PMID- 3190742
OWN - NLM
STAT- MEDLINE
DCOM- 19881125
LR  - 20190623
IS  - 0006-2952 (Print)
IS  - 0006-2952 (Linking)
VI  - 37
IP  - 20
DP  - 1988 Oct 15
TI  - Comparative cellular uptake and cytotoxicity of a complex of daunomycin-low 
      density lipoprotein in human squamous lung tumour cell monolayers.
PG  - 3981-6
AB  - In an attempt to target cytotoxic drugs to tumour cells daunomycin-low density 
      lipoprotein (LDL) complexes were synthesised. Human squamous lung tumour cells in 
      vitro have large numbers of high affinity cell surface LDL receptors (Vmax = 19 
      ng LDL/micrograms cell protein per 24 hr; Km = 23 micrograms/ml). Cellular uptake 
      of daunomycin and LDL-daunomycin was rapid and approached equilibrium by 
      approximately 3 hr. Intracellular daunomycin concentrations were similar at each 
      time point regardless of whether free drug or the complex was used. The degree of 
      intracellular drug metabolism differed markedly with significantly higher 
      production of daunomycinol following exposure to free daunomycin for 90 min. 
      Daunomycin and LDL-daunomycin were equally cytotoxic in vitro (respective 
      clonogenic ID90s of 1 microgram/ml and 0.7 microgram/ml). Fluorescence microscopy 
      indicated that both free daunomycin and LDL-daunomycin have a punctate, granular 
      distribution within the cytoplasm.
FAU - Kerr, D J
AU  - Kerr DJ
AD  - CRC Department of Medical Oncology, University Glasgow, U.K.
FAU - Hynds, S A
AU  - Hynds SA
FAU - Shepherd, J
AU  - Shepherd J
FAU - Packard, C J
AU  - Packard CJ
FAU - Kaye, S B
AU  - Kaye SB
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - England
TA  - Biochem Pharmacol
JT  - Biochemical pharmacology
JID - 0101032
RN  - 0 (Lipoproteins, LDL)
RN  - ZS7284E0ZP (Daunorubicin)
SB  - IM
MH  - Carcinoma, Squamous Cell/*metabolism
MH  - Cell Survival/drug effects
MH  - Daunorubicin/administration & dosage/*metabolism/pharmacology
MH  - Humans
MH  - Lipoproteins, LDL/administration & dosage/*metabolism
MH  - Lung Neoplasms/*metabolism
MH  - Microscopy, Fluorescence
MH  - Tumor Cells, Cultured
EDAT- 1988/10/15 00:00
MHDA- 1988/10/15 00:01
CRDT- 1988/10/15 00:00
PHST- 1988/10/15 00:00 [pubmed]
PHST- 1988/10/15 00:01 [medline]
PHST- 1988/10/15 00:00 [entrez]
AID - 0006-2952(88)90083-4 [pii]
AID - 10.1016/0006-2952(88)90083-4 [doi]
PST - ppublish
SO  - Biochem Pharmacol. 1988 Oct 15;37(20):3981-6. doi: 10.1016/0006-2952(88)90083-4.