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
|
| Central Adiposity | Retinoic acid receptor (P19793) | Protease inhibitors inhibit CRABP-1-modified@ and cytochrome P450 3A-mediated synthesis of cis-9-retinoic acid@ a key activator of the retinoid X receptor@which leads to central adiposity. [ ADR Type 1 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
|
| Hyperlipidaemia | Cellular retinoic acid-binding protein 1 (P29762) | Protease inhibitors inhibit CRABP-1-modified@ and cytochrome P450 3A-mediated synthesis of cis-9-retinoic acid@ a key activator of the retinoid X receptor@which leads to hyperlipidaemia [ ADR Type 1 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
|
| Hyperlipidaemia | Cytochrome P450 3A43 (Q9HB55) | Protease inhibitors inhibit CRABP-1-modified@ and cytochrome P450 3A-mediated synthesis of cis-9-retinoic acid@ a key activator of the retinoid X receptor@which leads to hyperlipidaemia [ ADR Type 1 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
|
| Hyperlipidaemia | Retinoic acid receptor (P19793) | Protease inhibitors inhibit CRABP-1-modified@ and cytochrome P450 3A-mediated synthesis of cis-9-retinoic acid@ a key activator of the retinoid X receptor@which leads to hyperlipidaemia [ ADR Type 1 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
|
| Impair Hepatic Chylomicron Uptake | low density lipoprotein-receptor-related protein (LRP) (Q86VZ4) | Protease-inhibitor binding to LRP would impair hepatic chylomicron uptake and triglyceride clearance by the endothelial LRP-lipoprotein lipase complex. [ ADR Type 1 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
|
| Impaired Fat Storage And Lipid Release | Peroxisome proliferator-activated receptor gamma (P37231) | HIV-1 protease inhibitor-induced peripheral lipodystrophy is a result of impaired CRABP1-mediated cis-9-retinoic acid stimulation of RXR:PPAR-?@ resulting in reduced differentiation and increased apoptosis of peripheral adipocytes@ with impaired fat storage and lipid release. [ ADR Type 2 3 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
|
| Insulin Resistance | Cellular retinoic acid-binding protein 1 (P29762) | Protease inhibitors inhibit CRABP-1-modified@ and cytochrome P450 3A-mediated synthesis of cis-9-retinoic acid@ a key activator of the retinoid X receptor@which leads to insulin resistance [ ADR Type 1 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
|
| Insulin Resistance | Cytochrome P450 3A43 (Q9HB55) | Protease inhibitors inhibit CRABP-1-modified@ and cytochrome P450 3A-mediated synthesis of cis-9-retinoic acid@ a key activator of the retinoid X receptor@which leads to insulin resistance [ ADR Type 1 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
|
| Insulin Resistance | Retinoic acid receptor (P19793) | Protease inhibitors inhibit CRABP-1-modified@ and cytochrome P450 3A-mediated synthesis of cis-9-retinoic acid@ a key activator of the retinoid X receptor@which leads to insulin resistance. [ ADR Type 1 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
|
| Lipodystrophy | Cytochrome P450 3A43 (Q9HB55) | Protease inhibitors inhibit CRABP-1-modified@ and cytochrome P450 3A-mediated synthesis of cis-9-retinoic acid@ a key activator of the retinoid X receptor@which leads to peripheral fat wasting (lipodystrophy) [ ADR Type 1 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
|
| Lipodystrophy | Retinoic acid receptor (P19793) | Protease inhibitors inhibit CRABP-1-modified@ and cytochrome P450 3A-mediated synthesis of cis-9-retinoic acid@ a key activator of the retinoid X receptor@which leads to peripheral fat wasting (lipodystrophy) [ ADR Type 1 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
|
| Peripheral Fat Wasting (Lipodystrophy) | Cellular retinoic acid-binding protein 1 (P29762) | Protease inhibitors inhibit CRABP-1-modified@ and cytochrome P450 3A-mediated synthesis of cis-9-retinoic acid@ a key activator of the retinoid X receptor@which leads to peripheral fat wasting (lipodystrophy) [ ADR Type 1 ] | Pathogenesis of HIV-1-protease inhibitor-associated peripheral lipodystrophy, hyperlipidaemia, and insulin resistance
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