Uptake of low-density lipoprotein by malignant cells--possible therapeutic applications.
Cells acquire cholesterol via de novo synthesis and receptor-mediated uptake of low-density lipoprotein (LDL), the major cholesterol-carrying lipoprotein in blood. Human leukemic cells and certain tumor tissues display elevated receptor-mediated uptake of LDL as compared with the corresponding normal cells or tissues. LDL has therefore been proposed as a potential carrier for chemotherapeutic agents. Various methods have been employed to incorporate antineoplastic lipophilic drugs into LDL, and the resultant drug-LDL complexes have been shown to be cytotoxic toward tumor cells in vitro. Initial experiments with tumor-bearing animals suggest that LDL may be a promising carrier for drugs in the treatment of malignant diseases.
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Department of Clinical Pharmacology, Karolinska Hospital, Stockholm, Sweden.
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D001692:Biological Transport; D008078:Cholesterol, LDL / Q000378:metabolism*; D004337:Drug Carriers; D004705:Endocytosis; D017324:Hematoporphyrin Derivative; D006415:Hematoporphyrins / Q000008:administration & dosage / Q000493:pharmacokinetics; D006801:Humans; D007938:Leukemia / Q000378:metabolism; D008077:Lipoproteins, LDL / Q000378:metabolism* / Q000493:pharmacokinetics; D008563:Membrane Lipids / Q000378:metabolism; D051379:Mice; D009369:Neoplasms / Q000378:metabolism*; D009374:Neoplasms, Experimental / Q000188:drug therapy / Q000378:metabolism; D051381:Rats; D011973:Receptors, LDL / Q000378:metabolism
D000970:Antineoplastic Agents; D008078:Cholesterol, LDL; D004337:Drug Carriers; D006415:Hematoporphyrins; D008077:Lipoproteins, LDL; D008563:Membrane Lipids; D011973:Receptors, LDL; D017324:Hematoporphyrin Derivative